What are amitriptyline tablets used for? Why is amitriptyline dangerous?

INN: Amitriptyline

Manufacturer: Technologist of PrJSC

Anatomical-therapeutic-chemical classification: Amitriptyline

Registration number in the Republic of Kazakhstan: No. RK-LS-5No. 022186

Registration period: 19.05.2016 - 19.05.2021

KNF (medicine included in the Kazakhstan National Formulary of Medicines)

ALO (Included in the List of free outpatient drug provision)

ED (Included in the List of drugs within the framework of the guaranteed volume of free medical care, subject to purchase from the Single Distributor)

Limit purchase price in the Republic of Kazakhstan: 4.54 KZT

Instructions

Tradename

Amitriptyline

International nonproprietary name

Amitriptyline

Dosage form

Compound

One tablet contains

active substance- amitriptyline hydrochloride in terms of amitriptyline 25 mg;

Excipients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, hypromellose, magnesium stearate, colloidal silicon dioxide, polyethylene glycol 6000, titanium dioxide (E 171), talc, polysorbate 80, carmoisin (E 122).

Description

Round, film-coated tablets, light pink to pink in color, with top and bottom convex surfaces. On the fault, under a magnifying glass, you can see the core surrounded by one continuous layer.

Pharmacotherapeutic group

Psychoanaleptics. Antidepressants. Non-selective inhibitors of neuronal monoamine reuptake. Amitriptyline

ATX code N06AA09

Pharmacological properties

Pharmacokinetics

Amitriptyline is well absorbed from the gastrointestinal tract, with maximum plasma concentrations achieved within about 6 hours after oral administration.

The bioavailability of amitriptyline is 48 ± 11%, 94.8 ± 0.8% is bound to plasma proteins. These parameters do not depend on the patient's age.

The half-life is 16 ± 6 hours, the volume of distribution is 14 ± 2 l/kg. Both parameters increase significantly with increasing patient age.

Amitriptyline is significantly demethylated in the liver to the main metabolite, nortriptyline. Metabolic pathways include hydroxylation, N-oxidation and conjugation with glucuronic acid. The drug is excreted in the urine, mainly in the form of metabolites, in free or conjugated form. Clearance is 12.5 ± 2.8 ml/min/kg (independent of the patient’s age), less than 2% is excreted in the urine.

Pharmacodynamics

Amitriptyline is a tricyclic antidepressant. It has pronounced antimuscarinic and sedative properties. The therapeutic effect is based on a decrease in presynaptic reuptake (and, as a result, inactivation) of norepinephrine and serotonin (5HT) by presynaptic nerve endings.

Despite the fact that a pronounced antidepressant effect, as a rule, appears 10-14 days after the start of treatment, inhibition of activity can be observed within an hour after administration. This indicates that the mechanism of action may be complemented by other pharmacological properties of the drug.

Indications for use

Depression of any etiology (especially when it is necessary to obtain a sedative effect).

Directions for use and doses

Treatment should be started with small doses, gradually increasing them, carefully monitoring the clinical response and any manifestations of intolerance.

Adults: The recommended starting dose is 75 mg per day, taken in divided doses or at night. Depending on the clinical effect, the dose may be increased to 150 mg/day. It is advisable to increase the dosage at the end of the day or before bedtime.

The sedative effect usually manifests itself quickly. The antidepressant effect of the drug may appear after 3-4 days; it may take up to 30 days for the effect to develop adequately.

To reduce the likelihood of relapse, a maintenance dose of 50-100 mg should be taken in the evening or before bed.

Elderly patients (over 65 years): The recommended starting dose is 10-25 mg three times daily, with gradual increases as needed. For patients in this age group who cannot tolerate high doses, a daily dose of 50 mg may be sufficient. The required daily dose can be prescribed either in several doses or once, preferably in the evening or before bedtime.

Mode of application

The tablets should be swallowed whole, without chewing, and washed down with water.

The drug should be taken in accordance with the terms prescribed by the doctor, since stopping treatment on your own can be dangerous to health. No improvement in the patient's condition can be observed up to 4 weeks after the start of treatment.

Side effects

Like other medicines, Amitriptyline film-coated tablets can sometimes cause side effects in some patients, especially when prescribed for the first time. Not all of the side effects listed were observed during treatment with amitriptyline; some of them occurred when using other drugs belonging to the amitriptyline group.

Adverse reactions are classified by frequency of occurrence: very often (> 1/10), often (from > 1/100 to< 1/10), не часто (от >1/1000 to< 1/100), редко (от >1/10000 to< 1/1,000), очень редко (< 1/10000), включая единичные случаи.

The cardiovascular system: arterial hypotension, fainting, orthostatic arterial hypotension, hypertension, tachycardia, palpitations, myocardial infarction, arrhythmias, heart block, stroke, nonspecific ECG changes and changes in atrioventricular conduction. Cardiac arrhythmias and severe hypotension are most likely to occur with high doses or deliberate overdose. These conditions may also occur in patients with pre-existing heart disease while taking standard doses of the drug.

From the outside nervous system: dizziness, fatigue, headache, weakness, confusion, attention disorders, disorientation, delirium, hallucinations, hypomania, agitation, anxiety, restlessness, drowsiness, insomnia, nightmares, numbness, tingling sensation, paresthesia of the limbs, peripheral neuropathy, incoordination, ataxia, tremor, coma, seizures, EEG changes, extrapyramidal disorders, including pathological involuntary movements and tardive dyskinesia, dysarthria, tinnitus.

There have been reports of cases of suicidal thoughts or behavior during or early after discontinuation of treatment with amitriptyline.

Effects due to anticholinergic activity: dry mouth, blurred vision, mydriasis, accommodation disturbances, increased intraocular pressure, constipation, paralytic ileus intestines, hyperpyrexia, urinary retention, dilatation of the urinary tract.

Allergic reactions:skin rash, urticaria, photosensitivity, swelling of the face and tongue.

From the blood and lymphatic system: suppression of bone marrow activity, including agranulocytosis, leukopenia, eosinophilia, purpura, thrombocytopenia.

WITHon the side of the gastrointestinal tract: nausea, epigastric discomfort, vomiting, anorexia, stomatitis, taste change, diarrhea, inflammation parotid glands, darkening of the tongue and, in rare cases, hepatitis (including liver dysfunction and cholestatic jaundice).

From the endocrine system: testicular enlargement and gynecomastia in men, breast enlargement and galactorrhea in women, increased or decreased libido, impotence, sexual dysfunction, changes in the secretion of antidiuretic hormone (ADH).

From the side of metabolism: increase or decrease in blood glucose levels; increased appetite and weight gain may be a reaction to the drug or a consequence of relieving depression.

From the hepatobiliary system: rarely - hepatitis (including liver dysfunction and jaundice).

From the skin and subcutaneous tissue: increased sweating and hair loss.

From the kidneys and urinary tract: frequent urination.

When using high doses of the drug, as well as in elderly patients, confusion is possible, which requires a dose reduction.

Withdrawal syndrome. Abruptly stopping treatment after long-term use of the drug may cause nausea, vomiting and headache. Gradual dose reduction reportedly caused transient symptoms within two weeks, including irritability, restlessness and disturbances in sleep and dreams. These symptoms do not indicate addiction to the drug. Rare cases of manic or hypo manic states that occurred within 2-7 days after stopping long-term treatment with tricyclic antidepressants.

You must follow your doctor's instructions regarding stopping taking the drug.

There have also been reports of withdrawal symptoms in neonates whose mothers received tricyclic antidepressants.

Class-specific effects

Epidemiological studies conducted primarily in patients aged 50 years and older show an increased risk of bone fractures in patients taking selective serotonin reuptake inhibitors and tricyclic antidepressants. The mechanism leading to this risk is unknown.

Contraindications

Hypersensitivity to amitriptyline or to any of the components of the drug

Concomitant therapy with MAO inhibitors (MAO inhibitors must be discontinued at least 14 days before starting treatment with amitriptyline)

Coronary heart disease, recent myocardial infarction

Heart rhythm and conduction disturbances, congestive heart failure

Manic psychosis

Severe liver failure

Lactation period

Children under 16 years old

Drug interactions

Altretamine

When amitriptyline is used concomitantly with altretamine, there is a risk of severe postural hypotension.

Alpha-2 adrenergic agonists

Analgesics

There may be an increase in the side effects of nefopam and the risk of seizures while taking tramadol. Levacetylmethadol should not be co-administered with amitriptyline due to the increased risk of ventricular arrhythmia.

Anesthetics

Concomitant therapy with amitriptyline may increase the risk of arrhythmias and hypotension.

Antiarrhythmic drugs

There is an increased risk of developing ventricular arrhythmia when coadministered with drugs that prolong the QT interval, including amiodarone, disopyramide, procainamide, propafenone and quinidine. Therefore, this combination of drugs should be avoided.

Antibacterial drugs

Taking rifampicin reduces the plasma concentrations of some tricyclic antidepressants and, consequently, their antidepressant effect.

Concomitant use with linezolid may lead to stimulation of the central nervous system and the development of arterial hypertension.

Monoamine oxidase inhibitors (MAOIs)

Monoamine oxidase inhibitors may enhance the effect of tricyclic antidepressants such as amitriptyline. Cases of hyperthermic crises, severe convulsive seizures, and death have been recorded.

Prescription of amitriptyline is possible only 2 weeks after discontinuation of MAO inhibitors. CNS excitation and increased blood pressure have been observed during the use of MAOIs.

Antiepileptic drugs

Concomitant use with antiepileptic drugs may lead to a decrease in the seizure threshold.

Barbiturates and carbamazepine can reduce, and methylphenidate increase, the antidepressant effect of amitriptyline.

Antihistamines

Purpose antihistamines may increase the anticholinergic and sedative effects of amitriptyline. Concomitant use of terfenadine should be avoided due to increased risk development of ventricular arrhythmia.

Antihypertensive drugs

Amitriptyline may block the antihypertensive effects of guanethidine, debrisoquine, betanidine and possibly clonidine. During treatment with tricyclic antidepressants, it is advisable to re-evaluate the patient's antihypertensive therapy.

Sympathomimetics

Amitriptyline should not be administered with sympathomimetics such as epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine and phenylpropanolamine.

Other CNS depressants

Amitriptyline may increase the body's response to alcohol, barbiturates, and other central nervous system depressants. In turn, barbiturates can reduce, and methylphenidate can enhance, the antidepressant effect of amitriptyline.

Monitoring of patients simultaneously receiving large doses of etchlorvinol is necessary. Transient delirium has been reported in patients who received 1 g of etchlorvinol and 75-150 mg of amitriptyline.

Disulfiram

Concomitant use of amitriptyline with disulfiram and other acetaldehydrogenase inhibitors may precipitate delirium.

Concomitant use can inhibit the metabolism of tricyclic antidepressants. In patients taking disulfiram, amitriptyline and alcohol simultaneously, there is an increase in plasma concentrations and a decrease in the effectiveness of disulfiram.

Anticholinergic drugs

When used together with anticholinergic drugs, it is possible to increase anticholinergic side effects, such as urinary retention, glaucoma attack, intestinal obstruction, especially in elderly patients.

Neuroleptics

There may be an increased risk of developing ventricular arrhythmias.

Pimozide and thioridazine should not be co-administered as amitriptyline may increase plasma levels of thioridazine, leading to an increased risk of cardiovascular side effects.

Use with antipsychotics may increase plasma concentrations of tricyclic antidepressants and the anticholinergic side effects of phenothiazine and possibly clozapine.

Antiviral drugs

The protease inhibitor ritonavir may increase plasma concentrations of amitriptyline.

Therefore, careful monitoring of therapeutic and side effects is necessary when these drugs are coadministered.

Antiulcer drugs

When taken simultaneously with cimetidine, it is possible to increase the plasma concentration of amitriptyline with the risk of developing toxic effects.

Anxiolytics and hypnotics

Simultaneous use enhances the sedative effect.

Beta blockers

There is an increased risk of ventricular arrhythmia associated with concomitant use of sotalol.

Beta blockers (sotalol)

The risk of ventricular arrhythmias increases.

Calcium channel blockers

Diltiazem and verapamil may lead to increased plasma concentrations of amitriptyline.

Diuretics

There is an increased risk of developing orthostatic hypotension.

Dopaminergic drugs

Concomitant use with entacapone and brimonidine should be avoided. CNS toxicity has been observed during the use of selegiline.

Muscle relaxants

Concomitant use with baclofen increases its muscle relaxant effect.

Nitrates

The effect of the sublingual form of nitrates may be reduced (due to dry mouth).

Estrogen-containing oral contraceptives

Oral contraceptives reduce the antidepressant effect of amitriptyline, but the side effects of the drug may be increased by increasing its plasma concentration.

Thyroid drugs

The effect of tricyclic antidepressants, such as amitriptyline, may be enhanced when combined with medications used to treat thyroid gland(eg levothyroxine).

St. John's wort

St. John's wort may reduce plasma levels of amitriptyline.

Concomitant use of amitriptyline and electroshock may increase the risk of therapy. This combination treatment should only be used if absolutely necessary.

special instructions

Amitriptyline should be administered with caution to patients with a history of seizures, patients with impaired liver function and, due to its atropine-like effects, patients with a history of urinary retention or patients with angle-closure glaucoma or increased intraocular pressure. In patients with angle-closure glaucoma, even moderate doses can cause an attack.

While taking amitriptyline, it is necessary to carefully monitor the condition of patients with cardiovascular disorders, thyroid hyperplasia, as well as persons taking drugs for the treatment of thyroid pathologies or anticholinergic drugs; It is necessary to carefully adjust the doses of all drugs when prescribing amitriptyline in combination.

Hyponatremia is associated with the use of all types of antidepressants (usually in the elderly, possibly due to insufficient secretion of antidiuretic hormone); this state should be considered in patients who develop drowsiness, confusion, or seizures while taking antidepressants.

Elderly patients

Elderly patients have an increased risk of developing adverse reactions, especially agitation, confusion and postural hypotension. The initial dose of the drug must be increased with extreme caution under close medical supervision.

Schizophrenia

When prescribing amitriptyline for the treatment of the depressive component of schizophrenia, the psychotic symptoms of the disease may increase. In the same way, with manic-depressive psychosis, patients may experience a shift into the manic phase. Paranoid delusions may increase, with or without hostility. In any of these cases, it is recommended to reduce the dose of amitriptyline or prescribe an additional strong tranquilizer.

In patients with depression, the risk of possible suicide remains throughout treatment, so such patients require careful medical monitoring until significant remission occurs.

Electroconvulsive therapy

Surgical interventions

When planning surgical interventions amitriptyline should be discontinued several days before surgery. If surgery must be performed without delay, the anesthetist should be informed about the use of amitriptyline, since anesthesia may increase the risk of hypotension and arrhythmia.

Suicide/suicidal ideation or clinical deterioration

Depression is associated with an increased risk of suicidal ideation, self-harm, and suicide attempts. The risk exists until stable remission occurs. Improvement may not be observed during the first weeks or more of treatment, so patients should be monitored by a physician until signs of improvement appear. According to general clinical data, the risk of suicide increases by initial stage recovery period.

Other mental states for which amitriptyline is prescribed may also be associated with an increased risk of suicide. In addition, these conditions may accompany major depressive disorder. Therefore, during treatment of patients with other mental disorders, the same precautions should be observed as with major depressive disorders.

Patients with a history of suicide attempt or a high likelihood of suicidal ideation before starting amitriptyline should be closely monitored during treatment as they are at greater risk of suicidal ideation or suicide attempt.

Patients with a history of suicidal events or a significant degree of suicidal ideation are known to be at high risk for suicidal ideation or suicidal behavior before treatment and should be closely monitored during treatment.

Meta-analysis of placebo-controlled clinical trials on the use of antidepressants in adult patients with mental disorders showed an increased risk of suicidal behavior in patients treated with antidepressants for less than 25 years compared with those who received placebo.

Careful monitoring of patients, especially those at high risk, should accompany drug therapy, especially in its early stages and after dose changes. Patients (and their caregivers) should be warned to monitor for any clinical deterioration, suicidal behavior or thoughts, or unusual changes in behavior, and to immediately seek professional advice if such symptoms occur.

Excipients

The drug contains the dye carmoisin (E 122), therefore the use of Amitriptyline tablets in children is contraindicated.

Use during pregnancy or breastfeeding

The safety of amitriptyline when used during pregnancy and lactation has not been established.

It is not recommended to use amitriptyline during pregnancy, especially during the first and last trimester, unless there is a compelling indication. In such patients, it is necessary to evaluate the benefits of treatment and possible risks to the fetus, newborn or mother. Despite the drug's widespread use for many years without serious consequences, there is no evidence of the safety of amitriptyline during pregnancy.

Clinical experience with the use of amitriptyline during pregnancy is limited. There is evidence of a negative effect of the drug on pregnancy in animals when administered at extremely high doses. Withdrawal symptoms, including respiratory depression and restlessness, have been observed in neonates whose mothers took tricyclic antidepressants during the last trimester of pregnancy. Urinary retention in newborns has also been associated with maternal use of amitriptyline.

Amitriptyline is found in breast milk. Because of the potential for serious adverse reactions to amitriptyline in children, a decision must be made to either stop breastfeeding or discontinue the drug.

Features of influence medicine on the ability to drive a vehicle or potentially dangerous machinery

Amitriptyline can impair concentration. Patients should be warned about the possible risks when driving or operating machinery.

Overdose

High doses of amitriptyline may cause temporary confusion, difficulty concentrating, or transient hallucinations.

Overdose can cause hypothermia, drowsiness, tachycardia, other arrhythmias with disturbances in the bundle branches, congestive heart failure, signs of conduction disturbances on the ECG, dilated pupils, disorders of the oculomotor system, convulsions, severe hypotension, drowsiness, hypothermic stupor and coma.

Other symptoms that may occur include psychomotor agitation, muscle rigidity, hyperactive reflexes, hyperthermia, vomiting or other reactions listed above.

If an overdose is suspected, urgent hospitalization is required.

Taking 750 mg of the drug may result in serious toxicity. Symptoms of overdose increase with the simultaneous use of alcohol and other psychotropic drugs.

The effects of overdose are mainly due to the anticholinergic (atropine-like) effect of the drug on the nerve endings of the brain. There is also a quinidine-like effect on the myocardium.

Peripheral effects

Standard manifestations: sinus tachycardia, hot dry skin, dry mouth and tongue, dilated pupils, urinary retention.

The most important signs of toxicity on the ECG are prolongation of the QRS complex, which indicates a high risk of ventricular tachycardia. In very severe poisoning, the ECG may take on an abnormal appearance. In rare cases, prolongation of the P-R interval or heart block may occur. Cases of QT prolongation and torsade de pointes have also been reported.

Main effects

Ataxia, nystagmus, and drowsiness are usually observed, which can lead to deep coma and respiratory depression. With extensor plantar reflexes, increased tone and hyperreflexia may be observed. In a deep coma, all reflexes may be absent. Divergent strabismus may occur. Manifestations of hypotension and hypothermia are possible. Convulsions are observed in more than 5% of cases.

During recovery, confusion, psychomotor agitation, and visual hallucinations may occur.

Treatment

An ECG and, in particular, an assessment of the QRS interval are indicated, since its prolongation indicates an increased risk of arrhythmias and seizures. Oral activated charcoal or nasogastric intubation for protection respiratory tract, if the patient took a dose of more than 4 mg/kg within one hour. Second dose activated carbon administered after 2 hours to patients with signs of central toxicity who can swallow independently.

To treat tachyarrhythmia, it is recommended to correct hypoxia and acidosis. Even in the absence of acidosis, adult patients with arrhythmia or clinically significant prolongation of the QRS interval on the ECG should receive an intravenous infusion of 50 mmol sodium bicarbonate.

If convulsive syndrome develops, intravenous administration of diazepam or lorazepam. Providing access to oxygen, correcting acid-base and metabolic disorders. Diphenine is contraindicated in overdose of tricyclic antidepressants because, like them, diphenine blocks sodium channels and may increase the risk of heart rhythm disturbances. Glucagon is used to correct myocardial depression and hypotension.

Release form and packaging

Film-coated tablets, 25 mg

10 tablets each in a blister pack (blister) made of polyvinyl chloride film and rolled packaging material based on aluminum foil.

Antidepressant

Active substance

Amitriptyline (amitriptyline)

Release form, composition and packaging

Pills from white to white with a slightly yellowish tint, flat-cylindrical in shape, with a chamfer; Light marbling is allowed.

Excipients: microcrystalline cellulose - 40 mg, lactose monohydrate (milk sugar) - 40 mg, pregelatinized starch - 25.88 mg, colloidal silicon dioxide (aerosil) - 400 mcg, talc - 1.2 mg, magnesium stearate - 1.2 mg.

Pills from white to white with a slightly yellowish tint, flat-cylindrical in shape, with a chamfer and a notch; Light marbling is allowed.

Excipients: microcrystalline cellulose - 100 mg, lactose monohydrate (milk sugar) - 100 mg, pregelatinized starch - 64.7 mg, colloidal silicon dioxide (aerosil) - 1 mg, talc - 3 mg, magnesium stearate - 3 mg.

10 pieces. - contour cellular packaging (1) - cardboard packs.
10 pieces. - contour cell packaging (2) - cardboard packs.
10 pieces. - contour cell packaging (3) - cardboard packs.
10 pieces. - contour cell packaging (4) - cardboard packs.
10 pieces. - contour cell packaging (5) - cardboard packs.
100 pieces. - polymer jars (1) - cardboard packs.

pharmachologic effect

Antidepressant (tricyclic antidepressant). It also has some analgesic (of central origin), antiserotonin effect, helps eliminate bedwetting and reduces appetite.

It has a strong peripheral and central anticholinergic effect due to its high affinity for m-cholinergic receptors; strong sedative effect associated with affinity for H1-histamine receptors and alpha-adrenergic blocking effect.

It has the properties of a class IA antiarrhythmic drug; like quinidine in therapeutic doses, it slows down ventricular conduction (in overdose it can cause severe intraventricular block).

The mechanism of antidepressant action is associated with an increase in the concentration and/or serotonin in the central nervous system (CNS) (decreasing their reabsorption).

The accumulation of these neurotransmitters occurs as a result of inhibition of their reuptake by the membranes of presynaptic neurons. With long-term use, it reduces the functional activity of beta-adrenergic and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, restores the balance of these systems, disturbed by depressive states. In anxiety-depressive conditions, it reduces anxiety, agitation and depressive symptoms.

The mechanism of antiulcer action is due to the ability to have a sedative and m-anticholinergic effect. Effectiveness for bedwetting appears to be due to anticholinergic activity leading to increased bladder distensibility, direct beta-adrenergic stimulation, alpha-adrenergic agonist activity with increased sphincter tone, and central uptake blockade. It has a central analgesic effect, which is believed to be associated with changes in the concentration of monoamines in the central nervous system, especially serotonin, and an effect on endogenous opioid systems.

The mechanism of action in bulimia nervosa is unclear (may be similar to that in depression). A clear effect of the drug on bulimia has been shown in patients both without depression and in its presence, while a decrease in bulimia can be observed without a concomitant weakening of depression itself.

During general anesthesia, it reduces blood pressure and body temperature. Does not inhibit monoamine oxidase (MAO).

The antidepressant effect develops within 2-3 weeks after the start of use.

Pharmacokinetics

Absorption is high.

The bioavailability of amitriptyline is 30-60%, its active metabolite nortriptyline is 46-70%. Time to reach C max after oral administration is 2.0-7.7 hours. V d 5-10 l/kg. Effective therapeutic blood concentrations for amitriptyline are 50-250 ng/ml, for nortriptyline 50-150 ng/ml.

Cmax 0.04-0.16 µg/ml. Passes (including nortriptyline) through histohematic barriers, including the blood-brain barrier, placental barrier, and penetrates into breast milk. Protein binding - 96%.

Metabolized in the liver with the participation of isoenzymes CYP2C19, CYP2D6, has a “first pass” effect (by demethylation, hydroxylation) with the formation of active metabolites - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites. T1/2 from blood plasma is 10-26 hours for amitriptyline and 18-44 hours for nortriptyline. Excreted by the kidneys (mainly in the form of metabolites) - 80% in 2 weeks, partially with bile.

Indications

Depression (especially with anxiety, agitation and sleep disorders, including in childhood, endogenous, involutional, reactive, neurotic, drug-induced, with organic brain damage).

As part of complex therapy, it is used for mixed emotional disorders, psychoses in schizophrenia, alcohol withdrawal, behavioral disorders (activity and attention), nocturnal enuresis (except for patients with bladder hypotension), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic diseases, atypical facial pain, postherpetic neuralgia, post-traumatic neuropathy, diabetic or other peripheral neuropathy), headaches, migraines (prevention), gastric ulcers and duodenum.

Contraindications

Hypersensitivity, use in conjunction with MAO inhibitors and 2 weeks before treatment, myocardial infarction (acute and subacute periods), acute alcohol intoxication, acute intoxication with hypnotics, analgesics and psychoactive drugs, angle-closure glaucoma, severe AV and intraventricular conduction disorders (branch block His bundle, AV block II stage), lactation period, childhood up to 6 years old.

Carefully. Amitriptyline should be used with caution in persons with alcoholism, bronchial asthma, schizophrenia (possible activation of psychosis), bipolar disorder, epilepsy, with suppression of bone marrow hematopoiesis, diseases of the cardiovascular system (CVS) (angina pectoris, arrhythmia, heart block, chronic failure, myocardial infarction, arterial hypertension), intraocular hypertension, stroke , decreased motor function of the gastrointestinal tract (GIT) (risk of paralytic ileus), liver and/or renal failure, thyrotoxicosis, prostatic hyperplasia, urinary retention, hypotension of the bladder, during pregnancy (especially the first trimester), in old age.

Dosage

Administered orally, without chewing, immediately after meals (to reduce irritation of the gastric mucosa).

Adults

For adults with depression, the initial dose is 25-50 mg at night, then gradually the dose can be increased taking into account the effectiveness and tolerability of the drug to a maximum of 300 mg/day. in 3 doses (the largest part of the dose is taken at night). When a therapeutic effect is achieved, the dose can be gradually reduced to the minimum effective, depending on the patient's condition. The duration of the course of treatment is determined by the patient’s condition, the effectiveness and tolerability of the therapy and can range from several months to 1 year, and if necessary, more. In old age with mild disorders, as well as with bulimia nervosa, as part of complex therapy for mixed emotional disorders and behavioral disorders, psychosis with schizophrenia and alcohol withdrawal, a dose of 25-100 mg/day is prescribed. (at night), after achieving a therapeutic effect, switch to the minimum effective doses - 10-50 mg/day.

For the prevention of migraines, with chronic pain syndrome of a neurogenic nature (including prolonged headaches), as well as in the complex therapy of gastric and duodenal ulcers - from 10-12.5-25 to 100 mg/day. (the maximum dose is taken at night).

Children

For children as an antidepressant: from 6 to 12 years old - 10-30 mg/day. or 1-5 mg/kg/day. fractionally, in adolescence - up to 100 mg/day.

For nocturnal enuresis in children 6-10 years old - 10-20 mg/day. at night, 11-16 years - up to 50 mg/day.

Side effects

Associated with the anticholinergic effect of the drug: blurred vision, paralysis of accommodation, mydriasis, increased intraocular pressure (only in persons with a local anatomical predisposition - a narrow anterior chamber angle), tachycardia, dry mouth, confusion (delirium or hallucinations), constipation, paralytic ileus, difficulty urinating.

From the side of the central nervous system: drowsiness, fainting, fatigue, irritability, anxiety, disorientation, hallucinations (especially in elderly patients and patients with Parkinson's disease), anxiety, psychomotor agitation, mania, hypomania, memory impairment, decreased ability to concentrate, insomnia, "nightmarish "dreams, asthenia; headache; dysarthria, tremor of small muscles, especially the arms, hands, head and tongue, peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus; ataxia, extrapyramidal syndrome, increased frequency and intensification epileptic seizures; changes in the electroencephalogram (EEG).

From the SSS side: tachycardia, palpitations, dizziness, orthostatic hypotension, nonspecific changes on the electrocardiogram (ECG) (S-T interval or T wave) in patients without heart disease; arrhythmia, blood pressure lability (decrease or increase in blood pressure), intraventricular conduction disturbances (widening of the QRS complex, changes P-Q interval, bundle branch block).

From the gastrointestinal tract: nausea, heartburn, gastralgia, hepatitis (including impaired liver function and cholestatic jaundice), vomiting, increased appetite and body weight or decreased appetite and body weight, stomatitis, changes in taste, diarrhea, darkening of the tongue.

From the endocrine system: increase in size (swelling) of the testicles, gynecomastia; increase in the size of the mammary glands, galactorrhea; decreased or increased libido, decreased potency, hypo- or hyperglycemia, hyponatremia (decreased vasopressin production), syndrome of inappropriate secretion of antidiuretic hormone (ADH). Allergic reactions: skin rash, itching, photosensitivity, angioedema, urticaria.

Others: hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, urinary retention, pollakiuria.

With long-term treatment, especially in high doses, if it is abruptly stopped, it is possible development of withdrawal syndrome: nausea, vomiting, diarrhea, headache, malaise, sleep disturbances, unusual dreams, unusual agitation; with gradual withdrawal after long-term treatment - irritability, motor restlessness, sleep disturbances, unusual dreams.

The connection with the drug has not been established: lupus-like syndrome (migratory arthritis, the appearance of antinuclear antibodies and positive rheumatoid factor), liver dysfunction, ageusia.

Overdose

Symptoms.

From the side of the central nervous system: drowsiness, stupor, coma, ataxia, hallucinations, anxiety, psychomotor agitation, decreased ability to concentrate, disorientation, confusion, dysarthria, hyperreflexia, muscle rigidity, choreoathetosis, epileptic syndrome.

From the SSS side: decreased blood pressure, tachycardia, arrhythmia, intracardiac conduction disturbances, ECG changes (especially QRS) characteristic of intoxication with tricyclic antidepressants, shock, heart failure; in very rare cases - cardiac arrest.

Others: respiratory depression, shortness of breath, cyanosis, vomiting, hyperthermia, mydriasis, increased sweating, oliguria or anuria.

Symptoms develop 4 hours after an overdose, reach a maximum after 24 hours and last 4-6 days. If an overdose is suspected, especially in children, the patient should be hospitalized.

Treatment: for oral administration: gastric lavage, intake of activated charcoal; symptomatic and supportive therapy; for severe anticholinergic effects (lowering blood pressure, arrhythmia, coma, myoclonic epileptic seizures) - administration of cholinesterase inhibitors (the use of physostigmine is not recommended due to the increased risk of seizures); maintaining blood pressure and water-electrolyte balance. Monitoring of cardiovascular functions (including ECG) is indicated for 5 days (relapse may occur after 48 hours or later), anticonvulsant therapy, artificial ventilation lungs (ventilator), etc. resuscitation measures. Hemodialysis and forced diuresis are ineffective.

Drug interactions

When ethanol is used together with drugs that depress the central nervous system (including other antidepressants, barbiturates, benzadiazepines and general anesthetics), a significant increase in the depressant effect on the central nervous system, respiratory depression and hypotensive effect is possible. Increases sensitivity to drinks containing ethanol.

Increases the anticholinergic effect of drugs with anticholinergic activity (for example, phenothiazine derivatives, antiparkinsonian drugs, atropine, biperiden, antihistamines), which increases the risk of side effects (from the central nervous system, vision, intestines and bladder). When used together with anticholinergic blockers, phenothiazine derivatives and benzodiazepines, there is a mutual enhancement of the sedative and central anticholinergic effects and an increased risk of epileptic seizures (lowering the threshold of convulsive activity); Phenothiazine derivatives may also increase the risk of neuroleptic malignant syndrome.

When used together with anticonvulsants, it is possible to enhance the inhibitory effect on the central nervous system, reduce the threshold of convulsive activity (when used in high doses) and reduce the effectiveness of the latter.

When used together with antihistamines, clonidine - increased inhibitory effect on the central nervous system; c - increases the risk of paralytic intestinal obstruction; with drugs that cause extrapyramidal reactions - an increase in the severity and frequency of extrapyramidal effects.

With the simultaneous use of amitriptyline and indirect anticoagulants (coumarin or indadione derivatives), the anticoagulant activity of the latter may increase. Amitriptyline may enhance depression caused by glucocorticosteroids (GCS). Medicines used to treat thyrotoxicosis increase the risk of developing agranulocytosis. Reduces the effectiveness of phenytoin and alpha-blockers.

Inhibitors of microsomal oxidation (cimetidine) prolong T1/2, increase the risk of developing toxic effects of amitriptyline (a dose reduction of 20-30% may be required), inducers of microsomal liver enzymes (barbiturates, carbamazepine, phenytoin, nicotine and oral contraceptives) reduce plasma concentrations and reduce the effectiveness of amitriptyline.

Combined use with disulfiram and other acetaldehydrogenase inhibitors provokes delirium.

Fluoxetine and fluvoxamine increase plasma concentrations of amitriptyline (a 50% reduction in amitriptyline dose may be required).

With the simultaneous use of amitriptyline with clonidine, guanethidine, betanidine, reserpine and methyldopa - a decrease in the hypotensive effect of the latter; with cocaine - the risk of developing cardiac arrhythmias.

Antiarrhythmic drugs (such as quinidine) increase the risk of developing rhythm disturbances (possibly slowing down the metabolism of amitriptyline).

Pimozide and probucol can increase cardiac arrhythmias, which manifests itself in prolongation QT interval on the ECG.

It enhances the effect of epinephrine, norepinephrine, isoprenaline, ephedrine and phenylephrine on the cardiovascular system (including when these drugs are part of local anesthetics) and increases the risk of developing heart rhythm disturbances, tachycardia, and severe arterial hypertension.

When co-administered with alpha-adrenergic agonists for intranasal administration or for use in ophthalmology (with significant systemic absorption), the vasoconstrictor effect of the latter may be enhanced.

At joint reception with thyroid hormones - mutual enhancement of the therapeutic effect and toxic effects (including cardiac arrhythmias and stimulating effects on the central nervous system).

M-anticholinergic drugs and antipsychotic drugs (neuroleptics) increase the risk of developing hyperpyrexia (especially in hot weather).

When co-administered with other hematotoxic drugs, increased hematotoxicity is possible.

Incompatible with MAO inhibitors (increased frequency of periods of hyperpyrexia, severe convulsions, hypertensive crises and patient death are possible).

special instructions

Before starting treatment, blood pressure monitoring is necessary (in patients with low or labile blood pressure, it may decrease even more); during the treatment period - control of peripheral blood (in some cases, agranulocytosis may develop, and therefore it is recommended to monitor the blood picture, especially with an increase in body temperature, development of flu-like symptoms and sore throat), during long-term therapy - control of the functions of the cardiovascular system and liver. In the elderly and patients with cardiovascular diseases, monitoring of heart rate, blood pressure, and ECG is indicated. Clinically insignificant changes may appear on the ECG (smoothing of the T wave, depression of the S-T segment, widening of the QRS complex).

Caution is required when suddenly moving into vertical position from a lying or sitting position.

During the treatment period, the use of ethanol should be avoided.

Prescribed no earlier than 14 days after discontinuation of MAO inhibitors, starting with small doses.

If you suddenly stop taking it after long-term treatment, withdrawal syndrome may develop.

Amitriptyline in doses above 150 mg/day. reduces the threshold of convulsive activity (the risk of epileptic seizures in predisposed patients should be taken into account, as well as in the presence of other factors predisposing to the occurrence of convulsive syndrome, for example, brain damage of any etiology, simultaneous use of antipsychotic drugs (neuroleptics), during the period of abstinence from ethanol or withdrawal of medications with anticonvulsant properties, such as benzodiazepines). Severe depression is characterized by a risk of suicidal actions, which can persist until significant remission is achieved. In this regard, at the beginning of treatment, a combination with drugs from the group of benzodiazepines or antipsychotic drugs and constant medical supervision (entrust trusted persons with the storage and dispensing of drugs) may be indicated. In children, adolescents and young adults (under 24 years of age) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and behavior. Therefore, when prescribing amitriptyline or any other antidepressants in this category of patients, the risk of suicide should be weighed against the benefits of their use. In short-term studies, the risk of suicide did not increase in people over 24 years of age, but it decreased slightly in people over 65 years of age. During treatment with antidepressants, all patients should be monitored for early detection of suicidal tendencies.

In patients with cyclic affective disorders during the depressive phase, manic or hypomanic states may develop during therapy (reducing the dose or discontinuing the drug and prescribing an antipsychotic drug is necessary). After relief of these conditions, if indicated, treatment in low doses can be resumed.

Due to possible cardiotoxic effects, caution is required when treating patients with thyrotoxicosis or patients receiving thyroid hormone preparations.

In combination with electroconvulsive therapy, it is prescribed only under the condition of careful medical supervision.

In predisposed patients and elderly patients, it can provoke the development of drug-induced psychoses, mainly at night (after discontinuation of the drug, they disappear within a few days).

May cause paralytic ileus, primarily in patients with chronic constipation, the elderly, or those forced to bed rest.

Before performing general or local anesthesia, the anesthesiologist should be warned that the patient is taking amitriptyline.

Due to the anticholinergic effect, there may be a decrease in tear production and a relative increase in the amount of mucus in the tear fluid, which can lead to damage to the corneal epithelium in patients using contact lenses.

With long-term use, an increase in the incidence of dental caries is observed. The need for riboflavin may be increased.

Animal reproduction studies have shown adverse effects on the fetus, and there are no adequate and well-controlled studies in pregnant women. In pregnant women, the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus.

Children are more sensitive to acute overdose, which should be considered dangerous and potentially fatal to them.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous species activities that require increased concentration and speed of psychomotor reactions.

Pregnancy and lactation

In pregnant women, the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus.

Passes into breast milk and may cause drowsiness in nursing infants. To avoid the development of withdrawal syndrome in newborns (manifested by shortness of breath, drowsiness, intestinal colic, increased nervous excitability, increased or decreased blood pressure, tremors or spastic phenomena), amitriptyline is gradually discontinued at least 7 weeks before the expected birth.

Use in childhood

Contraindicated for children under 6 years of age.

In children, adolescents and young adults (under 24 years of age) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and behavior. Therefore, when prescribing amitriptyline or any other antidepressants in this category of patients, the risk of suicide should be weighed against the benefits of their use

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

Store the drug in a dry place, protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children.

Shelf life - 3 years. Do not use after expiration date.

Antidepressant: Amitriptyline
Manufacturer: Zentiva Pharma LLC (Russia)
Active substance: Amitriptyline

Pharmacological action of an antidepressant

Amitriptyline belongs to the group of tricyclic antidepressants. Its action is based on blocking the reuptake of dopamine, serotonin and norepinephrine by CNS neurons. In addition, amitriptyline has an analgesic effect, as well as antibulimic and antiulcer effects. The drug is also effective in combating bedwetting. With regular and long-term use, it restores the balance of serotonin and norepinephrine transmission, shaken due to depression.
A pronounced antidepressant effect, as a rule, appears 2-4 weeks after the start of antidepressant use. For depression complicated by anxiety, amitriptyline reduces both depressive symptoms and agitation and anxiety. The antiulcer effect of the drug is due to its ability to block the functioning of histamine H2 receptors in the cells of the stomach. Thus, effective pain relief is achieved, as well as accelerated healing of stomach and duodenal ulcers.
The high effectiveness of amitriptyline in the treatment of bulimia nervosa does not yet have a scientific basis. However, it is well known that the drug shows good results in the fight against this disease (improvement in patients with bulimia occurs regardless of the presence/absence of depressive conditions; the antibulimic effect occurs even in the absence of an antidepressant effect).
A domestic study conducted in one of the Samara clinics showed that patients feel a significant reduction in anxiety and agitation, as well as motor restlessness already in the first days of taking amitriptyline. At 2-3 weeks of treatment, patients felt improved mood, increased self-esteem, a sharp decline feelings of sadness, depression and hopelessness. The feeling of guilt and suicidal tendencies disappeared.
In addition, a marked improvement in sleep was observed among all patients taking amitriptyline. Night sleep was completely normalized, sound and uninterrupted.

Indications for use

• treatment of depression of any origin (endogenous, neurotic, involutional, medicinal, reactive, with anxiety, sleep disorders and agitation, depression during alcohol withdrawal, as well as organic brain disorders);
• Treatment of mixed emotional disorders;
• Treatment of schizophrenic psychoses;
• Treatment of bulimia nervosa and psychogenic anorexia;
• Treatment of nocturnal enuresis, including in children (the drug is contraindicated in patients with bladder hypotension);
• Treatment of phobic disorders;
• Elimination of behavioral disorders (including activity and attention);
• Peptic ulcer of the stomach and duodenum;
• Prevention of headaches;
• Treatment of patients with chronic pain syndrome (atypical facial pain, migraines, chronic pain in cancer patients, postherpetic neuralgia, rheumatic pain, post-traumatic, peripheral and diabetic neuropathy).

Directions for use and dosage

Amitriptyline is taken orally during or after meals. You should start taking the drug at 50-75 mg/day. The dose should be divided into several doses of 25 mg each. In order to achieve an optimal therapeutic effect, the dose can be gradually increased by 25-50 mg. Extremely permissible dosage is 150-200 mg per day. However, most of it should be taken before bed. For extremely severe depression that cannot be treated, it is possible to increase the dose to 300 mg or even more, depending on individual tolerance to the drug. In such a situation, it is advisable to begin treatment with intravenous/intramuscular administration of the substance.
The therapeutic effect should appear no later than a month after starting to take amitriptyline. In this case, the dosage is gradually reduced, however, if signs of depression recur, you should return to the previous effective dose. If the drug does not show effectiveness after a 3-4 week course of treatment, it should be abandoned.
For elderly patients, the minimum dose is 25 mg/day, which can be increased gradually to 50-100 mg/day. When preventing headaches, as well as neurogenic pain, it is recommended to use the drug in an amount of 12.5-25 mg/day with a possible increase in dosage to 100 mg/day.
For severe depression, the drug is administered intramuscularly/intravenously at a dose of 10-20-30 mg, up to 3-4 injections per day. The maximum daily dose can be gradually increased and is 150 mg. After 7-14 days of injections, they switch to taking amitriptyline orally. Children (necessarily over 12 years of age) and elderly people are prescribed the minimum doses; dosage increases should occur more slowly.

Contraindications

Amitriptyline should not be taken by people with heart failure in the stage of decompensation, cardiac muscle conduction disorders, the period of myocardial infarction (including recovery after it), and arterial hypertension. The drug is prohibited for patients with prostatic hypertrophy, bladder atony, paralytic intestinal obstruction, as well as acute disorders of the liver and kidneys.
Pregnant women, nursing mothers, and children under 6 years of age (if taken orally) are prohibited from taking amitriptyline. Patients with hypersensitivity to amitriptyline should also not take this drug.

Side effects

Blurred vision, increased intraocular pressure, dry mouth, constipation, increased body temperature. These are consequences of the body’s adaptation to the drug, so they usually go away soon (sometimes it is necessary to reduce the dose). The following side effects occur from the nervous system: irritability, headache, tinnitus, sleep disorders, drowsiness, anxiety, etc. In addition, heart rhythm disturbances, heartburn, nausea, vomiting, taste disturbances, and increase in size may occur. mammary glands, as well as allergic reactions: skin itching, rash, urticaria. (see also Norpramin)

Storage conditions

The drug is stored out of the reach of small children at temperatures from 10 to 25°C in a dry, dark place.
Amitriptyline is also available under the brand names:

• • Amizol
  • Amirol
  • Amitriptyline

Antidepressant "Amitriptyline": 62 comments and patient reviews:

1. Sergey, 26, St. Petersburg Author of the post

   I’ve been taking it for depression for almost a month, 50 mg before bed. I woke up, some energy and activity appeared. Before that, I took Fevarin, to no avail, with bursts of mania. I'm happy with almost everything about Amitriptyline, but the side effects are overwhelming: problems with memory, terrible dryness, worse vision, shaking hands. But the antidepressant effect so far pays for this whole bouquet.

2. Belarus Post author

   I’m on the 4th day for VSD, asthenia, and depression, the doctor said two tablets (50 mg) a day, on the first day I almost went crazy, I reduced the dose to 0.5 twice a day, now I’m suffering from insomnia, dizziness, I can’t nothing to focus on. I knew that the first days would be hard, but not the same...

3. margarita

   Hello, I have been taking amitriptyline for two weeks and it seems to me that my anxiety, fear, and fear have decreased. It’s just that my vision and memory have gotten worse

4. Faith

   I was betrayed by a loved one. It was a strong blow for me. I took amitriptyline for six months, up to 3 tablets a day. It helped. Good product. I’ve gained a little weight, but compared to what I had before, it’s a small thing.

5. Julia

   I was prescribed this drug for chronic pain syndrome. Daily headaches, weakness. In general, neurasthenia with chronic tension headaches. Prescribed 10 mg at night. At first I took half a tablet (5 mg). The next day there was no headache. Gradually I switched to a whole tablet at night (10 mg).
   What to say? I’ve been drinking for three months now, but they told me to drink for at least six months. The drug is strong, in anti-depressant doses it is almost unrealistically heavy. There are many bad side effects, the worst of which is the cardio-toxic effect. My heart is beating so hard that I can hear my own pulse in my ears.
   And my head doesn't hurt!!!
   On the one hand, it’s scary to live with such tachycardia, but on the other hand, it’s scary to quit, in case the pain returns...
   In addition, it causes constipation and greatly increases appetite, without removing the asthenic component. In general, there is fat, but no energy. Hence the weight gain...
   Even in such small doses - 10 mg. For a blood pressure effect, the dose should be 150-200 mg.
   Unthinkable!

6. Natalia

   Pensioners are often at a loss after retirement, having become accustomed to a constant work schedule. I was no exception - I lost interest in life, I was pressed by some kind of longing for youth, I had nowhere to put myself. A friend suggested the drug “Biotredin”. And what? For me, it became a real panacea for the blues and thoughts that life is over.

7. Sasha

   When people get sick, it is a very big grief. I myself have recently begun to feel unwell. People need drugs such as Amitriptyline. So, I was in a very bad mood every day. Lived like in a dream. I woke up in the morning and already felt tired. My wife, she is a nurse, bought the drug from me. I want to say that he helped me a lot. Now everything is the same as before. I’m not sad and I want to live every day, and I’m grateful for that!!!

8. Galya

   I’ve been taking it for two weeks, they prescribed it to me after a cystoscopy, 25 mg, I’ve had urinary neuralgia for 13 years, nothing helped, I had severe pain, I constantly went to the toilet. And this medicine apparently cures me. It doesn’t hurt almost anymore.

9. Alex

   Please tell me, I have 10 mg tablets. how many times do you need to drink and for how long to walk during the day and it didn’t matter, excuse my French, and at night to sleep like a log and not stare at the ceiling until the morning...

10. Julia

    The drug is one of the cheapest, which is probably why it has so many side effects. I constantly want to sleep, my memory and vision are deteriorating, I have no strength or desire for anything. In combination with Pantogam Active, the condition improved slightly, some vigor appeared, but still, due to the lack of the desired effect, I switched to other tablets.

11. Vovan

    But it didn’t help me!

12. Tatiana

    Good afternoon The drug was prescribed to my mother. After an ischemic stroke, she began to recover, but hysterics appeared, 4 months ago she buried her dad, she always says that he is coming to pick her up. I took hydrozepam, maybe from it? One way or another, after the first amitriptyline tablet at night, he slept for the second day, the nurses could not wake him up. Yesterday the therapist stopped me from taking hydrosepam and amitriptyline and said that she was just sleeping. Today they called an ambulance, they say that she is unconscious, they are waiting for a therapist and a neurologist. I’m in Moscow, I just returned yesterday, my mother is in Ukraine, I don’t know what to do, I don’t trust local doctors anymore, I read somewhere that amitripcilline is generally contraindicated for cardiovascular disorders. If anyone can give useful advice, please help. Thank you! [email protected]

13. Konstantin 31 years old, Moscow

    I tried to take it with a small dose, but I couldn’t, my heart rate increased and there were interruptions in my heart rhythm. I took 1/4 25 mg for 3 days. I had to cancel. Tried to start 3 times, same result.

14. Arthur

    Hello everyone, after the second injection I stopped treatment, the condition was terrible. Can anyone tell me when to completely stop using amitripline?

15. Igor

    I had headaches as if I had a helmet on my head I didn’t sleep well I was irritated by the lamp light especially in rooms and car headlights the doctor diagnosed depression I started taking amitriptyline after 3 weeks my blood pressure started in my sleep I jump up because my heart is racing panic sets in This wasn’t the case earlier Everything that wasn’t there at all appeared It’s a dangerous thing, I don’t know what to do yet.

16. Elvira

    I took amitriptyline 3 months. I started reducing the dose to 1/4 at night. Nothing during the day, and again in the morning alarming symptoms began. I went to the doctor and she prescribed a new drug, fevarin. She said that for older people (I’m 59 years old) this that’s what you need. So I don’t know what’s better?

17. Svetlana

    My mother-in-law was prescribed this drug. She had fears, panic, and an excited state. After the appointment everything improved. Now there are exacerbations, we immediately start giving these pills and she calms down on about the third day. Complains of dry mouth only and memory. And so all is well.

18. Alexander

    I used drugs for many years, then started drinking heavily. Now I’m taking amitriptyline, I have anxiety, I’m sleeping soundly (2 tablets in the morning). Got a job, started a family. Amitriptyline is a drug for drug and alcohol addiction. Among the “side effects” are dry mouth, memory and attention have deteriorated.

19. Tatyana, 58 years old

    Three times in my life, amitriptyline helped me out like no other remedy when stress accumulated and a state of complete inability to “take the blows” and the inability to work with people, asthenia, set in. Despite the fact that as a psychotherapist she helped everyone, but she could not “settle” her life. Calm came, anxiety, tearfulness, uncertainty, and fear of circumstances disappeared. Only dry mouth is a side effect. The previous time I started drinking with 25 mg 3 times a day, without increasing the dose, but for a long time (up to 9 months) on the recommendation of a doctor. Now again the same period of life. I started on my own without a doctor. But I know that you need to “go away” by gradually reducing the dose every 5 days by 1/4. Nycomed is a better company. But for some reason, its reserves are “melting” in the city. And there are no 25 mg doses at all now. And dividing halves is inconvenient and troublesome. By the way, tell me, do they let him cross the border?

20. Denis 27, Irkutsk

    The drug is good, for me, at least. I drink it at night. I suffered from sleep disorders, anxiety, panic, “not good” thoughts in the morning, fatigue, etc. I started taking amitriptyline - everything was ok. At first - yes, the next day there was fatigue, lethargy, attention disorder, but this lasted about a week. An adaptation period, as I understand it. Afterwards - performance, vitality, and “bad” thoughts are gone.

21. Vladlena

    I have been taking the drug since the summer in combination with chlorprothixene. At the beginning there was no effect, there were some side effects, mostly very severe dryness, but after a month everything went away, I went to work, everything was great. Now I take 25 mg in the morning, 25 mg in the afternoon and 50 mg at night. The doctor and I tried to reduce the dose, but it didn’t work out yet, he said that it’s 3 months again. We drink, and then taper. The sleep is wonderful, but my attention is very impaired, for attention I was prescribed another medicine, I took a course and it became easier.

22. Pauline

    Prescribed for depression. Of course it helped. I drink for a week, I live calmly for a couple of months, not paying attention to stress. But when the effect ends, it’s just tough, don’t come to me, I destroy everything. The other day I started drinking a quarter again, in addition to all the side effects (dry mouth, weakness, sleep, deterioration of attention) numbness in my hands was added, the right one went away, but the left one is still dangling 🙁 But I can’t give up yet, I’m afraid. I don’t know what to replace it with yet. Tomorrow see the doctor.

23. Anastasia

    I took amitriptyline and it caused dryness and an unpleasant taste in my mouth, and I developed a fear of communication, as well as the skin on my hands began to crack.

24. Marina, 36 years old, Almaty

    I was in a psychoneurological clinic, they don’t use ammitriptyline there now. They treated me with expensive, new antidepressants... after discharge I became ill again, and the evening panics did not leave me alone. I’m now taking ammitriptyline on an outpatient basis, and I can’t be happier with how I feel. only for some reason they prescribed half of it in the morning and afternoon. I sleep like a horse day and night...what should I do? Someone tell me if it is possible to drink it in the afternoon. And yet, the course was prescribed for only a month, and then switch to tranquilizers, also for a month. I’m afraid to quit ammitriptyline...and maybe it will somehow help me out of depression in a month of taking it. Thanks a lot

25. yogann

    First you need to think about whether to accept it or you can still do without it, otherwise we grab everything that they advise and whatever comes to hand.

26. Svetlana, 49 years old, St. Petersburg

    Everything is very individual. If you experience side effects that worsen your quality of life, you should inform your doctor. For example, I was given strong side effects from Paxil, fluoxetine, and Lerivon, but I have been on amitriptyline for the 3rd month and have been working. Enjoying the life. I drank 2 months 3 times a day: in the morning 1/2, in the afternoon 1/2 and at night - a whole tablet, and since November daily dose removed it. There was only one side effect: I gained 5 kg... But this is nothing.

27. Alevtina

    I took this drug six months ago. Before I started taking it, I suffered from terrible depression, I didn’t want to live: I blamed myself for everything, I was afraid. I started taking amitriptyline 50 mg 3 times a day, I slept from it almost around the clock, dizziness, and tinnitus. But after a week, positive thoughts began to appear, my mood improved. I realized that my fears were greatly exaggerated, and I now consider my mistakes (not so terrible) as experience. After the first improvements, I lowered the dose, although they said it was impossible, not enough time had passed. I stopped taking it much earlier than prescribed. There was no withdrawal syndrome, I haven’t taken amitriptyline since the summer and everything is fine. But you still need to listen to doctors and take it as prescribed. The drug is good, at least it helped me a lot, otherwise I couldn’t get out of bed, I kept crying.
    Thank you to my family for being patient and supporting me)

G.

Yes, I also took it for 3 weeks, with increasing doses. I had secondary depression and didn’t sleep well, so in principle he helped me! But at the beginning of days 2 and 3 the condition was bad, everything was annoying! and after drinking the course that was prescribed to me, it became like I’m sorry, fuck everything.... I take everything that I really like less to heart)))

28. Maria, 35 years old, Moscow

    For those who are afraid to get hooked. I have been drinking in autumn-spring courses for a long time now. It turns out to be a natural break.
    There was a time when I only drank at night. But I noticed that my heart rate was increasing. I divided the dose into two doses: in the morning and in the afternoon. The action is the same, but the feeling is much more pleasant.

29. Natasha 36 years old Saratov

    They prescribed this disgusting thing, the condition is like a coma, I’ll stop drinking them, I tried it for only three days, all three days I felt depressed, heaviness throughout the body, but I need something completely different - performance and good mood, and here there’s just some kind of moronic calm, taking 1/4 of a tablet twice caused panic attacks. No, I’d rather do without antidepressants, it’s neurologists and psychiatrists who can’t do without prescribing them, let them prescribe them to those who have MDP, not VSD .before them, I only felt better, but on you - they ruined everything with this amitriptyline.

30. Tanya

    I just started taking amitriptyline 1/6 at night. Guys, a young man left me, these tablets in a small dose help a lot, I forgot about him and now I don’t care who he is or what he is!)))))))))))))))))))))))))))))))))))) I'm enjoying myself

31. Dmitriy

    After taking it, I had very pronounced side symptoms - half of my body went completely numb, especially in the morning (after 2 tablets at night) the dry mouth was terrible. I quit drinking it, walked around for another 2 days, withdrawal started, wow. I started catching glitches in the minibus. I won't touch this crap again.

32. Svetlana

    Good afternoon, I used to take amitriptyline, but then it stopped helping, a year ago I started taking it again, and it helped for the time being. I want to know how long the body should rest after taking amitriptyline...

33. Zhanna

    I’m saved only by it…..I’m already afraid that I won’t sit down on it and become dependent….It helps with headaches when you want to sleep, but the brain doesn’t turn off at all…and in the morning you get up in a terrible mood and condition….So that’s just it This is how I save myself, I try to drink only at night….

34. Angelica

    what happens if you take 2.5 packs of amitriptyline

35. Larisa
36. okrwkukdh
37. esbswrrre

    Cool + for the post

38. TerryRom

    Folks, I can suggest an excellent group for finding sponsors and kept women in Krasnodar.

Amitriptyline is an antidepressant from the group of non-selective neurotransmitter uptake inhibitors. According to its chemical structure, it belongs to tricyclic compounds. It is used in the treatment of many types of depression and their somatic manifestations. Why is Amitriptyline prescribed? The drug has antihistamine and anticholinergic effects, which allows it to be used for spastic conditions of smooth muscles.

Action and indications

The effect of the antidepressant Amitriptyline is that the drug prevents the reuptake of neurotransmitters such as serotonin, dopamine, and norepinephrine from the synaptic cleft. This tricyclic compound promotes the accumulation of nervous system mediators, prolonging and enhancing their action, which relieves symptoms of depression. Prescribing Amitriptyline after a stroke compensates for the lack of dopamine due to death nerve cells that produce it.

Amitriptyline also exhibits an adrenergic blocking effect and has an analgesic effect. Suppression of acetylcholine receptors allows the drug to be used for abdominal pain, bedwetting and overactive bladder. An antidepressant is also used in the treatment of ulcers by suppressing the formation of hydrochloric acid in the stomach. Suppression of acid production by the lining cells of the stomach also leads to a decrease in appetite, which is used in the treatment of bulimia.

List of pathologies that Amitriptyline helps with:

1. Depression of various origins, including those with an anxious and apathetic component, as well as somatic manifestations mental disorders.
2. Eating disorders as a manifestation of depression: bulimia (ravenous hunger), anorexia.
3. Prevention of migraine attacks.
4. Bedwetting in children and overactive bladder in adults.
5. Neuralgia and chronic pain syndrome for fibromyalgia, irritable bowel syndrome, cancer, etc.
6. Various phobias.
7. Post-stroke condition, especially in older people.
8. Withdrawal syndrome, i.e. abstinence from alcohol and drugs.
9. Psychosis in schizophrenia.

Side effects Amitriptyline:

1. Increased sensitivity to light due to paralysis of accommodation (dilated pupil).
2. Intestinal atony, manifested in constipation, sometimes dynamic obstruction.
3. Stomach atony, heartburn, belching, nausea.
4. Decreased bladder tone and urinary retention.
5. Hypertension.
6. Dry mouth and unpleasant odor from oral cavity.
7. Irritability.
8. Drowsiness.
9. Disturbances in the hormonal system: an increase in the hormone prolactin and swelling of the mammary glands, sometimes the release of milk from them, a violation menstrual cycle.
10. Changes in blood biochemistry from the liver: increased aminotransferases, direct bilirubin (cholestasis syndrome - bile stagnation).
11. Hyperglycemia.

Important! Amitriptyline withdrawal syndrome may be accompanied by cholinergic effects - drooling, gastrointestinal cramps and diarrhea.

This is a drug with a powerful effect that affects the cardiovascular and nervous system. Contraindications to the use of Amitriptyline:

1. Exacerbation of ulcerative processes in the stomach and duodenum.
2. Tachycardia (rapid heartbeat).
3. Hypertonic disease.
4. Atony of the stomach and intestines, stenosis of the pyloric part of the stomach.
5. Decreased bladder tone.
6. Prostatic hyperplasia.
7. Decompensated heart failure.
8. Angle-closure glaucoma.
9. The use of other drugs from the group of antidepressants - serotonin syndrome is possible.
10. Chronic convulsive states- an antidepressant may increase the frequency of attacks of epilepsy and other movement disorders.
11. Drinking alcohol. Amitriptyline may increase nervous system depression ethyl alcohol.
12. Thyrotoxicosis.

How to take Amitriptyline for depression? Take the drug for the first time at night after meals in a dosage of 25-50 mg. For the next 5 days, take 50 mg three times a day.

The therapeutic effect in the treatment of depressive conditions appears after 2-4 weeks of use. If the symptoms of depression disappear, then the dose is reduced to 50 mg per day. This maintenance dose is taken for three months to prevent relapses.

To prevent migraine pain, use 25 mg-100 mg daily.

Before completely stopping Amitriptyline, doctors gradually reduce the dosage of the drug. It is possible to prescribe adaptogens (rhodiola, ginseng) to prevent Amitriptyline withdrawal syndrome; addiction to it can be controlled by correct treatment tactics.

golmozg.ru

Amitriptyline

Compound

Amitriptyline dragees and tablets contain 10 or 25 mg active substance in the form of amitriptyline hydrochloride.

Additional substances in the tablets are: microcrystalline cellulose, talc, lactose monohydrate, silicon dioxide, magnesium stearate, pregelatinized starch.

Additional substances in the dragees are: magnesium stearate, potato starch, talc, polyvinylpyrrolidone, lactose monohydrate.

1 ml of solution contains 10 mg of active substance. Additional substances are: hydrochloric acid (sodium hydroxide), dextrose monohydrate, water for infusion, sodium chloride, benzethonium chloride.

Release form

The drug is available in the form of tablets, dragees and solution.

pharmachologic effect

Tricyclic antidepressant. Has a sedative, thymoleptic effect. It has an additional analgesic effect of central origin.

Pharmacodynamics and pharmacokinetics

MNN: Amitriptyline.

The drug reduces appetite, eliminates nighttime urinary incontinence, and has an antiserotonin effect. The drug has a strong central and peripheral anticholinergic effect. The antidepressant effect is achieved by increasing the concentration of serotonin in the nervous system and norepinephrine in synapses. Long-term therapy leads to a decrease in the functional activity of serotonin and beta-adrenergic receptors in the brain. Amitriptyline reduces the severity of depressive symptoms, agitation, and anxiety in anxiety-depressive conditions. By blocking H2-histamine receptors in the stomach wall (parietal cells), an antiulcer effect is provided. The medication is able to reduce body temperature, level blood pressure with general anesthesia. The drug does not inhibit monoamine oxidases. The antidepressant effect appears after 3 weeks of therapy.

The maximum concentration of the substance in the blood occurs after a few hours, usually after 2-12. Excreted as metabolites in urine. Binds well to proteins.

Indications for use of Amitriptyline

What are tablets and solution usually prescribed for?

The drug is indicated for depression (agitation, anxiety, sleep disturbances, alcohol withdrawal, organic brain lesions, neurotic withdrawal), behavioral disorders, mixed emotional disorders, nocturnal enuresis, chronic pain syndrome (for cancer pathology, postherpetic neuralgia), for nervous bulimia, for migraines (for prevention), for ulcerative lesions digestive system. Indications for the use of Amitriptyline in tablets and in other forms of release are the same.

Contraindications

According to the annotation, the medicine is not used for myocardial infarction, intolerance to the main component, for closed-angle glaucoma, acute intoxication with psychoactive, analgesic, hypnotic drugs, for acute alcohol intoxication. The medication is contraindicated in breastfeeding, severe intraventricular conduction disorders, and antioventricular conduction disorders. With pathology of the cardiovascular system, with suppression of bone marrow hematopoiesis, manic-depressive psychoses, bronchial asthma, chronic alcoholism, decreased motor function of the digestive system, stroke, pathology of the liver and kidneys, intraocular hypertension, urinary retention, prostatic hyperplasia, with hypotension of the bladder , thyrotoxicosis, pregnancy, epilepsy Amitriptyline is prescribed with caution.

Side effects of Amitriptyline

Nervous system: agitation, hallucinations, disorientation, fainting, asthenia, drowsiness, anxiety, hypomanic state, increased depression, depersonalization, motor restlessness, increased epileptic seizures, extrapyramidal syndrome, ataxia, myoclonus, paresthesia in the form of peripheral neuropathy, small muscle tremor, headache.

Anticholinergic effects: increased intraocular pressure, blurred vision, mydriasis, dry mouth, tachycardia, difficulty urinating, paralytic ileus, delirium, confusion, decreased sweating.

Cardiovascular system: instability of blood pressure, intraventricular conduction disorders, arrhythmia, orthostatic hypotension, dizziness, palpitations, tachycardia.

Digestive tract: darkening of the tongue, diarrhea, changes in taste perception, vomiting, heartburn, gastralgia, hepatitis, cholestatic jaundice.

Endocrine system: galactorrhea, hyperglycemia, decreased potency or increased libido, increased size of the mammary glands, gynecomastia, testicular swelling, syndrome of inappropriate ADH secretion, hyponatremia. Hypoproteinemia, pollakiuria, urinary retention, enlarged lymph nodes, hyperpyrexia, swelling, tinnitus, and hair loss are also noted.

When discontinuing the drug, unusual agitation, sleep disturbances, malaise, headache, diarrhea, nausea, unusual dreams, restlessness, and irritability are noted. At intravenous administration There is a burning sensation, lymphangitis, thrombophlebitis, and an allergic response.

Reviews of the side effects of Amitriptyline are quite frequent. When using the drug, addiction may also occur.

Amitriptyline, instructions for use (Method and dosage)

The medicine is taken orally immediately after eating, without chewing, which ensures the least irritation of the stomach walls. The initial dosage is 25-50 mg at night for adults. Within 5 days, the amount of the drug is increased to 200 mg per day in 3 doses. If there is no effect within 2 weeks, the dose is increased to 300 mg.

Solutions are administered slowly intravenously and intramuscularly, 20-40 mg 4 times a day with a gradual transition to oral administration. The course of therapy is no more than 8 months. For prolonged headaches, for migraines, chronic pain syndrome of neurogenic origin, for migraines, 12.5-100 mg per day is prescribed.

Instructions for use of Amitriptyline Nycomed are similar. Before use, be sure to familiarize yourself with the contraindications for the drug.

Overdose

Manifestations from the nervous system: coma, stupor, increased drowsiness, anxiety, hallucinations, ataxia, epileptic syndrome, choreoathetosis, hyperreflexia, dysarthria, rigidity muscle tissue, confusion, disorientation, impaired concentration, psychomotor agitation.

Manifestations of an overdose of Amitriptyline from the cardiovascular system: disturbance of intracardiac conduction, arrhythmia, tachycardia, drop in blood pressure, shock, heart failure, rarely - cardiac arrest.

Anuria, oliguria, increased sweating, hyperthermia, vomiting, shortness of breath, depression of the respiratory system, and cyanosis are also noted. Maybe drug poisoning.

To avoid negative consequences overdose requires emergency gastric lavage and administration of cholinesterase inhibitors in case of severe anticholinergic manifestations. It is also required to maintain water and electrolyte balance, blood pressure levels, control over the functioning of the cardiovascular system, and carry out resuscitation and anticonvulsant measures if necessary. Forced diuresis, as well as hemodialysis, have not proven effective in treating an overdose of Amitriptyline.

Interaction

A hypotensive effect, respiratory depression, and a depressant effect on the nervous system are observed with the joint prescription of medications that depress the functioning of the central nervous system: general anesthetics, benzodiazepines, barbiturates, antidepressants and others. The drug enhances the severity of the anticholinergic effect when taking amantadine, antihistamines, biperiden, atropine, antiparkinsonian drugs, phenothiazine. The drug enhances the anticoagulant activity of indadione, coumarin derivatives, and indirect anticoagulants. There is a decrease in the effectiveness of alpha-blockers and phenytoin. Fluvoxamine and fluoxetine increase the concentration of the drug in the blood. The risk of developing epileptic seizures increases, and the central anticholinergic and sedative effects also increase when combined with benzodiazepines, phenothiazines, and anticholinergics. Simultaneous administration of methyldopa, reserpine, betanidine, guanethidine, clonidine reduces the severity of their hypotensive effect. When taking cocaine, arrhythmia develops. Delirium develops when taking acetaldehydrogenase inhibitors, disulfiram. Amitriptyline enhances the effects of phenylephrine, norepinephrine, epinephrine, and isoprenaline on the cardiovascular system. The risk of hyperpyrexia increases when taking antipsychotics and m-anticholinergics.

Terms of sale

Prescription or not? The medicine is not sold without a prescription.

Storage conditions

In a dry, dark place, out of reach of children, at a temperature of no more than 25 degrees Celsius.

Best before date

No more than 3 years.

special instructions

Before carrying out therapy, monitoring blood pressure levels is mandatory. Parenteral Amitriptyline is administered exclusively under the supervision of a physician in a hospital setting. In the first days of treatment it is necessary to observe bed rest. A complete abstinence from ethanol intake is required. Abrupt refusal of therapy can cause withdrawal syndrome. The drug at a dose of more than 150 mg per day leads to a decrease in the threshold of convulsive activity, which is important to consider when developing epileptic seizures in patients with a predisposition. It is possible to develop hypomanic or manic states in persons with cyclical, affective disorders during the depressive phase. If necessary, treatment is resumed with small doses after relief of these conditions. Caution should be exercised when treating patients with thyrotoxicosis when treating individuals taking thyroid hormone medications due to the possible risk of cardiotoxic effects. The medication can provoke the development of paralytic intestinal obstruction in elderly people, as well as those prone to chronic constipation. It is imperative to warn anesthesiologists about taking amitriptyline before performing local or general anesthesia. Long-term therapy provokes the development of caries. The need for riboflavin may increase. Amitriptyline passes into breast milk and causes increased drowsiness in infants. The medication affects driving.

The medicine is described in Wikipedia.

Amitriptyline and alcohol

Amitriptyline analogues

Analogues of the drug are: Sarotene and Amitriptyline Hydrochloride.

Reviews of Amitriptyline

Reviews from doctors

Counts good antidepressant, however, has many side effects, for example: drowsiness, indifference, dry mouth. May be addictive. The product should be taken only as prescribed by a doctor.

Reviews of Amitriptyline Nycomed on forums

A good drug for depression. There are opinions about the narcotic effect of the medication. Lots of side effects.

Amitriptyline price, where to buy

The price of Amitriptyline in 10 mg tablets in Russia is 25 rubles for 50 pieces. You can buy 25 mg tablets in Moscow for 50 rubles per 50 pieces.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

WER.RU

• Amitriptyline tablets 25 mg 50 pcs. Moscow endocrine plant
• Amitriptyline-Grindeks tablets 10 mg 50 pcs.
• Amitriptyline tablets 10 mg 50 pcs. ALSI Pharma
• Amitriptyline tablets 25 mg 50 pcs. Ozon LLC

ZdravZone

• Amitriptyline 25 mg No. 50 tabletsMoscow endocrine plant Federal State Unitary Enterprise
• Amitriptyline 25 mg No. 50 tablets /Ozone/Ozone LLC
• Amitriptyline 20mg/2ml No. 10 amp. Moscow Endocrine Plant Federal State Unitary Enterprise
• Amitriptyline 25 mg No. 50 tablets Takeda Pharma A/S Denmark/Takeda Fa
• Amitriptyline 10 mg No. 50 tabletsAlsi Pharma CJSC

Pharmacy IFC

• AmitriptylineNycomed, Denmark

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Pharmacy24

• Amitriptylinosis GNCLS (Ukraine, Kharkov)
• AmitriptylineTechnolog (Ukraine, Uman)

PaniPharmacy

• Amitriptyline h/x tablet. 0.025g No. 25Technologist
• Amitriptyline h/x tablet. 0.025g No. 25Technologist

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BIOSPHERE

• Amitriptyline 25 mg No. 50 tablet Zentiva a.s. (Slovakia)

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NOTE! Information about medications on the site is for reference and general information, collected from publicly available sources and cannot serve as a basis for making a decision on the use of medications in the course of treatment. Before use medicinal product Be sure to consult your doctor for amitriptyline.

medside.ru

Amitriptyline and products based on it: indications, instructions, reviews

Amitriptyline is a synthetic drug used to treat depression, nervous disorders, psychogenic anorexia and other pathologies caused by psychological disorders. Belongs to tricyclic antidepressants.

Amitriptyline is produced by many pharmaceutical companies, both under the same trade name and under other names: Amirol, Triptisol, Elivel, Amizol, etc.

The active ingredient in all drugs is amitriptyline hydrochloride. Tablet forms are available containing 10 and 25 mg of the active ingredient per tablet, and injection forms contain 20 mg of amitriptyline in each ampoule (2 ml).

In addition to the active ingredient, the composition also contains auxiliary substances. They differ from one manufacturer to another. Most often, the injection solution contains glucose and water, and the tablets contain starch, MCC, lactose monohydrate, talc and magnesium stearate.

Pharmacological action and its mechanism

Amitriptyline has antidepressant, anticholinergic, antiulcer, antiserotinic, some analgesic, sedative, thymoleptic effects, and also eliminates enuresis.

The antidepressant effect of the drug is manifested due to its ability to suppress the reverse neuronal uptake of norepinephrine, serotonin and dopamine membranes of presynaptic neurons.

The accumulation of these neurotransmitters ensures an improvement in psychological state and the disappearance of signs of depression.

When using drugs in this group, the so-called “antidepressive threshold” must be taken into account. It manifests itself in individual perception of the drug, as a result of which for each patient it is necessary to select a dose of the drug that will reduce the uptake of neurotransmitters by 5-10 times.

If this is not achieved, then the antidepressant effect will not appear, but only nonspecific effects and side effects will be present. The antidepressant effect of treatment with the drug appears no earlier than after 2-3 weeks of continuous use.

Thanks to the demonstrated thymoleptic effect, there is an improvement in well-being and mood.

The anticholinergic effect is provided by a strong affinity for m-cholinergic receptors. Due to its affinity for h2-histamine receptors and its alpha-adrenergic blocking effect, the drug has a strong sedative effect.

The antiulcer effect of the drug is achieved due to its property of blocking h3 receptors in gastric cells. In this case, there is an elimination of pain and acceleration of healing of ulcerative-erosive lesions of the gastrointestinal mucosa.

The analgesic effect of the drug is associated with an increase in the concentration of monoamines, in particular serotonin, in the central nervous system.

Elimination of urinary incontinence at night is provided by anticholinergic action, which increases the ability of the bladder to distend, as well as beta-adrenergic stimulation, which leads to increased sphincter tone.

The mechanism of action of the drug in the fight against bulimia has not yet been clarified. Amitriptyline is effective for bulimia with and without depression.

Pharmacokinetics of the drug

Amitriptyline is well and quickly absorbed when it enters the gastrointestinal tract. The maximum content in the blood is observed after 2-6 hours, the half-life is about 10-26 hours. The active substance binds to blood proteins very well, almost 95%.

The drug is metabolized in the liver, forming active and inactive metabolites. The elimination of the drug is ensured by the kidneys. Complete elimination from the body occurs in 1-2 weeks.

The drug penetrates the histohematic and placental barriers, as well as into breast milk.

Indications for use

Indications for the use of Amitriptyline are as follows:

Contraindications for use

Amitriptyline has a large number of contraindications that significantly limit the possibility of its use; taking the medication is prohibited if:

• myocardial infarction in the acute and recovery period;
• acute liver diseases;
• heart failure;
• disorders of myocardial conduction functions;
• hypertension;
• exacerbations of gastric and duodenal ulcers;
• impaired renal function;
• prostate hypertrophy;
• paralytic ileus;
• pyrolytic stenosis;
• atony of the bladder;
• pregnancy;
• breastfeeding;
• children under 6 years of age (tablets) and 12 years of age (injection forms);
• hypersensitivity to the components of the drug;
• simultaneous use of MAO inhibitors, as well as with a break of less than 2 weeks after taking them.

Particular care should also be taken when using the medicine when:

• alcoholism;
• bronchial asthma;
• epilepsy;
• inhibition of the hematopoietic process;
• glaucoma;
• schizophrenia;
• manic-depressive psychosis;
• intraocular hypertension.

How to take the medicine - scheme and dosage

Amitriptyline tablets are taken orally during or immediately after a meal.

The dosage of the drug is selected on a strictly individual basis. The initial daily dose is usually from 50 to 75 mg, divided into 2-3 doses.

The dose of the drug must be gradually increased until the best therapeutic effect is achieved. Usually it is enough to increase the intake to 150-200 mg per day, but in some cases it may be necessary to take 300 mg or more (up to the maximum tolerated dose). In this case, the daily dose is also divided into 3 doses, with most of the dose taken at night.

2 weeks to a month after achieving the required severity of the therapeutic effect, the dosage of the drug begins to be gradually reduced. Abruptly discontinuing the drug is prohibited due to the possible development of withdrawal syndrome.

If the symptoms of depression begin to return, then taking the medication in high doses is started again. The drug is discontinued (gradually) if there is no treatment success within a month of therapy. Elderly patients are advised not to exceed a daily dose of 100 mg.

In case of severe severe depression, the drug is taken intravenously or intramuscularly at a dose of 10-40 mg up to 4 times a day.

The maximum permissible daily dose is 150 mg. After 1-2 weeks, injections should be gradually replaced with the tablet form of the drug.

To get rid of migraines and chronic neurogenic pain, the drug is taken at a dose of 12.5-100 mg per day.

For the treatment of childhood enuresis, the drug is prescribed 10-25 mg at bedtime. The dose is calculated individually based on the recommendation of 2.5 mg per kg of child weight.

For childhood depression, 1.5 mg per kg of body weight is prescribed.

Cases of overdose

Excessive use of Amitriptyline may result in an overdose. Since everyone has a different sensitivity threshold to the drug, it is impossible to accurately say the amount of the drug that will provoke this condition.

In case of overdose, the following are noted: disorientation, shortness of breath, fever, dizziness, dilated pupils, disturbances of consciousness, arrhythmia, increased drowsiness, hypotension, respiratory depression, hallucinations, agitation, convulsions, coma.

If any symptoms of overdose occur, stop taking the drug immediately and contact a medical facility for help. Gastric lavage, normalization of water-electrolyte balance and blood pressure, and symptomatic therapy are carried out.

Monitoring the state of the cardiovascular system for at least 5 days is very important, since the attack may recur after 48 hours or more.

Amitriptyline, when taken in large quantities, causes numerous side effects. Taking it can provoke the development of problems with almost all organs and systems.

Due to blocking of m-cholinergic receptors, it can:

• increase intraocular pressure;
• dry mouth occurs;
• impaired vision;
• delayed urination;
• constipation and intestinal obstruction occur;
• sweating increases;
• accommodation paresis develops;
• body temperature rises.

These side effects usually disappear after getting used to the drug or as a result of reducing the dose.

Other side effects caused by the complex manifestation of all the actions of the drug are also possible:

• disturbances in concentration;
• excessive sleepiness;
• nightmares;
• dizziness;
• dysarthria;
• tachycardia;
• changes in the blood picture;
• nausea;
• anorexia;
• motor excitement;
• symptoms of heart failure;
• hallucinations;
• heartburn;
• arrhythmia;
• noise in ears;
• stomatitis;
• pain and discomfort in the epigastrium;
• change in tongue color;
• decreased libido;
• taste disturbance;
• glucosuria;
• swelling of the testicles;
• angioedema;
• breast growth;
• weight gain;
• hair loss;
• galactorrhea;
• blood pressure lability;
• enlarged lymph nodes.

With long-term use of high doses of the drug, cardiotoxicity is likely to develop.

Separately, it should be noted the symptoms characteristic of withdrawal syndrome: increased excitability, diarrhea, nausea, headaches, vomiting, irritability, sleep disturbances with unusual dreams.

special instructions

Amitriptyline reduces attention and causes drowsiness. Because of this, its use is not recommended when driving, as well as performing work that requires increased concentration.

Drug and alcohol

While using Amitriptyline, drinking alcohol is strictly prohibited, as this can lead to serious consequences.

This is explained by the similarity of the mechanisms of action of the drug and alcohol, which is expressed in the mutual strengthening of the effect on the body and the most pronounced toxic effect.

With the simultaneous use of alcohol and medication, the temperature and blood pressure may rise significantly, the heart rhythm may be disturbed, and paralytic obstruction may occur.

In addition, due to the inhibitory effect on the respiratory center, breathing may be impaired until it stops completely and death occurs.

Also, the simultaneous use of alcohol and Amitriptyline has a very negative effect on the liver and kidneys. Toxic liver necrosis and severe renal dysfunction may develop.

Other important nuances

It is prohibited to take the drug if there are serious dysfunctions of these organs.

The use of the drug during pregnancy and lactation is prohibited. Tablets are taken from the age of 6 years, and injection solution– from 12.

Practical application experience

Amitriptyline is a fairly old drug, so there are a sufficient number of reviews about it from both doctors and patients. For the most part they are positive, but there are also nuances.

A word from the experts

Amitriptyline is one of the most effective antidepressants. When taking it, patients experience an improvement in mood almost after the first doses, and after a week of treatment, an increase in self-esteem is observed.

After a full course of treatment, one can note the disappearance of nightmares, improved sleep quality and the disappearance of suicidal tendencies.

Psychiatrist

Amitriptyline gives fairly good results in the treatment of depression and other psychoneurotic disorders. It is somewhat difficult to select the optimal dose. It is very important to inform patients about possible side effects and withdrawal syndrome.

Maria Karlovna, general practitioner

Ordinary people say

I was prescribed Amitriptyline to relieve panic, anorexia and depression. I started to notice the first improvements after 10 days of taking it.

Now I live and enjoy life, I’m no longer afraid to go out and ride in public transport, my sleep has improved and my appetite has appeared.

Tips for taking Amitriptyline from patients:

• take only as prescribed by a doctor;
• carefully read the instructions before starting treatment and keep them throughout the entire treatment period;
• do not exceed recommended doses;
• Increase the dose gradually;
• Under no circumstances should it be taken simultaneously with alcohol.

Pros and cons based on reviews and practical experience

• high efficiency;
• affordable price.

• many contraindications and side effects;
• prescription sales.

Purchasing the drug and its analogues

average price Amitriptyline in pharmacies:

• table 25 mg No. 50 – 29 -60 rubles;
• table 10 mg No. 50 – 20-50 rubles;
• 2ml ampoules No. 10 – 25-67 rubles.

The drug is dispensed from pharmacies strictly according to a doctor's prescription.

Quite a lot of Amitriptyline analogs are produced that have a similar active ingredient: Vero-Amitriptyline, Nycomed Damilena maleinate, Saroten retard, Elivel, Amizol, Elivel, Amirol.

In some cases, it is possible to replace it with a drug of the same pharmacological group: Clofranil, Doxepin, Melipramine, etc. Such a replacement of drugs can only be carried out by the attending physician.

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neurodoc.ru

Amitriptyline - instructions for use, what it helps with, spectrum of use, rules for taking an antidepressant, analogue drugs

Amitriptyline instructions for use are classified as tricyclic antidepressants. These are some of the strongest drugs at a fairly reasonable price. But today, experts are divided on the possibility of recommending this drug in the first line of therapy.

Due to the presence of a large number of side effects of tricyclic antidepressants, their poor tolerability profile, and violation of the rules for taking medications by patients, which leads to an increase in morbidity, and sometimes to fatal outcome, many experts, including international ones, pay more attention to new generation drugs. They are comparable in effect to Amitriptyline, but have fewer side effects. Nevertheless, Amitriptyline is used quite successfully in psychiatric practice.

What is Amitriptyline?

Amitriptyline is an antidepressant, one of the most common. In addition to depression, it fights anxiety and has a pronounced hypnotic and calming (sedative) effect. In certain doses it can act as a psychoenergetic and stimulant. For each patient, the interval in which the drug has such an effect is individual.

When it is exceeded, the calming properties of the drug come to the fore, and the stimulating and depression-reducing properties recede into the background. Of its group of drugs, Amitriptyline is considered the most reliable, effective and cheapest. You can find Amitriptyline tablets starting at 26 rubles for 10 tablets.

Very often when depressive disorders Treatment does not begin with this group of drugs, but, for example, with monoamine oxidase inhibitors. If you are taking any thymoanaleptics (antidepressants) or anxiolytics (drugs that reduce anxiety), you need to warn your doctor.

Because some drugs are very dangerous to use together. For example, MAO inhibitors should never be taken together with tricyclic antidepressants. This threatens death. If you need to change one drug to another, there should be a pause of at least 2 weeks between taking MAO inhibitors and tricyclic antidepressants.

Before taking the drug Amitriptyline, the instructions for use must be read carefully and strictly follow the indicated dosages. This product is produced both in ampoules and tablets. For outpatient use, Amitriptyline tablets are usually prescribed.

Amitriptyline: instructions for use (official)

Range of application of the drug

What can amitriptyline help with? Amitriptyline is an antidepressant, therefore, its main purpose is to fight depression. It is applicable for any type of depression, but most often Amitriptyline tablets are indicated for use in depressive states of an endogenous nature (that is, arising for internal reasons).

What does Amitriptyline help with, besides depression? Amitriptyline tablets are indicated for use in migraines and are prescribed as a preventive measure. It is given to children with enuresis, if the cause of the pathology does not lie in the bladder with weak tone. Amitriptyline is a medicine that works well:

• with anxiety;
• diverse pathological fears(phobias);
• eating disorders (bulimia and anorexia) of a neurogenic nature.

Unlike many other drugs of its group, it does not cause hallucinations, at least in most cases. In some cases, this antidepressant is also used by somatic medicine in very small dosages to reduce symptoms. neurotic conditions.

Rules for taking Amitriptyline

How is the drug taken? Strictly as prescribed by a doctor, as it interacts when taken orally with drugs for the treatment of other serious pathologies. The instructions for use recommend taking amitriptyline after meals and according to the schedule, starting with minimal doses and increasing the dosage by 25 mg every day until the working dose is reached.

The minimum dose is considered to be 50 mg per day per dose; 150 mg/day, 200/250/300 mg per day can be prescribed as a working dose. The size of this dose is determined by the severity of the pathological process. The daily dose is recommended to be divided into several doses (2-4). The last dose should be taken before bedtime. The instructions for the antidepressant Amitriptyline also prescribe slowly stopping taking it, gradually reducing the dose.

Consequences of abrupt refusal

If you abruptly stop taking the drug, the patient may experience the so-called “withdrawal syndrome”:

1. discomfort;
2. headache;
3. nervousness;
4. sleep disorders.

These are not signs of dependence on the drug, but the consequences of its sudden withdrawal. For children and elderly people, the medicine is prescribed in reduced doses. In the case of severe forms of depression, complicated by suicidal thoughts or actions, treatment of the patient with Amitriptyline in large doses is possible only in a hospital. Since in some cases there is a suicidal effect of the drug, including a delayed one.

Side effects and contraindications

This drug is usually well tolerated, but, nevertheless, it may cause an allergy to the active substance or excipients. chemical substances in the composition. Visual symptoms (accommodation disorder), intestinal dysfunction (constipation, diarrhea, heartburn and paresis) are noted.

Impaired urinary function (urinary retention, atony of the bladder), vestibulopathy, lethargy, apathy, increased drowsiness (especially with too intense dose increases), decreased libido. When used in large doses or too quickly administered intravenously, convulsive epileptiform seizures may occur. In some cases, there are disturbances in sensitivity (temperature, pain, etc.), spontaneous and pathological leakage of milk from the mammary glands, gynecomastia, weight gain, liver dysfunction, changes in the blood count.

Analogues for the drug Amitriptyline: tablets Saroten Retard, Elivel, Amitriptyline-Grindeks, Amitriptyline Nikomend

This remedy is not prescribed to children under 12 years of age, women during pregnancy, especially in the first and last trimester (except in extreme cases) and nursing mothers. During the experiments, the teratogenic effect of the drug was revealed. If the medicine could not be discontinued while the child is pregnant, then at least a week before giving birth, you need to reduce the dosage and stop taking it before delivery so that the child does not develop withdrawal syndrome.

While taking this medication, you should not engage in activities that require attention and quick reaction, including driving a car.

Drugs with similar effects

Amitriptyline – INN (that is, international generic name). Patented products containing Amitriptyline as an active ingredient include:

• Saroten Retard,
• Elivel,
• Damile Maleinat,
• Amitriptyline-Grindeks,
• Vero-Amitriptyline,
• Amitriptyline Nycomend.

The latter is quite common. For Amitriptyline Nycomed 25 mg, the instructions for use are similar to those for regular domestic Amitriptyline; it costs approximately 53 rubles per package. Prescription drug. Prescriptions for such drugs are written using Latin. For Amitriptyline the prescription is for Latin will look like this:

Amitriptyline

Rp.: Tab. Amitriptylini 0.025 No. 20

D.S. 2 tablets each 4 times a day after meals to treat depression.

Video: Treatment of panic attacks and neuroses and the concept of the meaning of life

Gross formula

C 20 H 23 N

Pharmacological group of the substance Amitriptyline

Nosological classification (ICD-10)

CAS Code

50-48-6

Characteristics of the substance Amitriptyline

Tricyclic antidepressant. Amitriptyline hydrochloride is a white, odorless, crystalline powder, easily soluble in water, ethanol, and chloroform. Molecular weight 313.87.

Pharmacology

pharmachologic effect- antidepressant, anxiolytic, thymoleptic, sedative.

Inhibits the reuptake of neurotransmitters (norepinephrine, serotonin) by the presynaptic nerve endings of neurons, causes the accumulation of monoamines in the synaptic cleft and enhances postsynaptic impulses. With long-term use, it reduces the functional activity (desensitization) of beta-adrenergic and serotonin receptors in the brain, normalizes adrenergic and serotonergic transmission, and restores the balance of these systems, disturbed during depressive states. Blocks m-cholinergic and histamine receptors of the central nervous system.

When taken orally, it is quickly and well absorbed from the gastrointestinal tract. The bioavailability of amitriptyline by different routes of administration is 30-60%, its metabolite - nortriptyline - 46-70%. Cmax in the blood after oral administration is achieved within 2.0-7.7 hours. Therapeutic concentrations in the blood for amitriptyline are 50-250 ng/ml, for nortriptyline - 50-150 ng/ml. Blood protein binding is 95%. Easily passes, like nortriptyline, through histohematic barriers, including the BBB, placental, and penetrates into breast milk. T1/2 is 10-26 hours, for nortriptyline - 18-44 hours. In the liver it undergoes biotransformation (demethylation, hydroxylation, N-oxidation) and forms active - nortriptyline, 10-hydroxy-amitriptyline, and inactive metabolites. It is excreted by the kidneys (mainly in the form of metabolites) within several days.

In anxiety-depressive conditions, it reduces anxiety, agitation and depressive symptoms. The antidepressant effect develops within 2-3 weeks after the start of treatment. If you suddenly stop taking it after long-term treatment, withdrawal syndrome may develop.

Use of the substance Amitriptyline

Depression of various etiologies (especially with severe anxiety and agitation), incl. endogenous, involutional, reactive, neurotic, with organic brain damage, medicinal; schizophrenic psychoses, mixed emotional disorders, behavioral disorders, bulimia nervosa, childhood enuresis(except for children with bladder hypotension), chronic pain syndrome (neurogenic), migraine prevention.

Contraindications

Hypersensitivity, use of MAO inhibitors in the previous 2 weeks, myocardial infarction (acute and recovery periods), heart failure in the stage of decompensation, intracardiac conduction disorders, severe arterial hypertension, benign prostatic hyperplasia, bladder atony, paralytic ileus, pyloric stenosis, peptic ulcer stomach and duodenum in the acute stage, acute diseases of the liver and/or kidneys with severe impairment of their function, blood diseases, children under 6 years of age (for injection forms- up to 12 years old).

Restrictions on use

Epilepsy, coronary artery disease, arrhythmia, heart failure, angle-closure glaucoma, intraocular hypertension, hyperthyroidism.

Use during pregnancy and breastfeeding

Contraindicated during pregnancy.

Treatment should be stopped during treatment breast-feeding.

Side effects of the substance Amitriptyline

Caused by blockade of peripheral m-cholinergic receptors: dry mouth, urinary retention, constipation, intestinal obstruction, blurred vision, accommodation paresis, increased intraocular pressure, increased sweating.

From the nervous system and sensory organs: headache, dizziness, ataxia, increased fatigue, weakness, irritability, drowsiness, insomnia, nightmares, motor agitation, tremor, paresthesia, peripheral neuropathy, EEG changes, impaired concentration, dysarthria, confusion, hallucinations, tinnitus.

From the cardiovascular system: tachycardia, orthostatic hypotension, arrhythmia, blood pressure lability, widening of the QRS complex on the ECG (impaired intraventricular conduction), symptoms of heart failure, fainting, changes in the blood picture, incl. agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, purpura.

From the gastrointestinal tract: nausea, vomiting, heartburn, anorexia, discomfort in the epigastrium, gastralgia, increased activity of liver transaminases, stomatitis, taste disturbance, darkening of the tongue.

From the side of metabolism: galactorrhea, changes in ADH secretion; rarely - hypo- or hyperglycemia, impaired glucose tolerance.

From the genitourinary system: changes in libido, potency, testicular swelling, glucosuria, pollakiuria.

Allergic reactions: skin rash, itching, angioedema, urticaria.

Others: increase in the size of the mammary glands in women and men, hair loss, enlarged lymph nodes, photosensitivity, weight gain (with long-term use), withdrawal syndrome: headache, nausea, vomiting, diarrhea, irritability, sleep disturbance with vivid, unusual dreams, increased excitability (after long-term treatment, especially in high doses, with abrupt cessation of taking the drug).

Interaction

Incompatible with MAO inhibitors. Strengthens the inhibitory effect on the central nervous system of neuroleptics, sedatives and hypnotics, anticonvulsants, analgesics, anesthetics, alcohol; exhibits synergism when interacting with other antidepressants. When used together with neuroleptics and/or anticholinergic drugs, the development of a febrile temperature reaction and paralytic intestinal obstruction is possible. Potentiates the hypertensive effects of catecholamines and other adrenergic stimulants, which increases the risk of developing heart rhythm disturbances, tachycardia, and severe arterial hypertension. May reduce the antihypertensive effect of guanethidine and drugs with a similar mechanism of action, as well as weaken the effect anticonvulsants. When used simultaneously with anticoagulants - derivatives of coumarin or indanedione - it is possible to increase the anticoagulant activity of the latter. Cimetidine increases plasma concentrations of amitriptyline with possible development toxic effects, inducers of microsomal liver enzymes (barbiturates, carbamazepine) - reduce. Quinidine slows the metabolism of amitriptyline; estrogen-containing oral contraceptives may increase bioavailability. Concomitant use with disulfiram and other acetaldehyde dehydrogenase inhibitors may provoke delirium. Probucol may increase cardiac arrhythmias. Amitriptyline may enhance glucocorticoid-induced depression. When used together with drugs for the treatment of thyrotoxicosis, the risk of developing agranulocytosis increases. Use caution when combining amitriptyline with digitalis and baclofen.

Overdose

Symptoms: hallucinations, convulsions, delirium, coma, cardiac conduction disturbances, extrasystole, ventricular arrhythmia, hypothermia.

Treatment: gastric lavage, taking an activated carbon suspension, laxatives, fluid infusion, symptomatic therapy, maintaining body temperature, monitoring the function of the cardiovascular system for at least 5 days, because relapse of disorders may occur after 48 hours or later. Hemodialysis and forced diuresis are ineffective.

Routes of administration

Inside, intramuscularly.

Precautions for the substance Amitriptyline

Amitriptyline can be taken no earlier than 14 days after stopping MAO inhibitors. Reduced doses are recommended for elderly patients and children. Should not be prescribed to patients with mania. Due to the possibility of suicide attempts in patients with depression, regular monitoring of patients is necessary, especially in the first weeks of treatment, as well as administration in the minimum required doses to reduce the risk of overdose. If there is no improvement in the patient's condition within 3-4 weeks, it is necessary to reconsider the treatment tactics. During treatment, you should avoid drinking alcohol, as well as avoid activities that require increased attention and speed of reactions.