Medicinal reference book geotar. Medicinal reference book geotar Effective and safe treatment

There are contraindications. Before starting use, consult your doctor.

Commercial names abroad (abroad) - Apo-Levocarb, Carbilev, Cronomet, Dopadura C, Dopicar, Duodopa, Half Sinemet, Kardopal, Lebocar, Levocarb, Levocomp, Levodopa Comp, Levodopa-Carbi, Levomed, Levomet, Parcopa, Pardopa, Parkimet, Sinacarb, Sinemet, Striaton.

All drugs used in neurology and psychiatry.

You can ask a question or leave a review about the medicine (please, do not forget to indicate the name of the drug in the text of the message).

Preparations containing Levodopa (L) and Carbidopa (K) - ATC code N04BA02:

Common forms of release (more than 100 offers in Moscow pharmacies)
Name	Release form	Packaging, pcs.	Manufacturer country	Price in Moscow, r	Offers in Moscow
Nakom	tablets 250mg L + 25mg K	100	Slovenia, Lek	1010- (average 1418) -2854	707↗
Tidomet Forte	tablets 250mg L + 25mg K	100	India, Torrent	570- (average 674↗) -757	244↗
Tremonorm	tablets 250mg L + 25mg K	100	Israel, Teva	637- (average 705) -897	173↗
Rarely encountered and discontinued release forms (less than 100 offers in Moscow pharmacies)
Carbidopa/Levodopa	tablets 250mg L + 25mg K	100	Cyprus, Remedica	No	No
Tidomet LS	tablets 100 mg L + 10 mg K	100	India, Torrent	No	No
Duellin	tablets 250mg L + 25mg K	50	Hungary, Egis	No	No
Zimox	tablets 250mg L + 25mg K	30	Greece, Faran	No	No
Syndopa	tablets 250mg L + 25mg K	50	India, San	No	No

Nakom - official instructions for use. The drug is a prescription, the information is intended only for healthcare professionals!

Clinical and pharmacological group

An antiparkinsonian drug is a combination of a dopamine precursor and a peripheral dopa decarboxylase inhibitor.

pharmachologic effect

Antiparkinsonian drug. Levodopa reduces the symptoms of Parkinson's disease by increasing dopamine levels in the brain. Carbidopa, which does not cross the BBB, interferes with the extracerebral decarboxylation of levodopa, thereby increasing the amount of levodopa that enters the brain and is converted into dopamine.

Nacom® has a more pronounced therapeutic effect Compared with levodopa, it provides long-term maintenance of therapeutic plasma concentrations of levodopa at doses that are approximately 80% lower than those required with levodopa alone.

The effect of the drug appears within the first day after the start of administration, sometimes after taking the first dose. The maximum effect is achieved within 7 days.

Pharmacokinetics

Carbidopa:

Suction

After oral administration of carbidopa in a single dose in patients with Parkinson's disease, Tmax ranges from 1.5 hours to 5 hours.

Metabolism and excretion

Metabolized in the liver.

Among the metabolites excreted in the urine, the main ones are alpha-methyl-3-methoxy-4-hydroxyphenylpropionic acid and alpha-methyl-3.4-dihydroxyphenylpropionic acid, which account for about 14% and 10% of excreted metabolites, respectively. Two other metabolites are found in smaller quantities. One of them was identified as 3.4-dihydroxyphenyl-acetone, the other was tentatively identified as N-methyl-carbidopa. The content of each of these substances is no more than 5% of total number metabolites. Unchanged carbidopa is also detected in urine. No conjugates were identified.

Removal

Urinary excretion of unchanged drug is mainly completed within 7 hours and amounts to 35%.

Levodopa:

Suction

Levodopa is rapidly absorbed from the gastrointestinal tract and is actively metabolized. Despite the fact that more than 30 different metabolites are formed, levodopa is mainly converted to dopamine, epinephrine, and norepinephrine.

After oral administration of levodopa in a single dose in patients with Parkinson's disease, Tmax is 1.5-2 hours and is maintained at a therapeutic level for 4-6 hours.

Removal

Metabolites are quickly excreted in the urine - about 1/3 of the dose is excreted within 2 hours.

T1/2 of levodopa is about 50 minutes.

When taking a combination of carbidopa and levodopa, T1/2 of levodopa increases to approximately 1.5 hours.

Effect of carbidopa on levodopa metabolism

Carbidopa increases the concentration of levodopa in the blood plasma. With previous administration of carbidopa, the concentration of levodopa in the blood plasma increases approximately 5 times, and the time to maintain therapeutic concentrations in plasma increases from 4 to 8 hours. When taking carbidopa and levodopa simultaneously, similar results were obtained.

In patients with Parkinson's disease who had previously taken carbidopa, when taking levodopa in a single dose, T1/2 of levodopa increased from 3 to 15 hours. The concentration of levodopa increases due to carbidopa by at least 3 times. The concentration of dopamine and homovanillic acid in the blood plasma and urine decreases with prior administration of carbidopa.

Indications for use of the drug NACOM®

• treatment of Parkinson's disease and parkinsonism syndrome.

Dosage regimen

The optimal daily dose is determined through careful individual selection. The shape of the tablet allows it to be divided into two parts with minimal effort.

During treatment, adjustments to both the individually selected dose and the frequency of taking the drug may be required. Studies have shown that peripheral dopa decarboxylase is saturated with carbidopa when the latter is taken at a dose of about 70-100 mg per day. Nausea and vomiting may occur in patients receiving lower doses of carbidopa.

If Nakoma is prescribed, standard medications for the treatment of parkinsonism, with the exception of those containing levodopa alone, can be continued, and their doses should be re-selected.

The initial dose is selected according to the indications and the patient's response to treatment. The initial dose of Nacom® is 1/2 tablet 1-2 times a day. However, this dose may not provide the optimal amount of carbidopa that the patient will require. Therefore, if necessary, add 1/2 Nakoma tablet every day or every other day until the optimal effect is achieved. The therapeutic effect is observed on the first day, and sometimes after taking the first dose. Full effect The drug is achieved within 7 days.

When switching from levodopa preparations, the latter should be discontinued at least 12 hours before starting treatment with Nakom® (24 hours in the case of prolonged-release levodopa preparations). The daily dose of Nacom® should provide approximately 20% of the previous daily dose of levodopa.

For patients who have taken more than 1.5 g of levodopa, the initial dose of Nakoma is 1 tablet 3-4 times a day.

During maintenance therapy, if necessary, the dose of Nakoma can be increased by 1/2-1 tablet every day or every other day until the maximum dose is reached - 8 tablets per day. Experience with carbidopa at doses greater than 200 mg per day is limited.

Side effect

Most often - dyskinesia, including involuntary movements (including choreiform, dystonic), as well as nausea.

Early signs on the basis of which a decision can be made to discontinue the drug are muscle twitching and blepharospasm.

From the central nervous system and peripheral nervous system: NNS, episodes of bradykinesia (“on-off” syndrome), dizziness, drowsiness, paresthesia, episodes of psychotic states, including illusions, hallucinations and paranoid thinking, depression with or without the development of suicidal intentions, dementia , sleep disorders, agitation, confusion, increased libido.

In rare cases, convulsions, but a causal relationship with taking the drug Nakom® has not been established.

From the outside digestive system: possible anorexia, vomiting, bleeding from the gastrointestinal tract, exacerbation of peptic ulcer duodenum, diarrhea, darkening of saliva.

From the body as a whole: possible fainting, chest pain.

From the outside of cardio-vascular system: arrhythmias and/or palpitations, orthostatic effects (including episodes of increased or decreased blood pressure), phlebitis.

From the hematopoietic system: leukopenia, anemia (including hemolytic), thrombocytopenia, agranulocytosis.

From the outside respiratory system: possible dyspnea.

Dermatological reactions: possible alopecia, rash, darkening of the secretion of the sweat glands.

From the outside genitourinary system: darkening of urine.

Allergic reactions: angioedema, urticaria, itchy skin, Henoch-Schönlein disease.

Other side effects that may occur as a result of taking levodopa:

From the digestive system: dyspepsia, dry mouth, feeling of bitterness in the mouth, sialorrhea, dysphagia, bruxism, attacks of hiccups, pain and discomfort in the abdomen, constipation, flatulence, burning sensation of the tongue.

Metabolism: loss or increase in body weight, edema.

From the central nervous system: weakness, fainting, fatigue, headache, asthenia, decreased mental activity, disorientation, ataxia, stupor, increased hand tremors, muscle cramps, trismus, activation of latent Bernard-Horner syndrome, insomnia, anxiety, euphoria, psychomotor agitation, unsteady gait.

From the senses: diplopia, blurred vision, dilated pupils, oculogyric crises.

From the genitourinary system: urinary retention, urinary incontinence, priapism.

From laboratory parameters: increased activity of alkaline phosphatase, AST, ALT, LDH, increased bilirubin, urea nitrogen in plasma, increased serum creatinine, hyperuricemia, positive test Coombs, decreased hemoglobin and hematocrit, hyperglycemia, leukocytosis, bacteriuria, erythrocyturia.

Medicines containing carbidopa and levodopa may cause false positive reaction for ketone bodies in urine, if test strips are used to determine ketonuria. This reaction will not change after boiling urine samples. False-negative results can be obtained when using the glucose oxidase method for determining glycosuria.

Contraindications to the use of the drug NACOM®

• angle-closure glaucoma;
• melanoma established or suspected;
• skin diseases unknown etiology;
• simultaneous use with non-selective MAO inhibitors;
• hypersensitivity to the components of the drug.

The drug should be used with caution when serious illnesses cardiovascular system, incl. in case of myocardial infarction with disturbances heart rate(in history), heart failure, severe diseases of the respiratory system, including bronchial asthma, seizures (history), including epileptic, erosive and ulcerative lesions of the gastrointestinal tract (due to the possibility of bleeding from the upper gastrointestinal tract), decompensated diseases endocrine system, including diabetes mellitus, severe renal failure, severe liver failure, open-angle glaucoma.

Use of the drug NACOM® during pregnancy and breastfeeding

The effect of Nakoma on the course of pregnancy in women is unknown. Experimental studies have revealed that the combination of levodopa and carbidopa causes visceral and skeletal changes in animals. Therefore, the use of the drug is possible only when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.

It is not known whether they are isolated from breast milk levodopa and carbidopa.

There is one report of levodopa excretion in breast milk in a nursing mother with Parkinson's disease. Therefore, due to the possible serious harmful effects of the drug on the newborn and taking into account the importance of therapy for the mother, if it is necessary to use the drug during lactation, the issue of either stopping breastfeeding or discontinuing the drug Nacom® should be decided.

Use for liver dysfunction

Use with caution in patients with severe hepatic impairment.

Use for renal impairment

Use with caution in patients with renal failure severe.

Use in children

special instructions

As with the use of levodopa, when prescribing Nakoma to patients who have had a myocardial infarction and have atrial, nodal or ventricular arrhythmias, a thorough preliminary examination is necessary. In such patients, it is necessary to monitor cardiac activity, especially when prescribing the first dose and during the dose selection period.

Patients with open-angle glaucoma should prescribe Nacom® with caution and subject to constant monitoring intraocular pressure during treatment.

Since side effects are more likely to occur with a combination of carbidopa and levodopa than with levodopa alone, patients should be closely monitored during dosage titration. In particular, Nacom® causes involuntary movements more often than levodopa. The appearance of involuntary movements may require a dose reduction. Blepharospasm may be an early sign of overdose in some patients. If the therapeutic response to the drug levodopa is inconsistent, and the signs and symptoms of Parkinson's disease are not controlled throughout the day, then switching to Nacom® usually reduces the fluctuation in response to the drug.

Nacom® provides patients with adequate reduction of symptoms of Parkinson's disease.

Nacom® is also indicated for patients with parkinsonism taking vitamin preparations containing pyridoxine hydrochloride (vitamin B6).

Nacom® can be prescribed to patients already receiving drugs containing only levodopa, however, levodopa should be discontinued at least 12 hours before starting treatment with Nacom®. Nacom® should be prescribed in doses that provide approximately 20% of the previous dose of levodopa.

Patients who have previously taken levodopa may experience dyskinesia, because Carbidopa allows more levodopa to reach the brain, and thus more dopamine is produced. The appearance of dyskinesia may require a dose reduction.

Like levodopa, Nacom® may cause involuntary movements or mental disorders. It is assumed that these reactions are due to an increase in dopamine levels in the brain. These phenomena may require dose reduction. All patients taking Nacom® should be monitored for the possibility of developing depressive state with suicidal tendencies. Patients who have experienced psychosis require a careful approach when selecting therapy.

Nakom® and psychotropic drugs should be prescribed with caution. When antiparkinsonian drugs are abruptly discontinued, a symptom complex resembling neuroleptic malignant syndrome has been described, including muscle rigidity, increased body temperature, mental disturbances, and increased serum CPK concentrations. Therefore, careful examination of patients is necessary during sharp decline dose of Nakoma® or its withdrawal, especially if the patient is receiving antipsychotics. As with levodopa, during long-term treatment Nakom recommends periodic monitoring of the functions of the liver, hematopoietic, cardiovascular systems and kidneys.

If you want to general anesthesia, then Nacom® can be taken as long as the patient is allowed oral fluids and medications.

If treatment is temporarily interrupted, Nakoma can be resumed at the usual dose as soon as the patient is able to take the drug orally.

Use in pediatrics

The safety of the drug in young and middle-aged children has not been established.

Overdose

Symptoms: increased side effects.

Treatment: Close observation and ECG monitoring should be ensured to identify possible arrhythmias, and adequate antiarrhythmic therapy should be administered if necessary. It is necessary to take into account the possibility that, along with Nacom®, the patient was taking other medications.

Drug interactions

When using Nakom in patients receiving antihypertensive therapy, symptomatic orthostatic hypotension was observed (at the beginning of treatment with Nakom®, in such cases, dose adjustment of the antihypertensive drug may be required).

When levodopa is used simultaneously with MAO inhibitors (except for MAO type B inhibitors), circulatory disorders are possible (taking MAO inhibitors should be discontinued 2 weeks before starting levodopa). This is due to the accumulation of dopamine and norepinephrine under the influence of levodopa, the inactivation of which is inhibited by MAO inhibitors. As a result, there is a high probability of developing agitation, increased blood pressure, tachycardia, facial flushing and dizziness.

There are isolated reports of adverse reactions, including increased blood pressure and dyskinesia, in the case of combined use of tricyclic antidepressants and Nakoma.

The bioavailability of carbidopa and/or levodopa is reduced with simultaneous use of iron sulfate or iron gluconate.

With simultaneous use of levodopa with beta-agonists, ditilin and inhalation anesthesia agents, the risk of developing heart rhythm disturbances may increase.

Dopamine D2 receptor antagonists (eg, phenothiazines, butyrophenones and risperidone), as well as isoniazid, may reduce the therapeutic effect of levodopa.

There are reports of blocking the beneficial therapeutic effects of levodopa in Parkinson's disease as a result of taking phenytoin and papaverine. Patients taking these medications concomitantly with Nakom® require careful monitoring to promptly detect a decrease in therapeutic effect.

Lithium preparations increase the risk of developing dyskinesias and hallucinations.

When used simultaneously, methyldopa increases side effect Nakoma.

Concomitant use of tubocurarine increases the risk of arterial hypotension.

Absorption of levodopa may be impaired in some patients on a high-protein diet because levodopa competes with certain amino acids.

Carbidopa interferes with the action of pyridoxine hydrochloride (vitamin B6), which accelerates the biotransformation of levodopa into dopamine in peripheral tissues.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

List B. The drug should be stored out of the reach of children at a temperature not exceeding 25°C. Shelf life - 3 years. Do not use after the expiration date stated on the package.

Dispensed only with a doctor's prescription.

Included in the list medicines, dispensed with a doctor's prescription with the provision of additional free medical care certain categories of citizens entitled to receive state social assistance.

TRADE NAMES

Vero-Levocarbidopa, Dopar 275, Duellin, Zymox, Izikom, Izikommite, Carbidopa and levodopa, Credanil 25/250, Levodopa + Carbidopa, Nakom, Sindopa, Sinemet, Striaton, Tidomet LS, Tidomet plus, Tidomet forte, Tremonorm.

DRUG FORM

Pills.
Controlled release tablets.

HOW DOES THE DRUG WORK?

Antiparkinsonian combination remedy. Levodopa is a precursor to dopamine. Dopamine is formed in the deep structures of the brain; its deficiency causes the development of parkinsonism (shaking paralysis).

Dopamine itself does not penetrate the brain well, so it makes no sense to take it in pill form. Its predecessor, levodopa, penetrates the brain, accumulates in the basal ganglia, where it is converted into dopamine, replenishing its deficiency. As a result, muscle tension, trembling decreases, stiffness, drooling, and swallowing disorders go away. The drug is well absorbed in the intestines, but some of it is already converted into dopamine in the blood, which causes side effects. In this regard, it is advisable to combine levodopa with substances that block the enzyme that destroys levodopa. Carbidopa inhibits the destruction of levodopa and the formation of dopamine in peripheral tissues, which can significantly reduce the dose of levodopa, increase its concentration in the brain and reduce side effects. The optimal combination of levodopa and carbidopa is 4:1 or 10:1.

IN WHAT CASES IS THE MEDICATION PRESCRIBED?

For the treatment of Parkinson's disease, symptomatic parkinsonism (except those caused by antipsychotic drugs).

APPLICATION OF THE DRUG

ADMISSION RULES
The drug is taken orally with meals, 1/4 tablet 2-3 times a day, with a small amount of water.

Then the dose is increased by 1/4 tablet every 2-3 days until therapeutic effect. Typically, the optimal effect is observed when taking 1-2 tablets per day. Maximum daily dose 1.5 g levodopa and 150 mg carbidopa (6 tablets).

Foods high in protein may reduce the absorption of the drug.

DURATION OF ADMISSION
The effect of the drug appears within the first day from the start of treatment, sometimes after taking the first dose. The full effect is achieved within 7 days.

The treatment is long-term. During treatment, periodic monitoring of mental status, general, biochemical analyzes blood, general analysis urine, blood pressure, pulse.

IN CASE OF MISSING A DOSE
If you miss a dose, take the medicine as soon as you remember. If it is close to your next pill, skip the dose and take the medicine as usual. You should not take a double dose of the drug.

OVERDOSE
Cases of overdose have not been described.

EFFECTIVE AND SAFE TREATMENT

CONTRAINDICATIONS
Hypersensitivity, angle-closure glaucoma, severe psychosis or psychoneurosis, melanoma and suspicion of it and skin diseases of unknown etiology, pregnancy, lactation, age under 12 years.

SIDE EFFECTS
At the beginning of treatment: nausea, vomiting, loss of appetite, epigastric pain, difficulty swallowing, ulcerogenic effect (in predisposed patients); in some cases - rhythm disturbances, decreased blood pressure when changing position.
During further treatment: spontaneous movements (hyperkinesis), dyskinesia; hemolytic anemia, leukopenia, thrombocytopenia; mental disorders, insomnia, increased excitability, depression; tachycardia, constipation, weight gain (with long-term use).

YOU MUST TELL YOUR DOCTOR
you are suffering peptic ulcer stomach or duodenum and there is abdominal pain, vomiting blood or black stools (signs of bleeding from an ulcer, which requires emergency measures help).
You are taking antidepressants, drugs to lower blood pressure, vitamins, and anticonvulsants.
You are taking any other medications, including over-the-counter medications, herbs, and dietary supplements.
Have you ever had allergic reaction for any medicine.

If you are pregnant
Do not take during pregnancy!

If you are breastfeeding
Do not take while breastfeeding!

If you suffer from other diseases
Patients with glaucoma should monitor intraocular pressure. Sick diabetes mellitus Dose adjustment may be required hypoglycemic drugs, blood sugar levels need to be monitored. When planning surgical intervention treatment is not stopped until anesthesia is administered.

If you drive a car/work with machinery
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. If you give the drug to children

Contraindicated in children under 12 years of age.

INTERACTIONS
Use with other medications
Weaken the effect of the drug: anticonvulsants, antipsychotics (neuroleptics), antidepressants, vitamin B6 (pyridoxine), papaverine, clonidine and reserpine.

With simultaneous use of the drug with anti-asthmatic drugs and anesthetics, the risk of developing heart rhythm disturbances may increase.

With lithium preparations, the risk of developing uncontrolled movements and hallucinations increases; with methyldopa - worsening side effects.

You should not combine the drug with MAO inhibitors (antidepressants). Monoamine oxidase inhibitors should be discontinued 2 weeks before starting treatment.

STORAGE RULES
Store at a temperature not exceeding 25 °C in a dry, dark place out of reach of children.

Recipe (international)

Rp.: Levodopa 0.5 (Levopa)
D.t. d. N. 500 in caps, gelat.
S. 1 capsule 4 times a day.

Recipe (Russia)

Prescription form - 107-1/у

Active substance

Levodopa, Benserazide

pharmachologic effect

Antiparkinsonian drug. Active substance It is a precursor of dopamine, which it turns into as a result of decarboxylation.
The drug reduces rigidity and hypokinesia, tremor, dysphagia and salivation, increases range of motion, and restores the ability to concentrate.

Mode of application

For adults: Method of administration and dosage of Levodopa
Inside, with a small amount of food or after a meal, with water and without chewing. Since there is competition between aromatic amino acids and levodopa for absorption, large amounts of protein should be avoided while using the drug.
The average daily dose of carbidopa required to suppress the peripheral conversion of levodopa is 70-100 mg. Exceeding 200 mg of carbidopa does not entail a further increase in the therapeutic effect. The daily dose of levodopa should not exceed 2000 mg.
The initial dose is 1/2 tablet 2 times a day, if necessary, it can be increased by 1/2 tablet per day. As a rule, at the beginning replacement therapy daily dose should not exceed 3 tablets per day (1 tablet 3 times a day).
Use at this dosage is recommended at the beginning of treatment of severe cases of parkinsonism.
As an exception, the daily dose of the drug can be increased during monotherapy, but should not exceed 8 tablets (1 tablet 8 times a day). Use of more than 6 tablets per day should be done with great caution.

Indications

Parkinson's disease, parkinsonism syndrome (except for parkinsonism caused by antipsychotics).

Contraindications

- hypersensitivity to levodopa, benserazide or any other component of the drug;

- severe dysfunction of the endocrine system;

- glaucoma;

- severe liver dysfunction;

- severe renal dysfunction;

- severe dysfunction of the cardiovascular system;

- endogenous and exogenous psychoses;

- simultaneous use with non-selective MAO inhibitors, a combination of MAO type A and MAO type B inhibitors (which is equivalent to non-selective MAO inhibition);

- women of childbearing age who do not use reliable methods of contraception;

- pregnancy;

- period of breastfeeding;

Side effects

From the hematopoietic system: very rarely - hemolytic anemia, transient leukopenia, thrombocytopenia.

From the nervous system: often - headache, dizziness, convulsions, spontaneous movement disorders (such as chorea and athetosis), episodes of freezing, weakening of the effect towards the end of the dose period, on-off phenomenon, increased manifestations of restless legs syndrome; very rarely - severe drowsiness, episodes of sudden drowsiness.

Mental disorders: rarely - agitation, anxiety, depressed mood, insomnia, delirium, aggression, depression, anorexia, moderate enthusiasm, pathological gambling, hypersexuality, increased libido; very rarely - hallucinations, temporary disorientation.

From the cardiovascular system: very rarely - arrhythmias, orthostatic hypotension (weakens after reducing the dose of the drug), increased blood pressure; frequency unknown - hot flashes.

From the digestive system: very rarely - nausea, vomiting, diarrhea, isolated cases of loss or change in taste, dryness of the oral mucosa; frequency unknown - gastrointestinal bleeding.

From the skin and subcutaneous tissues: rarely - skin itching, rash.

From laboratory parameters: infrequently - transient increase in the activity of liver transaminases, alkaline phosphatase, increase in bilirubin concentration, increase in urea and creatinine in the blood, change in urine color to red, darkening when standing.

Other: frequency unknown - febrile fever, excessive sweating.

Release form

Tablets 100 mg + 25 mg: 20, 30, 50, 60 or 100 pcs.
Tablets 200 mg+50 mg: 20, 30, 50, 60 or 100 pcs.

ATTENTION!

The information on the page you are viewing is created for informational purposes only and does not in any way promote self-medication. The resource is intended to provide healthcare workers with additional information about certain medications, thereby increasing their level of professionalism. Use of the drug "" in mandatory involves consultation with a specialist, as well as his recommendations on the method of use and dosage of the medicine you have chosen.

pharmacodynamics. Carbidopa and Levodopa-Teva is a combined antiparkinsonian drug containing the metabolic precursor of dopamine, levodopa, and the peripheral dopadecarboxylase inhibitor, carbidopa.

It is believed that the symptoms of Parkinson's disease are associated with insufficient dopamine. Normally, dopamine functions as a neurotransmitter and is synthesized in certain brain cells that control muscle activity. Movement disorders considered a consequence of dopamine deficiency.

The antiparkinsonian effect of levodopa is due to its conversion to dopamine by decarboxylation directly in the central nervous system, which leads to replenishment of dopamine deficiency in nerve cells.

Carbidopa does not cross the BBB and interferes with the extracerebral decarboxylation of levodopa, thereby increasing the entry of levodopa into the brain and its conversion to dopamine in the central nervous system, which leads to a decrease in the severity of symptoms of Parkinson's disease in many patients.

Pharmacokinetics. Levodopa and carbidopa are well absorbed, the Cmax of the drug in the blood plasma is reached after 1-3 hours. Half-life of levodopa is about 2 hours in the presence of carbidopa. As a result of the action of carbidopa, the elimination of levodopa from blood plasma is reduced by 50%. In the presence of carbidopa, levodopa is mainly metabolized to amino acids and, in small quantities, to catecholamine derivatives. All metabolites of carbidopa and levodopa are excreted in the urine.

INDICATIONS

Parkinson's disease and syndrome.

APPLICATION

The tablet has a dividing line, that is, the tablet can be divided in half.

The optimal daily dose of carbidopa/levodopa is determined by careful titration individually for each patient.

Depending on the severity of the disease, it may take about 6 months to achieve the optimal therapeutic effect.

Patients, not taking levodopa. For patients starting to take the drug, the initial dose is ½ tablet 1-2 times a day. If necessary, you can add another ½ tablet every subsequent day until you reach required dose carbidopas.

The therapeutic effect of the drug appears on the same day, sometimes after just one dose. Full effective dose the drug is achieved within 7 days compared to weeks and months of using levodopa alone.

Patients taking levodopa. Levodopa should be discontinued at least 12 hours in advance (24 hours for dosage forms slow release) before starting therapy with Carbidopa and Levodopa-Teva. Usually the drug is taken in the morning, and levodopa is not used at night. The dose of the drug should be about 20% of the previous daily dose of levodopa.

Initial dose. Patients taking<1500 мг леводопы в сутки: начальная суточная доза должна составлять 75-100 мг карбидопы и 300-400 мг леводопы (применяют препарат с дозированием карбидопы/леводопы в соотношении 1:4), разделенная на 3-4 приема. Пациенты, принимающие >1500 mg of levodopa per day: the initial dose of the drug is 1 tablet 3-4 times a day.

Maintenance dose. When treating with Carbidopa and Levodopa-Teva, one should take into account individual characteristics patient, dosage should be gradually adjusted depending on the therapeutic effect.

If it is necessary to use levodopa at a higher dose, the dose of the drug can be increased to 1 tablet 3-4 times a day. If necessary, the dose can be increased by ½-1 tablet every day (maximum daily dose - 8 tablets).

If a patient is transferred to Carbidopa and Levodopa-Teva from levodopa in combination with other decarboxylase inhibitors, the use of the drugs should be discontinued at least 12 hours before starting Carbidopa and Levodopa-Teva. The drug is started with a dose equivalent to the amount of levodopa/decarboxylase inhibitor in previous drugs.

Patients taking other antiparkinsonian drugs. The combination of the drug with MAO-B inhibitors may increase the effectiveness of Carbidopa and Levodopa-Teva in controlled cases of akinesia and/or dyskinesia. Other standard antiparkinsonian drugs (except levodopa) can be continued while carbidopa and levodopa are being prescribed, although the dosage of these drugs or the dose of levodopa may need to be adjusted.

Elderly patients. The drug is prescribed to elderly people.

CONTRAINDICATIONS

hypersensitivity to active components or to any of the components of the drug; glaucoma; severe heart failure; severe cardiac arrhythmia; severe psychosis; simultaneous use of selective MAO type A inhibitors and non-selective MAO inhibitors (with the exception of certain MAO-B inhibitors in low doses). These drugs must be discontinued at least 2 weeks before prescribing Carbidopa and Levodopa-Teva; suspicious and undiagnosed skin diseases or a history of melanoma.

The drug is not used in patients for whom sympathomimetics are contraindicated.

SIDE EFFECTS

side effects that occur with the use of the drug are often associated with the neuropharmacological effects of dopamine. Usually these reactions are eliminated or their severity decreases when the dose is reduced. The most common are cases of dyskinesia, including choreo-like, dystonic and other involuntary movements. The development of muscle spasm and blepharospasm indicates that the dose should be reduced.

Other serious side effects include changes in thinking, including paranoid thinking and psychosis, depression with or without suicidal tendencies, and dementia. There have been cases of pathological gambling, increased libido and hypersexuality, especially when using the drug in high doses; these manifestations disappeared when the dose was reduced or drug therapy was discontinued.

The following side effects are associated with taking levodopa and its combination.

From the side of blood and lymphatic system: leukopenia, hemolytic and non-hemolytic anemia, thrombocytopenia, agranulocytosis.

From the outside immune system: hypersensitivity reactions, including angioedema, urticaria.

From the cardiovascular system: palpitation, heart rhythm disturbances, orthostatic effects, including arterial hypotension, tendency to loss of consciousness, fainting, hypertension, phlebitis.

From the nervous system: dizziness, bradykinesia, on-off phenomenon (may occur several months or even years after the start of levodopa treatment and is likely associated with disease progression (in such cases, dose and interval adjustment may be required)), ataxia, dyskinesia, chorea, dystonia, extrapyramidal and movement disorders, bradykinesia, increased hand tremors, muscle twitching, muscle spasms, trismus, paresthesia, falling, gait disturbance, neuroleptic malignant syndrome, convulsions, tendency to faint, loss of consciousness, activation of latent Bernard-Horner syndrome.

From the mental side: confusion, insomnia, nightmares, mania, dizziness, exhaustion, depression, suicide attempts, euphoria, dementia, altered mental status (including paranoid thoughts and transient psychosis), hallucinations, delusions, agitation, restlessness, agitation, fear, falling, disturbance gait, impaired thinking, disorientation, headache, stupor, convulsions, drowsiness, sudden attacks of drowsiness.

From the digestive system: dyspepsia, nausea, vomiting, dry mouth, bitter taste in the mouth, hypersalivation, dysphagia, bruxism, hiccups, abdominal pain, constipation, diarrhea, flatulence, dyspepsia, gastrointestinal pain, glossalgia, dark saliva, intestinal bleeding, burning sensation on the tongue, duodenal ulcer, gastrointestinal bleeding.

Metabolic disease: decrease or increase in body weight, edema, anorexia.

For the skin and subcutaneous tissues: itching, hyperemia, sweating, sweat coloration dark color, rash, hair loss, activation of malignant melanoma, Henoch-Schönlein disease.

From the respiratory system: pain in chest, hoarseness, chest pain, shortness of breath, breathing problems.

From the musculoskeletal system: muscle spasm.

From the urinary system: urinary retention, urinary incontinence, dark urine, priapism.

From the side of the organ of vision: blurred vision, blepharospasm, activation of latent Horner's syndrome, diplopia, mydriasis, oculomotor crisis, gaze convulsion. Blepharospasm may be early symptom overdose.

Laboratory indicators: increased liver function indicators such as alkaline phosphatase, ALT, AST, LDH, bilirubin, blood urea nitrogen, creatinine, uric acid, positive Coombs test, decreased hemoglobin and hematocrit, increased blood glucose levels, leukocytosis, bacteriuria, hematuria.

Other: general weakness, asthenia, fatigue, poor health, sudden exacerbation concomitant diseases, flushing of the face, hyperemia, malignant melanoma.

Levodopa is associated with drowsiness, but very rare cases of daytime sleepiness and sudden sleep onset have been reported in association with levodopa.

Impulse control violation: pathological gambling, increased libido, hypersexuality, impulsive desire to buy, overeating, impulsive eating when using dopamine agonists and/or other dopamine-containing drugs, including carbidopa and levodopa.

the drug should not be used to treat extrapyramidal reactions resulting from the use of drugs, and is also not recommended for the treatment of patients with Huntington's chorea.

The drug should be used with caution in persons with cardiovascular diseases and diseases of the kidneys, liver, respiratory tract, with BA, endocrine diseases, open-angle glaucoma, a history of gastric and/or duodenal ulcers (due to the likelihood of bleeding from the upper digestive tract), hematemesis, Cushing's syndrome, mental disorders, a history of seizures.

The initial dose for patients with myocardial infarction, atrial, nodal and ventricular arrhythmia is prescribed if the patient is under constant medical supervision and his cardiac function is monitored.

If it is necessary to perform an operation under anesthesia, the drug is discontinued the day before. The use of the drug is resumed after surgery as soon as the patient is able to take it.

All patients using the drug should be closely monitored for mental changes, depressive syndrome with accompanying suicidal intentions. Patients with psychosis (including a history) require special attention. If psychotic symptoms increase, Carbidopa and Levodopa-Teva should be discontinued.

In patients who have been previously treated with levodopa alone, dyskinesia is possible because carbidopa allows more levodopa to reach the brain and thus more dopamine to be formed. The appearance of dyskinesia requires a dose reduction.

Just like levodopa, the drug can cause involuntary movements and mental disorders. Patients who have had involuntary movements and psychoses during treatment with levodopa require special attention when using the drug Carbidopa and Levodopa-Teva. Such reactions are caused by an increase in the amount of dopamine in the brain, which is a consequence of the use of levodopa, and taking Carbidopa and Levodopa-Teva can cause a relapse.

Patients with a history of orthostatic hypotension require careful monitoring, especially when starting to use Carbidopa and Levodopa-Teva. Such patients may require appropriate treatment.

When antiparkinsonian drugs are abruptly stopped, a syndrome similar to neuroleptic malignant syndrome is observed, including muscle rigidity, increased body temperature, mental changes and increased plasma CPK levels, especially when patients were treated with antipsychotics. Therefore, it is necessary to monitor patients with any sudden cessation or change in dosage of Carbidopa and Levodopa-Teva, especially those who are also receiving antipsychotics.

Psychoactive drugs such as phenothiazines or butyrophenones should be co-administered with caution. Treatment of patients with a history of seizures requires special care.

As with the use of levodopa, periodic checks of hepatic, hematopoietic, cardiovascular and renal functions throughout the entire treatment.

In patients with chronic open-angle glaucoma, the drug should be prescribed with caution, subject to constant monitoring of intraocular pressure and careful monitoring of its changes during treatment.

Levodopa may cause drowsiness and sudden episodes of sleepiness. Cases of sudden episodes of drowsiness during daytime activities are rare. However, patients should be informed about the possible occurrence of such symptoms, and if they occur, consider reducing the dose or discontinuing treatment.

Impulse control disorder. Patients should be closely monitored for the occurrence of impulse control disorders. Patients and their environment should be warned about possible changes in behavior that indicate a violation of impulse control, such as pathological gambling, increased libido, hypersexuality, impulsive desire to buy, overeating, impulsive eating, when using dopamine agonists, including cabergoline. In this case, you should reduce the dose of the drug or stop using it.

Laboratory research. Typically, creatinine and urea levels are lower than with levodopa. Transient abnormalities include increased blood urea, ALT, AST, LDH, bilirubin, alkaline phosphatase, and protein-bound iodine.

There is a decrease in hemoglobin, hematocrit, an increase in glucose in the blood plasma and white blood cells, an increase in the number of bacteria and blood in the urine.

Marked positive tests on erythrocyte antibodies both when using Carbidopa and Levodopa-Teva, and when using only levodopa, but hemolytic anemia is practically not observed.

Carbidopa and Levodopa-Teva may cause a false-positive result when measuring urinary ketones using a litmus test; this reaction is not altered by boiling urine. The use of methods using glucose oxidase may give a false negative result when testing for glycosuria.

It has been reported that patients with Parkinson's disease have increased risk melanoma development. It is not known whether this risk is due to Parkinson's disease or other factors, such as the use of drugs to treat Parkinson's disease. Therefore, it is recommended to constantly monitor the condition of the skin to detect possible melanoma and periodically undergo skin examination by a qualified specialist (for example, a dermatologist) during treatment with Carbidopa and Levodopa-Teva.

If the drug is discontinued, the dose is reduced gradually, and the patient's health condition should be carefully monitored.

Use during pregnancy and lactation. Although the effect of the drug on pregnancy is unknown, both levodopa and its combination with carbidopa have caused malformations internal organs and skeleton in animal experiments. The drug is contraindicated during pregnancy and breastfeeding. All women of reproductive age using carbidopa/levodopa should use effective methods contraception.

It is unknown whether carbidopa or levodopa is excreted into breast milk in humans. To prevent the occurrence of negative reactions in children, a decision should be made: interrupt breastfeeding or stop taking the drug, given its importance for the mother.

Children. The safety of the drug for children has not been established, so it is not prescribed to patients under the age of 18 years.

The ability to influence the speed of reaction during control vehicles or working with other mechanisms. Considering that sensitive patients may experience adverse reactions(dizziness, hallucinations, uncontrolled movements, drowsiness, cases of sudden sleep, blurred vision), while taking the drug you should refrain from driving vehicles and performing other work that requires concentration.

INTERACTIONS

the drug should be used with caution simultaneously with:

• antihypertensive drugs. In patients taking certain antihypertensive drugs, the addition of combinations of levodopa with a decarboxylase inhibitor caused the development of symptomatic orthostatic hypotension, therefore, at the beginning of treatment with the drug, it may be necessary to adjust the dose of the antihypertensive drug;
• antidepressants. There are a small number of reports of negative reactions, including hypertension and dyskinesia, caused by the simultaneous use of tricyclic antidepressants and levodopa with carbidopa. Carbidopa and Levodopa-Teva can only be used with selective MAO-B inhibitors in recommended doses (for example, selegiline);
• anesthetics. Concomitant use of anesthetics may cause arrhythmia;
• anticholinergic drugs. May act synergistically with levodopa in reducing tremor, and this feature is often used to enhance therapeutic effect; however, they can sharpen involuntary movements. At high doses, they may also reduce the beneficial effects of levodopa by slowing its absorption, thereby increasing gastric metabolism of the drug;
• other medicines. Phenothiazines, benzodiazepines, isoniazid, butyrophenones, phenytoin and papaverine may reduce the therapeutic effect of levodopa. The metabolism of levodopa is increased by the use of anticonvulsants.

Given that levodopa competes with certain amino acids, absorption of the drug may be impaired in some patients on a high protein diet.

The addition of carbidopa prevents the increase in the level of metabolism of levodopa into dopamine, which is caused by the action of vitamin B 6. The drug can be used in patients with parkinsonism who are taking vitamin preparations containing pyridoxine hydrochloride (vitamin B 6).

Combination therapy with selegiline can lead to severe orthostatic hypotension, which is not typical for Carbidopa and Levodopa-Teva.

Iron supplements may inhibit the absorption of levodopa.

Sympathomimetics may increase the cardiovascular side effects of levodopa.

When used concomitantly with antacids, the effect on the bioavailability of levodopa has not been studied.

Dopamine antagonists, amantadine, can be used together with the drug. If these drugs are prescribed in addition to therapy with Carbidopa and Levodopa-Teva, dose adjustment may be required.

Metoclopramide increases the concentration of levodopa in the blood plasma.

The combined use of catecholomethyltransferase inhibitors (tolcapone, entacapone) and levodopa/carbidopa may increase the bioavailability of levodopa.

Can be used with other antiparkinsonian drugs that do not contain levodopa.

symptoms: early signs of overdose - cardiac arrhythmia, involuntary movements, tonic blepharospasm, muscle twitching, hypertension, increased heart rate, decreased appetite, confusion, anxious agitation, insomnia, restlessness.

Treatment: artificially induce vomiting, rinse the stomach immediately.

Symptomatic therapy: infusions are prescribed with caution, paying attention to airway patency; When arrhythmia occurs, appropriate treatment is used with ECG monitoring. The value of dialysis in cases of overdose has not been studied. The use of pyridoxine is ineffective.

STORAGE CONDITIONS

at temperatures up to 25 °C.

Date added: 11/13/2019

© Compendium 2017

Prices CARBIDOPA AND LEVODOPA-TEVA in cities of Ukraine

Vinnitsa 433.16 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA ..... 410.9 UAH/pack.
« RECIPE» Vinnitsa, st. Kyiv, 47, tel.: +380676221540

Dnieper 474.99 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 430.4 UAH/pack.
« RECIPE» Dnepr, st. Monomakha Vladimir, 11, tel.: +380675233077

Zhytomyr 437.66 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 418.99 UAH/pack.
« PHARMACY BAM» Zhytomyr, st. Kyiv, 25, tel.: +380981699870

Zaporozhye 443.98 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 442.9 UAH/pack.
« WE WANT HEALTH» Zaporozhye, st. Entuziastov, 3, tel.: +380612772929

Ivano-Frankivsk 445.24 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 445.24 UAH/pack.
« PLANTAIN» Ivano-Frankivsk, st. Trolleybusnaya, 1, tel.: +380673724761

Kyiv 473.45 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 382.95 UAH/pack.
« WE WANT HEALTH» Kyiv, ave. Mayakovsky, 60/10, tel.: +380445321478

Kropyvnytskyi 437.66 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 418.99 UAH/pack.
« PLANTAIN» Kropyvnytskyi, st. Pashutinskaya, 75, tel.: +380677196874

Lutsk 456.69 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 447 UAH/pack.
« PHARMACY WHOLESALE PRICES» Lutsk, st. Sverstyuka Evgeniya, 1, tel.: +380800505911

Lviv 454.62 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 389.9 UAH/pack.
« WE WANT HEALTH» Lviv, st. Chernigovskaya, 6, tel.: +380322600953

Nikolaev 482 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 482 UAH/pack.
« PHARMACY 24» Nikolaev, st. Chkalova, 91A, tel.: +380512769961

Odessa 442.29 UAH/pack.

CARBIDOPA AND LEVODOPA-TEVA table 25 mg + 250 mg blister No. 100, Teva Ukraine ..... 401.95 UAH/pack.
« WE WANT HEALTH» Odessa, st. Heroes of Defense of Odessa, 52A, tel..

Formula: C10H14N2O4, chemical name: (2S)-3-(3,4-dihydroxyphenyl)-2-hydrazino-2-methylpropanoic acid.
Pharmacological group: neurotropic drugs/antiparkinsonian drugs/antiparkinsonian drugs in combinations; intermediates / dopaminomimetics / dopaminomimetics in combinations.
Pharmachologic effect: antiparkinsonian.

Pharmacological properties

Carbidopa inhibits peripheral dopa decarboxylase. Together with levodopa, it reduces the formation of dopamine in the periphery and increases the amount of levodopa that enters the central nervous system. Carbidopa also inhibits peripheral oxytriptan decarboxylase (a serotonin precursor). Carbidopa does not penetrate the blood-brain barrier. When taken orally, the maximum concentration is achieved after 1.5 - 5 hours. Carbidopa is metabolized in the liver. Excretion of unchanged carbidopa in urine is 35% and is completed within 7 hours. It is also excreted in the urine in the form of the following metabolites: alpha-methyl-3,4-dihydroxyphenylpropionic acid, alpha-methyl-3-methoxy-4-hydroxyphenylpropionic acid, N-methyl-carbidopa, 3,4-dihydroxyphenyl-acetone.

Indications

Together with levodopa: parkinsonism syndrome (except parkinsonism, which is caused by drugs, for example, antipsychotics), Parkinson's disease.

Method of administration of carbidopa and dose

Carbidopa is used together with levodopa in a ratio of 1 to 10 or 1 to 4; The daily dose of carbidopa is 75 - 200 mg in several doses.
Carbidopa is used in combination with levodopa. The use of carbidopa with levodopa is contraindicated during therapy with monoamine oxidase inhibitors (except low-dose monoamine oxidase type B inhibitors).
While using carbidopa, you must avoid activities that require rapid psychomotor reactions and high concentration (including driving).

Contraindications for use

Hypersensitivity, severe dysfunction of the kidneys, liver, endocrine and/or cardiovascular system, angle-closure glaucoma, severe psychosis, melanoma, age under 18 years.

Restrictions on use

Diseases of the lungs, liver, kidneys, endocrine, cardiovascular systems, a history of arrhythmia, myocardial infarction, osteomalacia, peptic ulcer, mental disorders; in patients with diseases that may require the use of antihypertensive, sympathomimetic drugs (including bronchial asthma).

Use during pregnancy and breastfeeding

The use of carbidopa during pregnancy is not recommended, except in cases with strict indications. During carbidopa therapy breastfeeding stop.

Side effects of carbidopa

Side effects have occurred when carbidopa was used together with levodopa.
Nervous system: sleep disturbances, spontaneous movements, dizziness, agitation, depression.
The cardiovascular system: arrhythmias, orthostatic hypotension.
Digestive system: nausea, anorexia, vomiting, epigastric pain, ulcerogenic effect, dysphagia.
Hematopoiesis: thrombocytopenia.

Interaction of carbidopa with other substances

At joint use combinations of carbidopa and levodopa with iron sulfate may reduce the bioavailability of levodopa and carbidopa.
The combination of carbidopa with levodopa can reduce the severity of side effects (especially arrhythmias, nausea, vomiting) and the dose of levodopa. However, there may be a tendency towards early development mental disorders and dyskinesias that are associated with the action of levodopa.

Overdose

With an overdose of carbidopa, side effects increase. Patient monitoring (especially electrocardiograms) and symptomatic treatment are necessary.

Trade names of drugs containing the active ingredient carbidopa

Combined drugs:
Levodopa + Carbidopa: Duellin®, Zymox, Izikom, Carbidopa/Levodopa, Credanil 25/250, Nacom®, Sindopa, Sinemet, Sinemet SR, Striaton, Tidomet forte, Tremonorm;
Levodopa + Entacapone + [Carbidopa]: Stalevo.