Home Oral cavity The powerful antipsychotic Chlorprothixene - instructions for use are required to be studied; reviews from doctors and patients are mixed. Chlorprothixene Interactions with other drugs

Oral cavity

The powerful antipsychotic Chlorprothixene - instructions for use are required to be studied; reviews from doctors and patients are mixed. Chlorprothixene Interactions with other drugs

The description is valid on 18.06.2014

Latin name: Chlorprothixen
ATX code: N05AF03
Active substance: Chlorprothixene
Manufacturer: Zentiva k.s (Czech Republic)

Compound

One tablet of Chlorprothixene contains 15 or 50 mg hydrochloride(depending on the release form).

Excipients: lactose monohydrate, calcium stearate, corn starch, talc, sucrose.

Composition of the tablet shell: hypromellose, macrogoal, opaspray M-1-1-6181, talc.

Release form

Pills, coated in blisters of 10 pieces. There are three blisters in a cardboard box.

There is also an option in drops And solution for injection in ampoules 2 ml (50 mg), in packages of 10 and 100 ampoules.

pharmachologic effect

The drug is antipsychotic means ( antipsychotic ), which happens due to the fact that dopamine receptors it has a blocking effect. By blocking these receptors, the drug also has analgesic And antiemetic actions.

In addition, Chlorprothixene has antihistamine And hypotensive actions, blocking α1-adrenergic receptors, 5-HT2 receptors, and H1 histamine receptors.

Indications for use of Chlorprothixene

Chlorprothixene is a sedative antipsychotic , having a wide range of indications, which include:

hungover withdrawal syndrome , found in drug addiction and alcoholism;
, including manic states and which proceed with anxiety, psychomotor agitation and agitation;
behavioral disorders in children;
agitation, hyperactivity, irritability, confusion in older people;
pain (the drug is used together with).

Pharmacodynamics and pharmacokinetics

When taken orally, the bioavailability of Chlorprothixene is approximately 12%. The drug is quickly absorbed from the intestine, and after 2 hours the maximum concentration of the drug is reached in the blood serum.

The half-life of excretion from the body is approximately 16 hours. The drug penetrates through placental barrier and small amounts are excreted along with breast milk. They have no neuroleptic activity and are excreted in urine and feces.

Contraindications

The drug is contraindicated for use in:

any depression of the central nervous system, including depression caused by taking opiates , alcohol or barbiturates ;
vascular collapse;
pheochromocytoma ;
diseases of the hematopoietic organs;
hypersensitivity to the components present in Chlorprothixene.

Side effects

For digestive system: psychomotor inhibition, increased fatigue, mild extrapyramidal syndrome , . In some cases, there may be a significant increase in anxiety, which is most common in schizophrenics or patients with mania.
For of cardio-vascular system: orthostatic possible hypotension , changes on the ECG, .
For the digestive system: there is a possibility of occurrence cholestatic jaundice .
For hematopoietic system: possible leukocytosis , , leukopenia.
For the visual organs: Clouding of the lens and cornea may occur, followed by deterioration of vision.
For metabolism: carbohydrate metabolism may be disrupted, sweating may increase, body weight and appetite may increase.
For endocrine system: amenorrhea , gynecomastia , galactorrhea , weakening libido and potency.
Dermatological reactions: may appear photodermatitis , photosensitivity .
Effects caused by anticholinergic action: disturbances of accommodation, dysuria , dry mouth.

Instructions for use of Chlorprothixene (Method and dosage)

For hangover withdrawal symptoms caused by drug addiction or alcoholism

Daily dose The drug in tablets is 500 mg and is divided into 2-3 doses. As a rule, the course of treatment lasts for 7 days. When withdrawal symptoms disappear, gradually reduce the dose. The daily maintenance dose is 15-45 mg, which is enough to reduce the risk of developing another binge and stabilize the patient’s condition.

For psychoses, including manic states and schizophrenia

Treatment begins with a daily dose of 50-100 mg, the dosage is gradually increased until the optimal effect is achieved, usually up to 300 mg. For some cases, the dosage should be increased to 1200 mg per day. The daily maintenance dose is approximately 100-200 mg. As a rule, the daily dose of the drug is divided into two or three doses, and it is recommended to take a smaller dose during the day, and a larger dose in the evening, due to the pronounced sedative effect of the drug.

For neuroses, depressive states and psychosomatic disorders

Alone or as an addition to therapy with antidepressants, the drug is used for depression, and especially for conditions that are combined with anxiety. For psychosomatic disorders that are accompanied by depressive disorders and anxiety, as well as for neuroses, a daily dose of up to 90 mg can be prescribed. Usually the daily dosage is divided into several doses. Given the absence of drug dependence on the drug or the development of addiction to it, you can take Chlorprothixene for quite a long time without any particular risks.

Instructions for use for insomnia

An hour before bedtime, take 15-30 mg of the drug.

For pain

The drug is capable of potentiating analgesic effects, so it can be used to treat patients suffering from pain. In such cases, the drug is prescribed together with analgesics , the dosage is 15-300 mg.

Overdose

In case of overdose may occur following symptoms: hyper - or , convulsions , extrapyramidal symptoms, shock or coma.

In case of an overdose of Chlorprothixene, supportive and symptomatic treatment. Gastric lavage should be done as soon as possible; it is also recommended to take sorbent . It is necessary to take measures aimed at maintaining cardiovascular and respiratory systems. Can not use , since it may cause a decrease blood pressure. Extrapyramidal disorders can be treated with Biperiden, and seizures can be treated with.

Interaction

Simultaneous use of the drug with ethanol or preparations containing ethanol, as well as , sleeping pills , sedative , neuroleptic and opioid analgesics may enhance the inhibitory effect of Chlorprothixene on the central nervous system.

The drug enhances the effect with antihypertensive drugs .

When taking Chlorprothixene simultaneously with adrenaline may happen And arterial hypotension.

The drug reduces the threshold of convulsive activity, so patients require additional dosage adjustment of antiepileptic drugs.

Simultaneous use of the drug with, Metoclopramide , or phenothiazines may cause extrapyramidal disorders.

The property of Chlorprothixene, which blocks dopamine receptors, also reduces the effectiveness of the drug. Levodopa .

Terms of sale

The drug is available in pharmacies with a prescription.

Storage conditions

The medicine Chlorprothixene should be stored in a cool place with an ambient temperature of no more than 25°C and in the absence of light.

Best before date

The drug is stored for 2 years.

special instructions

Caution should be exercised when prescribing Chlorprothixene to patients who suffer from epilepsy , in case of a tendency to collapse, with severe respiratory and cardiovascular failure, severe kidney and liver disorders, hypertrophy prostate gland, expressed.

The drug has a negative effect on activities associated with high speed physical and mental reactions - driving vehicles, working at heights, servicing cars, etc.

Chlorprothixene analogs

Level 4 ATX code matches:

Chlorprothixene 15 Lechiva , Chlorprothixene 50 Lechiva , Truskal .

Synonyms

Tarazan , Chlorprothixene hydrochloride , Vetakalm , Minithixen , Taktaran , Truxil , Chlothixene , Trictal , Taraktan , .

For children

To correct behavioral disorders in children, the drug is prescribed at a rate of 0.5-2 mg per kilogram of the child’s body weight.

With alcohol

During pregnancy and lactation

If possible, Chlorprothixene should not be prescribed for treatment during pregnancy and lactation.

Reviews of Chlorprothixene

Judging by the reviews of Chlorprothixene on the forums, it is excellent sleeping pills . As for its action in psychoses , then opinions differ here - some believe that the drug (manufactured by the Zentiva company) perfectly relieves psychosis, while others (who are the majority) believe that the drug is poorly suited for these purposes. Basically, the opinions of those who said what Chlorprothixene tablets are for boiled down to the fact that it is an excellent sleeping pill that helps with psychosis.

From negative reviews It is possible to distinguish the feeling that occurs after taking the drug and a slight lethargy. Some experienced significant anxiety caused by. But at the same time, the largest number of reviews are positive.

Instructions for use

Active ingredients

Release form

Pills

Compound

Active ingredient: Chlorprothixenum Concentration active substance(mg): 15

Pharmacological effect

Antipsychotic drug (neuroleptic), thioxanthene derivative. It has antipsychotic, antidepressant, sedative, antiemetic effects, and has alpha-adrenergic blocking activity. It is believed that the antipsychotic effect is associated with the blockade of postsynaptic dopamine receptors in the brain. antiemetic effect is associated with blockade of the chemoreceptor trigger zone medulla oblongata. the sedative effect is due to an indirect weakening of the activity of the reticular system of the brain stem. suppresses the release of most hormones of the hypothalamus and pituitary gland. however, as a result of blockade of the prolactin inhibitory factor, which inhibits the release of prolactin from the pituitary gland, the concentration of prolactin increases. in chemical structure and pharmacological properties thioxanthenes are similar to piperazine phenothiazine derivatives.

Pharmacokinetics

Metabolized in the liver. It is excreted primarily by the kidneys.

Indications

Chlorprothixene is a sedative antipsychotic with wide range indications, which include: psychosis, including schizophrenia and manic states, occurring with psychomotor agitation, agitation and anxiety; hangover withdrawal syndrome in alcoholism and drug addiction; hyperactivity, irritability, agitation, confusion in elderly patients; behavioral disorders in children; depressive states , neuroses, psychosomatic disorders;insomnia; pain (in combination with analgesics).

Contraindications

CNS depression of any origin (including those caused by alcohol, barbiturates or opiates); comatose states;vascular collapse; diseases of the hematopoietic organs; pheochromocytoma; hypersensitivity to the components of Chlorprothixene.

Precautionary measures

Keep out of the reach of children.

Use during pregnancy and breastfeeding

Contraindicated for use during pregnancy and lactation.

Directions for use and doses

Chlorprothixene is taken orally. The dose, frequency and duration of use are determined individually. The average daily dose, divided into 2-3 doses, is 500 mg.

Side effects

Drowsiness, tachycardia, dry mouth, excessive sweating, difficulty of accommodation. These side effects, which usually occur at the beginning of therapy, often disappear as it continues. Orthostatic hypotension may occur, especially when using Chlorprothixene in high dosages. Dizziness, dysmenorrhea, skin rashes, constipation is rare. Extrapyramidal symptoms are especially rare. Isolated cases of a decrease in the convulsive threshold, the occurrence of transient benign leukopenia and hemolytic anemia have been described. With long-term use, especially in high doses, the following may be observed: cholestatic jaundice, galactorrhea, gynecomastia, decreased potency and/or libido, increased appetite, increased body weight.

Interaction with other drugs

When used simultaneously with anesthetics, opioid analgesics, sedatives, hypnotics, antipsychotics, ethanol, ethanol-containing drugs, the inhibitory effect on the central nervous system is enhanced. When used simultaneously with antihypertensive drugs, the hypotensive effect is enhanced. When used simultaneously with anticholinergic, antihistamine, antiparkinsonian drugs, the anticholinergic effect is enhanced. action. When used simultaneously with drugs that cause extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal reactions is possible; with levodopa - the antiparkinsonian effect of levodopa may be inhibited; with lithium carbonate - pronounced extrapyramidal symptoms and neurotoxic effects are possible. When used simultaneously with epinephrine, blockade of the alpha-adrenergic effects of epinephrine is possible and, as a result, severe arterial hypotension and tachycardia develop. When used simultaneously with phenothiazines, metoclopramide, haloperidol, reserpine, the development of extrapyramidal disorders is possible; with quinidine - an increased inhibitory effect on the heart is possible.

special instructions

It should not be used for epilepsy, a tendency to collapse, parkinsonism, heart defects in the stage of decompensation, tachycardia, cerebral atherosclerosis, severe liver and kidney dysfunction, hematopoietic disorders, cachexia, in old age. If it is necessary to use chlorprothixene, the risks and benefits should be compared treatment in patients with chronic alcoholism, diseases of the cardiovascular system (increased risk of developing transient arterial hypotension), Reye's syndrome, as well as glaucoma or a predisposition to it, peptic ulcer stomach and duodenum, urinary retention, Parkinson's disease, epileptic seizures, hypersensitivity to other thioxanthenes or phenothiazines. When using chlorprothixene, false positive results are possible immunological test for pregnancy using urine, as well as false positive results of a urine test for bilirubin. Avoid drinking alcohol during the treatment period. Impact on the ability to drive vehicles and operate machinery During the treatment period, you should refrain from engaging in potentially hazardous activities that require increased attention and rapid psychomotor reactions .

1 film-coated tablet contains chlorprothixene 15 or 50 mg; 10 pcs in a blister, 3 blisters in a box.

pharmachologic effect

pharmachologic effect- analgesic, antiemetic, antidepressant, sedative, neuroleptic.

Blocks dopamine, histamine, serotonin, alpha-adrenergic and cholinergic receptors in the central nervous system.

Indications for the drug Chlorprothixene 15 Lechiva

Psychoses, incl. schizophrenia, depressive states during menopause, states of excitation associated with fear and tension, discirculatory encephalopathy, traumatic brain injuries, delirium tremens, sleep disorders during anxiety states ; psychosomatic, neurotic disorders

Contraindications

in children; in patients with burns; dermatoses with persistent itching. Absolute:

hypersensitivity, poisoning with drugs that depress the central nervous system (including alcohol), coma of any etiology. Relative: epilepsy, parkinsonism, tendency to collapse, severe dysfunction of the kidneys, liver, heart and breathing, closed-angle glaucoma, myasthenia gravis, pregnancy, lactation (should be avoided breastfeeding

Side effects

), elderly age. Extrapyramidal disorders, increased fatigue, headache , dry mouth, orthostatic hypertension, tachycardia, accommodation disturbances, blurred vision, constipation, urination disorders, jaundice, amenorrhea, galactorrhea, gynecomastia, changes in libido, disorders carbohydrate metabolism

Interaction

, increased appetite, weight gain, agranulocytosis, leukopenia, photosensitivity, photodermatitis, withdrawal syndrome (with sudden cessation of treatment).

Directions for use and doses

Enhances the effect of drugs that depress the central nervous system, incl. alcohol. Orally, during or after meals, without chewing, with water. The dosage regimen is determined individually. Usually

adults: 30-50 mg 3-4 times a day. Treatment begins with low doses, then the dose is gradually increased until signs of the disease disappear. Most of the dose is usually given at night. The daily dose for adults should not exceed 600 mg.

Precautionary measures

It is recommended to stop treatment by gradually reducing the dosage. During therapy, you should avoid drinking alcohol, exposure to extreme temperatures, insolation, potentially dangerous species activities that require increased attention and speed of psychomotor reactions.

Storage conditions for the drug Chlorprothixene 15 Lechiva

In a dry place, at a temperature of 10-25 °C.

Keep out of the reach of children.

Shelf life of the drug Chlorprothixene 15 Lechiva

3 years.

Do not use after the expiration date stated on the package.

Synonyms of nosological groups

Category ICD-10	Synonyms of diseases according to ICD-10
F20 Schizophrenia	Dementia praecox
	Bleuler's disease
	Sluggish schizophrenia
	Sluggish schizophrenia with apatoabulic disorders
	Exacerbation of schizophrenia

	Acute form of schizophrenia
	Acute schizophrenia
	Acute schizophrenic disorder
	Acute attack of schizophrenia
	Psychosis discordant
	Psychosis of schizophrenic type
	Dementia early
	Febrile form of schizophrenia
	Chronic schizophrenia
	Chronic schizophrenic disorder
	Cerebral organic failure in schizophrenia
	Schizophrenic conditions
	Schizophrenic psychosis
	Schizophrenia
F29 Non-organic psychosis, unspecified	Hallucinatory-delusional disorders
	Hallucinatory-delusional syndrome
	Intoxication psychosis
	Manic-delusional disorders
	Manic chronic psychoses
	Manic psychosis
	Acute psychosis
	paranoid psychosis
	Paranoid psychosis
	Subacute psychosis
	Presenile psychosis
	Psychosis
	Intoxication psychosis
	Paranoid psychosis
	Psychosis in children
	Psychoses of childhood

	Reactive psychoses
	Chronic psychoses
	Chronic hallucinatory psychosis
	Chronic psychosis
	Chronic psychotic disorder
	Schizophrenic psychosis
F41 Other anxiety disorders	Relief of anxiety
	Non-psychotic anxiety disorders
	Alarm state
	Anxiety
	Anxious and suspicious states
	Chronic anxiety
	Sense of anxiety
F91 Behavioral disorders	Destructive behavior
	Behavior disorder
	Behavioral disorders
	Behavioral disorders
	Behavioral disorders in children
	Behavioral disorder
	Behavioral disorder in adolescents over 15 years of age and adults
	Behavioral disorders in childhood
	Behavioral disorders in old age
	Behavioral disorders in children
	conduct disorder
	Mixed behavior disorders
	Juvenile and other behavioral disorders
G47.0 Disturbances in falling asleep and maintaining sleep [insomnia]	Insomnia
	Insomnia, especially difficulty falling asleep
	Desynchronosis
	Long-term sleep disturbance
	Difficulty falling asleep
	Difficulty falling asleep
	Difficulty falling asleep
	Insomnia
	Short-term and transient sleep disturbances
	Short-term and chronic disorders sleep
	Short or shallow sleep
	Sleep disturbance
	Sleep disturbance, especially during the falling asleep phase
	Sleep disorders
	Sleep disorders
	Neurotic sleep disorder
	Shallow, shallow sleep
	Shallow sleep
	Poor sleep quality
	Night awakening
	Night awakenings
	Sleep pathology
	Post-somnia disorder
	Transient insomnia
	Problems falling asleep
	Early awakening
	Early morning awakening
	Early awakenings
	Sleep disorder
	Sleep disorder
	Persistent insomnia
	Difficulty falling asleep
	Difficulty falling asleep
	Difficulty falling asleep in children
	Difficulty falling asleep
	Difficulty falling asleep
	Persistent insomnia
	Deterioration of sleep
	Chronic insomnia
	Frequent night and/or early morning awakenings
	Frequent awakenings at night and a feeling of shallow sleep
L20 Atopic dermatitis	Allergic skin diseases
	Allergic skin diseases of non-infectious etiology
	Allergic skin diseases of non-microbial etiology
	Allergic skin diseases
	Allergic skin lesions
	Allergic manifestations on the skin
	Allergic dermatitis
	Allergic dermatosis
	Allergic diathesis
	Allergic pruritic dermatosis
	Allergic skin disease
	Allergic skin irritation
	Allergic dermatitis
	Atopic dermatitis
	Allergic dermatosis
	Exudative diathesis
	Itchy atopic eczema

	Skin allergic disease
	Skin allergic reaction for drugs and chemicals
	Skin reaction to medications
	Skin allergic disease
	Acute eczema
	Common neurodermatitis
	Chronic atopic dermatitis
	Exudative diathesis
L29 Itching	Itchy dermatitis
	Dermatosis with persistent itching
	Other pruritic dermatoses
	Itching of the scalp
	Itchy skin
	Itching with partial obstruction of the bile ducts
	Itchy eczema
	Pruritic dermatoses
	Pruritic allergic dermatosis
	Pruritic dermatitis
	Pruritic dermatosis
	Itchy skin
	Skin itching due to dermatosis
	Excruciating itching
	Limited pruritic dermatitis
	Severe itching
	Endogenous skin itching
N95.1 Menopausal and menopausal conditions in women	Atrophy of the mucous membrane of the lower genitourinary tract caused by estrogen deficiency
	Vaginal dryness
	Autonomic disorders in women
	Hypoestrogenic conditions
	Estrogen deficiency in menopausal women
	Dystrophic change in the mucous membrane during menopause
	Natural menopause
	Intact uterus
	Climax
	Female menopause
	Menopause in women
	Menopausal depression
	Menopausal ovarian dysfunction
	Menopause
	Menopausal neurosis
	Menopause
	Menopause complicated by psychovegetative symptoms
	Menopausal symptom complex
	Menopausal autonomic disorder
	Menopausal psychosomatic disorder
	Menopausal disorder
	Menopausal disorder in women
	Menopausal condition
	Menopausal vascular disorder
	Menopause
	Menopause premature
	Menopausal vasomotor symptoms
	Menopause
	Estrogen deficiency
	Feeling hot
	Pathological menopause
	Perimenopause
	Menopause period
	Postmenopausal period
	Postmenopausal period
	Postmenopausal period
	Postmenopausal period
	Premature menopause
	Premenopause
	Premenopausal period
	Tides
	Hot flashes
	Flushing to the face in menopause and postmenopause
	Hot flashes/feelings of heat during menopause
	Palpitations during menopause
	Early menopause in women
	Disorders during menopause
	Menopausal syndrome
	Vascular complications of menopause
	Physiological menopause
	Estrogen deficiency conditions
R45.1 Restlessness and agitation	Agitation
	Anxiety
	Explosive excitability
	Internal excitement
	Excitability
	Excitation
	Excitement is acute
	Psychomotor agitation
	Hyperexcitability
	Motor excitement
	Relief of psychomotor agitation
	Nervous excitement
	Restlessness
	Night restlessness
	Acute stage of schizophrenia with agitation
	Acute mental agitation
	Paroxysm of excitement
	Overexcitement
	Increased excitability
	Increased nervous excitability
	Increased emotional and cardiac excitability
	Increased arousal
	Mental excitement
	Psychomotor agitation
	Psychomotor agitation
	Psychomotor agitation
	Psychomotor agitation in psychosis
	Psychomotor agitation of an epileptic nature
	Psychomotor paroxysm
	Psychomotor seizure
	Symptoms of arousal
	Symptoms of psychomotor agitation
	State of agitation
	State of anxiety
	State of excitement
	A state of heightened anxiety
	State of psychomotor agitation
	States of anxiety
	States of arousal
	States of excitement in somatic diseases
	State of excitement
	Feeling restless
	Emotional excitement
R45.6 Physical aggressiveness	Aggressive behavior
	Aggressive state
	Aggressiveness
	Aggressive conditions
	Aggression
	Auto aggression
R45.7 State of emotional shock and stress, unspecified	Impact of stress factors
	Impact of extreme situations
	Prolonged emotional stress
	Neuropsychic stress
	Professional stress
	Psychological stress during air travel
	Psycho-emotional overload and stress
	Psycho-emotional tension in stressful situations
	Psycho-emotional stress
	Stressful condition
	Stress
	Stressful state
	Stressful situations
	Stressful conditions
	Stresses of everyday life
	Chronic stress
	Chronic stress
	T90.5 Consequences of intracranial injury	Residual effects of traumatic brain injury
Convalescence after traumatic brain injury
Condition after traumatic brain injury
Conditions after traumatic brain injury
Conditions after traumatic brain injury
Traumatic encephalopathy

Chlorprothixene Zentiva: instructions for use and reviews

Latin name: Chlorprothixen-Zentiva

ATX code: N05AF03

Active substance: chlorprothixene

Manufacturer: Zentiva k.s (Czech Republic, Slovakia), Zentiva Saglik Urunleri Sanayi ve Ticaret A.S. (Türkiye), s.c. Zentiva, S.A. (Romania)

Update description and photo: 21.11.2018

Chlorprothixene Zentiva is a drug with antipsychotic, moderate antidepressant and pronounced sedative effects.

Release form and composition

Dosage form of Chlorprothixene Zentiva - coated tablets film-coated: round biconvex shape, orange (15 mg each) or light brown to light yellow (50 mg each); the color of the kernel at the break is from almost white to white (in a cardboard pack there are 3 or 5 contour strip packs of 10 pcs.).

Composition of 1 tablet:

active substance: chlorprothixene hydrochloride – 15 or 50 mg;
auxiliary components (15/50 mg): corn starch – 10/37.5 mg; lactose monohydrate – 92/135 mg; sucrose – 10/20 mg; calcium stearate – 1.5/3.75 mg; talc – 1.5/3.75 mg;
shell (15/50 mg): hypromellose 2910/5 – 2.011/3.659 4 mg; macrogol 6000 – 0.069/0.133 3 mg; macrogol 300 – 0.49/0.916 6 mg; talc – 1.43/2.419 4 mg; aluminum varnish based on sunset yellow dye (E110) – 1/0 mg; titanium dioxide – 0.342 3 mg.

Pharmacological properties

Pharmacodynamics

Chlorprothixene is an antipsychotic, a thioxanthene derivative. It has antipsychotic, moderate antidepressant and pronounced sedative effects. The antipsychotic effect is associated with the blocking effect of chlorprothixene on dopamine receptors. The analgesic and antiemetic properties of the drug are also associated with the blockade of these receptors. Chlorprothixene is able to block α1-adrenergic receptors, 5-HT2 receptors, as well as H1-histamine receptors, which determines its adrenergic blocking hypotensive and antihistamine effect.

Pharmacokinetics

When taken orally, the bioavailability of chlorprothixene is approximately 12%. After oral administration, it is absorbed well and quickly. In the liver and intestinal walls it undergoes first-pass metabolism. Has a first pass effect through the liver.

Chlorprothixene penetrates the placental barrier and into breast milk.

Excretion is carried out by the intestines and kidneys: chlorprothixene - 29%, chlorprothixene sulfoxide - 41%.

The half-life ranges from 8 to 12 hours.

Indications for use

Indications for Chlorprothixene Zentiva are the following conditions and diseases:

insomnia;
psychoses, including manic states and schizophrenia, accompanied by psychomotor agitation, anxiety and agitation;
depressive states, neuroses, psychosomatic disorders;
withdrawal syndrome in alcoholism and drug addiction;
behavioral disorders in children;
confusion, hyperactivity, agitation, irritability in elderly patients;
pain (in combination with analgesics).

Contraindications

Absolute:

bone marrow suppression;
pathological changes in the blood;
pheochromocytoma;
lactose or fructose intolerance, glucose-galactose malabsorption or lactase deficiency, isomaltase/sucrase deficiency (Chlorprothixene Zentiva contains lactose and sucrose);
depression of the central nervous system of any origin (including those associated with the intake of alcohol, opiates or barbiturates);
vascular collapse;
comatose states;
age up to 6 years;
individual intolerance to the components of the drug, including phenothiazines.

Relative (Chlorprothixene Zentiva is prescribed under medical supervision):

tendency to collapse;
diabetes;
glaucoma (including the presence of a predisposition to its occurrence);
urinary retention and the risk of its development with clinical manifestations prostatic hyperplasia;
renal/liver failure;
Reye's syndrome;
Parkinson's disease (associated with increased extrapyramidal disorders);
pronounced cardiovascular and respiratory failure associated with acute infectious diseases, asthma or emphysema (there is high risk transient increase in blood pressure);
severe cerebral atherosclerosis;
peptic ulcer of the stomach and duodenum;
epilepsy (associated with the likelihood of increased seizures as a result of a lowered seizure threshold);
pregnancy and lactation period.

Instructions for use of Chlorprothixene Zentiva: method and dosage

Chlorprothixene Zentiva is intended for oral administration. Long-term therapy is possible, since the drug does not cause addiction or drug dependence.

psychoses, including manic states and schizophrenia: initial daily dose – 50–100 mg. The dose is gradually increased until the optimal effect is achieved, usually 300 mg. The average maintenance dose is 100 to 200 mg per day. Maximum – 600 mg per day. Usually the daily dose is divided into 2-3 doses, the smaller part should be taken in the daytime, the larger part in the evening;
withdrawal syndrome for drug addiction and alcoholism: daily dose – 500 mg in 2-3 doses. Duration of use – 7 days. After the condition improves, the dose is gradually reduced. The maintenance daily dose ranges from 15 to 45 mg. Taking Chlorprothixene Zentiva allows you to stabilize your condition and reduce the likelihood of developing another binge;
hyperactivity, irritability, agitation, confusion in elderly patients: from 15 to 90 mg per day in 3 divided doses;
behavioral disorder in children: 0.5–2 mg/kg;
neuroses, depressive states, psychosomatic disorders: daily dose – 90 mg in 2-3 doses;
insomnia: 15–30 mg 60 minutes before bedtime;
pain (in combination with analgesics): 15–300 mg per day.

Side effects

Possible adverse reactions (> 10% - very common; > 1% and< 10% – часто; >0.1% and< 1% – нечасто; >0.01% and< 0,1% – редко; < 0,01% – очень редко):

cardiovascular system: orthostatic hypotension (especially when using high doses of Chlorprothixene Zentiva), transient changes QT interval on the electrocardiogram and tachycardia;
nervous system: dizziness, increased fatigue, drowsiness, psychomotor retardation, mild extrapyramidal hypokinetic-hypertensive syndrome, akathisia (during the first 6 hours after administration), dystonic reactions, persistent tardive dyskinesia (disorders usually appear at the beginning of therapy and often disappear on their own as it continues); rarely - tardive dystonia, neuroleptic malignant syndrome;
endocrine system: rarely – dysmenorrhea; with long-term use of high doses of Chlorprothixene Zentiva - galactorrhea, diabetes mellitus, gynecomastia, decreased potency/libido, increased sweating, changes in carbohydrate metabolism, increased appetite, weight gain;
digestive system: xerostomia (transient); rarely - constipation, cholestatic jaundice (with a long course, especially with the use of high doses, the development of a disorder is most likely between 2 and 4 weeks of therapy);
hematopoietic organs: rarely – agranulocytosis (the disorder most often develops at 4–10 weeks of treatment); in isolated cases - transient benign leukopenia and hemolytic anemia;
sensory organs: clouding of the lens/cornea with possible violation vision, accommodation paresis (occurs at the beginning of treatment and disappears as you continue taking Chlorprothixene Zentiva);
other: skin rash, urinary retention, dermatitis, flushing, withdrawal syndrome, photosensitivity.

Overdose

Main symptoms: drowsiness, hyper- or hypothermia, convulsions, coma, shock, extrapyramidal symptoms.

In case of overdose, symptomatic and supportive therapy is usually prescribed. As much as possible short time gastric lavage should be performed, activated carbon. Activities aimed at maintaining the functioning of the cardiovascular and respiratory systems are also shown. Epinephrine should not be used as it may cause a subsequent decrease in blood pressure. Extrapyramidal disorders can be treated with biperiden, and seizures with diazepam.

special instructions

Taking the drug may lead to false indicators of hyperbilirubinemia, false positive result when conducting an immunobiological urine test for pregnancy, changing the QT interval on the electrocardiogram.

Alcohol abuse increases depression of the central nervous system.

The development of dystonic reactions is most often observed in children and young patients. As a rule, they appear at the beginning of therapy and may subside within 24–48 hours after stopping Chlorprothixene Zentiva.

Parkinsonian extrapyramidal effects may be observed during the first few days of treatment, but their frequency usually increases as the dose is increased; their appearance is more common in elderly patients and older children

Tardive dyskinesia at the beginning of treatment is dose-dependent, but its frequency may increase with a long course and as the total dose is reached. After discontinuation of Chlorprothixene Zentiva, the disorder may persist.

The risk of developing extrapyramidal and hypotensive reactions in adolescents is higher than in adult patients.

When using Chlorprothixene Zentiva, a blood test is required to determine leukocyte formula, indicator monitoring liver function, conducting an ophthalmological examination, as well as careful observation to identify early signs tardive dystonia and dyskinesia.

The occurrence of neuroleptic malignant syndrome is possible at any time during therapy, but more often its development is observed soon after the start of taking Chlorprothixene Zentiva or after transferring the patient from another antipsychotic, during combined use with other psychoactive drugs or after increasing the dose.

From ethanol intake, as well as exposure to insolation and extreme high temperatures It is recommended to abstain.

Therapy should be discontinued gradually, this will reduce the likelihood of developing withdrawal syndrome.

Impact on the ability to drive vehicles and complex mechanisms

While taking Chlorprothixene Zentiva, patients should exercise caution when driving vehicles.

Use during pregnancy and lactation

According to the instructions, Chlorprothixene Zentiva should not be used during pregnancy/lactation, if possible.

Use in childhood

Therapy with Chlorprothixene Zentiva is contraindicated in patients under 6 years of age.

For impaired renal function

Chlorprothixene Zentiva, when indicated for concomitant renal failure, should be used under medical supervision.

For liver dysfunction

Chlorprothixene Zentiva for liver failure should be used under medical supervision.

Drug interactions

ethanol and ethanol-containing drugs, anesthetics, opioid analgesics, sedatives, hypnotics, antipsychotics: the inhibitory effect of chlorprothixene on the central nervous system is enhanced;
antiepileptic drugs (in patients with epilepsy): the threshold of convulsive activity is reduced (additional dose adjustment is required);
m-cholinergic blockers, antihistamines and antiparkinsonian drugs: the anticholinergic effect of chlorprothixene is enhanced;
phenothiazines, metoclopramide, haloperidol, reserpine: extrapyramidal disorders may occur;
levodopa: its effectiveness decreases;
phenylephrine: vasoconstrictor effect may be reduced;
dopamine (in high doses), epinephrine and ephedrine: peripheral vasoconstrictor effect may be perverted;
epinephrine: hypotension and tachycardia may develop;
antihypertensive drugs: their effect is enhanced;
quinidine: risk of development adverse reactions on the part of the heart increases;
guanethidine: the hypotensive effect is reduced;
bromocriptine: hyperprolactinemia may develop, which requires adjustment of the dosage regimen;
ototoxic drugs (especially antibiotics): chlorprothixene may mask symptoms of ototoxicity (in the form of tinnitus, dizziness).

Analogues

An analogue of Chlorprothixene Zentiva is Truxal.

Terms and conditions of storage

Store at temperatures up to 25 °C. Keep away from children.

Shelf life – 3 years.

Catad_pgroup Antipsychotics (neuroleptics)

Chlorprothixene - instructions for use

Registration number:

LP-004840 - 110518

Trade name of the drug

Chlorprothixene

International nonproprietary or generic name

Chlorprothixene

Dosage form:

Film-coated tablets.

Compound

One film-coated tablet, 15 mg, contains:

Active substance:

Chlorprothixene hydrochloride - 15,000 mg

Excipients:

Corn starch - 10,000 mg
Lactose monohydrate - 92,000 mg
Sucrose - 10,000 mg
Calcium stearate -1,500 mg
Talc - 1,500 mg

Film casing:

Opadry 32F250007 red - 5,000 mg

One film-coated tablet, 50 mg, contains:

Active substance:

Chlorprothixene hydrochloride - 50,000 mg

Excipients:

Corn starch - 37,500 mg
Lactose monohydrate - 135,000 mg
Sucrose - 20,000 mg
Calcium stearate - 3,750 mg
Talc - 3,750 mg

Film casing:

Opadry 32F220033 yellow - 7,500 mg

Description

15 mg tablets:

Biconvex, orange film-coated tablets.

50 mg tablets:

Biconvex film-coated tablets from light brown to light yellow.

Pharmacotherapeutic group

Antipsychotic (neuroleptic).

ATX code: N05AF03.

Pharmacological properties

Chlorprothixene is an antipsychotic drug derived from thioxanthene. It has antipsychotic, pronounced sedative and moderate antidepressant effects.

Pharmacodynamics

The antipsychotic effect of neuroleptics is associated with blockade of dopamine receptors, and also, possibly, blockade of 5-HT (5-hydroxytryptamine) receptors. In vivo, chlorprothixene has a high affinity for dopamine receptors type D1 and D2. Chlorprothixene also has high affinity for 5-HT2 receptors, α1-adrenergic receptors, histamine (H1) and cholinergic muscarinic receptors. The receptor binding profile of chlorprothixene is very similar to that of clozapine, but it has approximately 10 times higher affinity for dopamine receptors.

Chlorprothixene reduces the severity or eliminates anxiety, obsessions, psychomotor agitation, restlessness, insomnia, as well as hallucinations, delusions and other psychotic symptoms. The very low incidence of extrapyramidal effects (about 1%) and tardive dyskinesia (about 0.05%) indicate that chlorprothixene can be successfully used for maintenance treatment of patients with psychotic disorders.

Low doses of chlorprothixene have an antidepressant effect, which makes useful application drug for mental disorders characterized by anxiety, depression and restlessness. Also, during therapy with chlorprothixene, the severity of associated psychosomatic symptoms. Chlorprothixene does not cause addiction, dependence or tolerance. In addition, chlorprothixene potentiates the effect of analgesics, has its own analgesic effect, as well as antipruritic and antiemetic effects.

Pharmacokinetics

Suction

When administered orally, maximum plasma concentrations are achieved in approximately 2 hours (range 0.5-6 hours). The average oral bioavailability of chlorprothixene is approximately 12% (range 5-32%).

Distribution

The apparent volume of distribution (Vd)p is approximately 15.5 l/kg. Binding to plasma proteins is more than 99%. Chlorprothixene penetrates the placental barrier.

Biotransformation

The metabolism of chlorprothixene occurs primarily through sulfoxidation and N-demethylation of the side chain. Ring hydroxylation and N-oxidation are less pronounced. Chlorprothixene is determined in bile, which indicates the presence of enterohepatic circulation of the drug. Metabolites of chlorprothixene lack neuroleptic activity.

Removal

The half-life is approximately 16 hours (range 4-33 hours). The average systemic clearance (Cls) corresponds to approximately 1.2 l/min. Chlorprothixene is excreted in feces and urine.

In women who are breastfeeding, chlorprothixene is excreted in milk in small quantities. The ratio between the concentration of the drug in breast milk and blood plasma varies from 1.2 to 2.6.

There were no differences in plasma concentrations or elimination rates between the control group and the alcoholic group, regardless of whether the latter were sober or acutely intoxicated at the time of the study.

Indications for use

Schizophrenia and other psychoses occurring with psychomotor agitation, agitation and anxiety.
Withdrawal syndrome in alcoholism and drug addiction.
Depressive states, neuroses, psychosomatic disorders with anxiety, tension, restlessness, insomnia, sleep disorders.
Epilepsy and oligophrenia, combined with mental disorders: agitation, agitation, mood lability and behavioral disturbances.
Pain (in combination with analgesics).
Geriatrics: hyperactivity, agitation, irritability, confusion, anxiety, behavioral and sleep disorders.

Contraindications

Increased sensitivity to chlorprothixene or any of the excipients.
Hypersensitivity to drugs of the thioxanthene group.
Vascular collapse, depression of consciousness of any origin (including those caused by alcohol, barbiturates or opiates), coma.
Known uncorrectable hypokalemia or hypomagnesemia.
Patient history of clinically significant cardiovascular diseases(eg, bradycardia (heart rate less than 50 beats per minute), recently suffered a heart attack myocardium, decompensated heart failure, cardiac hypertrophy, arrhythmias for which class IA and III antiarrhythmics are prescribed), ventricular arrhythmias or polymorphic ventricular tachycardia pirouette type (lorsade de Pointes).
Congenital long QT syndrome or acquired long QT interval (QTC over 450 ms in men and 470 ms in women).
Concomitant use with drugs that significantly prolong the QT interval.
Lactose or fructose intolerance, lactase deficiency, glucose-galactose malabsorption, sucrase/isomaltase deficiency (due to the presence of lactose and sucrose in the composition).

Carefully

Organic diseases of the brain; mental retardation; a family history of relatives suffering from cardiovascular diseases, as well as cases of prolongation of the QT interval; seizure disorders; severe liver and renal failure; rare pathological condition in the form of a shallow anterior chamber of the eye and its narrow angle (the development of attacks of acute glaucoma associated with pupil dilation is possible); myasthenia gravis; benign prostatic hypertrophy; pheochromocytoma; prolactin-dependent neoplasms; severe arterial hypotension or orthostatic disorders; Parkinson's disease; diseases of the hematopoietic system; hyperthyroidism; painful urination, urinary retention; pyloric stenosis; intestinal obstruction; presence of risk factors for stroke; diabetes; abuse of opiates and alcohol; pregnancy, breastfeeding period; children's and adolescence under 18 years of age (due to lack of strictly controlled studies).

Use during pregnancy and breastfeeding

Pregnancy

Clinical experience in pregnant women is limited. Chlorprothixene should not be prescribed during pregnancy unless the expected benefit to the patient exceeds possible risk for the fetus. Newborns exposed to antipsychotic drugs (including chlorprothixene) during the third trimester of pregnancy are at risk of developing adverse reactions, including extrapyramidal symptoms and/or the onset of withdrawal symptoms, which may vary in severity and duration after delivery. Cases of agitation, increased and decreased tone, tremors, drowsiness, respiratory distress, and eating disorders have been recorded. Therefore, newborns should be closely monitored.

Breast-feeding

Taking into account the fact that chlorprothixene is present in human milk in small concentrations, it is unlikely to have any effect negative impact per child if the drug is prescribed to the mother in therapeutic doses. The dose administered orally to the child is approximately 2% of the daily maternal dose, adjusted for body weight. During treatment with Chlorprothixene, breastfeeding is allowed if deemed clinically necessary. However, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.

Fertility

Adverse effects such as hyperprolactinemia, galactorrhea, amenorrhea, ejaculation disorders, and erectile dysfunction have been recorded in humans (see section " Side effect"). These adverse reactions may have a negative impact on sexual function and fertility in women and/or men.

If clinically significant hyperprolactinemia, galactorrhea, amenorrhea or manifestations occur sexual dysfunction it is necessary to consider reducing the dosage (if possible) or discontinuing the drug. These side effects are reversible after discontinuation of the drug.

Potential Impact medicine fertility has not been studied in animals.

Directions for use and doses

The tablets are swallowed whole with water.

The dosage is selected individually depending on the patient's condition. As a rule, small doses are prescribed at the beginning of treatment, which are increased to the optimal effective level as quickly as possible depending on the therapeutic response.

Schizophrenia and other psychoses. Manic states

Treatment begins with 50-100 mg/day, gradually increasing the dose to

achieving optimal effect, usually up to 300 mg/day. In some cases, the dose may be increased to 1200 mg/day. The maintenance dose is usually 100-200 mg/day.

The daily dose of chlorprothixene is usually divided into 2-3 doses, given the sedative effect of chlorprothixene, it is recommended to prescribe a smaller part of the daily dose in the daytime, and the larger part in the evening.

Withdrawal syndrome in alcoholism and drug addiction

The daily dose, divided into 2-3 doses, is 500 mg for a period of up to 7 days. After symptoms of withdrawal disappear, the dose is gradually reduced. A maintenance dose of 30-75 mg/day allows you to stabilize the condition, reduces the risk of developing another binge, a further dose reduction may be required.

Depressive states, neuroses, psychosomatic disorders

Chlorprothixene can be used for depression, especially when combined with anxiety, tension, as an addition to antidepressant therapy or independently. Chlorprothixene can be prescribed for neuroses and psychosomatic disorders accompanied by anxiety and depressive disorders at a dose of up to 75 mg/day. The daily dose is usually divided into 2-3 doses. Since taking chlorprothixene does not cause addiction or drug dependence, it can be used for a long time. The maximum dose is 150 mg/day.

Epilepsy and mental retardation combined with mental disorders

The daily dose is 50 mg and is usually divided into 2-3 doses. The daily dose can be increased to 75-100 mg/day. For epilepsy, adequate anticonvulsant dosage should be maintained.

Elderly patients

In elderly patients, the dosage is selected individually; the dose range is 15-75 mg/day.

Insomnia

15-30 mg 1 hour before bedtime once.

Pain

The ability of chlorprothixene to potentiate the action of analgesics can be used in the treatment of patients with pain. In these cases, chlorprothixene is prescribed in doses of 75 to 300 mg per day; it can be used in conjunction with analgesics.

Children and teenagers (up to 18 years old)

Renal dysfunction

In patients with impaired renal function, the dosage should be selected with caution, and serum levels of the drug should be monitored whenever possible.

Liver dysfunction

In patients with impaired liver function, the dosage should be selected with caution, and serum levels of the drug should be monitored whenever possible.

Side effect

The most common adverse reactions, which may occur in more than 10% of patients, are dry mouth, increased salivation, drowsiness and dizziness.

Majority side effects depend on the dose of the drug used. The incidence of side effects and their severity are most pronounced at the beginning of treatment and decrease as therapy continues.

Information on the incidence of side effects is presented based on literature data and spontaneous reports.

The frequency of adverse reactions listed below was determined according to the World Health Organization classification: very often (≥ 1/10), often (≥1/100 to<1/10), нечасто (от ≥1/1000 до <1/100), редко (от ≥1/10000 до <1/1000), очень редко (<1/10000), либо неизвестно (не может быть оценена на основании существующих данных).

Blood and lymphatic system disorders:

rarely - thrombocytopenia, neutropenia, leukopenia, agranulocytosis.

Immune system disorders:

rarely - hypersensitivity, anaphylactic reactions.

Endocrine system disorders:

rarely - hyperprolactinemia.

Metabolic and nutritional disorders:

often - increased appetite, weight gain; infrequently - loss of appetite, weight loss; rarely - hyperglycemia, impaired glucose tolerance.

Mental disorders:

often - insomnia, nervousness, agitation, decreased libido.

Nervous system disorders:

very often - drowsiness, dizziness; often - dystonia, headache; infrequently - tardive dyskinesia, parkinsonism, seizures, akathisia; very rarely neuroleptic malignant syndrome.

Visual disorders:

often - disturbance of accommodation, visual impairment; infrequently - involuntary movements of the eyeballs.

Cardiac disorders:

often - tachycardia, palpitations; rarely - prolongation of the QT interval on the electrocardiogram.

Vascular disorders:

infrequently - arterial hypotension, flushing of the face with a feeling of heat; very rarely - venous thromboembolism.

Disorders of the respiratory system, chest and mediastinal organs:

rarely - shortness of breath.

Gastrointestinal disorders:

very often - dry mouth, increased salivation; often - constipation, dyspepsia, nausea; infrequently - vomiting, diarrhea.

Disorders of the liver and biliary tract:

infrequently - changes in laboratory parameters of liver function; very rarely - jaundice.

Disorders of the skin and subcutaneous tissues:

often - increased sweating; uncommon - skin rash, itching, photosensitivity, dermatitis.

Musculoskeletal and connective tissue disorders:

often - myalgia; infrequently - muscle rigidity.

Renal and urinary tract disorders:

infrequently - urinary retention, painful urination.

Pregnancy, postpartum and perinatal conditions:

unknown - neonatal withdrawal syndrome.

Disorders of the genital organs and breast:

uncommon - ejaculation disorders, erectile dysfunction; rarely - gynecomastia, galactorrhea, amenorrhea.

General disorders and disorders at the injection site:

often - asthenia, fatigue.

Extrapyramidal disturbances may occur, especially in the early stages of treatment. In most cases, these side effects are successfully controlled by dose reduction and/or use of antiparkinsonian drugs. However, routine use of antiparkinsonian drugs to prevent side effects is not recommended. They do not improve the symptoms of tardive dyskinesia and may worsen them. It is recommended to reduce the dose or, if possible, discontinue treatment with chlorprothixene.

For persistent akathisia, benzodiazepines or propranolol may be helpful.

When taking chlorprothixene, as with other antipsychotics, the following rare side effects have also been reported: prolongation of the QT interval, ventricular arrhythmias - ventricular fibrillation, ventricular tachycardia, sudden death and polymorphic ventricular tachycardia of the "pirouette" type (Torsade de Pointes).

During the use of antipsychotic drugs, cases of priapism have been recorded - prolonged erection, usually painful, which can lead to erectile dysfunction. The frequency of this phenomenon is unknown (see section " special instructions»).

Abrupt cessation of chlorprothixene may be accompanied by withdrawal reactions. The most common symptoms are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, nervousness, anxiety and agitation. Patients may also experience dizziness, extra sensations of hot and cold, and tremors. Symptoms typically begin within 1-4 days of discontinuation and decrease within 7-14 days.

Overdose

Symptoms

Drowsiness, coma, convulsions, shock, extrapyramidal symptoms, hyperthermia/hypothermia. In severe cases, kidney failure is possible.

In case of overdose and simultaneous use with drugs that affect cardiac activity, the development of ECG changes, prolongation of the QT interval, polymorphic ventricular tachycardia of the “pirouette” type (Torsade de Pointes), cases of cardiac arrest and ventricular arrhythmia have been reported.

Treatment

Symptomatic and supportive. Gastric lavage should be carried out as quickly as possible, and the use of activated carbon is recommended. Measures should be taken to maintain the functioning of the respiratory and cardiovascular systems. Epinephrine should not be used as this may lead to a subsequent decrease in blood pressure. Seizures can be treated with diazepam, and extrapyramidal disorders with biperiden.

A dose of 2.5 g - 4 g can be fatal, in children about 4 mg/kg. Adults survived after taking 10 g, and a three-year-old child after taking 1000 mg.

Interaction with other drugs

Chlorprothixene may enhance the sedative effect of alcohol, the effect of barbiturates and other CNS depressants.

Chlorprothixene should not be prescribed together with guanethidine and similarly active drugs, since antipsychotics can enhance or weaken the effect of antihypertensive drugs; the antihypertensive effect of guanethidine and similarly active drugs is reduced.

Concomitant use of antipsychotics and lithium drugs increases the risk of neurotoxicity.

Tricyclic antidepressants and antipsychotics mutually inhibit each other's metabolism.

Chlorprothixene may reduce the effectiveness of levodopa and the effect of adrenergic drugs.

The simultaneous use of Chlorprothixene and drugs with established anticholinergic effects enhances their anticholinergic effects.

Concomitant use with metoclopramide and piperazine increases the risk of developing extrapyramidal disorders.

The antihistamine effect of chlorprothixene may suppress or eliminate the alcohol/disulfiram reaction.

The increase in the QT interval on the electrocardiogram, characteristic of therapy with antipsychotic drugs, can be enhanced by concomitant use of drugs that significantly prolong the QT interval:

antiarrhythmic drugs of classes IA and III (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some macrolide antibiotics (erythromycin) and quinolone antibiotics (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium and other drugs; significantly increasing the QT interval. The simultaneous use of Chlorprothixene and the above drugs should be avoided. Chlorprothixene should be used with caution concurrently with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics) and drugs that can increase plasma concentrations of chlorprothixene due to a possible increased risk of QT prolongation and life-threatening arrhythmias.

Neuroleptics are metabolized by hepatic isoenzymes of the cytochrome P450 system. Drugs that inhibit the 2D6 isoenzyme (eg, paroxetine, fluoxetine, chloramphenicol, disulfiram, isoniazid, monoamine oxidase inhibitors, oral contraceptives, and, to a lesser extent, buspirone, sertraline and citalopram) may increase plasma levels of chlorprothixene.

special instructions

When using any antipsychotic, there is a risk of developing neuroleptic malignant syndrome (hyperthermia, muscle rigidity, fluctuation of consciousness, instability of the autonomic nervous system). Patients with pre-existing psychoorganic syndrome, mental retardation, as well as those who abuse opiates and alcohol make up a significant proportion of deaths. Treatment: discontinuation of the antipsychotic. Symptomatic therapy and general supportive treatment measures. Dantrolene and bromocriptine may be effective. After taking antipsychotics by mouth, symptoms may persist for more than one week.

In patients with such rare conditions as a small anterior chamber of the eye and a narrow angle, acute attacks of glaucoma associated with pupil dilation are possible.

Due to the risk of developing malignant arrhythmias, chlorprothixene should be used with caution in patients with a history of cardiovascular disease and in patients with a family history of long QT interval.

ECG monitoring is necessary before starting treatment.

Chlorprothixene is contraindicated if the QTC interval at baseline is more than 450 ms in men and 470 ms in women (see section "Contraindications").

During therapy, the need for ECG monitoring should be assessed by the physician, taking into account the individual characteristics of the patient. During treatment, reduce the dosage if the QT interval is prolonged or discontinue therapy if the QTC is > 500 ms.

The simultaneous use of other antipsychotic drugs should be avoided (see section "Interaction with other drugs").

Like other antipsychotics, chlorprothixene should be used with caution in patients with psychoorganic syndrome, seizures, liver, kidney and cardiovascular diseases in the later stages, as well as patients with myasthenia gravis and benign prostatic hyperplasia.

Caution must be exercised when using the drug in patients with

pheochromocytoma,
prolactin-dependent tumors,
severe arterial hypotension or orthostatic regulation
Parkinson's disease,
diseases of the hematopoietic system,
hyperthyroidism,
urinary disorders, urinary retention,
pyloric stenosis (pyloric stenosis), intestinal obstruction.

Like other psychotropic drugs, chlorprothixene may change the concentration of insulin and glucose in the blood, so patients with diabetes may require dosage adjustments of antidiabetic drugs.

Patients undergoing long-term treatment, especially with high doses, are subject to careful monitoring over time with periodic assessment of the need to reduce the maintenance dose. Cases of venous thromboembolism (VTE) have been reported while taking antipsychotic drugs. Due to the fact that patients treated with antipsychotic drugs are often at risk for developing VTE, risk factors for VTE should be identified before and during treatment with chlorprothixene and precautions taken.

It has been reported that antipsychotics with α-adrenergic blocking effects may cause priapism; it is possible that chlorprothixene also has this property. If severe priapism occurs, medical intervention may be required. Patients should be warned about the need to urgently seek medical help if objective and subjective signs of priapism appear.

Use of the drug in children and adolescents under 18 years of age

A sufficient number of studies have not been conducted to study the effectiveness and safety of the use of chlorprothixene for the treatment of children and adolescents.

Elderly patients

Cerebrovascular adverse reactions

In randomized placebo-controlled clinical trials of certain atypical antipsychotics in patients with dementia, a 3-fold increase in the risk of cerebrovascular adverse reactions was observed. The mechanism for this increased risk is unknown. An increased risk cannot be ruled out when using other antipsychotics in other groups of patients. Chlorprothixene should be used with caution in patients at risk of stroke. Elderly individuals are particularly at risk of developing orthostatic hypotension.

Increased mortality in older patients with dementia

Data from two large observational studies showed that older patients with dementia taking antipsychotic drugs had a nonsignificant increased risk of death compared with patients not taking antipsychotic drugs. There is no sufficient data to accurately assess the magnitude of the risk and the reasons for its increase. Chlorprothixene is not registered for the treatment of behavioral disorders in elderly patients with dementia.

Excipients

Impact on the ability to drive vehicles and operate machinery

Chlorprothixene is a drug that has a sedative effect. Patients receiving psychotropic drugs may experience some impairment of general attention and concentration, so they should be warned about the need to be careful when driving vehicles and operating machinery.