Chlorprothixene 15mg when alcohol is allowed. Chlorprothixene. Dosage depending on the disease and concomitant condition

Instructions for use

Chlorprothixen Zentiva instructions for use

Dosage form

Film-coated tablets, orange, round, biconvex.

Compound

1 tab. chlorprothixene hydrochloride 15 mg

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

Pharmacodynamics

The antipsychotic effect of chlorprothixene is associated with its blocking effect on dopamine receptors. The antiemetic and analgesic properties of the drug are also associated with the blockade of these receptors. Chlorprothixene is able to block 5-HT2 - receptors, α1 - adrenoreceptors, as well as H1 - histamine receptors, which determines its adrenoblocking hypotensive and antihistamine properties.

Pharmacokinetics

The bioavailability of chlorprothixene when taken orally is about 12%. Chlorprothixene is rapidly absorbed from the intestine, Cmax in serum is reached after 2 hours. T1 / 2 is about 16 hours. Chlorprothixene crosses the placental barrier and is excreted in breast milk in small amounts. Metabolites do not have antipsychotic activity, are excreted in feces and urine.

Side effects

Drowsiness, tachycardia, dry mouth, excessive sweating, difficulty in accommodation. These side effects, which usually occur at the beginning of therapy, often disappear as therapy is continued.

Orthostatic hypotension may occur, especially with high doses of Chlorprothixene Zentiva.

Dizziness, dysmenorrhea, skin rashes, constipation are rare. Extrapyramidal symptoms are especially rare.

Isolated cases of a decrease in the convulsive threshold, the occurrence of transient benign leukopenia and hemolytic anemia are described.

With prolonged use, especially at high doses, there may be observed: cholestatic jaundice, galactorrhea, gynecomastia, decreased potency and / or libido, increased appetite, weight gain.

Selling Features

prescription

Special conditions

Chlorprothixene Zentiva should be administered with caution to patients suffering from epilepsy, parkinsonism, with severe cerebral atherosclerosis, with a tendency to collapse, with severe cardiovascular and respiratory failure, with severe liver and kidney dysfunction, diabetes mellitus, prostatic hypertrophy.

The use of Chlorprothixene Zentiva can lead to a false positive result when conducting an immunobiological urine pregnancy test, a false increase in the level of bilirubin in the blood, a change in the QT interval on the electrocardiogram.

Influence on the ability to drive vehicles and control mechanisms

Taking Chlorprothixene Zentiva has a negative effect on activities that require a high rate of mental and physical reactions (for example, driving vehicles, servicing machines, working at height, etc.).

Overdose

Symptoms. Drowsiness, hypo- or hyperthermia, extrapyramidal symptoms, convulsions, shock, coma.

Treatment. Symptomatic and supportive. As soon as possible, gastric lavage should be performed, the use of a sorbent is recommended. Measures should be taken to support the activity of the respiratory and cardiovascular systems. Do not use adrenaline, because. this can lead to a subsequent decrease in blood pressure. Convulsions can be stopped with diazepam, and extrapyramidal disorders with biperiden.

Indications

Chlorprothixene Zentiva is a sedative neuroleptic with a wide range of indications, which include:

Psychoses, 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 the intake of alcohol, barbiturates or opiates);

Coma states;

vascular collapse;

Diseases of the hematopoietic organs;

Pheochromocytoma;

Hypersensitivity to the components of the drug.

Chlorprothixene Zentiva should, if possible, be given to pregnant women and during breastfeeding.

Use in elderly patients

drug interaction

The inhibitory effect of chlorprothixene on the central nervous system may be enhanced when taken simultaneously with ethanol and ethanol-containing drugs, anesthetics, opioid analgesics, sedatives, hypnotics, neuroleptics.

The anticholinergic effect of chlorprothixene is enhanced with the simultaneous use of anticholinergic, antihistamine and antiparkinsonian drugs.

The drug enhances the effect of antihypertensive drugs.

The simultaneous use of chlorprothixene and adrenaline can lead to arterial hypotension and tachycardia.

The use of chlorprothixene leads to a decrease in the threshold of convulsive activity, which requires additional dose adjustment of antiepileptic drugs in patients with epilepsy.

The ability of chlorprothixene to block dopamine receptors reduces the effectiveness of levodopa.

Perhaps the appearance of extrapyramidal disorders with the simultaneous use of phenothiazines, metoclopramide, haloperidol, reserpine.

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Mode of application

Dosage

Psychoses, including schizophrenia and manic states.

Treatment begins with 50-100 mg / day, gradually increasing the dose until the optimal effect is achieved, 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 Zentiva is usually divided into 2-3 doses, given the pronounced sedative effect of Chlorprothixene Zentiva, it is recommended to prescribe a smaller part of the daily dose in the daytime, and most of it in the evening.

Hangover withdrawal syndrome in alcoholism and drug addiction.

The daily dose, divided into 2-3 doses, is 500 mg. The course of treatment usually lasts 7 days. After the disappearance of withdrawal symptoms, the dose is gradually reduced. A maintenance dose of 15-45 mg / day allows you to stabilize the condition, reduces the risk of developing another binge.

In elderly patients with hyperactivity, irritability, agitation, confusion, 15-90 mg / day is prescribed. The daily dose is usually divided into 3 doses.

In children, for the correction of behavioral disorders, Chlorprothixene Zentiva is prescribed at the rate of 0.5-2 mg / kg of body weight.

Depressive states, neuroses, psychosomatic disorders.

Chlorprothixene Zentiva can be used for depression, especially when combined with anxiety, tension, as an adjunct to antidepressant therapy or on its own. Chlorprothixene Zentiva can be prescribed for neurosis and psychosomatic disorders accompanied by anxiety and depressive disorders up to 90 mg / day. The daily dose is usually divided into 2-3 doses. Since taking Chlorprothixene Zentiva does not cause the development of addiction or drug dependence, it can be used for a long time.

Insomnia. 15-30 mg in the evening 1 hour before bedtime.

Pain. The ability of Chlorprothixene Zentiva to potentiate the action of analgesics can be used in the treatment of patients with pain. In these cases, Chlorprothixene Zentiva is prescribed together with analgesics in doses of 15 to 300 mg.

Chlorprothixen Zentiva: instructions for use and reviews

Latin name: Chlorprothixen-Zentiva

ATX code: N05AF03

Active substance: chlorprothixene (chlorprothixene)

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

Description and photo update: 21.11.2018

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

Release form and composition

Dosage form of Chlorprothixene Zentiva - film-coated tablets: round, biconvex, orange (15 mg each) or from 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 bundle 3 or 5 blister 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 a neuroleptic, a derivative of thioxanthene. It has an antipsychotic, moderate antidepressant and pronounced sedative effect. The antipsychotic effect is associated with the blocking effect of chlorprothixene on dopamine receptors. Also, the analgesic and anti-emetic properties of the drug are associated with the blockade of these receptors. Chlorprothixene is able to block a1-adrenergic receptors, 5-HT2 receptors, and H1-histamine receptors, which determines its adrenoblocking hypotensive and antihistamine action.

Pharmacokinetics

When taken orally, the bioavailability of chlorprothixene is approximately 12%. After oral administration, it is absorbed well and quickly. It undergoes first pass metabolism in the liver and intestinal walls. It has the effect of the first passage through the liver.

Chlorprothixene crosses the placental barrier and into breast milk.

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

The half-life is in the range of 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 / sucrose deficiency (Lactose and sucrose are part of Chlorprothixene Zentiva);
depression of the central nervous system of any origin (including those associated with the intake of alcohol, opiates or barbiturates);
vascular collapse;
coma;
age up to 6 years;
individual intolerance to the components of the drug, including phenothiazines.

Relative (Chlorprothixen 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 in clinical manifestations of prostatic hyperplasia;
renal/liver failure;
Reye's syndrome;
Parkinson's disease (associated with increased extrapyramidal disorders);
severe cardiovascular and respiratory failure associated with acute infectious diseases, asthma or emphysema (there is a high risk of transient increase in blood pressure);
severe atherosclerosis of cerebral vessels;
peptic ulcer of the stomach and duodenum;
epilepsy (associated with the likelihood of more frequent seizures as a result of lowering the seizure threshold);
pregnancy and lactation.

Instructions for use 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.

psychosis, including manic states and schizophrenia: the initial daily dose is 50-100 mg. Gradually increase the dose 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, a smaller part should be taken in the daytime, a large part in the evening;
withdrawal syndrome in drug addiction and alcoholism: daily dose - 500 mg in 2-3 doses. Duration of application - 7 days. After improvement of the condition, the dose is gradually reduced. The maintenance daily dose is in the range of 15 to 45 mg. Taking Chlorprothixene Zentiva allows you to stabilize the condition, reduce the likelihood of developing another binge;
hyperactivity, irritability, agitation, confusion in elderly patients: 15 to 90 mg per day in 3 divided doses;
behavioral disorders in children: 0.5–2 mg/kg;
neurosis, 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 often; > 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 in the Q-T interval on the electrocardiogram and tachycardia;
nervous system: dizziness, fatigue, drowsiness, psychomotor retardation, mild extrapyramidal hypokinetic-hypertensive syndrome, akathisia (during the first 6 hours after administration), dystonic reactions, persistent tardive dyskinesia (disturbances usually appear at the beginning of therapy and often as it continues disappear on their own) rarely - tardive dystonia, neuroleptic malignant syndrome;
endocrine system: rarely - dysmenorrhea; with prolonged 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 (is transient); rarely - constipation, cholestatic jaundice (with a long course, especially with the use of high doses, the development of a disorder between 2 and 4 weeks of therapy is most likely);
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 visual impairment, paresis of accommodation (occurs at the beginning of treatment and disappears as you continue taking Chlorprothixene Zentiva);
others: 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. Gastric lavage and activated charcoal intake should be carried out as soon as possible. It also shows activities aimed at maintaining the work of the cardiovascular and respiratory systems. Epinephrine should not be used, as this may cause a subsequent decrease in blood pressure. Extrapyramidal disorders can be stopped with biperiden, convulsions with diazepam.

special instructions

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

Alcohol abuse increases the depression of the central nervous system.

Most often, the development of dystonic reactions is 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.

In the first few days of treatment, parkinsonian extrapyramidal effects may occur, but usually their frequency increases as the dose increases; more often their appearance is noted 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 the abolition of Chlorprothixene Zentiva, the disturbance may persist.

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

During the use of Chlorprothixene Zentiva, a blood test and determination of the leukocyte formula, monitoring of liver function parameters, an ophthalmological examination, and careful observation in order to detect early signs of tardive dystonia and dyskinesia are required.

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

It is recommended to refrain from taking ethanol, as well as exposure to insolation and extremely high temperatures.

Cancel therapy should be gradual, this will reduce the likelihood of developing a withdrawal syndrome.

Influence on the ability to drive vehicles and complex mechanisms

While taking Chlorprothixene Zentiva, patients should be careful when driving vehicles.

Use during pregnancy and lactation

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

Application in childhood

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

For impaired renal function

Chlorprothixene Zentiva, if indicated, should be used under medical supervision in concomitant renal insufficiency.

For impaired liver function

Chlorprothixene Zentiva in hepatic insufficiency should be used under medical supervision.

drug interaction

ethanol and ethanol-containing drugs, anesthetics, opioid analgesics, sedatives, hypnotics, neuroleptics: the inhibitory effect of chlorprothixene on the central nervous system is enhanced;
antiepileptic drugs (in patients with epilepsy): the threshold for convulsive activity decreases (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 is reduced;
phenylephrine: vasoconstrictor effect may decrease;
dopamine (at high doses), epinephrine and ephedrine: peripheral vasoconstrictor action may be perverted;
epinephrine: arterial hypotension and tachycardia may develop;
antihypertensive drugs: their effect is enhanced;
quinidine: the risk of adverse reactions from the heart increases;
guanethidine: the hypotensive effect is reduced;
bromocriptine: hyperprolactinemia may develop, which requires correction of the dosing regimen;
ototoxic drugs (especially antibiotics): chlorprothixene may mask symptoms of ototoxicity (tinnitus, dizziness).

Analogues

An analogue of Chlorprothixene Zentiva is Truxal.

Terms and conditions of storage

Store below 25°C. Keep away from children.

Shelf life - 3 years.

Latin name

Chlorprothixenum

Release form

Film-coated tablets

1 film-coated tablet contains:
active substance: chlorprothixene hydrochloride 15 mg,
excipients: corn starch, lactose monohydrate, sucrose, calcium stearate, talc;
shell composition: hypromellose 2910/5, macrogol 6000, macrogol 300, talc, aluminum varnish based on sunset yellow dye.

Package

30 tablets.

pharmachologic effect

The antipsychotic effect of Chlorprothixene is associated with its blocking effect on dopamine receptors. The antiemetic and analgesic properties of the drug are also associated with the blockade of these receptors. Chlorprothixene is able to block 5-HT2 - receptors, α1 - adrenoreceptors, as well as H1 - histamine receptors, which determines its adrenoblocking hypotensive and antihistamine properties.

Pharmacokinetics

Indications

Chlorprothixene is a sedative neuroleptic with a wide range of indications, which include:

psychoses, 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

Hypersensitivity to Chlorprothixene components;
depression of the central nervous system of any origin (including those caused by the intake of alcohol, barbiturates or opiates);
coma;
vascular collapse;
diseases of the hematopoietic organs;
pheochromocytoma.

Use during pregnancy and lactation

Chlorprothixene should, if possible, be given to pregnant women and during breastfeeding.

Dosage and administration

Psychoses, including schizophrenia and manic states.

Treatment begins with 50-100 mg/day, gradually increasing the dose until the optimal effect is achieved, 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 Zentiva is usually divided into 2-3 doses, given the pronounced sedative effect of Chlorprothixene Zentiva, it is recommended to prescribe a smaller part of the daily dose in the daytime, and most of it in the evening.

Hangover withdrawal syndrome in alcoholism and drug addiction.

In elderly patients

In the presence of hyperactivity, irritability, agitation, confusion, 15-90 mg / day is prescribed. The daily dose is usually divided into 3 doses.

To correct behavioral disorders, Chlorprothixene Zentiva is prescribed at the rate of 0.5-2 mg/kg of body weight.

Depressive states, neuroses, psychosomatic disorders.

Insomnia. 15 - 30 mg in the evening 1 hour before bedtime.

Side effects

Drowsiness, tachycardia, dry mouth, excessive sweating, difficulty in accommodation. These side effects, which usually occur at the beginning of therapy, often disappear as therapy is continued.

Orthostatic hypotension may occur, especially with high doses of Chlorprothixene.

Dizziness, dysmenorrhea, skin rashes, constipation are rare. Extrapyramidal symptoms are especially rare.

Isolated cases of a decrease in the convulsive threshold, the occurrence of transient benign leukopenia and hemolytic anemia are described.

With prolonged use, especially at high doses, there may be observed: cholestatic jaundice, galactorrhea, gynecomastia, decreased potency and / or libido, increased appetite, weight gain.

special instructions

Chlorprothixene should be administered with caution to patients suffering from epilepsy, parkinsonism, with severe cerebral atherosclerosis, with a tendency to collapse, with severe cardiovascular and respiratory failure, with severe liver and kidney dysfunction, diabetes mellitus, prostatic hypertrophy.
The use of Chlorprothixene can lead to a false positive result during an immunobiological urine pregnancy test, a false increase in the level of bilirubin in the blood, a change in the QT interval on the electrocardiogram.
During treatment with the drug, it is recommended to refrain from drinking alcohol, to avoid increased insolation.

Influence on the ability to drive vehicles and control mechanisms
The intake of Chlorprothixene has a negative effect on activities that require a high rate of mental and physical reactions (for example, driving vehicles, servicing machines, working at height, etc.).

Instructions for use

Active ingredients

Release form

Tablets

Compound

Active ingredient: Chlorprothixenum (Chlorprothixenum) Active ingredient concentration (mg): 15

Pharmacological effect

Antipsychotic agent (neuroleptic), a derivative of thioxanthene. has an antipsychotic, antidepressant, sedative, antiemetic effect, 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 the blockade of the chemoreceptor trigger zone of the medulla oblongata. sedative effect is due to an indirect weakening of the activity of the reticular system of the brain stem. inhibits the release of most hormones of the hypothalamus and pituitary gland. however, as a result of the blockade of the prolactin-inhibiting factor, which inhibits the release of prolactin from the pituitary gland, the concentration of prolactin increases. The chemical structure and pharmacological properties of thioxanthenes are similar to piperazine derivatives of phenothiazine.

Pharmacokinetics

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

Indications

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

Contraindications

depression of the central nervous system of any origin (including those caused by the intake of alcohol, barbiturates or opiates); coma; 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 lactation

Contraindicated for use during pregnancy and lactation.

Dosage and administration

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

Side effects

Drowsiness, tachycardia, dry mouth, excessive sweating, difficulty in accommodation. These side effects, which usually occur at the beginning of therapy, often disappear as it continues. Orthostatic hypotension may occur, especially when Chlorprothixene is used in high dosages. Dizziness, dysmenorrhea, skin rashes, and constipation are rare. Extrapyramidal symptoms are especially rare. Isolated cases of a decrease in the convulsive threshold, the occurrence of transient benign leukopenia and hemolytic anemia are described. body weight.

Interaction with other drugs

With simultaneous use with anesthetics, opioid analgesics, sedatives, hypnotics, antipsychotics, with ethanol, ethanol-containing drugs, the inhibitory effect on the central nervous system increases. action. When used simultaneously with agents that cause extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal reactions is possible; with levodopa - it is possible to inhibit the antiparkinsonian action of levodopa; with lithium carbonate - pronounced extrapyramidal symptoms, neurotoxic effect are possible. With simultaneous use with epinephrine, blockade of the alpha-adrenergic effects of epinephrine and the development of severe hypotension and tachycardia as a result are possible. With simultaneous use with phenothiazines, metoclopramide, haloperidol, reserpine, extrapyramidal disorders may develop; with quinidine - it is possible to increase the inhibitory effect on the heart.

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 necessary, the use of chlorprothixene should be compared with the risk and benefit treatment in patients with chronic alcoholism, diseases of the cardiovascular system (increased risk of developing transient arterial hypotension), Reye's syndrome, as well as in glaucoma or a predisposition to it, peptic ulcer of the stomach and duodenum, urinary retention, Parkinson's disease, epileptic seizures, increased sensitivity to other thioxanthenes or phenothiazines. When using chlorprothixene, false positive results of an immunological pregnancy test using urine, as well as false positive results of a urine test for bilirubin, are possible. During the treatment period, avoid drinking alcohol. assessment of the ability to drive vehicles and control mechanisms During the period of treatment, one should refrain from engaging in potentially hazardous activities that require increased attention, rapid psychomotor reactions.

Catad_pgroup Antipsychotics (Neuroleptics)

Chlorprothixene - instructions for use

Registration number:

LP-004840 - 110518

Trade name of the drug

Chlorprothixene

International nonproprietary or grouping name

Chlorprothixene

Dosage form:

Film-coated tablets.

Compound

One 15 mg film-coated tablet 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 sheath:

Opadry 32F250007 red - 5,000 mg

One 50 mg film-coated tablet 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 sheath:

Opadry 32F220033 yellow - 7.500 mg

Description

Tablets 15 mg:

Orange biconvex film-coated tablets.

Tablets 50 mg:

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

Pharmacotherapeutic group

Antipsychotic drug (neuroleptic).

ATX code: N05AF03.

Pharmacological properties

Chlorprothixene is a neuroleptic, a derivative of thioxanthene. It has an antipsychotic, pronounced sedative and moderate antidepressant effect.

Pharmacodynamics

The antipsychotic effect of neuroleptics is associated with the blockade of dopamine receptors, and also, possibly, the blockade of 5-HT (5-hydroxytryptamine) receptors. In vivo, chlorprothixene has a high affinity for dopamine D1 and D2 receptors. Chlorprothixene also has a high affinity for 5-HT2 receptors, a1-adrenergic receptors, histamine (H1) and cholinergic muscarinic receptors. The receptor binding profile of chlorprothixene is very similar to that of clozapine, however, it has an approximately 10-fold 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 therapy in patients with psychotic disorders.

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

Pharmacokinetics

Suction

When administered orally, peak plasma concentrations are reached after about 2 hours (range 0.5-6 hours). The mean oral bioavailability of chlorprothixene is about 12% (range 5-32%).

Distribution

The apparent volume of distribution (Vd)p is about 15.5 l/kg. Plasma protein binding is more than 99%. Chlorprothixene crosses the placental barrier.

Biotransformation

Metabolism of chlorprothixene is carried out mainly by 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. Chlorprothixene metabolites lack neuroleptic activity.

breeding

The elimination half-life is about 16 hours (range 4-33 hours). The average systemic clearance (Cls) corresponds to approximately 1.2 l / min. Excretion of chlorprothixene is carried out with feces and urine.

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

No differences in plasma concentrations or elimination rates were found between the control group and the group of patients suffering from alcoholism, regardless of whether the latter were sober or in a state of acute intoxication during 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 disturbances.
Epilepsy and oligophrenia, combined with mental disorders: agitation, agitation, mood lability and behavioral disorders.
Pain (in combination with analgesics).
Geriatrics: hyperactivity, agitation, irritability, confusion, anxiety, behavioral and sleep disturbances.

Contraindications

Hypersensitivity to chlorprothixene or any of the excipients.
Hypersensitivity to drugs of the thioxanthenes group.
Vascular collapse, depression of consciousness of any origin (including those caused by the intake of alcohol, barbiturates or opiates), coma.
Known uncorrectable hypokalemia or hypomagnesemia.
Patient history of clinically significant cardiovascular disease (eg, bradycardia (heart rate less than 50 beats per minute), recent myocardial infarction, decompensated heart failure, cardiac hypertrophy, arrhythmias for which class IA and III antiarrhythmics are prescribed), ventricular arrhythmias or polymorphic ventricular tachycardia of the "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).
Simultaneous administration with drugs that significantly lengthen the QT interval.
Lactose or fructose intolerance, lactase deficiency, glucose-galactose malabsorption, sucrase / isomaltase deficiency (due to the presence of lactose and sucrose).

Carefully

Organic diseases of the brain; mental retardation; the presence in the family history of relatives suffering from cardiovascular diseases, as well as cases of prolongation of the QT interval; convulsive disorders; severe liver and kidney failure; a rare pathological condition in the form of a shallow anterior chamber of the eye and its narrow angle (it is possible to develop attacks of acute glaucoma associated with pupil dilation); severe pseudoparalytic 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; the presence of risk factors for stroke; diabetes; abuse of opiates and alcohol; pregnancy, breastfeeding period; children and adolescents under 18 years of age (due to the lack of strictly controlled studies).

Use during pregnancy and during breastfeeding

Pregnancy

Clinical experience with pregnant women is limited. Chlorprothixene should not be administered during pregnancy unless the expected benefit to the patient outweighs the potential risk to the fetus. Newborns exposed to antipsychotics (including chlorprothixene) during the third trimester of pregnancy are at risk of adverse reactions, including extrapyramidal symptoms and/or withdrawal symptoms, which may vary in severity and duration postpartum. There have been cases of agitation, increased and decreased tone, tremor, drowsiness, respiratory distress, and malnutrition. Therefore, newborns should be closely monitored.

Breast-feeding

Given the fact that chlorprothixene is present in low concentrations in breast milk, it is unlikely to have a negative effect on the child if the mother is prescribed the drug in therapeutic doses. The oral dose to the child is approximately 2% of the daily maternal dose adjusted for body weight. During treatment with Chlorprothixene, breast-feeding is allowed if it is considered clinically necessary. Nevertheless, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.

Fertility

A person has recorded such undesirable effects as hyperprolactinemia, galactorrhea, amenorrhea, ejaculation disorders, and erectile dysfunction (see section "Side Effects"). These adverse reactions may have a negative effect on the sexual function and fertility of women and/or men.

In the event of clinically significant hyperprolactinemia, galactorrhea, amenorrhea, or manifestations of sexual dysfunction, consideration should be given to reducing the dosage (if possible) or discontinuing the drug. These side effects are reversible after discontinuation of the drug.

The potential effect of the drug on fertility in animals has not been studied.

Dosage and administration

The tablets are swallowed whole with a glass of water.

The dosage is selected individually depending on the patient's condition. As a rule, small doses are given 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

achieve 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 most of it 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 the disappearance of withdrawal symptoms, 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, 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 adjunct to antidepressant therapy or on its own. Chlorprothixene can be prescribed for neurosis 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 the development of addiction or drug dependence, it can be used for a long time. The maximum dose is 150 mg / day.

Epilepsy and oligophrenia, combined with mental disorders

The daily dose is 50 mg and is usually divided into 2-3 doses. The daily dose may be increased to 75-100 mg/day. In epilepsy, an adequate dosage of the anticonvulsant 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 is possible to use it in conjunction with analgesics.

Children and teenagers (under 18)

Kidney dysfunction

In patients with impaired renal function, the dosage should be selected with caution, and, if possible, monitor the level of the drug in the blood serum.

Liver dysfunction

In patients with impaired liver function, the dosage should be selected with caution, and, if possible, monitor the level of the drug in the blood serum.

Side effect

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

Most side effects depend on the dose of the drug used. The frequency of occurrence 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 on the basis of literature data and spontaneous reports.

The frequency of adverse reactions listed below was determined according to the classification of the World Health Organization: very often (≥ 1/10), often (from ≥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, convulsions, akathisia; very rarely neuroleptic malignant syndrome.

Violations of the organ of vision:

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

Heart disorders:

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

Vascular disorders:

infrequently - arterial hypotension, flushes of blood to the skin of the face with a feeling of heat; very rarely - venous thromboembolism.

Respiratory, thoracic and mediastinal disorders:

rarely - shortness of breath.

Gastrointestinal disorders:

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

Liver and biliary tract disorders:

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

Skin and subcutaneous tissue disorders:

often - increased sweating; infrequently - 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.

Genital and breast disorders:

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

General disorders and disorders at the injection site:

often - asthenia, fatigue.

Extrapyramidal disorders may occur, especially in the early stages of treatment. In most cases, these side effects are successfully controlled by dose reduction and / or the use of antiparkinsonian drugs. However, the routine use of antiparkinsonian agents to prevent side effects is not recommended. They do not alleviate the manifestations of tardive dyskinesia and may worsen them. Dose reduction or, if possible, discontinuation of treatment with chlorprothixene is recommended.

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).

Against the background of the use of antipsychotics, cases of priapism have been recorded - a prolonged erection, usually painful, which can lead to erectile dysfunction. The frequency of this phenomenon is unknown (see section "Special Instructions").

Abrupt discontinuation 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, additional sensations of heat and cold, and tremors. Symptoms typically begin within 1-4 days of withdrawal and improve within 7-14 days.

Overdose

Symptoms

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

In case of overdose and concomitant 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 soon as possible, the use of activated charcoal is recommended. Measures should be taken to support the activity of the respiratory and cardiovascular systems. Epinephrine should not be used, as this may lead to a subsequent decrease in blood pressure. Convulsions can be stopped 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 10 g, and a three-year-old child after 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 administered together with guanethidine and similarly acting agents, since antipsychotics may enhance or weaken the effect of antihypertensive agents; the antihypertensive effect of guanethidine and similarly acting drugs is reduced.

The simultaneous use of neuroleptics and lithium preparations 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 an established anticholinergic effect enhances their anticholinergic effects.

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

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

The increase in the QT interval on the electrocardiogram, characteristic of antipsychotic therapy, can be enhanced by the simultaneous administration of drugs that significantly lengthen the QT interval:

class IA and III antiarrhythmic drugs (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 prolonging the QT interval. The concomitant use of Chlorprothixene and the above drugs should be avoided. Chlorprothixene should be used with caution concomitantly with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics) and drugs that can increase the concentration of chlorprothixene in plasma, due to a possible increase in the risk of prolongation of the QT interval and the occurrence of life-threatening arrhythmias.

Antipsychotics 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

Against the background of the use of any antipsychotic, there is a possibility of developing a malignant neuroleptic syndrome (hyperthermia, muscle rigidity, fluctuation of consciousness, instability of the autonomic nervous system). Patients with pre-existing psycho-organic syndrome, mental retardation, as well as opiate and alcohol abusers account for a significant proportion of deaths. Treatment: withdrawal of antipsychotics. 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 rare conditions such as a shallow anterior chamber and a narrow anterior chamber angle, acute glaucoma attacks associated with pupillary 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 a prolonged QT interval.

Before starting treatment, it is necessary to monitor the ECG.

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 in case of prolongation of the QT interval 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, convulsions, diseases of the liver, kidneys and cardiovascular system in the later stages, as well as in patients with severe pseudoparalytic 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 incontinence, urinary retention,
pyloric stenosis (pyloric stenosis), intestinal obstruction.

Like other psychotropic drugs, chlorprothixene can change the concentration of insulin and glucose in the blood, so patients with diabetes may need to adjust the doses of antidiabetic drugs.

Patients undergoing long-term treatment, especially with the use of high doses, are subject to careful monitoring in dynamics with a 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 antipsychotics are often at risk of developing VTE, risk factors for VTE should be identified before and during treatment with chlorprothixene and precautions should be taken.

It has been reported that antipsychotics with a-adrenergic blocking activity can 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 for emergency medical attention in the event of the appearance of objective and subjective signs of priapism.

The use of the drug in children and adolescents under 18 years of age

A sufficient number of studies aimed at studying the efficacy and safety of the use of chlorprothixene for the treatment of children and adolescents have not been conducted.

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 increase in risk is unknown. An increased risk cannot be ruled out with the use of other antipsychotics in other groups of patients. Chlorprothixene should be used with caution in patients at risk of stroke. The elderly are particularly at risk of developing orthostatic hypotension.

Increased mortality in elderly patients with dementia

Data from two large observational studies showed that elderly patients with dementia who took antipsychotics had a slightly increased risk of death compared with patients who did not take antipsychotics. There are 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

Influence on the ability to drive vehicles and work with mechanisms

Chlorprothixene is a drug with 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 working with mechanisms.

Release form

Film-coated tablets, 15 mg, 50 mg.

10 tablets in a blister pack made of PVC film and printed lacquered aluminum foil.

1, 3 or 5 blister packs together with instructions for use are placed in a pack of cardboard.

30 or 60 tablets in a polymer jar with first opening control and a polymer lid.

1 polymer jar, together with instructions for use, is placed in a cardboard pack.

Best before date:

Do not use the drug after the expiration date.

Storage conditions:

At a temperature not higher than 25 °C. Keep out of the reach of children.

Holiday conditions

On prescription.

Registration certificate holder

Limited Liability Company "Pharmacy in the Plus" (000 "AVP"), Russia, 117186, Moscow, Nagornaya street, 20, building 1.

Manufacturer/organization accepting claims

Pharmproekt JSC, Russia, 192236, St. Petersburg, st. Sofiyskaya, 14.