Chlorprothixene 15 mg. Chlorprothixene: instructions for use. Influence on the ability to drive vehicles and complex mechanisms

The description is up to date 18.06.2014

Latin name: Chlorprothixen
ATX code: N05AF03
Active substance: Chlorprothixene (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, cornstarch, talc, sucrose.

The composition of the tablet shell: hypromellose, macrogol, hazardous spray 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 packs of 10 and 100 ampoules.

pharmachologic effect

The drug is antipsychotic means ( neuroleptic ), which is 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 to block α1-adrenergic receptors, 5-HT2 receptors, and H1-histamine receptors.

Indications for the use of Chlorprothixene

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

hangover 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 the elderly;
pain (the drug is used together with).

Pharmacodynamics and pharmacokinetics

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

The elimination half-life from the body is approximately 16 hours. The drug penetrates placental barrier and is excreted in small amounts in breast milk. They do not have antipsychotic activity, excretion occurs with 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 the composition of Chlorprothixene.

Side effects

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

Application instruction of Chlorprothixene (Way and dosage)

With a hangover withdrawal syndrome caused by drug addiction or alcoholism

The daily dose of 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, it is enough to reduce the risks of developing another binge and stabilize the patient's condition.

For psychosis, 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 reached, 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, while it is recommended to use a smaller dose in the daytime, and in the evening - most, due to the pronounced sedative effect of the drug.

With neurosis, depressive states and psychosomatic disorders

Alone or as an adjunct to therapy with antidepressants, the drug is used for depression, and especially for conditions that are combined with anxiety. With psychosomatic disorders that are accompanied by depressive disorders and anxiety, as well as with 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, it is possible to take Chlorprothixene for a sufficiently long time without any special risks.

Instructions for use for insomnia

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

For pain

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

Overdose

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

In case of an overdose of Chlorprothixene, supportive and symptomatic treatment is performed. As soon as possible, you need to do a gastric lavage, it is also recommended to take sorbent . It is required to take measures that are aimed at maintaining the activity of the cardiovascular and respiratory systems. Can not use because it can lower blood pressure. Extrapyramidal disorders can be stopped with Biperiden, and convulsions -.

Interaction

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

The drug enhances the effect of antihypertensive drugs .

While taking Chlorprothixene 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 administration of the drug with Metoclopramide , or phenothiazines may cause extrapyramidal disorders.

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

Terms of sale

The drug is dispensed in pharmacies by prescription.

Storage conditions

Chlorprothixen should be stored in a cool place with an ambient temperature of no more than 25 ° C and no light.

Best before date

The drug is stored for 2 years.

special instructions

Chlorprothixen should be used with caution in patients who suffer from epilepsy , in case of propensity to collapse, with severe respiratory and cardiovascular insufficiency, severe disorders of the kidneys and liver, prostatic hypertrophy, pronounced.

The drug has a negative effect on activities that are associated with a high rate of physical and mental reactions - driving, working at height, servicing machines, and so on.

Chlorprothixene's analogs

Coincidence in the ATX code of the 4th level:

Chlorprothixene 15 Lechiva , Chlorprothixene 50 Lechiva , Truskal .

Synonyms

Tarazan , Chlorprothixene hydrochloride , Vetakalm , Minithixen , Taktaran , Truxil , Chlotixen , Triktal , Taraktan , .

children

For correction of behavioral disorders in children, the drug is prescribed at the 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 about Chlorprothixene

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

From the negative reviews, one can single out, which occurs after taking the drug and a slight lethargy. Some have experienced significant anxiety caused by. But at the same time, the majority of reviews are positive.

Description

Brown coated tablets, round, with a biconvex surface. The cross section shows the core of an almost white color.

Compound

One tablet contains: active substance: chlorprothixene hydrochloride - 15 mg, 25 mg or 50 mg; Excipients: corn starch, powdered sugar, talc, calcium stearate, lactose monohydrate, Opadry II (brown) (including partially hydrolyzed polyvinyl alcohol, talc, macrogol 3350, titanium dioxide E 171, iron oxide yellow E 172, iron oxide red E 172, iron oxide black E 172, indigo carmine E 132).

Pharmacotherapeutic group

Antipsychotics. Derivatives of thioxanthene.
ATC Code: N05AF03.

Pharmacological properties

Chlorprothixene is an antipsychotic agent of the thioxanthenes group.
The antipsychotic effect of these drugs is associated with the blockade of dopamine receptors, and possibly also the blockade of 5-HT receptors (5-hydroxytryptamine, serotonin). In vivo, chlorprothixene has a high affinity for dopamine D1 and D2 receptors. Chlorprothixene also has a high affinity for 5-HT2 receptors and α1-adrenergic receptors, which is similar to high-dose phenothiazines, levomepromazine, chlorpromazine and thioridazine, as well as the atypical antipsychotic clozapine. It has been demonstrated that chlorprothixene has an affinity for histamine (H1) receptors at the level of diphenhydramine. In addition, chlorprothixene has an affinity for cholinergic muscarinic receptors. The receptor binding profile of chlorprothixene is very similar to that of clozapine, however, chlorprothixene has an approximately 10-fold higher affinity for dopamine receptors.
In all studies with behavioral models for antipsychotic activity (blocking dopamine receptors), chlorprothixene demonstrated a pronounced antipsychotic effect. A relationship has been demonstrated between the two in vivo models, in vitro affinity for dopamine D2 receptors, and the average daily oral dose of an antipsychotic.
In clinical use, chlorprothixene is a high-dose broad-spectrum sedative antipsychotic used to treat psychotic disorders other than depression.
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%) (based on 11,487 patients) 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 properties.
Pharmacokinetics
Suction
Peak plasma concentrations are reached approximately 2 hours (0.5 to 6 hours) after oral administration. The average oral bioavailability of chlorprothixene is about 12% (range 5 to 32%).
Distribution
The apparent volume of distribution (Vd) is about 15.5 l/kg. Plasma protein binding - more than 99%.
Chlorprothixene crosses the placental barrier.
Metabolism
Chlorprothixene is predominantly metabolized by sulfoxidation and N-demethylation of the side chain. Ring hydroxylation and N-oxidation occur to a lesser extent. Chlorprothixene was found in bile, suggesting enterohepatic recirculation. Metabolites do not have antipsychotic activity.
breeding
The half-life (T½) is about 15 hours (from 3 to 29 hours). The average systemic clearance (Cls) is approximately 1.2 l / min. Chlorprothixene is excreted by the kidneys and intestines.
Small amounts are excreted in breast milk. The milk/plasma ratio in breastfeeding women ranges 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 with alcoholism, regardless of whether the latter were sober or under the influence of alcohol during the study.
Elderly patients (over 65 years old)

Liver dysfunction
Application experience is not enough.
Kidney dysfunction
Application experience is not enough.

Indications for use

Psychotic disorders excluding depression.
Contraindications
Hypersensitivity to the active substance, other thioxanthenes or any of the excipients.
CNS depression, regardless of cause (for example, intoxication with alcohol, barbiturates or opiates), vascular collapse, coma.
Chlorprothixene may cause prolongation of the QT interval. Prolonged prolongation of the QT interval may increase the risk of malignant arrhythmias. Therefore, chlorprothixene is contraindicated in patients with a history of clinically significant cardiovascular disease (eg, severe bradycardia (< 50 ударов в минуту)), недавно перенесенным инфарктом миокарда, нелеченной сердечной недостаточностью, гипертрофией сердца, аритмиями, при которых назначают антиаритмические средства IA и III классов), а также пациентам с желудочковой аритмией или пируэтной желудочковой тахикардией (torsade de pointes).
Chlorprothixene is contraindicated in patients:
- with uncorrected hypokalemia,
- with uncorrected hypomagnesemia,
- with QT interval prolongation syndrome,
- at the same time taking drugs that prolong the QT interval.

Dosage and administration

adults
Psychoses: 50-100 mg/day in divided doses. The dose may be increased to 600 mg/day.
Maintenance dose: 100-200 mg/day in divided doses.
Children and teenagers
Chlorprothixene is not recommended for use in children and adolescents under 18 years of age due to the lack of adequate controlled studies.

Side effects

The most common side effects, 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. Especially at the beginning of treatment, movement disorders may occur. In most cases, these side effects are eliminated by dose reduction and / or the use of antiparkinsonian drugs. Prophylactic use of antiparkinsonian drugs is not recommended. Antiparkinsonian drugs do not help with tardive dyskinesia, on the contrary, they can exacerbate symptoms. Dose reduction or, if possible, discontinuation of treatment is recommended. For persistent akathisia, benzodiazepines or propranolol may help.
Information on the incidence of side effects is presented on the basis of literature data and spontaneous reports.
The frequency is indicated as: very often (>1/10); often (>1/100 and<1/10); нечасто (>1/1000 and<1/100); редко (>1/10000 and<1/1000); очень редко (< 1/10000); либо неизвестно (не может быть оценена на основании существующих данных).
From the blood and lymphatic system: rarely - thrombocytopenia, neutropenia, leukopenia, agranulocytosis.
From the immune system: rarely - hypersensitivity, anaphylactic reactions.
From the endocrine system: rarely - hyperprolactinemia.
From the side of metabolism and nutrition: often - increased appetite, weight gain; infrequently - loss of appetite, weight loss; rarely - hyperglycemia, impaired glucose tolerance.
Mental disorders: often - insomnia, nervousness, agitation, decreased libido.
From the nervous system: very often - drowsiness, dizziness; often - dystonia, headache; infrequently - tardive dyskinesia, parkinsonism, convulsions, akathisia; very rarely - neuroleptic malignant syndrome.
From the side of the organ of vision: often - disturbance of accommodation, visual impairment; infrequently - a spasm of the gaze.
From the side of the heart: often - tachycardia, palpitations; rarely - prolongation of the QT interval.
From the vascular side: infrequently - hypotension, hot flashes; very rarely - venous thromboembolism.
From the respiratory system, chest organs and mediastinum: rarely - shortness of breath.
From the gastrointestinal tract: very often - dry mouth, increased salivation; often - constipation, dyspepsia, nausea; infrequently - vomiting, diarrhea.
From the side of the liver and biliary tract: infrequently - a change in laboratory parameters of liver function; very rarely - jaundice.
From the skin and subcutaneous tissues: often - hyperhidrosis; infrequently - rash, itching, photosensitivity, dermatitis.
From the musculoskeletal system and connective tissue: often - myalgia; infrequently - muscle rigidity.
From the side of the kidneys and urinary tract: infrequently - violation of urination, urinary retention.
Influence on the course of pregnancy, postpartum and perinatal conditions: unknown - withdrawal syndrome in newborns.
From the genitals and mammary gland: infrequently - ejaculation disorders, erectile dysfunction; rarely - gynecomastia, galactorrhea, amenorrhea.
General disorders and disorders at the injection site: often - asthenia, fatigue.
When taking Chlorprothixene, as with other antipsychotics, the following rare side effects were observed: prolongation of the QT interval, ventricular arrhythmias (ventricular fibrillation, ventricular tachycardia), torsades de pointes and sudden death.
Cases of priapism, prolonged and usually painful penile erections, possibly leading to erectile dysfunction, have been reported with an unknown frequency when taking antipsychotics.
Abrupt discontinuation of Chloprothixene can lead to the development of a "withdrawal" syndrome. The most common symptoms are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, nervousness, anxiety, and agitation. Patients may also experience dizziness, impaired body temperature control, and tremors. Symptoms typically begin within 1-4 days of withdrawal and subside within 1-2 weeks.

Interaction with other drugs

Combinations requiring caution when using
Chlorprothixene may enhance the sedative effect of alcohol, the effects of barbiturates and other CNS depressants.
Antipsychotics may increase or decrease the effect of antihypertensive agents. The antihypertensive effect of guanethidine and similarly acting drugs is reduced.
The concomitant use of antipsychotics and lithium increases the risk of neurotoxicity. Tricyclic antidepressants and antipsychotics mutually inhibit each other's metabolism.
Chlorprothixene can reduce the effectiveness of levodopa and the effect of adrenergic drugs and increase the effect of anticholinergics.
Simultaneous use with metoclopramide and piperazine increases the risk of developing extrapyramidal disorders.
The antihistamine effect of chlorprotiixen may suppress or eliminate the alcohol/disulfiram reaction.
The prolongation of the QT interval associated with the use of antipsychotics may be exacerbated by the concomitant use of other drugs that prolong the QT interval.
Co-administration with the following drugs that prolong the QT interval is contraindicated:
- class IA and III antiarrhythmic drugs (e.g. quinidine, amiodarone, sotalol),
- some antipsychotic medicines (eg thioridazine),
- some macrolide antibiotics (eg erythromycin),
- some antihistamines (eg terfenadine, astemizole),
- some quinolone antibiotics (for example, moxifloxacin).
This list is not exhaustive, the concomitant use of other drugs that can cause a significant prolongation of the QT interval (such as cisapride, lithium) is also contraindicated.
The simultaneous use of drugs that cause electrolyte disturbances, such as thiazide diuretics, and that can increase the concentration of chlorprothixene in blood plasma should be avoided due to a possible increase in the risk of prolongation of the QT interval and the development of malignant arrhythmias.
Antipsychotics are metabolized by the liver cytochrome P450 system.
Medicinal products that inhibit cytochrome CYP 2D6 (eg, paroxetine, fluoxetine, chloramphenicol, disulfiram, isoniazid, MAO inhibitors, oral contraceptives, and to a lesser extent buspirone, sertraline, or citalopram) may increase plasma concentrations of chlorprothixene. The simultaneous use of chlorprothixene and drugs with anticholinergic action enhances this anticholinergic effect.

Precautionary measures

Malignant neuroleptic syndrome
When taking antipsychotics, cases of neuroleptic malignant syndrome have been reported with the following symptoms: hyperthermia, muscle rigidity, dysfunction of the autonomic nervous system, impaired consciousness, and elevated serum creatine kinase. The risk may be higher when taking a potent drug.
Among the cases with a fatal outcome, most of all patients with an existing organic brain syndrome, mental retardation and abusing opiates or alcohol.
Treatment: discontinuation of antipsychotics, symptomatic and general supportive inpatient treatment. Symptoms may persist for up to a week after oral antipsychotics are stopped.
Due to pupil dilation, patients with a shallow anterior chamber and angle-closure glaucoma may develop acute glaucoma.
Due to the risk of 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 conduct an ECG study. With a QT interval over 450 ms in men and 470 ms in women, Chlorprothixene is contraindicated.
During therapy, the need for an ECG is assessed by the doctor individually. If the QT interval is prolonged during treatment, it is necessary to prescribe lower doses of Chlorprothixene; if the QT interval is prolonged more than 500 ms, therapy should be discontinued.
During treatment, it is recommended to periodically assess the electrolyte balance.
The concomitant use of other antipsychotics should be avoided.
Chlorprothixene should be used with caution in patients with organic brain syndrome, convulsive disorders, severe hepatic or renal impairment, myasthenia gravis and benign prostatic hypertrophy.
Cases of the development of priapism have been reported with the use of antipsychotics with α-adrenergic blocking effect. The possibility of the presence of this effect in Chloprothixene is not excluded. Severe priapism may require medical intervention. Patients should be informed of the need to seek emergency medical attention if signs and symptoms of priapism develop.
Precautions should be observed in patients with:
- pheochromocytoma,
neoplasia due to prolactin
- severe hypotension or orthostatic dysregulation,
- Parkinson's disease,
- diseases of the hematopoietic system,
- hyperthyroidism,
- violation of urination, urinary retention, stenosis of the pylorus of the stomach, intestinal obstruction.
Chlorprothixene can change the concentration of insulin and glucose in the blood, so patients with diabetes may need to adjust the doses of hypoglycemic drugs.
To make a decision about the possibility of reducing the maintenance dose during long-term therapy, especially with maximum daily doses, it is necessary to regularly monitor the condition of patients.
It was reported about the development of venous thromboembolism while taking antipsychotics. Due to the fact that patients treated with antipsychotics are often at risk of developing venous thromboembolism, risk factors for developing venous thromboembolism should be identified before and during treatment with chlorprothixene and preventive measures should be taken.

Use in children and adolescents under 18 years of age

Chlorprothixene is not recommended for use in children and adolescents. There are insufficient data from studies on the efficacy and safety of chlorprothixene in children and adolescents. Therefore, Chlorprothixene should be prescribed to children and adolescents (under 18 years of age) only if there is an indication for use and after a careful assessment of the benefit-risk ratio.

Elderly patients

Cerebrovascular adverse reactions
Chlorprothixene should be used with caution in patients at risk of stroke.
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.
Elderly patients are particularly susceptible to orthostatic hypotension.
Increased mortality rate 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 recommended for the treatment of behavioral disorders in elderly patients with dementia.

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.

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.).

This is a fairly strong antipsychotic, has a wide spectrum of action.

The thioxanthene derivative is very effective in helping to overcome both mild and pronounced mental disorders, as well as a nervous breakdown and the consequences of alcohol intake.

Pharmacological action of the drug

This is a drug that has antipsychotic, neuroleptic(inhibits the action of the central nervous system), anticonvulsant, antiemetic(antiemetic), tranquilizing(soothing) effect.

It also tends to enhance the effect of analgesic (painkillers) drugs.

Has a good thymoleptic influence(an antidepressant effect, which is achieved by activating the noradrenergic transmission): the speed of thinking and initiative increase, the feeling of fatigue disappears in unusual conditions.

The antipsychotic effect of the drug is associated with its ability to block dopamine receptors, mesocortical and mesolimbic systems (eliminates delirium, hallucinations).

Chlorprothixene also has the property block adenomine and histamine receptors, which determines its adrenoblocking and antihistamine action.

The antiemetic property is explained by the ability to inhibit the trigger area of the vomiting center.

Suppresses the release of most pituitary and hypothalamic hormones.

What happens after taking the medicine

When taking the drug orally, the active ingredients are quickly absorbed. Chlorprothixene begins to act within 20 minutes after consumption, it is quickly absorbed in the intestine.

The maximum concentration in the blood is detected within 2-3 hours after taking the drug.

The half-life from the body is approximately 10-16 hours.

Chlorprothixene has the ability to cross the placenta and is excreted in breast milk in small amounts.

Excreted from the body with feces and urine. Accordingly, the organs that metabolize this drug are the kidneys and intestines.

Assuming that the daily dose is 300 mg, the content of chlorprothixene in metabolites is 29%, chlorprothixene sulfoxide - 41%.

Indications for use

The drug represents a group of fairly effective sedative neuroleptics and has an extensive indication group:

Contraindications for admission

Instructions for use Chlorprothixene indicates that the drug is categorically prohibited:

state of alcoholic intoxication or intoxication;
in case of consumption or overdose of narcotic drugs;
the action of the central nervous system is inhibited by any other factors;
increased level of sensitivity to the component (s) of the drug;
coma;
severe diseases of the hematopoietic organs;
bone marrow suppression;
children under 6 years old;
vascular collapse (sudden drops in blood pressure);
pregnancy;
parkinsonism.

Before you decide to take an antipsychotic drug, it must be studied - the drug has many side effects.

What the MRI of the brain shows you can see on our video and read to what is happening.

Take with caution

The instructions for use indicate that Chlorprothixene tablets also have relative contraindications (taking the drug is possible, but with great care), which consist in:

combination with other drugs and substances (for more details, see "Interaction with other drugs");
epilepsy of the clinical stage or at the stage of complications;
diseases of the renal and hepatic parenchyma;
decompensated defect;
somatic exhaustion;
tachycardia;
elderly age;
diseases of the cardiovascular system (possibly transient increase in blood pressure);
atherosclerosis of cerebral vessels at a pronounced stage;
stomach ulcer;
lesions of the duodenum;
glaucoma or predisposition to its occurrence;
respiratory disorders caused by asthma, the course of acute infectious diseases, pulmonary emphysema;
diabetes;
benign or malignant growth of the prostate mucosa, which has clinical manifestations (the drug may cause urinary retention).

In violation of the function of the kidneys and liver

The drug should be used with caution, since structural and functional disorders of these organs may occur.

You should be especially careful in the presence of the following concomitant diseases:

pheochromocytoma (hormonally active tumor in the adrenal glands);
Reye's syndrome (taking the drug increases the risk of developing hepatotoxicity);
urinary retention.

Mode of application

General indications for the use of Chlorprothixene Zentiva, which are indicated in instructions:

Accept orally by 25-50 milligrams 3-4 times a day. If necessary, it is possible to prescribe 60 grams per day (with a subsequent decrease in dosage), intramuscularly - up to 25-50 milligrams 2-3 times a day.

Usually, the largest dose of the drug is prescribed at bedtime.

Dosage depending on the disease and concomitant condition

The dosage depends largely on patient's condition:

Psychosomatic disorders and severe depressive states: Chlorprothixene is used as an auxiliary drug (as part of complex therapy). Usually, 60 to 90 mg per day is prescribed (the dose is divided into several doses).
Psychosis, schizophrenia, manic states: first, the drug is taken at 50-200 mg per day, then the daily rate increases to 250-300 mg. With advanced conditions of the disease, it is possible to increase the dosage to 1200 milligrams (the daily dose is divided into 3-4 doses, about 40% falls in the evening).
Supportive care: 100–200 milligrams per day.
neuroses: 10-15 mg at bedtime, less often - 30 mg at bedtime, in extreme cases - 45 mg at bedtime.
withdrawal syndrome(“hangover” or post-narcotic state): the drug is taken 3 times a day, in a volume of 500 mg (divided into 3 equal portions). In this case, the course lasts 5-7 days. After completion of the course, the dose of the drug is reduced to 15-45 milligrams per day (as maintenance therapy, to prevent relapses).
Irritability, hyperactivity, nervous agitation, confusion in elderly patients: therapy begins with a dosage of 15-90 mg per day, the dose is increased gradually, until an appropriate effect is achieved.
Insomnia: take 15-30 milligrams of medication an hour before bedtime.
Behavioral disorders in children: the dosage is calculated according to the formula 0.5-2 mg x the child's weight (kg). On average, it is prescribed: for neuroses 5-30 mg per day, for psychoses from 100 to 200 mg per day.
pain(to enhance the effect of analgesics): take 15-300 mg of the drug per day along with painkillers.
Skin itching(various origins): 15-100 milligrams per day divided into 4 doses.
R abortion claim, premature birth: 15 mg in portions (2-3 times a day), for 2-3 days. Then 7-10 days are prescribed reduced doses of the drug.

Injective administration of the drug is prescribed if the patient refuses to take pills or at the beginning of the course (for the fastest possible action of the drug).

Composition and form of release of the drug

Pills: biconvex, film-coated, 15 mg (orange tablets), 50 mg (light brown tablets), available in blister packs, 1 blister pack contains 10 tablets. 1 package contains 50 pieces.

Composition: active substance - chlorprothixene hydrochloride.

Auxiliary components: lactose monohydrate, talc, corn starch, calcium stearate, sucrose.

Shell composition: macrogol 6000, 300, talc, aluminum varnish, hypromellose 2910-5.

Injection: ampoules of 1 ml of a 2.5% solution, 2 ml of a 5% solution. 1 package contains 10 or 100 ampoules.

Drops: for oral administration

Side effects

As an individual reaction of the body, the following are possible symptoms:

Central nervous system: mild extrapyramidal syndrome, inhibition, feeling of fatigue, dizziness, drowsiness. In the first 6 hours after taking the drug, akatsia is possible (an irresistible desire to move, inability to sit still). Isolated cases of late dystonia. An increase in the level of anxiety is extremely rare, especially in patients with schizophrenia.
Digestive system: increased urination, constipation, dry mouth. After prolonged use of the drug, cholestatic jaundice may occur.
The cardiovascular system: flushing, tachycardia (rapid heartbeat), orthostatic hypotension, changes in the echocardiogram (QT interval).
Organs of vision: sometimes patients experience blurred vision, an inability to quickly focus.
Hematopoietic system: possible leukocytosis, hemolytic anemia, agranulocytosis (4-10 weeks of treatment), benign leukopenia.
Endocrine system: possible amanorrhea, frequent hot flashes, galactorrhea, gynecomastia, weakening of sexual desire and potency (with prolonged use of the drug), diabetes mellitus.
Metabolism: sometimes there is an increase in the amount of sweating, increased appetite, carbohydrate metabolism disorders, accompanied by weight gain (with prolonged use of the drug).
Epidermis: possible photodermatitis or photosensitivity.
vestibular apparatus: in some cases, there may be a violation of coordination of movements (trembling, slowness).

drug overdose

Symptoms: respiratory failure, convulsions, severe drowsiness, fever, tachycardia, lowering blood pressure, shock, coma, uncontrolled movements, excessive excitability.

Treatment: gastric lavage, laxatives or absorbents can be given. Supportive therapy should also be carried out in parallel, depending on the symptoms manifested.

The dialysis procedure will not be effective.

In the case of cardiovascular symptoms, do not give adrenaline (this can cause a drop in blood pressure).

Seizures can be eliminated with diazepam.

Bioperiden will effectively help in case of motor neuropathic disorders.

Do not try to induce vomiting, as particles of vomit may enter the respiratory tract.

special instructions

Instructions for use for the drug Chlorprothixen Zentiva indicates that you should also remember such moments:

Taking Chlorprothixene may give false results of a urine immunobiological pregnancy test, a blood test for bilirubin levels.
During the course of treatment, it is advisable not to drink alcohol, to avoid a significant amount of ultraviolet radiation.
For the period of intensive treatment, one should refrain from activities that require a high speed of physical and mental reactions (this includes working at height, driving a car, driving a crane ...).
In order to avoid the “withdrawal” syndrome (leveling the results of treatment), the drug should be gradually withdrawn from the body, gradually reducing the dosage.
The likelihood of fluctuations in blood pressure is higher in adolescents than in adults.
In the presence of diseases listed in the list of relative contraindications, you should carefully compare the need for treatment with this drug and the possible risks.
Prolonged use of the drug causes dependence and addiction.

Interaction with other drugs

The interaction of the drug with other drugs is quite good studied:

using Chlorprothixene in parallel with neuroleptics, hypnotics, anesthetics and sedatives, etenol-containing drugs, they can enhance the effect of Chloroprothixene on the central nervous system;
combination with antihistamine and anticholinergic drugs can lead to a slowdown in the conduction of nerve impulses;
Chloroprothixene enhances the effect of antihypertensive drugs;
the combination of the drug with adrenaline can provoke tachycardia, arterial hypotension;
Chloroprothixene reduces the effectiveness of levodopa;
the combination of the drug with phenothiazines, haloperidol, reserpine, metoclopramide can cause movement disorders (against the background of neurological complications).