Chlorprothixene Zentiva

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Chlorprothixene Zentiva: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Drug interactions
14. Analogs
15. Terms and conditions of storage
16. Terms of dispensing from pharmacies
17. Reviews
18. Price in pharmacies

Latin name: Chlorprothixen-Zentiva

ATX code: N05AF03

Active ingredient: chlorprothixene (chlorprothixene)

Manufacturer: Zentiva ks (Czech Republic, Slovakia), Zentiva Saglik Urunleri Sanayi ve Ticaret AS (Turkey), sc Zentiva, SA (Romania)

Description and photo update: 2018-21-11

Prices in pharmacies: from 175 rubles.

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Film-coated tablets, Chlorprothixene Zentiva

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

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 box there are 3 or 5 blisters 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 thioxanthene derivative. It has antipsychotic, moderate antidepressant and pronounced sedative effects. The antipsychotic effect is associated with the blocking effect of chlorprothixene on dopamine receptors. Also, the analgesic and antiemetic properties of the drug are associated with the blockade of these receptors. Chlorprothixene is able to block a1-adrenergic receptors, 5-HT2 receptors, as well as H1-histamine receptors, which determines its adrenergic blocking hypotensive and antihistaminic action.

Pharmacokinetics

When taken orally, the bioavailability of chlorprothixene is approximately 12%. After oral administration, it is absorbed well and quickly. In the liver and intestinal walls, it undergoes presystemic metabolism. 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 conditions, neuroses, psychosomatic disorders;
withdrawal symptoms 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;
intolerance to lactose or fructose, glucose-galactose malabsorption or lactase deficiency, isomaltase / sucrase deficiency (Chlorprothixene Zentiva contains lactose and sucrose);
depression of the central nervous system of any origin (including those associated with the intake of alcohol, opiates or barbiturates);
vascular collapse;
coma;
age up to 6 years;
individual intolerance to the components of the drug, including phenothiazines.

Relative (Chlorprothixene Zentiva is prescribed under medical supervision):

tendency to collapse;
diabetes;
glaucoma (including the presence of a predisposition to its occurrence);
urinary retention and the risk of its development in clinical manifestations of prostatic hyperplasia;
renal / hepatic impairment;
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 a transient increase in blood pressure);
pronounced atherosclerosis of the vessels of the brain;
peptic ulcer of the stomach and duodenum;
epilepsy (associated with the likelihood of increased frequency of seizures as a result of lowering the seizure threshold);
pregnancy and lactation.

Instructions for the use of Chlorprothixene Zentiva: method and dosage

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

Recommended dosage regimen:

psychoses, including manic states and schizophrenia: the initial daily dose is 50-100 mg. The dose is gradually increased until the optimal effect is achieved, usually 300 mg. The average maintenance dose is 100 to 200 mg per day. The maximum is 600 mg per day. Usually, the daily dose is divided into 2-3 doses, the smaller part should be taken in the daytime, the larger - in the evening;
withdrawal symptoms in drug addiction and alcoholism: daily dose - 500 mg in 2-3 doses. Duration of use is 7 days. After improvement of the condition, the dose is gradually reduced. The maintenance daily dose ranges from 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 daily in 3 divided doses;
behavioral disorder in children: 0.5–2 mg / kg;
neuroses, depressions, psychosomatic disorders: daily dose - 90 mg in 2-3 doses;
insomnia: 15-30 mg 60 minutes before bedtime;
pain (in combination with analgesics): 15-300 mg per day.

Side effects

Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):

cardiovascular system: orthostatic hypotension (especially when high doses of Chlorprothixene Zentiva are used), transient changes in the QT interval on the electrocardiogram and tachycardia;
nervous system: dizziness, increased fatigue, drowsiness, psychomotor lethargy, mild extrapyramidal hypokinetic-hypertensive syndrome, akathisia (within the first 6 hours after administration), dystonic reactions, persistent tardive dyskinesia (disorders usually appear at the beginning of therapy and often as it continues disappear on their own); rarely - late 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 is most likely between 2 and 4 weeks of therapy);
hematopoietic organs: rarely - agranulocytosis (the disorder most often develops at 4-10 weeks of treatment); in isolated cases - transient benign leukopenia and hemolytic anemia;
sensory organs: clouding of the lens / cornea with possible visual impairment, paresis of accommodation (occurs at the beginning of treatment and disappears as Chlorprothixene Zentiva continues to be taken);
others: skin rash, urinary retention, dermatitis, flushing, withdrawal, photosensitivity.

Overdose

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

In case of overdose, symptomatic and supportive therapy is usually prescribed. As soon as possible, gastric lavage and intake of activated charcoal should be performed. Also shown are activities aimed at maintaining the work of the cardiovascular and respiratory systems. Epinephrine should not be used because it can cause a subsequent drop 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 performing an immunobiological urine test for pregnancy, and a change in the QT interval on the electrocardiogram.

Alcohol abuse increases the depression of the central nervous system.

The most common development of dystonic reactions is observed in children and young patients. They usually appear at the beginning of therapy and may subside within 24–48 hours after Chlorprothixene Zentiva is discontinued.

In the first few days of treatment, parkinsonian extrapyramidal effects may occur, but usually their frequency increases with increasing dose; more often they occur in elderly patients and older children

Tardive dyskinesia at the beginning of treatment is dose-dependent, but its frequency may increase with a prolonged course and as the total dose is reached. After discontinuation of Chlorprothixene Zentiva, the violation 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 hepatic function indicators, an ophthalmological examination, as well as careful observation to identify early signs of tardive dystonia and dyskinesia are required.

The emergence of a malignant neuroleptic syndrome is possible at any time of therapy, but more often its development is noted soon after the start of taking Chlorprothixene Zentiva or after transferring the patient from another neuroleptic, 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.

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

Influence on the ability to drive vehicles and complex mechanisms

Patients should be careful while taking Chlorprothixene Zentiva while driving.

Application during pregnancy and lactation

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

Pediatric use

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

With impaired renal function

Chlorprothixene Zentiva according to indications with concomitant renal failure should be used under medical supervision.

For violations of liver function

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

Drug interactions

ethanol and ethanol-containing drugs, anesthetics, opioid analgesics, sedatives, hypnotics, antipsychotics: the inhibitory effect of chlorprothixene on the central nervous system increases;
antiepileptic drugs (in patients with epilepsy): the threshold of seizure activity decreases (additional dose adjustment is required);
m-anticholinergics, antihistamines and antiparkinsonian drugs: the anticholinergic effect of chlorprothixene increases;
phenothiazines, metoclopramide, haloperidol, reserpine: the appearance of extrapyramidal disorders may occur;
levodopa: its effectiveness decreases;
phenylephrine: the vasoconstrictor effect may decrease;
dopamine (in 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 developing adverse reactions from the heart increases;
guanethidine: the hypotensive effect decreases;
bromocriptine: hyperprolactinemia may develop, which requires correction of the dosage regimen;
ototoxic drugs (especially antibiotics): chlorprothixene can mask the symptoms of ototoxicity (such as tinnitus, dizziness).

Analogs

An analogue of Chlorprothixene Zentiva is Truxal.

Terms and conditions of storage

Store at temperatures up to 25 ° C. Keep out of the reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews of Chlorprothixene Zentiva

Reviews of Chlorprothixene Zentiva are mainly positive when used for the treatment of insomnia, including those associated with alcoholism, senile dementia, depression. In some cases, an insufficient therapeutic effect and the development of pronounced side reactions are noted.

Price for Chlorprothixene Zentiva in pharmacies

The approximate price for Chlorprothixene Zentiva (50 pcs. 15 or 50 mg) is 288-299 or 412-462 rubles.