Zuclopentixol - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Neuroleptics

Included in the formulation

Clopixol

pills inwards

H. Lundbeck A / S Denmark

Clopiksol Depot

solution w / m

H. Lundbeck A / S Denmark

Clopixol-Acuffase

solution w / m

H. Lundbeck A / S Denmark

Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

VED

ONLS

АТХ:

N.05.A.F.05 Zuclopentixol

Pharmacodynamics:

The drug has an antipsychotic, antipsychotic and sedative effect.

Affects the dopaminergic and adrenergic neurotransmission in the central nervous system. Antipsychotic action due to blockade of dopamine D₂receptors of the mesolimbic and mesocortical system, sedative - adrenoreceptor blockade of the reticular formation of the brain stem.

It most effectively eliminates psychotic manifestations in patients with behavioral disorders. In the initial period of therapy, a dose-dependent nonspecific sedative effect is expressed, which is quickly followed by tolerance. With parenteral administration, the antipsychotic effect is manifested after 4 hours and lasts 2-3 days, the sedative effect is manifested 2 hours after the administration, reaches a maximum for 8 hours and then significantly decreases. The depot form is indicated for prolonged (maintenance) therapy, especially in patients with poor oral tolerance.

Pharmacokinetics:Bioavailability after oral administration is about 45%. The dosage forms for intramuscular administration are subjected to enzymatic cleavage with isolation of the active ingredient. C_max is achieved with oral administration after 4 hours, with intramuscular injection - after 36 hours, with intramuscular injection of the depot form - after 7 days. Equilibrium concentration in the serum is achieved in most patients with oral administration for 5-7 days, with the introduction of a depot form - after about 3 months. The volume of distribution is approximately 20 l / kg, binding to plasma proteins is 98-99%. In high concentrations found in the liver, lungs, intestines and kidneys, in smaller concentrations - in the heart, spleen, brain and blood. Slightly penetrates the placental barrier and in small amounts excreted in breast milk. It is metabolized in three ways: sulfooxidation, N-dealkylation and conjugation with glucuronic acid with the formation of inactive metabolites, which are excreted mainly with feces and to a lesser degree (10%) in the urine (0.1% of the dose is excreted unchanged in the urine). Half-life with oral intake is approximately 20 hours, for a solution for injections - about 32 hours, for a depot form - 19 days. The system clearance is 0.86 (± 0.14) l / min.The pharmacokinetic parameters of zuclopentixol do not depend on the age of the patients. Effect of renal and liver functions has not been investigated, however, preferably based on the elimination of extrarenal, renal function should not significantly affect the concentration of the substance in the plasma (as opposed to severe liver dysfunction).

Indications:

Tablets: schizophrenia (acute and chronic) and other psychotic disorders, with hallucinations, paranoid delusions and impaired thinking; a state of agitation, heightened anxiety, hostility, aggressiveness; manic phase of manic-depressive psychosis; mental retardation, combined with psychomotor agitation, agitation and other behavioral disorders; senile dementia with paranoid ideas, disorientation, behavioral disorders, confusion.

Solution for injection: initial treatment of acute psychoses, including manic conditions, and chronic psychoses in the phase of exacerbation.

Depot-form: schizophrenia (acute and chronic) and other psychotic disorders, with hallucinations, paranoid delusions and mental disorders; a state of agitation, heightened anxiety, hostility, aggression.

ICD-10

V.F00-F09.F03 Dementia, unspecified

V.F00-F09.F09 Organic or symptomatic mental disorder, unspecified

V.F20-F29.F20.9 Schizophrenia, unspecified

V.F20-F29.F20 Schizophrenia

V.F30-F39.F30.9 Manic episode, unspecified

V.F30-F39.F30 Manic episode

V.F20-F29.F25.0 Schizoaffective disorder, manic type

V.F30-F39.F32.9 Depressive episode, unspecified

V.F30-F39.F32 Depressive episode

V.F90-F98.F91.9 Conduct disorder, unspecified

V.F90-F98.F91.8 Other conduct disorders

XVIII.R40-R46.R45.1 Anxiety and Excitement

Contraindications:Hypersensitivity, acute poisoning with alcohol, barbiturates, opiates, coma, dysfunction of the hematopoietic system, pheochromocytoma, pregnancy, breast-feeding, and convulsive syndrome, progressive diseases of the liver, kidneys, cardiovascular diseases (including arrhythmia, severe hypotension, orthostatic disorders regulation of blood circulation), lesions of the brain stem, including Parkinson's disease, prolactin-dependent tumors.

Carefully:To prevent withdrawal syndrome, the dose should be reduced gradually. With chronic liver damage, smaller doses are prescribed. The emergence of extrapyramidal disorders requires dose reduction and administration of antiparkinsonian agents.The development of malignant neuroleptic syndrome necessitates the immediate abolition of zuclopentixol and maintenance and symptomatic therapy. With the development of cholestatic hepatitis, therapy with zuclopentixol should be discontinued. During the treatment, alcohol intake is excluded. Do not use during work drivers of vehicles and people whose profession is associated with increased concentration of attention.

Pregnancy and lactation:Application during pregnancy and during breastfeeding is possible if the expected effect of therapy exceeds the potential risk for the fetus (animal experiments have revealed a teratogenic and embryotoxic effect, no studies have been performed in humans) and a newborn (less than 1% of the dose taken by the mother enters the baby's body ).

Dosing and Administration:Inside, intramuscularly. The dosage regimen is selected individually. When administered orally, the initial dose is usually 2-20 mg per day (can then be increased by 10-20 mg in 2-3 days to 75 mg per day or more); when administered intramuscularly (solution for injection) - 50-150 mg once, if necessary, repeated injections are carried out in 2-3 days (not less than a day). Depo-form - 200-400 mg every 2-4 weeks.Supportive therapy is recommended to be carried out in tablet form or depot form.

Side effects:

From the nervous system and sensory organs: extrapyramidal disorders (muscle rigidity (24%), hypo- or akinesia (17%), tremor (17%), dystonia (14%), motor akathisia and hyperkinesia) that occur primarily at the beginning of treatment, with high doses or with a sharp increasing the dose; dizziness (17%); drowsiness, violation of accommodation (10%); in isolated cases - malignant neuroleptic syndrome (hyperthermia, rigidity of muscles, akinesia, autonomic dysfunction, impaired consciousness up to coma); dyskinesia late and early, provocation of epileptiform seizures, anxiety, agitation, headache, depression, delirious syndrome (especially in combination with anticholinergics), an attack of closed-angle glaucoma.

From the cardiovascular system and blood: tachycardia, orthostatic hypotension, conduction disorders, ≥ 1% - violations of hemopoiesis (eg, agranulocytosis), in single cases - thrombosis of the veins of the lower limbs and pelvis.

On the part of the respiratory system: edema of the larynx, asthma, bronchopneumonia.

On the part of the digestive system: dry mouth (23%), constipation, paralytic intestinal obstruction, minor transient changes in hepatic samples, cholestatic hepatitis, jaundice.

From the side of metabolism: an increase in body weight, impaired glucose metabolism.

From the genitourinary system: delayed urination, menstrual disorders, sexual disorders.

From the skin: rash, erythema, itchy skin.

Other: lupus-like syndrome, fatigue (especially at the beginning of treatment), cerebral edema, increased secretion of salivary and sweat glands, galactorrhea.

Overdose:

Symptoms: increased drowsiness, impaired consciousness up to coma, convulsive syndrome, severe extrapyramidal disorders, arterial hypotension, shock, hypo- or hyperthermia.

Treatment: gastric lavage, monitoring of vital signs, symptomatic and supportive therapy.

Do not use epinephrine, as this may lead to a further decrease in blood pressure. With convulsions, diazepam can be used to stop extrapyramidal disorders using biperidene.

Interaction:Potentiates the depressant activity of barbiturates, tranquilizers, alcohol, glycine, etc. Metoclopramide, bromopride, alizaprid and piperazine increase the likelihood of developing extrapyramidal disorders. Reduces the effectiveness of dopamine receptor agonists (levodopa, bromocriptine, amantadine). Weaken the hypotensive effect of guanethidine, clonidine and methyldopa. Strengthens the effect of anticholinergics. Barbiturates and carbamazepine accelerate the metabolism of neuroleptics. Propranolol, tricyclic antidepressants, lithium preparations increase the concentration of zuclopentixol in the serum (mutually), while the application with lithium preparations may develop neurotoxic symptoms. Simultaneous use with epinephrine leads to a sharp drop in blood pressure. When combined with polypeptide antibiotics, a depressant effect on the respiratory center is possible.

Special instructions:A false positive result of a pregnancy test is possible.

Instructions

Zuclopentixol (Zuclopenthixolum)