Index of drugs

Acute and chronic schizophrenia and other psychoses, especially with symptoms such as hallucinations, delusions, thinking disorders, agitation, anxiety, hostility and aggressiveness. The manic phase of bipolar disorder.

1 tabl powl contains 10 mg or 25 mg of zuclopenthixol (as dihydrochloride). The preparation contains lactose and hydrogenated castor oil.

A thioxanthene derivative with a strong antipsychotic effect. The mechanism of action is associated with the blockade of dopaminergic receptors and 5-HT receptors. Zuklopentixol has a strong affinity for dopaminergic D receptors₁ and D₂, α₁-renergic and 5-HT₂but does not show affinity for cholinergic muscarinic receptors. It has weak affinity for histamine H receptors₁ and does not block α receptors₂-Adrenergic. Zuclopentixol shows transient sedation-dependent, dose-related effects. Calming effects occurring at the beginning of treatment are beneficial in acute / subacute phase of psychosis. Tolerance for non-specific sedative effects develops quickly. After oral administration, the drug is well absorbed from the gastrointestinal tract (bioavailability is about 44%). The maximum concentration in the blood reaches after about 4 hours. The plasma protein binds in about 98-99%. It is metabolized in the liver; metabolites are devoid of neuroleptic activity. It is excreted mainly in the faeces, in a small amount in the urine. T_0,5 is about 20 hours.

Hypersensitivity to the active substance or to any of the excipients. Circulatory collapse. Limited awareness regardless of etiology (eg alcohol poisoning, barbiturates, opioids). Coma.

Caution use in patients with organic cerebral syndrome, seizures, mental retardation, opioid and alcohol abusers, severe liver dysfunction, diabetes (there may be need to modify antidiabetic treatment) and risk factors for stroke. Patients who are given long-term treatment, especially high-dose, should be carefully monitored and subjected to periodic testing to determine if a maintenance dose can be reduced. The drug may cause QT interval prolongation - care should be taken in patients with risk factors for QT prolongation: with a genetic predisposition, hypokalemia, hypomagnesemia, history of cardiovascular disease (including QT prolongation, bradycardia <50 beats / min, fresh acute myocardial infarction, cardiac arrhythmias). People who are taking antipsychotics often have acquired risk factors for the development of venous thromboembolism, so before and during treatment with zuclopenthixol, all possible risk factors for this disease should be identified and preventive measures should be taken. The drug is not intended for the treatment of behavioral disorders associated with dementia. The drug contains lactose - should not be used in patients with hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose. In addition, the drug contains castor oil, which can cause stomach upset and diarrhea.

The drug should not be administered during pregnancy unless the expected benefits to the patient outweigh the theoretically possible risks to the fetus. Newborns whose mothers received neuroleptics during late pregnancy or during delivery may show signs of toxicity, such as lethargy, muscle tremors and hyperactivity, and low Apgar scores. Exposure to antipsychotics (including zuclopenthixol) during the third trimester of pregnancy may result in neonatal side effects including extrapyramidal symptoms and / or withdrawal symptoms that may vary in severity and duration after delivery. Cases of agitation, hypertonia, tremor, drowsiness, respiratory distress syndrome, and feeding disorders have been reported. Therefore, the condition of newborns should be carefully monitored.The concentration of zuclopenthixol present in breast milk is low and it is not expected that the drug administered in therapeutic doses would have an effect on the infant. During treatment with zuclopenthixol, a woman may continue breast-feeding if it is clinically important. However, it is recommended to observe the baby, especially in the first 4 weeks after birth.

Most often they occur at the beginning of treatment, and their severity and incidence generally decrease during therapy. Very common: drowsiness, akathisia, hyperkinesia, hypokinesia, dryness of the oral mucosa. Common: tachycardia, palpitations, tremor, dystonia, hypertension, dizziness, headache, paresthesia, attention disorders, amnesia, abnormal gait, accommodation disturbances, abnormal vision, dizziness, congestion and nasal congestion, shortness of breath, salivation, constipation , vomiting, indigestion, diarrhea, urination disorders, urinary retention, polyuria, increased sweating, pruritus, muscular pain, increased appetite, weight gain, weakness, fatigue, malaise, pain, insomnia, depression, anxiety, nervousness, abnormal dreams, agitation, decreased sex drive. Uncommon: tardive dyskinesia, hyperreflexia, dyskinesia, parkinsonism, syncope, ataxia, speech disorders, hypotension, convulsions, migraine, involuntary eye rotation, pupil dilation, hyperaesthesia, tinnitus, abdominal pain, nausea, bloating with regurgitation gases, rash, photosensitivity, pigmentation disorders, seborrhea, dermatitis, purpura, muscle stiffness, trismus, torticollis, decreased appetite, weight loss, hypotension, hot flushes, thirst, hypothermia, fever, abnormal liver function tests, ejaculation disorders, erectile dysfunction, orgasmic disorders in women, vaginal dryness, apathy, nightmares, increased sex drive, confusion. Rare: QT prolongation (in ECG), thrombocytopenia, neutropenia, leukopenia, agranulocytosis, hyperprolactinemia, hyperglycemia, impaired Glucose tolerance, hyperlipidemia, hypersensitivity, anaphylactic reaction, gynecomastia, galactorrhea, amenorrhea, priapism. Very rare: neuroleptic malignant syndrome, venous thromboembolic disease (including cases of pulmonary embolism and deep vein thrombosis), hepatitis, jaunts. Not known: drug discontinuation in a newborn. In addition, rare cases of prolongation of the QT interval, ventricular arrhythmias (incltorsade de pointes) and cases of sudden, unexplained deaths. Abrupt discontinuation may lead to withdrawal symptoms: nausea, vomiting, anorexia, diarrhea, watery runny nose, sweating, muscle pain, paresthesia, insomnia, agitation, anxiety and anxiety.

Orally. Adults. In general, small doses should be given initially and then increased as rapidly as possible to an optimal effective level depending on the response to treatment. The maintenance dose is usually given as a single dose in the evening, at bedtime.Acute schizophrenia and other acute psychoses, severe acute states of arousal, mania: usually 10-50 mg per day; in moderate and severe cases, 20 mg daily is given initially and the dose increased if necessary by 10-20 mg every 2-3 days up to a dose of 75 mg or more per day. The maximum single dose is 40 mg, the maximum daily dose - 150 mg.Chronic schizophrenia and other chronic psychoses: the maintenance dose is usually 20-40 mg per day.Special groups of patients. Elderly patients should receive doses at the lower end of the dose range. Use in children is not recommended due to lack of clinical experience. Patients with renal impairment may be given the medicine at the usual doses. In patients with impaired hepatic function, caution should be advised when adjusting the dose and, if possible, determining the serum concentration of the drug.Method of administration. The tablets should be swallowed with water.