Index of drugs

Table. 0.5 mg: psychotic disorders without depressive disorders; temporarily in depressive disorders other than in the course of psychosis.Table. 3 mg: treatment of schizophrenia.

1 tabl powl. contains 0.5 mg or 3 mg flupentixol as the dihydrochloride salt; coated tablets contain lactose.

A thioxanthene derivative with a strong antipsychotic effect. Flupenticol is a mixture of two geometric isomers, the active form cis (Z) -flupenticol and the trans (E) -fluupenticol form, approximately in a 1: 1 ratio. Cis (Z) -flupenticol has a strong affinity for dopaminergic D receptors₁ and D₂to α receptors₁-renergic and 5-HT receptors₂. It has only small antihistaminergic properties, it does not block α receptors₂-adrenergic, has no affinity for cholinergic muscarinic receptors. The bioavailability of the drug after oral administration is approximately 40%, C_max it reaches after about 4-5 h. In about 99% it is bound to plasma proteins. The metabolism of flupentixol occurs in three main ways - sulfoxidation, N-dealkylation in the side chain and conjugation with glucuronic acid. Metabolites are devoid of psychopharmacological activity. Flupenticol predominates over the metabolites in the brain and other tissues. It is excreted mainly in the faeces, in a small amount in the urine. T_0,5 in the elimination phase it is about 35 hours.

Hypersensitivity to flupentixol or to any of the excipients. Circulatory collapse. Decreased level of consciousness regardless of the etiology (eg alcohol intoxication, barbiturates or opiates), Sleeping. Incorrect blood composition. Phaeochromocytoma.

At doses up to 25 mg per day flupenticol is not indicated in patients with hyperactive and increased activity, because its activating effect may exacerbate these symptoms. If patients initially used sedatives or neuroleptics with sedative properties, they should be withdrawn gradually. 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. Flupenticol is not intended to treat behavioral disorders associated with dementia (an increased risk of death in elderly patients with dementia, using antipsychotics, the cause of the increased risk is not known). The drug should be used with caution in patients with: organic cerebral syndrome, convulsions; advanced liver disease; diabetes (antidiabetic therapy may need to be adjusted); with risk factors for stroke. Due to the risk of prolongation of the QT interval, caution should be exercised in patients with hypokalemia, hypomagnesemia or genetic predisposition, and in patients with a history of cardiac disorders such as QT prolongation, significant bradycardia (<50 bpm), and a fresh acute myocardial infarction myocardial or cardiac arrhythmias; concomitant use of other antipsychotics should be avoided. Before and during treatment, all possible risk factors for venous thromboembolism should be identified and appropriate preventive measures should be taken. All patients should be monitored for signs of suicidal ideation and behavior (especially in the early stages of recovery or after a change in the dose); this applies especially to patients under the age of 25 years and patients with a history of suicidal behavior or thoughts. When treating patients with other mental disorders, the same precautions should be taken as when treating patients with major depressive disorder. Treatment with flupentixol should be discontinued in case of symptoms of malignant neuroleptic syndrome. Table. powl. contain lactose, therefore they should not be used in patients with galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose. Additionally, tabl. powl.3 mg contain sunset yellow (E110) - aluminum lake, which may cause allergic reactions.

Do not use during pregnancy unless clearly necessary. Exposure to antipsychotics (including flupentixol) in the third trimester of pregnancy increases the risk of neonatal side effects, including extrapyramidal syndrome and / or withdrawal syndrome; have been described as agitation, hypertension, hypotonia, tremor, drowsiness, breathing disorders, feeding disorders - newborns should be carefully observed. Newborns whose mothers used neuroleptics in late pregnancy or during delivery may show symptoms of poisoning, such as lethargy, muscle tremors and hyperactivity, and low Apgar score. The concentration of flupentixol present in breast milk is low and it is unlikely that the drug administered in therapeutic doses will also act on the infant; the dose consumed by the child is <0.5% of the dose taken by the mother, expressed in mg / kg. You can continue breast-feeding during treatment with flupentixol, if clinically important, but it is recommended that you look at 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, headache, dizziness, disturbed accommodation, abnormal vision, shortness of breath, drooling, constipation, vomiting, indigestion, diarrhea, urination disorders, urinary retention, increased sweating, pruritus, muscle pain, increased appetite, weight gain, asthenia, fatigue, insomnia, depression, nervousness, agitation, decreased sex drive. Uncommon: tardive dyskinesia, dyskinesia, parkinsonism, speech disorders, seizures, involuntary eye rotation, abdominal pain, nausea, flatulence, rash, hypersensitivity to light, dermatitis, muscle stiffness, decreased appetite, hypotension, hot flush, abnormal liver function tests, erectile dysfunction, ejaculation disorders, confusion. Rare: QT prolongation (in ECG), thrombocytopenia, neutropenia, leukopenia, agranulocytosis, hyperprolactinemia, hyperglycemia, impaired Glucose tolerance, hypersensitivity, anaphylactic reaction, gynecomastia, amelioration, amenorrhea. Very rare: neuroleptic malignant syndrome, venous thromboembolic disease (including pulmonary embolism and deep vein thrombosis, jaundice, frequency unknown: neonatal withdrawal syndrome, suicidal thoughts, suicidal behavior) Rare QT prolongation, ventricular arrhythmias have been reported rarely ( ventricular fibrillation, ventricular tachycardia,torsade de pointes) and cases of sudden, unexplained deaths. Sudden discontinuation of the drug may lead to withdrawal symptoms; the most common symptoms are: nausea, vomiting, lack of appetite, diarrhea, rhinorrhea, sweating, muscle pain, paresthesia, insomnia, anxiety, anxiety and agitation; Dizziness, increased feelings of warmth or cold, and tremor may also occur.

Orally. Adults.Depression, depressive neuroses, psychosomatic disorders: initially 1 mg / day in a single dose in the morning or 0.5 mg 2 times a day. After a week, the dose can be increased to 2 mg a day if the clinical response is insufficient. The dose> 2 mg / day should be administered in 2 divided doses and should not exceed 3 mg. If, after a week of administration of the maximum dose, there is no apparent therapeutic effect, the drug should be discontinued.Schizophrenia: initially 3-15 mg / day in 2 or 3 divided doses. If necessary, the dose can be increased up to 40 mg / day. The maintenance dose is usually 5-20 mg / day. The maintenance dose is usually given as a single dose in the morning.Special groups of patients. There is no need to change the dosage in patients with impaired renal function. In patients with impaired hepatic function, it is advisable to identify the drug in the blood.Elderly patients should receive lower doses - half the recommended dose (0.5-1.5 mg / day) in the case of depression, depressive neuroses and psychosomatic disorders, and doses from the lower end of the dosage range in the case of schizophrenia. The drug is not recommended for use in children.Way of giving. Table. should be swallowed with water.