2010/09/21

Apo-Trifluoperazine

Composition, structure and packing

Coated tablets

1 tab. trifluoperazina hydrochloride 5 mg/10 mg.

Excipients: lactose, starch, microcrystalline cellulose, magnesium stearate, hydroxypropylmethylcellulose, polyethylene glycol, indigotine, titanium dioxide.

Clinico-pharmacological group: neuroleptics.

Pharmacological action

Neuroleptics, phenothiazine derivatives. Has a pronounced antipsychotic and antiemetic effects. It has alpha-adrenoceptor blocking activity. Anticholinergic and sedative effects are mild. Has some stimulating (activating) effect when applied in small doses.

The intensity and duration of antipsychotic action than chlorpromazine. It marked extrapyramidal disorders.

Pharmacokinetics

Absorption

It is well absorbed from the gastrointestinal tract. There are significant interpersonal variations Cmax in blood plasma.

Distribution

Well bound to plasma proteins. Penetrates through the placental barrier.

Metabolism

Biotransformiruetsya intensively, especially in the liver. Most of the pharmacologically inactive metabolites.

Withdrawal

Excreted in the urine, feces and bile.

Statement
schizophrenia and other mental illnesses occurring with delusions and hallucinations;
involutional psychoses, neuroses;
vomiting of central origin.

Dosage regimen

Dosage regimen is individually taking into account the severity. When the maximum therapeutic effect the dose is gradually reduced to maintenance. At the beginning of therapy anxiety adult appoint 1 mg 2 times / day.

Treatment of patients with psychotic disorders begin with a dose of 2-5 mg 2 times / day. To achieve optimal therapeutic effect in most patients is sufficient doses of 15-20 mg / day, sometimes necessary to increase the daily dose to 40 mg. The course of treatment usually lasts 2-3 weeks.

Children aged 6-12 years in the treatment of psychotic disorders appoint 1 mg 1-2 times / day, if necessary, the dose may be increased. To treat vomiting adult appoint 1-2 mg 2 times / day. Older patients with initial dose should be reduced in 2 times.

Side effect

From the side of the central nervous system: frequent - extrapyramidal disorders (dyskinesia, akineto-rigid effects, akathisia, hyperkinesis, tremor, vegetetivnye violations) at the beginning of treatment - drowsiness, dizziness, sleep disturbances, visual disturbances; Propafenone - tardive dyskinesia facial muscles, rarely - neuroleptic malignant syndrome (CSN).

On the part of the digestive system: at the beginning of treatment - dry mouth, anorexia, rarely - cholestatic jaundice.

On the part of the hemopoietic system: rarely - leukopenia, thrombocytopenia, agranulotsitopeniya, pancytopenia.

On the part of the cardiovascular system: at the beginning of treatment - tachycardia, moderate orthostatic hypotension, rarely - cardiac arrhythmias, ECG changes (prolongation of the interval QT, smoothing spikes T).

Allergic reactions: seldom - skin rash, urticaria, angioedema.

On the part of the endocrine system: rarely - galactorrhea, amenorrhea.

Contraindications
Comatose and depression caused by central depressant drug;
hemodyscrasia;
marked disturbances of liver function;
Pregnancy
Lactation (breastfeeding);
Hypersensitivity to trifluoperazinu and other derivatives of phenothiazine series.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Application for violations of liver function

Contraindications disturbancies liver function.

Cautions

With extreme caution should be used drug in patients with glaucoma (especially the form-closure), cardiovascular diseases, epilepsy, benign prostatic hyperplasia. Apo-trifluoperazin used only after comparing the risks and benefits of treatment in patients with pathological changes in blood picture, liver function disorders, alcohol intoxication and Reye syndrome, as well as in breast cancer, Parkinson's disease, gastric ulcers and duodenal ulcers, urinary retention, chronic respiratory diseases (particularly children), seizures.

Avoid simultaneous use of phenothiazines with adsorbing antidiarrhoeal means. In the period of treatment should be eliminated alcohol.

Effects on ability to drive vehicles and management mechanisms

During the drug should not perform work that requires high concentration and high speed of psychomotor reactions.

Overdose

Symptoms: may cause symptoms of CSN, the first of which may increase body temperature. In severe cases may experience various forms of impairment of consciousness up to coma.

Treatment: removal of preparation, the use of antiparkinsonian (tropatsin, cyclodol), n / to the introduction of caffeine-sodium benzoate (2 ml of 20% solution) and atropine (1 ml 0.1% solution), in / in the introduction of diazepam, glucose solution, nootropics, vitamins B and C, symptomatic therapy.

Drug Interactions

With simultaneous use of Apo-trifluoperazina with related chemical structures Prochlorperazine may occur long loss of consciousness.

With simultaneous use of Apo-trifluoperazina with other drugs, have a depressing effect on the central nervous system (means of anesthesia, opioid analgesics, barbiturates, tranquilizers, ethanol and etanolsoderzhaschie drugs) may be increased CNS depression and respiratory depression, with tricyclic antidepressants, MAO inhibitors or maprotilinom - increasing the risk of CSN, with the anticonvulsant drugs - may decrease the convulsive threshold, with preparations for the treatment of hyperthyroidism - increased risk of agranulocytosis; with other drugs that cause extrapyramidal reactions - may increase the frequency and severity of extrapyramidal disorders, with antihypertensive drugs - can be expressed as orthostatic hypotension; with ephedrine - possibly weakening the vasoconstrictive effects of ephedrine. Apo-trifluoperazin enhances anticholinergic effects of other drugs, with antipsychotic neuroleptic effect may decrease. Apo-trifluoperazin can suppress the action of amphetamines, levodopa, clonidine, guanetidina.

In the treatment of Apo-trifluoperazinom avoid injection of epinephrine, since possessing alpha-adrenoceptor blocking action, it can distort the effect of adrenaline, leading to a further decline in AD.

Suction phenothiazines broken when used with antacids, antiparkinsonian means preparations of lithium.

Terms and Conditions of storage

List B. The drug should be stored in dry, light, reach of children, at a temperature not above 30 ° C. Shelf life - 5 years.

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