Trifluperidol (Trifluperidolum) – (4- (meta-Trifluoromethylphenyl) -1-[3-(пара-фторбензоил)-пропил]-piperidinol-4 or 4-[4-(мета-Трифторметилфенил)-4-оксипиперидино]-4-fluorobutyrophenone), a typical antipsychotic (neuroleptic), butyrophenone derivative. Chemically close to haloperidol, but twice superior in neuroleptic action.
general information
In structure and action, it is close to haloperidol. It differs in the presence of the CF3 group, in the meta position, of the phenyl nucleus (in piperidine) instead of the chlorine atom in the para position in haloperidol.
It has a very strong antipsychotic activity, superior to haloperidol and comparable to thioproperazine (mazheptil). Enhances the effect of sleeping pills, drugs, analgesics. It has an anticonvulsant and effect (3 times more active than haloperidol in an experiment with blocking the emetic reaction to apomorphine). Possesses strong cataleptogenic activity. Has no anticholinergic effect; strongly blocks central dopamine receptors.
Trifluperidol is a very powerful antipsychotic agent. It quickly reduces hallucinatory-delusional arousal. The ability to stop manic and psychotic arousal is superior to other antipsychotics.
Small (up to 2 mg / day) and medium (up to 5 mg / day) doses of trifluperidol have a stimulating effect with overexcitation in the form of irritability, anxiety, and dysphoria. When taken in high doses, a strong sedative effect is observed.
Used for psychosis, by motor and mental excitement, especially for the relief of catatonic and hebephrenic excitement; with prolonged attacks of periodic schizophrenia; in conditions accompanied by severe depression and delirium; with alcoholic psychoses. Due to the extremely strong antipsychotic activity, it is often effective in the absence of effect or insufficient antipsychotic activity of haloperidol, zuclopenthixol and other antipsychotics. It can also be used as an antiemetic.
Assign inside and intramuscularly.
Inside used, starting with a dose of 0.00025-0.0005 g (0.25-0.5 mg) per day, then, depending on the effect and tolerance, increase the dose by 0.25-0.5 mg every 2-3 days … The daily dose is usually 2-6 mg (up to 8 mg). Assign in 2-4 doses after meals.
Children under the age of 5 are prescribed 1/4, and 5-15 years – 1/2 of the adult dose.
In chronic diseases, start with intramuscular injection of 1.25-2.5 mg, then gradually replace the injections by taking the drug inside.
For relief of acute delusional states, 1.25-2.5 mg (sometimes up to 5 mg) are administered intramuscularly once or repeatedly (in the form of a short course).
Side effects
Depression with a predominance of fear. In more than 90% of patients, trifluperidol causes neurological extrapyramidal disorders. Most often (about 60% of cases) at the beginning of therapy, hyperkinesis occurs, mainly akathisia. Dystonic spasms can be combined with vegetative phenomena (profuse sweat, salivation and lacrimation, massive vasomotor shifts, an increase or decrease in blood pressure, sometimes an increase in temperature), which allows them to be distinguished as extrapyramidal-vegetative crises. With prolonged use, pronounced phenomena of parkinsonism are observed.
Other side effects: drowsiness, anorexia, sweating, increased salivation, muscle cramps, allergic reactions such as skin rash, jaundice. Extremely rare side effects are hypotension, myelosuppression.
Precautionary measures
With caution, is prescribed simultaneously with barbiturates, narcotic analgesics, benzodiazepines.
Interactions
Strengthens the effect of opioid analgesics, antihypertensive drugs, antidepressants, alcohol-containing drugs, reduces the effect of antithrombotic agents, vitamin K antagonists, guanethidine, levodopa. Causes a dangerous increase in the action of ethinamate, this combination should be avoided. With the combined use of trifluperidol with drugs that depress the central nervous system, the depression of the central nervous system increases, and the degree of drop in blood pressure increases. When combined with antidepressants and antihistamines, excessive sedation occurs; when combined with procarbazine, severe lethargy may occur. The combination with guanfacine can increase the depressive effect of each drug.
The combined use of trifluperidol with antihypertensive drugs can lead to a strong drop in blood pressure, with bupropion – to an increased risk of a severe seizure, with antiepileptic drugs – to a change in the nature of seizures. When taken simultaneously with lithium preparations, toxicity increases; this can lead to a syndrome similar to encephalopathy. The combined use of trifluperidol and methyldopa can cause psychosis. When combined with M-anticholinergics, the anticholinergic effect increases, and intraocular pressure may increase.
Contraindications
Possible complications and contraindications are basically the same as with haloperidol.
Release form
Method of production: tablets of 0.0005 g (0.5 mg); 0.1% solution for oral administration in 10 ml vials (1 ml contains 1 mg of the drug); 0.25% solution in 1 ml ampoules.
Storage
Storage: List B.
