Trifluoperazine

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Image:Trifluoperazine.png
Trifluoperazine
Systematic (IUPAC) name
10-[3-(4-methylpiperazin-1-yl)propyl]- 2-(trifluoromethyl)-10H-phenothiazine
Identifiers
CAS number	117-89-5
ATC code	N05AB06
PubChem	5566
DrugBank	APRD00173
Chemical data
Formula	C21H24F3N3S
Mol. mass	407.497
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half life	10-20 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	oral, IM

Trifluoperazine (sold as Eskazinyl, Eskazine, Jatroneural, Modalina, Stelazine, Terfluzine, Trifluoperaz) is a typical antipsychotic drug of the phenothiazine group. It exerts its actions through a central adrenergic-blocking, a dopamine-blocking, and minimal anticholinergic blocking. ^[1]

Contents 1 Pharmacokinetics 2 Uses 3 Indications in Canada 4 Side effects 5 Formulations 6 Trivia 7 References 8 References

Pharmacokinetics

Little is known about human pharmacokinetics. One study has the following results: A study of the pharmacokinetics of trifluoperazine as a single 5-mg dose by mouth in 5 healthy subjects. Peak plasma concentrations of trifluoperazine were reached from 1.5 to 4.5 hours after ingestion and varied widely between subjects, ranging from 0.53 to 3.09 ng per mL. Elimination of trifluoperazine was multiphasic; the mean elimination half-life was estimated to be 5.1 hours over the period from 4.5 to 12 hours after ingestion, while the mean apparent terminal elimination half-life was estimated to be 12.5 hours to 13.6 hours.

Uses

The primarary indication of trifluoperazine is schizophrenia. Its use in many parts of the world has declined because of highly frequent and severe early and late tardive dyskinesia, a type of extrapyramidal symptom. The annual development rate of tardive dyskinesia may be as high as 4%.

Studies suggest that trifluoperazine may be able to reverse addiction to opioids. [1]

Indications in Canada

Indications in Canada for trifluoperazine include:

1. Anxiety states: it controls excessive anxiety, tension and agitation seen in neuroses or associated with somatic conditions.

2. The treatment or prevention of nausea and vomiting of various causes.

3. The management of psychotic disorders, such as acute or chronic catatonic, hebephrenic and paranoid schizophrenia; psychosis due to organic brain damage, toxic psychosis, and the manic phase of manic-depressive illness.

Phillip W. Long, M.D. Trifluoperazine.

Indications may vary in different countries.

Side effects

For further information see: phenothiazine

Serious side effects include akathisia, tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome.

A particular severe form of liver damage has been reported, making preexisting liver damage a contraindication.

Formulations

In the past, trifluoperazine was used in fixed combinations with the MAO inhibitor (antidepressant) tranylcypromine to attenuate the strong stimulating effects of this antidepressant. This combination was sold under the brand name Jatrosom. Likeweise a combination with amobarbital (strong sedative/hypnotic agent) for the amelioration of psychoneurosis and insomnia existed under the brand name Jalonac. Both combinations are not available any longer.

The drug is sold as tablet, liquid and 'Trifluperazine-injectable USP' for deep IM short-term use.

Trivia

In Philip K. Dick's novel A Maze of Death, the character Betty Jo Berm mentions, while describing an assortment of pills that she takes, "... "The blue ones are stelazine, which I use as an anti-emetic. You understand: I use it for that, but that isn't it's basic purpose. Basically Stelazine is a tranquilizer, in doses of less that twenty milligrams a day. In greater doses it's an anti-hallucinogenic agent. But I don't take it for that either. Now, the problem with stelazine is that it's a vasodilator."..."

References

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v • d • e Psycholeptics: antipsychotics (N05A)
Phenothiazine typical antipsychotics	Chlorpromazine • Fluphenazine • Mesoridazine • Perphenazine • Prochlorperazine • Promazine • Thioridazine/Sulforidazine • Trifluoperazine • Triflupromazine
Other typical antipsychotics	Indoles (Molindone) • Butyrophenones (Azaperone, Benperidol, Bromperidol, Droperidol, Haloperidol, Trifluperidol) • Thioxanthenes (Flupentixol, Chlorprothixene, Thiothixene, Zuclopenthixol) • diphenylbutylpiperidines (Fluspirilene, Penfluridol, Pimozide) • other (Loxapine)
Atypical antipsychotics	Butyrophenones (Melperone) • Indoles (Sertindole, Ziprasidone) • Benzamides (Sulpiride, Remoxipride, Amisulpride) • diazepines/oxazepines/thiazepines (Clozapine, Olanzapine, Quetiapine) • other (Aripiprazole, Risperidone, Paliperidone, Asenapine, Iloperidone, Zotepine)

References