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Trifluoperazine

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Trifluoperazine chemical structure
Trifluoperazine

10-[3-(4-methylpiperazin-1-yl)propyl]-
2-(trifluoromethyl)-10
H-phenothiazine
IUPAC name
CAS number
117-89-5
ATC code

N05AB06

PubChem
5566
DrugBank
APRD00173
Chemical formula C21H24F

3N3S

Molecular weight 407.497
Bioavailability
Metabolism Hepatic
Elimination half-life 10-20 hours
Excretion
Pregnancy category
Legal status
Routes of administration oral, IM


Trifluoperazine (sold as Eskazinyl®, Eskazine®, Jatroneural®, Modalina®, Stelazine®, Terfluzine®) is a typical antipsychotic drug of the phenothiazine group. Trifluoperazine is a highly potent drug (approx. 20-times more potent than Chlorpromazine).

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) extrapyramidal symptoms. 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]

Side effects

Also, all side-effects of chlorpromazine may occur. These are sedative, hypotensive, anticholinergic/sympatholytic and allergic-toxic ones. A partiular severe form of liver damage has been reported. Therefore, preexisting liver damage is a clear 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.


ru:Трифлуоперазин

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