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Trifluoperazine



Trifluoperazine
Systematic (IUPAC) name
10-[3-(4-methylpiperazin-1-yl)propyl]-
2-(trifluoromethyl)-10
H-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]

Additional recommended knowledge

Contents

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. Likewise 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

  1. ^ "Facts and Comparisons" III W. Port Plaza, Suite 300 St. Louis MO. USA 63146-3098 (telephone 314-216-2100 or 1-800-223-0554). (Note this book is currently used by Rite Aid Pharmacies in the USA as a reference aid and it is a loose bound updatable book. The updatable section called "Antipsychotic Agents" is (c)1990


References

  1. ^ "Facts and Comparisons" III W. Port Plaza, Suite 300 St. Louis MO. USA 63146-3098 (telephone 314-216-2100 or 1-800-223-0554). (Note this book is currently used by Rite Aid Pharmacies in the USA as a reference aid and it is a loose bound updatable book. The updatable section called "Antipsychotic Agents" is (c)1990
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Trifluoperazine". A list of authors is available in Wikipedia.
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