Trifluoperazine
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Trifluoperazine
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| Systematic (IUPAC) name | |
| 10-[3-(4-methylpiperazin-1-yl)propyl]- 2-(trifluoromethyl)-10H-phenothiazine |
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| Identifiers | |
| CAS number | |
| ATC code | N05 |
| PubChem | |
| DrugBank | |
| 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]
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[edit] 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.
[edit] Uses
The primary 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]
A multi-year UK study by the Alzheimer's Research Trust suggested that this and other neuroleptic anti-psychotic drugs commonly given to Alzheimer's patients with mild behavioural problems often make their condition worse. [2] The study concluded that
| “ | For most patients with AD, withdrawal of neuroleptics had no overall detrimental effect on functional and cognitive status and by some measures improved functional and cognitive status. Neuroleptics may have some value in the maintenance treatment of more severe neuropsychiatric symptoms, but this possibility must be weighed against the unwanted effects of therapy. The current study helps to inform a clinical management strategy for current practice, but the considerable risks of maintenance therapy highlight the urgency of further work to find, develop, and implement safer and more effective treatment approaches for neuropsychiatric symptoms in people with AD. | ” |
[edit] 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.
[edit] Side effects
For further information see: phenothiazine
Serious side effects include akathisia, an inner sense of tension, restlessness/torment; trifuoperazine can also be a potent akathisic agent, tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome.
A particular severe form of liver damage has been reported, making pre-existing liver damage a contraindication.
[edit] 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 N. 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.
[edit] 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."..."
[edit] References
- ^ "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
- ^ "Medication 'worsens Alzheimer's'", BBC News, Tuesday, 1 April 2008. Retrieved on 2008-04-01. "Neuroleptics provided no benefit for patients with mild behavioural problems, but were associated with a marked deterioration in verbal skills."
- ^ Ballard C, Lana MM, Theodoulou M, Douglas S, McShane R, et al. (2008). "A Randomised, Blinded, Placebo-Controlled Trial in Dementia Patients Continuing or Stopping Neuroleptics (The DART-AD Trial)". PLOS Medicine 5 (4, e76): e76. doi:.
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This article needs additional citations for verification. Please help improve this article by adding reliable references. Unsourced material may be challenged and removed. (November 2006) |
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[edit] References
- ^ "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
- ^ "Medication 'worsens Alzheimer's'", BBC News, Tuesday, 1 April 2008. Retrieved on 2008-04-01. "Neuroleptics provided no benefit for patients with mild behavioural problems, but were associated with a marked deterioration in verbal skills."
- ^ Ballard C, Lana MM, Theodoulou M, Douglas S, McShane R, et al. (2008). "A Randomised, Blinded, Placebo-Controlled Trial in Dementia Patients Continuing or Stopping Neuroleptics (The DART-AD Trial)". PLOS Medicine 5 (4, e76): e76. doi:.
