|Trade names||Stelazine, Eskazinyl, Eskazine, Jatroneural, others|
|Drug class||Typical antipsychotic|
|Main uses||Schizophrenia, generalized anxiety disorder, nausea|
|Side effects||Movement disorders, sleepiness, blurry vision, dry mouth, low blood pressure|
|By mouth, IM|
|Elimination half-life||10–20 hours|
|Chemical and physical data|
|Molar mass||407.50 g·mol−1|
|3D model (JSmol)|
Trifluoperazine, sold under the brand name Stelazine among others, is a typical antipsychotic primarily used to treat schizophrenia. It is also used, short term, for generalized anxiety disorder but is less preferred to benzodiazepines and use for nausea. It is taken by mouth.
Common side effects include movement disorders including tardive dyskinesia, sleepiness, blurry vision, dry mouth, and low blood pressure. Other severe side effects may include neuroleptic malignant syndrome, pancytopenia, and liver problems. It increases the risk of death in those with dementia. It is in the phenothiazine chemical class. It is believed to work by blocking the effects of dopamine.
Trifluoperazine was patented in 1955 and came into medical use in 1959. It is available as a generic medication. In the United States a month of medication at 5 mg twice per day costs about 27 USD as of 2021. This amount in the United Kingdom costs the NHS about £83.
Trifluoperazine is an effective antipsychotic for people with schizophrenia. There is low-quality evidence that trifluoperazine increases the chance of being improved when compared to placebo when people are followed up for 19 weeks. There is low-quality evidence that trifluoperazine reduces the risk of relapse when compared with placebo when people are followed for 5 months. As of 2014 there was no good evidence for a difference between trifluoperazine and placebo with respect to the risk of experiencing intensified symptoms over a 16-week period nor in reducing significant agitation or distress.
There is no good evidence that trifluoperazine is more effective for schizophrenia than lower-potency antipsychotics like chlorpromazine, chlorprothixene, thioridazine and levomepromazine, but trifluoperazine appears to cause more adverse effects than these drugs.
For nausea a dose of 1 to 2 mg twice per day may be used.
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%.
A 2004 meta-analysis of the studies on trifluoperazine found that it is more likely than placebo to cause extrapyramidal side effects such as akathisia, dystonia, and Parkinsonism. It is also more likely to cause somnolence and anticholinergic side effects such as red eye and xerostomia (dry mouth). All antipsychotics can cause the rare and sometimes fatal neuroleptic malignant syndrome. Trifluoperazine can lower the seizure threshold. The antimuscarinic action of trifluoperazine can cause excessive dilation of the pupils (mydriasis), which increases the chances of patients with hyperopia developing glaucoma.
Mechanism of action
Trifluoperazine has central antiadrenergic, antidopaminergic, and minimal anticholinergic effects. It is believed to work by blockading dopamine D1 and D2 receptors in the mesocortical and mesolimbic pathways, relieving or minimizing such symptoms of schizophrenia as hallucinations, delusions, and disorganized thought and speech.
Brand names include Eskazinyl, Eskazine, Jatroneural, Modalina, Stelazine, Stilizan, Terfluzine, Trifluoperaz, Triftazin.
In the United Kingdom and some other countries, trifluoperazine is sold and marketed under the brand 'Stelazine'.
The drug is sold as tablet, liquid and 'Trifluoperazine-injectable USP' for deep intramuscular short-term use. GP studying pharmacological data has indicated cases of neck vertebrae irreversible fusing leading to NHS preparations being predominantly of the liquid form trifluoperazine as opposed to the tablet form as in Stela zine etc.
In the past, trifluoperazine was used in fixed combinations with the MAO inhibitor (antidepressant) tranylcypromine (tranylcypromine/trifluoperazine) to attenuate the strong stimulating effects of this antidepressant. This combination was sold under the brand name Jatrosom N. Likewise a combination with amobarbital (potent sedative/hypnotic agent) for the amelioration of psychoneurosis and insomnia existed under the brand name Jalonac. In Italy the first combination is still available, sold under the brand name Parmodalin (10 mg of tranylcypromine and 1 mg of trifluoperazine).
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