Stelazine

Trifluoperazine

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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	CID 5566
IUPHAR ligand ID	214
DrugBank	DB00831
Chemical data
Formula	C21H24F3N3S
Mol. mass	407.497
Pharmacokinetic data
Metabolism	Hepatic
Half-life	10–20 hours
Therapeutic considerations
Pregnancy cat.	C(AU) C(US)
Legal status	POM (UK) ℞-only (US)
Routes	oral, IM
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Trifluoperazine (Eskazinyl, Eskazine, Jatroneural, Modalina, Stelazine, Terfluzine, Trifluoperaz, Triftazin) is a typical antipsychotic of the phenothiazine chemical class.

Contents [hide] 1 Uses 2 Pharmacology 3 Side effects 4 Contraindications 5 Formulations 6 References

[edit] Uses

The primary indication of trifluoperazine is schizophrenia. Other official indications may vary country by country, but generally it is also indicated for use in agitation and patients with behavioural problems, severe nausea and vomiting as well as severe anxiety. 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%.^{[citation needed]}

A 2006 study suggested 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 antipsychotic 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] Pharmacology

Trifluoperazine has central antiadrenergic,^[3] antidopaminergic,^[4][5] and minimal anticholinergic effects.^[6] 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.^[7]

[edit] Side effects

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.^[7] It is also more likely to cause somnolence and anticholinergic side effects such as blurred vision and xerostomia (dry mouth).^[7] All phenothiazines can cause the rare and sometimes fatal neuroleptic malignant syndrome.^[8] Trifluoperazine can lower the seizure threshold.^[9] The antimuscarinic action of trifluoperazine can cause excessive dilation of the pupils (mydriasis), which increases the chances of patients with hyperopia developing glaucoma.^[10]