Fluphenazine

Fluphenazine

200px
Systematic (IUPAC) name
2-[4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]piperazin-1-yl]ethanol
Clinical data
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	oral, IM, decanoate
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Bioavailability	40% - 50%
Metabolism	Hepatic
Biological half-life	15 to 30 hours
Excretion	bile/feces
Identifiers
CAS Number	69-23-8
ATC code	N05AB02 (WHO)
PubChem	CID 3372
IUPHAR/BPS	204
DrugBank	DB00623
Chemical data
Formula	C22H26F3N3OS
Molar mass	437.523 g/mol[[]]
(verify)

Fluphenazine is a typical antipsychotic drug used for the treatment of psychoses such as schizophrenia and acute manic phases of bipolar disorder. It belongs to the piperazine class of phenothiazines and is extremely potent; more potent than haloperidol and around fifty to seventy times the potency of chlorpromazine.

Its main use is as a long acting injection given once every two or three weeks to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness. In some countries this can be involuntary under Community Treatment Orders. Its side effect profile is similar to haloperidol, namely predominantly dopamine-blocking effects which give rise to akathisia, parkinsonism and tremor. Long term side effects include the potentially irreversible tardive dyskinesia and the potentially fatal neuroleptic malignant syndrome.

Brand names

Fluphenazine decanoate:	Modecate, Prolixin Decanoate, Dapotum D, Anatensol, Fludecate, Sinqualone Deconoate
Fluphenazine enanthate:	Dapotum Injektion, Flunanthate, Moditen Enanthate Injection, Sinqualone Enanthate
Fluphenazine hydrochloride:	Prolixin, Permitil, Dapotum, Lyogen, Moditen, Omca, Sediten, Selecten, Sevinol, Sinqualone, Trancin

Pharmacokinetics

Fluphenazine has an incomplete oral bioavailability of 40% to 50% (due to extensive first pass metabolization in the liver). Its half life is 15 to 30 hours.

Dosing

12.5 mg of fluphenazine decanoate is roughly equivalent to 100 mg of zuclopenthixol decanoate or 20 mg of flupentixol decanoate.

Side effects

Further information: Typical antipsychotic

Notable side effects include akathisia, extrapyramidal side effects, including tardive dyskinesia and Rabbit syndrome. The frequency and severity of extrapyramidal side effects are direct proportional to the dose given and the duration of treatment. Mostly notably, although rare, it can cause hypothermia because it inhibits ability to shiver.

Sedative, allergic-toxic and anticholinergic/sympatholytic side effects are less likely to occur compared with chlorpromazine. The direct deposition of fluphenazine in the cornea and retina has so far not been reported.

Neuroleptic malignant syndrome, although rare, is a potentially lethal side effect of all antipsychotics.

References

• "Fluphenazine". Davis's Drug Guide for Nurses, Eighth Edition. F.A. Davis Company, 2005. ISBN 0-8036-2455-7.
• FLUPHENAZINE DICHLORHYDRATE [Article in French] Biam Last Updated: 11 December 2000. Accessed 14 September 2005.

de:Fluphenazin