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Fluphenazine

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Fluphenazine
Clinical data
Trade namesProlixin, Modecate
AHFS/Drugs.comMonograph
MedlinePlusa682172
Pregnancy
category
  • AU: C
Routes of
administration		oral, IM, decanoate
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability2.7% (Oral)
MetabolismHepatic (via CYP2D6)[1]
Elimination half-life14.7 hours, 6-9 days (decanoate)[1]
ExcretionUrine, faeces
Identifiers
  • 2-[4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]piperazin-1-yl]ethanol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.000.639 Edit this at Wikidata
Chemical and physical data
FormulaC22H26F3N3OS
Molar mass437.523 g/mol g·mol−1
3D model (JSmol)
  • FC(F)(F)c2cc1N(c3c(Sc1cc2)cccc3)CCCN4CCN(CCO)CC4
  • InChI=1S/C22H26F3N3OS/c23-22(24,25)17-6-7-21-19(16-17)28(18-4-1-2-5-20(18)30-21)9-3-8-26-10-12-27(13-11-26)14-15-29/h1-2,4-7,16,29H,3,8-15H2 checkY
  • Key:PLDUPXSUYLZYBN-UHFFFAOYSA-N checkY
  (verify)

Fluphenazine (sold under the brand names Prolixin, Modecate) is a typical antipsychotic drug used for the treatment of chronic psychoses such as schizophrenia.[2][3] It is a phenothiazine with a piperazine side-chain. It works by antagonising (blocking) the dopamine D2 receptors in the brain. This also leads to some of its side effects like movement disorders (like parkinsonism and akathisia) and prolactin elevation. It is given via an intramuscular or subcutaneous depot injection (as its decanoate ester) or by mouth in the form of tablets.[1] In some countries only the depot formulations are currently available.[2][3] Compared to other antipsychotics it is less prone to causing sedation, low blood pressure or anticholinergic effects but is associated with a higher frequency of movement disorders.[1]

It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.[4]

Medical uses

Its primary uses is in the treatment of schizophrenia.[5] It appears to be about equal in effectiveness to low-potency antipsychotics.[6]

Adverse effects

Further information: Typical antipsychotic

Information sources:[5][7][8]

Common adverse effects (i.e. those that have an incidence ≥1%) include
  • Hypotension
  • Orthostatic hypotension
  • Somnolence/drowsiness
  • Weight gain
  • Erectile dysfunction
  • Oligomenorrhea or amenorrhea
  • Anticholinergic effects, such as:
- Dry mouth
- Constipation
- Nasal congestion
- Blurred vision
- Diminished sweating
  • Extrapyramidal side effects, such as:
- Tremor
- Akathisia
- Muscle rigidity
- Dystonia
- Parkinsonism
  • Dizziness
  • Epithelial keratopathy
  • Eye / vision finding
  • Retinitis pigmentosa
  • Photosensitivity
Uncommon side effects (0.1%≤incidence<1%) include
  • Agitation
  • Anxiety
  • Cerebral oedema
  • Depression
  • Euphoria
  • Headache
  • Ineffective temperature regulation
  • Restlessness
  • Weakness
  • Weight loss
  • Dyspepsia
  • Lens opacities (with prolonged use)
  • Photosensitivity
  • Pruritus
  • Diarrhoea
  • Galactorrhoea
  • Ejaculatory disorder
  • QT interval prolongation
Rare (incidence<0.1%) side effects include
Unknown frequency side effects include
  • Confusion
  • Decreased gag reflex
  • Silent pneumonia (likely rare)

References

  1. ^ a b c d Brayfield, A, ed. (13 December 2013). "Fluphenazine". Martindale: The Complete Drug Reference. London, UK: Pharmaceutical Press. Retrieved 14 July 2014.
  2. ^ a b Joint Formulary Committee (2013). British National Formulary (BNF) (65 ed.). London, UK: Pharmaceutical Press. pp. 237, 238. ISBN 978-0-85711-084-8.
  3. ^ a b Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3.
  4. ^ "WHO Model List of Essential Medicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
  5. ^ a b "PRODUCT INFORMATION MODECATE (Fluphenazine Decanoate Oily Injection)" (PDF). TGA eBusiness Services. Bristol-Myers Squibb Australia Pty Ltd. 1 November 2012. Retrieved 9 December 2013.
  6. ^ Tardy, M; Huhn, M; Engel, RR; Leucht, S (Aug 3, 2014). "Fluphenazine versus low-potency first-generation antipsychotic drugs for schizophrenia". The Cochrane database of systematic reviews. 8: CD009230. doi:10.1002/14651858.CD009230.pub2. PMID 25087165.
  7. ^ "FLUPHENAZINE HYDROCHLORIDE tablet, film coated [Sandoz Inc]". DailyMed. Sandoz Inc. October 2011. Retrieved 9 December 2013.
  8. ^ "Modecate Concentrate Injection 100mg/ml - Summary of Product Characteristics (SPC)". electronic Medicines Compendium. Sanofi. 11 January 2013. Retrieved 9 December 2013.
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