Fluphenazine

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Fluphenazine
Fluphenazine.svg
Systematic (IUPAC) name
2-[4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]piperazin-1-yl]ethanol
Clinical data
Trade names Prolixin, Modecate, Moditen others
AHFS/Drugs.com monograph
MedlinePlus a682172
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Legal status
Routes of
administration		 Oral, IM, depot injection (fluphenazine decanoate)
Pharmacokinetic data
Bioavailability 2.7% (Oral)
Metabolism unclear[1]
Biological half-life IM 15 hours (HCL), 7-10 days (decanoate)[1]
Excretion Urine, faeces
Identifiers
CAS Number 69-23-8 YesY
ATC code N05AB02 (WHO)
PubChem CID: 3372
IUPHAR/BPS 204
DrugBank DB00623 YesY
ChemSpider 3255 YesY
UNII S79426A41Z YesY
KEGG D07977 YesY
ChEBI CHEBI:5123 YesY
ChEMBL CHEMBL726 YesY
Chemical data
Formula C22H26F3N3OS
Molecular mass 437.523 g/mol
  • 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 YesY
  • Key:PLDUPXSUYLZYBN-UHFFFAOYSA-N YesY
  (verify)

Fluphenazine, sold under the brand names Prolixin among others, is a antipsychotic medication.[1] It is used in the treatment of chronic psychoses such as schizophrenia.[1] It is given by mouth, injection into a muscle, or just under the skin.[1] There is a long acting injectable version that may last for up to four weeks.[1]

Common side effects include movement problems, sleepiness, and increased weight. Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, neuroleptic malignant syndrome, and low white blood cell levels. In older people with psychosis as a result of dementia it may increase the risk of dying. It may also increase prolactin levels which may result in milk production. It is unclear if it is safe for use in pregnancy. Fluphenazine is a typical antipsychotic of the phenothiazine class. Its mechanism of action is not entirely clear but believed to be related to its ability as a dopamine antagonist.[1]

Fluphenazine came into use in 1959.[2] It is on the World Health Organization's List of Essential Medicines, most important medication needed in a basic health system.[3] It is available as a generic medication.[1] In the United States the pills costs between 0.22 and 0.42 USD per day for a typical dose.[1] The wholesale cost of the long acting form is between 0.20 and 6.20 USD per injection as of 2014.[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]

Side effects

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Further information: Typical antipsychotic

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

Common adverse effects (i.e. those that have an incidence ≥1%) include

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  • 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

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  • 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

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Unknown frequency side effects include
  • Confusion
  • Decreased gag reflex
  • Silent pneumonia (likely rare)

References

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