Fluphenazine

Fluphenazine
Fluphenazine.svg
Fluphenazine-xtal-2012-ball-and-stick.png
Clinical data
Trade namesProlixin, Modecate, Moditen others
AHFS/Drugs.comMonograph
MedlinePlusa682172
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Routes of
administration
by mouth, IM, depot injection (fluphenazine decanoate)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability2.7% (by mouth)
Metabolismunclear[1]
Elimination half-lifeIM 15 hours (HCL), 7-10 days (decanoate)[1]
ExcretionUrine, faeces
Identifiers
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)
  (verify)

Fluphenazine, sold under the brand names Prolixin among others, is an antipsychotic medication.[1] It is used in the treatment of chronic psychoses such as schizophrenia,[1][2] and appears to be about equal in effectiveness to low-potency antipsychotics like chlorpromazine.[3] It is given by mouth, injection into a muscle, or just under the skin.[1] There is also a long acting injectable version that may last for up to four weeks.[1] Fluphenazine decanoate, the depot injection form of fluphenazine, should not be used by people with severe depression.[4]

Common side effects include movement problems, sleepiness, depression and increased weight.[1] Serious side effects may include neuroleptic malignant syndrome, low white blood cell levels, and the potentially permanent movement disorder tardive dyskinesia.[1] In older people with psychosis as a result of dementia it may increase the risk of dying.[1] It may also increase prolactin levels which may result in milk production, enlarged breasts in males, impotence, and the absence of menstrual periods.[1] It is unclear if it is safe for use in pregnancy.[1] Fluphenazine is a typical antipsychotic of the phenothiazine class.[1] Its mechanism of action is not entirely clear but believed to be related to its ability to block dopamine receptors.[1] In up to 40% of those on long term phenothiazines, liver function tests become mildly abnormal.[5]

Fluphenazine came into use in 1959.[6] The injectable form is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[7] It is available as a generic medication.[1] In the United States the tablets costs between $0.22 and $0.42 per day for a typical dose.[1] The wholesale cost in the developing world of the long acting form is between US$0.20 and US$6.20 per injection as of 2014.[8] It was discontinued in Australia around mid 2017.[9]

Medical use[edit]

A 2013 Cochrane review found that fluphenazine's was an imperfect treatment and other inexpensive drugs less associated with side effects may be an just as good in people with schizophrenia.[10]

Side effects[edit]

Discontinuation[edit]

The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotics to avoid acute withdrawal syndrome or rapid relapse.[11] Symptoms of withdrawal commonly include nausea, vomiting, and loss of appetite.[12] Other symptoms may include restlessness, increased sweating, and trouble sleeping.[12] Less commonly there may be a felling of the world spinning, numbness, or muscle pains.[12] Symptoms generally resolve after a short period of time.[12]

There is tentative evidence that discontinuation of antipsychotics can result in psychosis.[13] It may also result in reoccurrence of the condition that is being treated.[14] Rarely tardive dyskinesia can occur when the medication is stopped.[12]

Mechanism of action[edit]

The drug acts primarily by blocking D2 receptores in the basal ganglia, cortical and limbic system.[15]

History[edit]

Fluphenazine came into use in 1959.[6]

Availability[edit]

The injectable form is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[7] It is available as a generic medication.[1] In the United States the tablets costs between 0.22 and 0.42 USD per day for a typical dose.[1] The wholesale cost in the developing world of the long acting form is between 0.20 and 6.20 USD per injection as of 2014.[8] It was discontinued in Australia around mid 2017.[9]

Other animals[edit]

In horses, it is sometimes given by injection as an anxiety-relieving medication, though there are many negative common side effects and it is forbidden by many equestrian competition organizations.[16]

See also[edit]

References[edit]

  1. ^ a b c d e f g h i j k l m n o p q "fluphenazine decanoate". The American Society of Health-System Pharmacists. Archived from the original on 2015-12-08. Retrieved Dec 1, 2015.
  2. ^ "Product Information: Modecate (Fluphenazine Decanoate Oily Injection )" (PDF). TGA eBusiness Services. Bristol-Myers Squibb Australia Pty Ltd. 1 November 2012. Archived from the original on 2 August 2017. Retrieved 9 December 2013.
  3. ^ Tardy M, Huhn M, Engel RR, Leucht S (August 2014). "Fluphenazine versus low-potency first-generation antipsychotic drugs for schizophrenia". The Cochrane Database of Systematic Reviews. 8 (8): CD009230. doi:10.1002/14651858.CD009230.pub2. PMID 25087165.
  4. ^ "Modecate Injection 25mg/ml - Patient Information Leaflet (PIL) - (eMC)". www.medicines.org.uk. Retrieved 2017-11-06.
  5. ^ "Fluphenazine". livertox.nih.gov. Retrieved 2017-11-06.
  6. ^ a b McPherson EM (2007). Pharmaceutical Manufacturing Encyclopedia (3rd ed.). Burlington: Elsevier. p. 1680. ISBN 9780815518563.
  7. ^ a b "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
  8. ^ a b "Fluphenazine Decanoate". International Drug Price Indicator Guide. Archived from the original on 2 August 2017. Retrieved 2 December 2015.
  9. ^ a b Rossi S, ed. (July 2017). "Fluphenazine - Australian Medicines Handbook". Australian Medicines Handbook. Adelaide, Australia: Australian Medicines Handbook Pty Ltd. Retrieved 8 August 2017.
  10. ^ Matar, Hosam E; Almerie, Muhammad Qutayba; Sampson, Stephanie J (2018-06-12). "Fluphenazine (oral) versus placebo for schizophrenia". Cochrane Database of Systematic Reviews. 6: CD006352. doi:10.1002/14651858.cd006352.pub3. ISSN 1465-1858. PMC 3796096. PMID 29893410.
  11. ^ Joint Formulary Committee, BMJ, ed. (March 2009). "4.2.1". British National Formulary (57 ed.). United Kingdom: Royal Pharmaceutical Society of Great Britain. p. 192. ISBN 978-0-85369-845-6. Withdrawal of antipsychotic drugs after long-term therapy should always be gradual and closely monitored to avoid the risk of acute withdrawal syndromes or rapid relapse.
  12. ^ a b c d e Haddad, Peter; Haddad, Peter M.; Dursun, Serdar; Deakin, Bill (2004). Adverse Syndromes and Psychiatric Drugs: A Clinical Guide. OUP Oxford. p. 207-216. ISBN 9780198527480.
  13. ^ Moncrieff J (July 2006). "Does antipsychotic withdrawal provoke psychosis? Review of the literature on rapid onset psychosis (supersensitivity psychosis) and withdrawal-related relapse". Acta Psychiatrica Scandinavica. 114 (1): 3–13. doi:10.1111/j.1600-0447.2006.00787.x. PMID 16774655.
  14. ^ Sacchetti, Emilio; Vita, Antonio; Siracusano, Alberto; Fleischhacker, Wolfgang (2013). Adherence to Antipsychotics in Schizophrenia. Springer Science & Business Media. p. 85. ISBN 9788847026797.
  15. ^ PubChem. "Fluphenazine". pubchem.ncbi.nlm.nih.gov. Retrieved 2019-09-30.
  16. ^ Loving NS (31 March 2012). "Effects of Behavior-Modifying Drug Investigated (AAEP 2011)". The Horse Media Group. Archived from the original on 6 January 2017. Retrieved 13 December 2016.