Chemistry:Perphenazine enanthate

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Short description: Typical antipsychotic medication
Perphenazine enanthate
Clinical data
Trade namesDecentan Depot, Peratsin Enantaatti, Trilafon, Trilafon Enantato, Trilafon Enantat, Trilifan Retard
Other namesPerphenazine enantate
Routes of
administration		Intramuscular injection
Drug classTypical antipsychotic
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC28H38ClN3O2S
Molar mass516.14 g·mol−1
3D model (JSmol)

Perphenazine enanthate, sold under the brand name Trilafon Enantat among others, is a typical antipsychotic and a depot antipsychotic ester which is used in the treatment of schizophrenia and has been marketed in Europe.[1][2][3][4][5][6] It is formulated in sesame oil and administered by intramuscular injection and acts as a long-lasting prodrug of perphenazine.[2][3][4][5][6] Perphenazine enanthate is used at a dose of 25 to 200 mg once every 2 weeks by injection, with a time to peak levels of 2 to 3 days and an elimination half-life of 4 to 7 days.[2][3][4][5][6]

v · d · e Pharmacokinetics of long-acting injectable antipsychotics
Medication Brand name Class Vehicle Dosage Tmax t1/2 single t1/2 multiple logPc Ref
Aripiprazole lauroxil Aristada Atypical Watera 441–1064 mg/4–8 weeks 24–35 days ? 54–57 days 7.9–10.0
Aripiprazole monohydrate Abilify Maintena Atypical Watera 300–400 mg/4 weeks 7 days ? 30–47 days 4.9–5.2
Bromperidol decanoate Impromen Decanoas Typical Sesame oil 40–300 mg/4 weeks 3–9 days ? 21–25 days 7.9 [7]
Clopentixol decanoate Sordinol Depot Typical Viscoleob 50–600 mg/1–4 weeks 4–7 days ? 19 days 9.0 [8]
Flupentixol decanoate Depixol Typical Viscoleob 10–200 mg/2–4 weeks 4–10 days 8 days 17 days 7.2–9.2 [8][9]
Fluphenazine decanoate Prolixin Decanoate Typical Sesame oil 12.5–100 mg/2–5 weeks 1–2 days 1–10 days 14–100 days 7.2–9.0 [10][11][12]
Fluphenazine enanthate Prolixin Enanthate Typical Sesame oil 12.5–100 mg/1–4 weeks 2–3 days 4 days ? 6.4–7.4 [11]
Fluspirilene Imap, Redeptin Typical Watera 2–12 mg/1 week 1–8 days 7 days ? 5.2–5.8 [13]
Haloperidol decanoate Haldol Decanoate Typical Sesame oil 20–400 mg/2–4 weeks 3–9 days 18–21 days 7.2–7.9 [14][15]
Olanzapine pamoate Zyprexa Relprevv Atypical Watera 150–405 mg/2–4 weeks 7 days ? 30 days –
Oxyprothepin decanoate Meclopin Typical ? ? ? ? ? 8.5–8.7
Paliperidone palmitate Invega Sustenna Atypical Watera 39–819 mg/4–12 weeks 13–33 days 25–139 days ? 8.1–10.1
Perphenazine decanoate Trilafon Dekanoat Typical Sesame oil 50–200 mg/2–4 weeks ? ? 27 days 8.9
Perphenazine enanthate Trilafon Enanthate Typical Sesame oil 25–200 mg/2 weeks 2–3 days ? 4–7 days 6.4–7.2 [16]
Pipotiazine palmitate Piportil Longum Typical Viscoleob 25–400 mg/4 weeks 9–10 days ? 14–21 days 8.5–11.6 [9]
Pipotiazine undecylenate Piportil Medium Typical Sesame oil 100–200 mg/2 weeks ? ? ? 8.4
Risperidone Risperdal Consta Atypical Microspheres 12.5–75 mg/2 weeks 21 days ? 3–6 days –
Zuclopentixol acetate Clopixol Acuphase Typical Viscoleob 50–200 mg/1–3 days 1–2 days 1–2 days 4.7–4.9
Zuclopentixol decanoate Clopixol Depot Typical Viscoleob 50–800 mg/2–4 weeks 4–9 days ? 11–21 days 7.5–9.0
Note: All by intramuscular injection. Footnotes: a = Microcrystalline or nanocrystalline aqueous suspension. b = Low-viscosity vegetable oil (specifically fractionated coconut oil with medium-chain triglycerides). c = Predicted, from PubChem and DrugBank. Sources: Main: See template.

See also

References

  1. ↑ Swiss Pharmaceutical Society (2000). Swiss Pharmaceutical Society. ed. Index Nominum 2000: International Drug Directory. Taylor & Francis. pp. 811–. ISBN 978-3-88763-075-1. https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA811. 
  2. ↑ 2.0 2.1 2.2 "Intramuscular preparations of antipsychotics: uses and relevance in clinical practice". Drugs 63 (5): 493–512. 2003. doi:10.2165/00003495-200363050-00004. PMID 12600227. 
  3. ↑ 3.0 3.1 3.2 "Depot antipsychotic drugs. Place in therapy". Drugs 47 (5): 741–73. May 1994. doi:10.2165/00003495-199447050-00004. PMID 7520856. 
  4. ↑ 4.0 4.1 4.2 "Psychopharmacology and adverse effects of antipsychotic long-acting injections: a review". Br J Psychiatry Suppl 52: S13–9. November 2009. doi:10.1192/bjp.195.52.s13. PMID 19880912. 
  5. ↑ 5.0 5.1 5.2 "The pharmacokinetics of long-acting antipsychotic medications". Curr Clin Pharmacol 9 (3): 310–7. 2014. doi:10.2174/15748847113089990051. PMID 23343447. 
  6. ↑ 6.0 6.1 6.2 "History and therapeutic rationale of long acting antipsychotics". Curr Clin Pharmacol 9 (1): 39–52. February 2014. doi:10.2174/15748847113089990057. PMID 23343446. 
  7. ↑ "Long-term treatment of chronic psychotics with bromperidol decanoate: clinical and pharmacokinetic evaluation.". Current Therapeutic Research 34 (1): 1–6. 1983. 
  8. ↑ 8.0 8.1 "Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. III. Serum levels". Acta Psychiatrica Scandinavica. Supplementum 279: 41–54. 1980. doi:10.1111/j.1600-0447.1980.tb07082.x. PMID 6931472. 
  9. ↑ 9.0 9.1 "Anxiolytic sedatives, hypnotics and neuroleptics.". Martindale: The Extra Pharmacopoeia (30th ed.). London: Pharmaceutical Press. 1993. pp. 364–623. 
  10. ↑ "Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches". The Journal of Clinical Psychiatry 45 (5 Pt 2): 50–9. May 1984. PMID 6143748. 
  11. ↑ 11.0 11.1 "Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man". British Journal of Clinical Pharmacology 7 (4): 325–31. April 1979. doi:10.1111/j.1365-2125.1979.tb00941.x. PMID 444352. 
  12. ↑ "Explaining the pharmacokinetics of fluphenazine through computer simulations. (Abstract.)". 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists.. Dallas, Texas. 1984. 
  13. ↑ "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittel-Forschung 20 (11): 1689–98. November 1970. PMID 4992598. 
  14. ↑ "Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis". Drugs 33 (1): 31–49. January 1987. doi:10.2165/00003495-198733010-00002. PMID 3545764. 
  15. ↑ "Pharmacokinetics of haloperidol decanoate. A 2-year follow-up". International Pharmacopsychiatry 17 (4): 238–46. 1982. doi:10.1159/000468580. PMID 7185768. 
  16. ↑ "On the pharmacokinetics of perphenazine: a clinical study of perphenazine enanthate and decanoate.". Current Therapeutic Research 36 (6): 1071–88. 1984. 





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