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Perphenazine enanthate

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Typical antipsychotic medication
Pharmaceutical compound
Perphenazine enanthate
Clinical data
Trade names Decentan Depot, Peratsin Enantaatti, Trilafon, Trilafon Enantato, Trilafon Enantat, Trilifan Retard
Other namesPerphenazine enantate
Routes of
administration 		Intramuscular injection
Drug class Typical antipsychotic
ATC code
Legal status
Legal status
  • Ingeneral: ℞(Prescription only)
Identifiers
  • 2-[4-[3-(2-chlorophenothiazin-10-yl)propyl]piperazin-1-yl]ethyl heptanoate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard 100.037.739 Edit this at Wikidata
Chemical and physical data
Formula C28H38ClN3O2S
Molar mass 516.14g·mol−1
3D model (JSmol)
  • CCCCCCC(=O)OCCN1CCN(CC1)CCCN2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl
  • InChI=1S/C28H38ClN3O2S/c1-2-3-4-5-11-28(33)34-21-20-31-18-16-30(17-19-31)14-8-15-32-24-9-6-7-10-26(24)35-27-13-12-23(29)22-25(27)32/h6-7,9-10,12-13,22H,2-5,8,11,14-21H2,1H3
  • Key:PWEGQJCIAMJJHC-UHFFFAOYSA-N

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]

Pharmacokinetics of long-acting injectable antipsychotics
MedicationBrand nameClassVehicleDosageTmaxt1/2 singlet1/2 multiplelogPcRef
Aripiprazole lauroxil AristadaAtypical Water a441–1064mg/4–8weeks24–35days?54–57days7.9–10.0
Aripiprazole monohydrate Abilify MaintenaAtypical Water a300–400mg/4weeks7days?30–47days4.9–5.2
Bromperidol decanoate Impromen DecanoasTypical Sesame oil 40–300mg/4weeks3–9days?21–25days7.9[7]
Clopentixol decanoate Sordinol DepotTypical Viscoleo b50–600mg/1–4weeks4–7days?19days9.0[8]
Flupentixol decanoate DepixolTypical Viscoleo b10–200mg/2–4weeks4–10days8days17days7.2–9.2[8] [9]
Fluphenazine decanoate Prolixin DecanoateTypical Sesame oil 12.5–100mg/2–5weeks1–2days1–10days14–100days7.2–9.0[10] [11] [12]
Fluphenazine enanthate Prolixin EnanthateTypical Sesame oil 12.5–100mg/1–4weeks2–3days4days?6.4–7.4[11]
Fluspirilene Imap, RedeptinTypical Water a2–12mg/1week1–8days7days?5.2–5.8[13]
Haloperidol decanoate Haldol DecanoateTypical Sesame oil 20–400mg/2–4weeks3–9days18–21days7.2–7.9[14] [15]
Olanzapine pamoate Zyprexa RelprevvAtypical Water a150–405mg/2–4weeks7days?30days–
Oxyprothepin decanoate MeclopinTypical ?????8.5–8.7
Paliperidone palmitate Invega SustennaAtypical Water a39–819mg/4–12weeks13–33days25–139days?8.1–10.1
Perphenazine decanoate Trilafon DekanoatTypical Sesame oil 50–200mg/2–4weeks??27days8.9
Perphenazine enanthateTrilafon EnanthateTypical Sesame oil 25–200mg/2weeks2–3days?4–7days6.4–7.2[16]
Pipotiazine palmitate Piportil LongumTypical Viscoleo b25–400mg/4weeks9–10days?14–21days8.5–11.6[9]
Pipotiazine undecylenate Piportil MediumTypical Sesame oil 100–200mg/2weeks???8.4
Risperidone Risperdal ConstaAtypical Microspheres 12.5–75mg/2weeks21days?3–6days–
Zuclopentixol acetate Clopixol AcuphaseTypical Viscoleo b50–200mg/1–3days1–2days1–2 days4.7–4.9
Zuclopentixol decanoate Clopixol DepotTypical Viscoleo b50–800mg/2–4weeks4–9days?11–21days7.5–9.0
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

[edit ]

References

[edit ]
  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.
  2. 1 2 3 Altamura AC, Sassella F, Santini A, Montresor C, Fumagalli S, Mundo E (2003). "Intramuscular preparations of antipsychotics: uses and relevance in clinical practice". Drugs. 63 (5): 493–512. doi:10.2165/00003495-200363050-00004. PMID 12600227. S2CID 46973260.
  3. 1 2 3 Davis JM, Matalon L, Watanabe MD, Blake L, Metalon L (May 1994). "Depot antipsychotic drugs. Place in therapy". Drugs. 47 (5): 741–73. doi:10.2165/00003495-199447050-00004. PMID 7520856. S2CID 46962898.
  4. 1 2 3 Taylor D (November 2009). "Psychopharmacology and adverse effects of antipsychotic long-acting injections: a review". Br J Psychiatry Suppl. 52: S13–9. doi:10.1192/bjp.195.52.s13 . PMID 19880912. S2CID 1692443.
  5. 1 2 3 Spanarello S, La Ferla T (2014). "The pharmacokinetics of long-acting antipsychotic medications". Curr Clin Pharmacol. 9 (3): 310–7. doi:10.2174/15748847113089990051. PMID 23343447.
  6. 1 2 3 De Risio A, Lang AP (February 2014). "History and therapeutic rationale of long acting antipsychotics". Curr Clin Pharmacol. 9 (1): 39–52. doi:10.2174/15748847113089990057. PMID 23343446.
  7. ↑ Parent M, Toussaint C, Gilson H (1983). "Long-term treatment of chronic psychotics with bromperidol decanoate: clinical and pharmacokinetic evaluation". Current Therapeutic Research. 34 (1): 1–6.
  8. 1 2 Jørgensen A, Overø KF (1980). "Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. III. Serum levels". Acta Psychiatrica Scandinavica. Supplementum. 279: 41–54. doi:10.1111/j.1600-0447.1980.tb07082.x. PMID 6931472.
  9. 1 2 Reynolds JE (1993). "Anxiolytic sedatives, hypnotics and neuroleptics.". Martindale: The Extra Pharmacopoeia (30th ed.). London: Pharmaceutical Press. pp. 364–623.
  10. ↑ Ereshefsky L, Saklad SR, Jann MW, Davis CM, Richards A, Seidel DR (May 1984). "Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches". The Journal of Clinical Psychiatry. 45 (5 Pt 2): 50–9. PMID 6143748.
  11. 1 2 Curry SH, Whelpton R, de Schepper PJ, Vranckx S, Schiff AA (April 1979). "Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man". British Journal of Clinical Pharmacology. 7 (4): 325–31. doi:10.1111/j.1365-2125.1979.tb00941.x. PMC 1429660 . PMID 444352.
  12. ↑ Young D, Ereshefsky L, Saklad SR, Jann MW, Garcia N (1984). Explaining the pharmacokinetics of fluphenazine through computer simulations. (Abstract.). 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists. Dallas, Texas.
  13. ↑ Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, van Nueten JM, Marsboom RH, Hérin VV, Schaper WK (November 1970). "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittel-Forschung. 20 (11): 1689–98. PMID 4992598.
  14. ↑ Beresford R, Ward A (January 1987). "Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis". Drugs. 33 (1): 31–49. doi:10.2165/00003495-198733010-00002. PMID 3545764.
  15. ↑ Reyntigens AJ, Heykants JJ, Woestenborghs RJ, Gelders YG, Aerts TJ (1982). "Pharmacokinetics of haloperidol decanoate. A 2-year follow-up". International Pharmacopsychiatry. 17 (4): 238–46. doi:10.1159/000468580. PMID 7185768.
  16. ↑ Larsson M, Axelsson R, Forsman A (1984). "On the pharmacokinetics of perphenazine: a clinical study of perphenazine enanthate and decanoate". Current Therapeutic Research. 36 (6): 1071–88. INIST 8951670.



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