Haloperidol decanoate

Haloperidol decanoate, sold under the brand name Haldol Decanoate among others, is a typical antipsychotic which is used in the treatment of schizophrenia.[1][2][3][4] It is administered by injection into muscle at a dose of 100 to 200 mg once every 4 weeks or monthly.[5][6][7] The dorsogluteal site is recommended.[5] A 3.75-cm (1.5-inch), 21-gauge needle is generally used, but obese individuals may require a 6.5-cm (2.5-inch) needle to ensure that the drug is indeed injected intramuscularly and not subcutaneously.[5] Haloperidol decanoate is provided in the form of 50 or 100 mg/mL oil solution of sesame oil and benzyl alcohol in ampoules or pre-filled syringes.[5][6][8] Its elimination half-life after multiple doses is 21 days.[9][10] The medication is marketed in many countries throughout the world.[2][11]

Pharmacokinetics of long-acting injectable antipsychotics
MedicationBrand nameClassVehicleDosageTmaxt1/2 singlet1/2 multiplelogPcRef
Aripiprazole lauroxilAristadaAtypicalWatera441–1064 mg/4–8 weeks24–35 days?54–57 days7.9–10.0
Aripiprazole monohydrateAbilify MaintenaAtypicalWatera300–400 mg/4 weeks7 days?30–47 days4.9–5.2
Bromperidol decanoateImpromen DecanoasTypicalSesame oil40–300 mg/4 weeks3–9 days?21–25 days7.9[12]
Clopentixol decanoateSordinol DepotTypicalViscoleob50–600 mg/1–4 weeks4–7 days?19 days9.0[13]
Flupentixol decanoateDepixolTypicalViscoleob10–200 mg/2–4 weeks4–10 days8 days17 days7.2–9.2[13][14]
Fluphenazine decanoateProlixin DecanoateTypicalSesame oil12.5–100 mg/2–5 weeks1–2 days1–10 days14–100 days7.2–9.0[15][16][17]
Fluphenazine enanthateProlixin EnanthateTypicalSesame oil12.5–100 mg/1–4 weeks2–3 days4 days?6.4–7.4[16]
FluspirileneImap, RedeptinTypicalWatera2–12 mg/1 week1–8 days7 days?5.2–5.8[18]
Haloperidol decanoateHaldol DecanoateTypicalSesame oil20–400 mg/2–4 weeks3–9 days18–21 days7.2–7.9[19][20]
Olanzapine pamoateZyprexa RelprevvAtypicalWatera150–405 mg/2–4 weeks7 days?30 days
Oxyprothepin decanoateMeclopinTypical?????8.5–8.7
Paliperidone palmitateInvega SustennaAtypicalWatera39–819 mg/4–12 weeks13–33 days25–139 days?8.1–10.1
Perphenazine decanoateTrilafon DekanoatTypicalSesame oil50–200 mg/2–4 weeks??27 days8.9
Perphenazine enanthateTrilafon EnanthateTypicalSesame oil25–200 mg/2 weeks2–3 days?4–7 days6.4–7.2[21]
Pipotiazine palmitatePiportil LongumTypicalViscoleob25–400 mg/4 weeks9–10 days?14–21 days8.5–11.6[14]
Pipotiazine undecylenatePiportil MediumTypicalSesame oil100–200 mg/2 weeks???8.4
RisperidoneRisperdal ConstaAtypicalMicrospheres12.5–75 mg/2 weeks21 days?3–6 days
Zuclopentixol acetateClopixol AcuphaseTypicalViscoleob50–200 mg/1–3 days1–2 days1–2 days4.7–4.9
Zuclopentixol decanoateClopixol DepotTypicalViscoleob50–800 mg/2–4 weeks4–9 days?11–21 days7.5–9.0
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.
Haloperidol decanoate
Clinical data
Trade namesHalomonth, Haldol Decanoate, Haldol Decanoas, Haloperidol Decanoate, Haloperidol Decanoat, Neoperidole, Serenase Dekanoat
Other namesKD-136; R-13672
Routes of
administration
Intramuscular injection
Drug classTypical antipsychotic
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC31H41ClFNO3
Molar mass530.12 g·mol−1
3D model (JSmol)

See also

References

  1. J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 619–. ISBN 978-1-4757-2085-3.
  2. Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000. pp. 509–. ISBN 978-3-88763-075-1.
  3. A. Kleemann; J. Engel; B. Kutscher; D. Reichert (2009). Pharmaceutical Substances: Syntheses, Patents and Applications of the most relevant APIs (5th ed.). Thieme. pp. 1376–. ISBN 978-3-13-179525-0.
  4. I.K. Morton; Judith M. Hall (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 139–. ISBN 978-94-011-4439-1.
  5. Louis A. Pagliaro; Ann M. Pagliaro (1999). Psychologists' Psychotropic Drug Reference. Psychology Press. pp. 260–. ISBN 978-0-87630-964-3.
  6. Richard Jed Wyatt; Robert H. Chew (20 May 2008). Wyatt's Practical Psychiatric Practice: Forms and Protocols for Clinical Use. American Psychiatric Pub. pp. 142–. ISBN 978-1-58562-687-8.
  7. Katherine M. Fortinash; Patricia A. Holoday Worret (13 June 2014). Psychiatric Mental Health Nursing - E-Book. Elsevier Health Sciences. pp. 572–. ISBN 978-0-323-29327-3.
  8. Mary Lee; Archana Desai (2007). Gibaldi's Drug Delivery Systems in Pharmaceutical Care. ASHP. pp. 281–. ISBN 978-1-58528-136-7.
  9. 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.
  10. Zuidema, J.; Pieters, F.A.J.M.; Duchateau, G.S.M.J.E. (1988). "Release and absorption rate aspects of intramuscularly injected pharmaceuticals". International Journal of Pharmaceutics. 47 (1–3): 1–12. doi:10.1016/0378-5173(88)90209-8. ISSN 0378-5173.
  11. https://www.drugs.com/international/haloperidol.html
  12. 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. https://scholar.google.com/scholar?cites=10379409109713994773
  13. Jørgensen A, Overø KF (1980). "Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. III. Serum levels". Acta Psychiatr Scand Suppl. 279: 41–54. doi:10.1111/j.1600-0447.1980.tb07082.x. PMID 6931472.
  14. Reynolds, J. E. F. (1993). Anxiolytic sedatives, hypnotics and neuroleptics. Martindale: The Extra Pharmacopoeia, 30th Edition (pp. 364–623). Pharmaceutical Press, London. https://scholar.google.com/scholar?cluster=8335042449033257176
  15. Ereshefsky L, Saklad SR, Jann MW, Davis CM, Richards A, Seidel DR (May 1984). "Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches". J Clin Psychiatry. 45 (5 Pt 2): 50–9. PMID 6143748.
  16. 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". Br J Clin Pharmacol. 7 (4): 325–31. doi:10.1111/j.1365-2125.1979.tb00941.x. PMC 1429660. PMID 444352.
  17. Young. D.: Ereshefsky. L.: Saklad. S.R.; Jann. M.W. and Garcia. N.: Explaining the pharmacokinetics of fluphenazine through computer simulations. (Abstract.) Presented at the 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists. Dallas. Texas (1984).
  18. 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". Arzneimittelforschung. 20 (11): 1689–98. PMID 4992598.
  19. 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.
  20. Reyntigens AJ, Heykants JJ, Woestenborghs RJ, Gelders YG, Aerts TJ (1982). "Pharmacokinetics of haloperidol decanoate. A 2-year follow-up". Int Pharmacopsychiatry. 17 (4): 238–46. doi:10.1159/000468580. PMID 7185768.
  21. 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), 1071–1088. https://scholar.google.com/scholar?cluster=12503004172250709786


This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.