Viscoleo is a thin or low-viscosity vegetable oil.[1] It is specifically a proprietary form of fractionated coconut oil and a medium-chain triglyceride (MCT) oil.[1][2] It is prepared from the dried, solid endosperm of the fruit Cocos nucifera (coconut tree) via hydrolysis, fractionation, and purification.[3] Viscoleo is composed of the medium-chain fatty acids caprylic acid (C8) (55–60%), capric acid (C10) (40%), lauric acid (C12) (1–5%), and caproic acid (C6) (0.5%).[4][5][3][6][7] It is used as an oil vehicle for several depot antipsychotics including clopentixol decanoate, flupentixol decanoate, pipotiazine palmitate, zuclopentixol acetate, and zuclopentixol decanoate.[1][8] Injectable antipsychotics using Viscoleo as a carrier may be absorbed more rapidly and have shorter durations than preparations using sesame oil.[8][9]

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[10]
Clopentixol decanoateSordinol DepotTypicalViscoleob50–600 mg/1–4 weeks4–7 days ?19 days9.0[11]
Flupentixol decanoateDepixolTypicalViscoleob10–200 mg/2–4 weeks4–10 days8 days17 days7.2–9.2[11][12]
Fluphenazine decanoateProlixin DecanoateTypicalSesame oil12.5–100 mg/2–5 weeks1–2 days1–10 days14–100 days7.2–9.0[13][14][15]
Fluphenazine enanthateProlixin EnanthateTypicalSesame oil12.5–100 mg/1–4 weeks2–3 days4 days ?6.4–7.4[14]
FluspirileneImap, RedeptinTypicalWatera2–12 mg/1 week1–8 days7 days ?5.2–5.8[16]
Haloperidol decanoateHaldol DecanoateTypicalSesame oil20–400 mg/2–4 weeks3–9 days18–21 days7.2–7.9[17][18]
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[19]
Pipotiazine palmitatePiportil LongumTypicalViscoleob25–400 mg/4 weeks9–10 days ?14–21 days8.5–11.6[12]
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.

References

  1. 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.
  2. ↑ Larsen, Susan W.; Thing, Mette A.; Larsen, Claus (2012). "Oily (Lipophilic) Solutions and Suspensions". Long Acting Injections and Implants. pp. 113–135. doi:10.1007/978-1-4614-0554-2_7. ISBN 978-1-4614-0553-5.
  3. 1 2 Kai A. R. Rönnholm (1986). Human Milk Feeding in Very Low-birth-weight Infants: A Study of Protein Requirement, as Estimated from Growth, Serum Protein, Amino Acid and Hemoglobin Concentrations, and Riboflavin Status During the Early Postnatal Weeks. Painovalssi. p. 23. ISBN 978-951-99786-8-0. MCT oil (Viscoleo, obtained from Adopan, Kastrup, Denmark) is prepared from dried, solid endosperm of the fruit of Cocos nucifera by hydrolysis, fractionation, and purification. It consists of a mixture of triglycerides containing only short- and medium-chain saturated fatty acids, mainly as octanoic and decanoic acids.
  4. ↑ Svendsen O, Aaes-Jørgensen T (November 1979). "Studies on the fate of vegetable oil after intramuscular injection into experimental animals". Acta Pharmacol Toxicol (Copenh). 45 (5): 352–78. doi:10.1111/j.1600-0773.1979.tb02404.x. PMID 539434. Viscoleo is a thin vegetable oil of triglycerides containing only short chain saturated fatty acids, caprylic acid (55%), capric acid (40%) and lauric acid (5%).
  5. ↑ Svendsen O (April 1983). "Local muscle damage and oily vehicles: a study on local reactions in rabbits after intramuscular injection of neuroleptic drugs in aqueous or oily vehicles". Acta Pharmacol Toxicol (Copenh). 52 (4): 298–304. doi:10.1111/j.1600-0773.1983.tb01104.x. PMID 6135293. Viscoleo@ and sesame oil are triglyceride vegetable oils. The triglycerides in Viscoleo@ contain short chain and saturated fatty acids, caprylic acid, capric acid and lauric acid, [...]
  6. ↑ Radha Raman Gupta (1988). Phenothiazines and 1,4-benzothiazines: Chemical and Biomedical Aspects. Elsevier. p. 688. ISBN 978-0-444-42967-4. Viscoleo® is a triglyceride vegetable oil containing short-chain saturated fatty acids as well as caprylic acid, capric acid, and lauric acid.
  7. ↑ Larsen SW, Rinvar E, Svendsen O, Lykkesfeldt J, Friis GJ, Larsen C (November 2001). "Determination of the disappearance rate of iodine-125 labelled oils from the injection site after intramuscular and subcutaneous administration to pigs". Int J Pharm. 230 (1–2): 67–75. doi:10.1016/s0378-5173(01)00860-2. PMID 11672957.
  8. 1 2 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.
  9. ↑ Remington GJ, Adams ME (April 1995). "Depot neuroleptic therapy: clinical considerations". Can J Psychiatry. 40 (3 Suppl 1): S5–11. doi:10.1177/070674379504003S02. PMID 7627927. S2CID 151908598.
  10. ↑ 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.
  11. 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.
  12. 1 2 Reynolds JE (1993). "Anxiolytic sedatives, hypnotics and neuroleptics.". Martindale: The Extra Pharmacopoeia (30th ed.). London: Pharmaceutical Press. pp. 364–623.
  13. ↑ 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.
  14. 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.
  15. ↑ 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.
  16. ↑ Janssen PA, Niemegeers CJ, Schellekens KH, Lenaerts FM, Verbruggen FJ, van Nueten JM, et al. (November 1970). "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittel-Forschung. 20 (11): 1689–98. PMID 4992598.
  17. ↑ 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.
  18. ↑ 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.
  19. ↑ 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.
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