Viscoleo

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
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 [10]
Clopentixol decanoate Sordinol Depot Typical Viscoleob 50–600 mg/1–4 weeks 4–7 days ? 19 days 9.0 [11]
Flupentixol decanoate Depixol Typical Viscoleob 10–200 mg/2–4 weeks 4–10 days 8 days 17 days 7.2–9.2 [11][12]
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 [13][14][15]
Fluphenazine enanthate Prolixin Enanthate Typical Sesame oil 12.5–100 mg/1–4 weeks 2–3 days 4 days ? 6.4–7.4 [14]
Fluspirilene Imap, Redeptin Typical Watera 2–12 mg/1 week 1–8 days 7 days ? 5.2–5.8 [16]
Haloperidol decanoate Haldol Decanoate Typical Sesame oil 20–400 mg/2–4 weeks 3–9 days 18–21 days 7.2–7.9 [17][18]
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 [19]
Pipotiazine palmitate Piportil Longum Typical Viscoleob 25–400 mg/4 weeks 9–10 days ? 14–21 days 8.5–11.6 [12]
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.
  1. ^ a b c 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. ^ a b 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. ^ a b 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. ^ a b 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. ^ a b 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. ^ a b 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, 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.
  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.