Abstract
Cis(Z)-clopenthixol decanoate in Viscoleo (Sordinol® Depot, Cisordinol® Depot, Clopixol® Inj.) was given intramuscularly to nine schizophrenic patients with dosage intervals of 1 or 2 weeks. Serum concentrations of the two geometric isomers of clopenthixol and its N-dealkyl metabolite were recorded in two successive dosage intervals. Significant correlations were found for dose vs area under the serum concentration curve and vs serum concentrations measured on individual days. The last mentioned concentrations are good measures of the area under the serum concentration curve, which expresses the drug load of the patient. The serum concentration curves in two successive dosage intervals were very similar. Maximum serum concentration was seen 5–7 days after injection and the mean maximum/minimum fluctuation was 1.6 with the 2-week dosage interval. The finding of very low amounts of the trans(E)-isomers of clopenthixol and the N-dealkyl-metabolite shows that isomerization of the cis(Z)-compounds into the corresponding trans(E)-isomers does not take place within the organism.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Aaes-Jørgensen T, Fredricson Overø K, Bøgesø KP, Jørgensen A (1977) Pharmacokinetic studies on clopenthixol decanoate; a comparison with clopenthixol in dogs and rats. Acta Pharmacol Toxicol 41:103–120
Aaes-Jørgensen T (1980) Specific high performance liquid chromatographic method for estimation of the cis(Z)-and trans(E)-isomers of clopenthixol and a N-dealkyl metabolite. J Chromatogr. 183: 239–245
Aaes-Jørgensen T, Gravem A, Jørgensen A (1981) Serum levels of the isomers of clopenthixol in patients given cis(Z)/trans(E)-clopenthixol. Acta Psychiatr Scand 64, suppl. 294:70–77
Bolvig Hansen L, Elley J, Rosted Christensen T, Larsen N-E, Næstoft J, Hvidberg EF (1979) Plasma levels of perphenazine and its major metabolites during simultaneous treatment with anticholinergic drugs. Br J Clin Pharmacol 7:75–80
Bjørndal F, Aaes-Jørgensen T (1982) Manibehandling med cis(Z)-clopenthixol (Cisordinol®, Clopixol®). Nord Psychiatr Tidskr 36: 321–324
Bjørndal N, Bjerre M, Gerlach J, Kristjansen P, Magelund G, Oestrich I, Wæhrens J (1980) High dosage haloperidol therapy in chronic schizophrenic patients; a double-blind study of clinical response, side effects, serum haloperidol, and serum prolactin. Psychopharmacology 67:17–23
Eggert Hansen C, Rosted Christensen T, Elley J, Bolvig Hansen L, Kragh-Sørensen P, Larsen N-E, Næstoft J, Hvidberg EF (1976) Clinical pharmacokinetic studies of perphenazine. Br J Clin Pharmacol 3:915–923
Fredricson Overø K (1980) A specific fluorimetric method for assay of drug levels in serum of patients treated with clopenthixol decanoate injections. Acta Psychiatr Scand 61, suppl 279:92–103
Hansen LB, Larsen N-E (1977) Plasma concentrations of perphenazine and its sulphoxide metabolite during continuous oral treatment. Psychopharmacology 53:127–130
Jacobsson L, Knorring L von, Mattsson B, Mjørndal T, Oreland L, Perris C, Rapp W, Edenius B, Kettner B, Magnusson KE, Villemoes P (1976) Penfluridol and thiothixene dosage, plasma levels and changes in psychopathology. Int Pharmacopsychiatr 11:206–214
Jørgensen A, Fredrícson Overø K (1980) Clopenthixol and flupentixol depot preparations in outpatient schizophrenics. III. Serum levels. Acta Psychiatr Scand 61, suppl. 279:41–54
Khan A Rauf (1969) Some aspects of clopenthixol metabolism in rats and humans. Acta Pharmacol Toxicol 27:202–212
Kolakowska T, Wiles DH, Gelder MG, McNeilly AS (1976) Clinical significance of plasma chlorpromazine levels. Psychopharmacology 49:101–107
Muusze RG, Visser-Van der Weel AJ, Verzijden R, Oei TT (1977) Fluorimetrische bepaling on de dunne laag van de blodconcentratie van thioxanthenen (Sordinol en Fluanxol) na orale en intramusculaire (depot) toediening. Bulletin van de coördinatiecommissie biochemisch onderzoek van de sectie psychiatrische instituten van de nationale Ziekenhuisraad, 10, No 1:1–8
Petersen PV, Møller Nielsen I, Pedersen V, Jørgensen A, Lassen N (1977) Thioxanthenes. In: Usdin E, Forst IS (eds) Psychotherapeutic drugs. Marcel Dekker, Inc. New York, pp 827–867
Rivera-Calimlim L, Nasrallah HA, Strauss J, Lasagna L (1976) Clinical response and plasma levels: Effect of dose, dosage schedules, and drug interactions on plasma chlorpromazine levels. Am J Psychiatry 133:646–652
Rivera-Calimlim L, Gift R, Nasrallah HA, Wyatt RH, Lasagna L (1978) Low plasma levels of CPZ in patients chronically treated with neuroleptics. Commun Psychopharmacol 2:113–121
Stauning J, Kirk L, Jørgensen A (1979) Comparison of serum levels after intramuscular injections of 2% and 10% cis(Z)-flupentixol decanoate in Viscoleo to patients. Psychopharmacology 67:69–72
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Aaes-Jørgensen, A., Kirk, L., Petersen, E. et al. Serum concentrations of the isomers of clopenthixol and a metabolite in patients given cis(Z)-clopenthixol decanoate in Viscoleo. Psychopharmacology 81, 68–72 (1983). https://doi.org/10.1007/BF00439276
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00439276