Abstract
1 Fluphenazine (1,2-ethanol 14C) was administered to seven human subjects as the dihydrochloride and as the enanthate and decanoate esters. 2 The subjects had previously been treated with fluphenazine injections for at least 6 months. 3 Fluphenazine was separated from its radioactive metabolites by selective solvent extraction. Plasma concentrations were measured for up to 21 days after dosing. 4 The preparations showed differences in peak concentrations, times of the peaks and half-times of the elimination phase. The longest half-times occurred with the decanoate and the shortest with the dihydrochloride. 5 It is postulated that the differences in kinetics relate principally to the release of the compound from the site of injection. 6 There was no evidence for presence of the esters in plasma, urine or faeces.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Adamson L., Curry S. H., Bridges P. K., Firestone A. F., Lavin N. I., Lewis D. M., Watson R. D., Xavier C. M., Anderson J. A. Fluphenazine decanoate trial in chronic in-patient schizophrenics failing to absorb oral chlorpromazine. Dis Nerv Syst. 1973 Apr-May;34(4):181–191. [PubMed] [Google Scholar]
- Curry S. H., Adamson L. Double-blind trial of fluphenazine decanoate. Lancet. 1972 Sep 9;2(7776):543–544. doi: 10.1016/s0140-6736(72)91943-5. [DOI] [PubMed] [Google Scholar]
- Curry S. H., D'Mello A., Mould G. P. Destruction of chlorpromazine during absorption in the rat in vivo and in vitro. Br J Pharmacol. 1971 Jul;42(3):403–411. doi: 10.1111/j.1476-5381.1971.tb07125.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Dreyfuss J., Ross J. J., Jr, Schreiber E. C. Excretion and biotransformation of the enanthate ester of fluphenazine- 14 C by the dog. J Pharm Sci. 1971 Jun;60(6):829–833. doi: 10.1002/jps.2600600606. [DOI] [PubMed] [Google Scholar]
- Johansson R., Borg K. O., Gabrielsson M. Determination of fluphenazine in plasma by ion-pair partition chromatography. Acta Pharm Suec. 1976;13(3):193–200. [PubMed] [Google Scholar]
- Jorgensen A., Gottfries C. G. Pharmacokinetic studies on flupenthixol and flupenthixol decanoate in man using tritium labelled compounds. Psychopharmacologia. 1972;27(1):1–10. doi: 10.1007/BF00421951. [DOI] [PubMed] [Google Scholar]
- Larsen N. E., Naestoft J. Determination of perphenazine and fluphenazine in whole blood by gas chromatography. Med Lab Technol. 1973 Apr;30(2):129–132. [PubMed] [Google Scholar]
- Schreiber E. C., Grozier M. L. [Metabolic studies with long-acting compounds]. Therapie. 1973 May-Jun;28(3):441–458. [PubMed] [Google Scholar]
- Smulevitch A. B., Minsker E. I., Mazayeva N. A., Volkova R. P., Lukanina S. K. The problem of clinical activity of long-acting neuroleptics. Compr Psychiatry. 1973 May-Jun;14(3):227–233. doi: 10.1016/s0010-440x(73)80015-x. [DOI] [PubMed] [Google Scholar]
- Whelpton R., Curry S. H. Methods for study of fluphenazine kinetics in man. J Pharm Pharmacol. 1976 Dec;28(12):869–873. doi: 10.1111/j.2042-7158.1976.tb04082.x. [DOI] [PubMed] [Google Scholar]
- Wiles D. H., Franklin M. Radioimmunoassay for fluphenazine in human plasma. Br J Clin Pharmacol. 1978 Mar;5(3):265–268. doi: 10.1111/j.1365-2125.1978.tb01636.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- YALE H. L., SOWINSKI F., COHEN A. I. ESTERS OF 4-(3-(2-(TRIFLUOROMETHYL)PHENOTHIAZIN-10-YL)PROPYL)-1-PIPERAZINEUETHANOL AS LONG-ACTING TRANQUILIZING AGENTS. SYNTHESIS OF 4-(3-(2-(TRIFLUOROMETHYL)-PHENOTHIAZIN-10-YL)PROPYL)-1-PIPERAZINEUETHANOL-ETHYL-C14 AND ITS ESTER WITH HEPTANOIC ACID. 3. J Med Chem. 1963 Jul;6:347–350. doi: 10.1021/jm00340a002. [DOI] [PubMed] [Google Scholar]