Fluphenazine Pharmacokinetics and Therapeutic Response

Overview

Journal Psychopharmacology (Berl)

Specialty Pharmacology

Date 1981 Jan 1

PMID 6787637

Citations 15

Authors

M W Dysken

J I Javaid

S S Chang

C Schaffer

A Shahid

J M Davis

Affiliations

Soon will be listed here.

Abstract

We conducted a double-blind study of therapeutic outcome versus mean steady-state levels in 29 newly admitted schizophrenic and schizoaffective patients who were treated with a constant dose of fluphenazine HCI over a 2-week period. both an upper and lower end of the therapeutic window were suggested by three nonresponders whose plasma levels were above 2.8 ng per ml and by two nonresponders and one partial responder whose plasma levels were below 0.2 ng per ml. The mean terminal half-life of fluphenazine (+ or - SD) was 16.4 + or - 13.3 h. We found that concomitant use of benztropn mesylate during the initial 4 weeks of fluphenazine treatment did not significantly alter fluphenazine plasma levels.

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References

KOLAKOWSKA T, Wiles D, Gelder M, McNeilly A . Clinical significance of plasma chlorpromazine levels. II. Plasma levels of the drug, some of its metabolites and prolactin in patients receiving long-term phenothiazine treatment. Psychopharmacology (Berl). 1976; 49(1):101-7. View

Nasrallah H, Strauss J, Lasagna L . Clinical response and plasma levels: effect of dose, dosage schedules, and drug interactions on plasma chlorpromazine levels. Am J Psychiatry. 1976; 133(6):646-52. DOI: 10.1176/ajp.133.6.646. View

Simpson G, Cooper T, Bark N, Sud I, Lee J . Effect of antiparkinsonian medication on plasma levels of chlorpromazine. Arch Gen Psychiatry. 1980; 37(2):205-8. DOI: 10.1001/archpsyc.1980.01780150095010. View

Garver D, Davis J, Dekirmenjian H, JONES F, Casper R, HARASZTI J . Pharmacokinetics of red blood cell phenothiazine and clinical effects. Acute dystonic reactions. Arch Gen Psychiatry. 1976; 33(7):862-6. DOI: 10.1001/archpsyc.1976.01770070092011. View

Cooper T . Plasma level monitoring of antipsychotic drugs. Clin Pharmacokinet. 1978; 3(1):14-38. DOI: 10.2165/00003088-197803010-00002. View

Dekirmenjian H, Javaid J, Duslak B, Davis J . Determination of antipsychotic drugs by gas-liquid chromatography with a nitrogen detector using a simple acetylation technique. J Chromatogr. 1978; 160(1):291-6. DOI: 10.1016/s0021-9673(00)91810-7. View

Casper R, Garver D, Dekirmenjian H, Chang S, Davis J . Phenothiazine levels in plasma and red blood cells. Their relationship to clinical improvement in schizophrenia. Arch Gen Psychiatry. 1980; 37(3):301-5. DOI: 10.1001/archpsyc.1980.01780160071008. View

Lader M . Monitoring plasma concentrations of neuroleptics. Pharmakopsychiatr Neuropsychopharmakol. 1976; 9(4):170-7. DOI: 10.1055/s-0028-1094491. View

Curry S, Whelpton R, De Schepper P, Vranckx S, Schiff A . Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man. Br J Clin Pharmacol. 1979; 7(4):325-31. PMC: 1429660. DOI: 10.1111/j.1365-2125.1979.tb00941.x. View

10.

Sakalis G, Chan T, Sathananthan G, Schooler N, Goldberg S, Gershon S . Relationships among clinical response, extrapyramidal syndrome and plasma chlorpromazine and metabolite ratios. Commun Psychopharmacol. 1977; 1(2):157-66. View

11.

Casey J, Hollister L, KLETT C, LASKY J, Caffey Jr E . Combined drug therapy of chronic schizophrenics. Controlled evaluation of placebo, dextro-amphetamine, imipiramine, isocarboxazid and trifluoperazine added to maintenance doses of chlorpromazine. Am J Psychiatry. 1961; 117:997-1003. DOI: 10.1176/ajp.117.11.997. View

12.

Sakalis G, Chan T, Gershon S, Park S . The possible role of metabolites in therapeutic response to chlorpromazine treatment. Psychopharmacologia. 1973; 32(3):279-84. DOI: 10.1007/BF00422150. View

13.

Casey J, LASKY J, KLETT C, Hollister L . Treatment of schizophrenic reactions with phenothiazine derivatives. A comparative study of chlorpromazine, triflupromazine, mepazine, prochlorperazine, perphenazine, and phenobarbital. Am J Psychiatry. 1960; 117:97-105. DOI: 10.1176/ajp.117.2.97. View

14.

Javaid J, Dekirmenjian H, Dysken M, Davis J . Measurement of fluphenazine by gas chromatography in human plasma and red blood cells. Adv Biochem Psychopharmacol. 1980; 24:585-9. View

15.

Smith R, Crayton J, Dekirmenjian H, Klass D, Davis J . Blood levels of neuroleptic drugs in nonresponding chronic schizophrenic patients. Arch Gen Psychiatry. 1979; 36(5):579-84. DOI: 10.1001/archpsyc.1979.01780050089011. View

16.

Hammar C, Holmstedt B, RYHAGE R . Mass fragmentography. Identification of chlorpromazine and its metabolites in human blood by a new method. Anal Biochem. 1968; 25(1):532-48. DOI: 10.1016/0003-2697(68)90131-0. View

17.

Garver D, Dekirmenjian H, Davis J, Casper R, Ericksen S . Neuroleptic drug levels and therapeutic response: preliminary observations with red blood cell bound butaperazine. Am J Psychiatry. 1977; 134(3):304-7. DOI: 10.1176/ajp.134.3.304. View

18.

Phillipson O, McKeown J, Baker J, Healey A . Correlation between plasma chlorpromazine and its metabolites and clinical ratings in patients with acute relapse of schizophrenic and paranoid psychosis. Br J Psychiatry. 1977; 131:172-84. DOI: 10.1192/bjp.131.2.172. View

19.

Curry S . Determination of nanogram quantities of chlorpromazine and some of its metabolites in plasma using gas-liquid chromatography with an electron capture detector. Anal Chem. 1968; 40(8):1251-5. DOI: 10.1021/ac60264a031. View

20.

Mackay A, Healey A, Baker J . The relationship of plasma chlorpromazine to its 7-hydroxy and sulphoxide metabolites in a large population of chronic schizophrenics. Br J Clin Pharmacol. 2012; 1(5):425-30. PMC: 1402470. DOI: 10.1111/j.1365-2125.1974.tb00281.x. View