caa a22 4500 465737714 CHVBK 20180323111759.0 cr unu---uuuuu 170327e19900501xx s 000 0 eng 10.1007/BF02253726 doi (NATIONALLICENCE)springer-10.1007/BF02253726 Reversible metabolism of haloperidol and reduced haloperidol in Chinese schizophrenic patients [Elektronische Daten] [Michael Jann, Y. Francis Lam, Wen-Ho Chang] Haloperidol disposition has been associated with reversible metabolism: it is reversibly reduced to its metabolite, reduced haloperidol, which has less pharmacologic activity than the parent compound. To characterize the interconversion process, six healthy male schizophrenics were administered a single dose of 10 mg haloperidol or reduced haloperidol in a randomized crossover manner. Using a general pharmacokinetic model for the interconversion process, the clearances of haloperidol and reduced haloperidol are 1.15±0.32 l/h/kg and 0.76±54 l/h/kg, respectively. These clearances are similar to that obtained by the usual mammillary model analysis. With a single 10 mg dose administration of either drug, about 23% of the biotransformation of haloperidol involves the reduction pathway. Back conversion from the reduced metabolite to the parent drug through oxidation contributes even less to the total biotransformation of reduced haloperidol. This action of interconversion or saturation under chronic drug administration is unknown. Reversible metabolism of haloperidol could partially account for the wide therapeutic range for haloperidol as reported in the literature. Springer-Verlag, 1990 Haloperidol nationallicence Reduced haloperidol nationallicence Interconversion nationallicence Reversible metabolism nationallicence Jann Michael Mercer University Southern School of Pharmacy, USA aut Francis Lam Y. Department of Pharmacology, UTHSCSA and Clinical Assistant Professor of Pharmacy, College of Pharmacy, The University of Texas at Austin, USA aut Chang Wen-Ho Laboratory of Biological Psychiatry, National Defense Medical Center, and Taipei City Psychiatric Center, Taiwan, Republic of China aut Psychopharmacology Springer-Verlag 101/1(1990-05-01), 107-111 0033-3158 101:1<107 1990 101 213 https://doi.org/10.1007/BF02253726 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF02253726 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Jann Michael Mercer University Southern School of Pharmacy, USA aut NATIONALLICENCE 700 1- Francis Lam Y. Department of Pharmacology, UTHSCSA and Clinical Assistant Professor of Pharmacy, College of Pharmacy, The University of Texas at Austin, USA aut NATIONALLICENCE 700 1- Chang Wen-Ho Laboratory of Biological Psychiatry, National Defense Medical Center, and Taipei City Psychiatric Center, Taiwan, Republic of China aut NATIONALLICENCE 773 0- Psychopharmacology Springer-Verlag 101/1(1990-05-01), 107-111 0033-3158 101:1<107 1990 101 213 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer