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Abstract

Hydroxylation of pentamidine by rat liver microsomes.

B J Berger, V V Reddy, S T Le, R J Lombardy, J E Hall and R R Tidwell
Journal of Pharmacology and Experimental Therapeutics March 1991, 256 (3) 883-889;
B J Berger
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V V Reddy
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S T Le
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R J Lombardy
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J E Hall
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R R Tidwell
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Abstract

The antiprotozoal/antifungal drug pentamidine [1,5-bis(4-amidinophenoxy)pentane] has been recently shown to be metabolized by rat liver fractions to at least six putative metabolites as detected by high-performance liquid chromatography. Two minor metabolites have been previously identified as N-hydroxypentamidine and N,N'-dihydroxypentamidine. In this study, the two major microsomal metabolites have been identified as the 2-pentanol and 3-pentanol analogs of pentamidine [1,5-di(4-amidinophenoxy)-2-pentanol; and 1,5-bis(4-amidinophenoxy)-3-pentanol]. As well, a seventh putative metabolite has been discovered and identified as para-hydroxybenzamidine, a fragment of the original drug. Whereas the cytochromes P-450 have been demonstrated as the enzyme system responsible for pentamidine metabolism, hydroxylation of the drug was not inducible by phenobarbital, beta-naphthoflavone, clofibrate, isosafrole, pregnenolone-16 alpha-carbonitrile, ethanol or pentamidine pretreatment of rats. The kinetics of the production of the two major microsomal metabolites has been determined as Km = 56 +/- 19 microM and Vmax = 126 +/- 21 pmol/min/mg microsomal protein for the 2-pentanol analog, and Km = 28 +/- 0.28 microM and Vmax = 195 +/- 2.4 pmol/min/mg microsomal protein for the 3-pentanol analog. Therefore, the mixed-function oxidases readily convert pentamidine to hydroxylated metabolites, but exactly which isozyme(s) of cytochrome P-450 is responsible is not clear.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 256, Issue 3
1 Mar 1991
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Abstract

Hydroxylation of pentamidine by rat liver microsomes.

B J Berger, V V Reddy, S T Le, R J Lombardy, J E Hall and R R Tidwell
Journal of Pharmacology and Experimental Therapeutics March 1, 1991, 256 (3) 883-889;

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Abstract

Hydroxylation of pentamidine by rat liver microsomes.

B J Berger, V V Reddy, S T Le, R J Lombardy, J E Hall and R R Tidwell
Journal of Pharmacology and Experimental Therapeutics March 1, 1991, 256 (3) 883-889;
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