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The Strathprints institutional repository is a digital archive of University of Strathclyde research outputs.

Strathprints serves world leading Open Access research by the University of Strathclyde, including research by the Strathclyde Institute of Pharmacy and Biomedical Sciences (SIPBS), where research centres such as the Industrial Biotechnology Innovation Centre (IBioIC), the Cancer Research UK Formulation Unit, SeaBioTech and the Centre for Biophotonics are based.

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The effects of inducing agents on the metabolism of pentamidine by isolated rat hepatocytes

Atsriku, C. and Grant, M.H. and Skellern, G.G. and Watson, D.G. (2004) The effects of inducing agents on the metabolism of pentamidine by isolated rat hepatocytes. Toxicology, 194 (3). pp. 234-235. ISSN 0300-483X

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Abstract

Abstract of toxicology paper. The aromatic diamidine, pentamidine isethionate, has been used for over four decades for the chemotherapy of African human trypanosomiasis (sleeping sickness) in affected areas world-wide (Goa and Campoli-Richards, 1987). Pentamidine (P) is also used for the treatment of Pneumocyctis carinii pneumonia commonly associated with AIDS victims and over 45% of patients who receive the drug are known to suffer severe adverse reactions (Sands et al., 1985). However, emergence of drug resistant strains of trypanosomes has become a major barrier to the efficacy of trypanocidal diamidines (Peregrine, 1994). In view of poor prospects for new drug development, attempts to sustain efficacy of the drug have focussed on research into the causes of parasite drug resistance as well as drug toxicity. The inhibition or induction of hepatic drug metabolising enzymes following multiple drug therapy or exposure to environmental chemicals can alter the metabolism profile and pharmacokinetics of a given drug, leading to either a toxicological response or therapeutic failure. The aim of this study was to investigate the effects of two classical cytochrome P450 inducers, phenobarbitone (PB) and 3-methylcholanthrene (3MC), as well as a pyrethroid insecticide, deltamethrin (DM), on the metabolism of P by isolated rat hepatocytes.