Zidovudine azido-reductase in human liver microsomes: activation by ethacrynic acid, dipyridamole, and indomethacin and inhibition by human immunodeficiency virus protease inhibitors.

AZT (zidovudine, 3'-azido-3'-deoxythymidine), although metabolized primarily to AZT-glucuronide, is also metabolized to 3'-amino-3'-deoxythmidine (AMT) by reduction of the azide to an amine. The formation of the myelotoxic metabolite AMT has not been well characterized, but inhibition of AMT formation would be of therapeutic benefit. The aim of this study was to identify compounds that inhibit AMT formation.

Inhibition of haloperidol reduction by non-steroidal anti-inflammatory drugs in human liver cytosol.

A thorough knowledge of drug-drug interactions is crucial as the practice of multiple drug therapy escalates. In vitro studies using human liver enzymes are a valuable and non-invasive tool for predicting potential drug interactions in vivo. 1.

Effects of perfusate flow rate on measured blood volume, disse space, intracellular water space, and drug extraction in the perfused rat liver preparation: characterization by the multiple indicator dilution technique.

The effect of hepatic blood flow on the elimination of several highly cleared substrates was studied in the once-through perfused rat liver preparation. A constant and low input concentration of ethanol (2.0 mM), [14C]-phenacetin and [3H]-acetaminophen (0.

Relevance of plasma, glandular and urinary kallikrein in renal hypertrophy in streptozotocin-diabetic rats.

The relevance of plasma, glandular and renal kallikrein as an intrarenal hemodynamic regulator, in renal hypertrophy, in 1-5 weeks streptozotocin diabetic rats has been investigated. The fasting plasma glandular kallikrein level significantly decreased with increasing duration of diabetes (p less than 0.05).

Absorption and metabolism of acetaminophen by the in situ perfused rat small intestine preparation.

The in situ perfused rat small intestine preparation was used to examine the extents of segmental absorption and metabolism of acetaminophen (A). Additionally, the preparation was employed to investigate any intestinal excretion of A and its conjugates from the circulation to the intestinal lumen. In this preparation, blood perfusate (300 ml) recirculated the intestinal preparation at 7.