Current Drug Metabolism - Volume 22, Issue 5, 2021

Background: Hydroxymethyl glutaryl-CoA (HMG-CoA) reductase inhibitors (Statins) are used to treat dyslipidemia. Generally, the statins are the substrates of CYP enzymes, P-glycoprotein (P-gp), and organic anion transporting polypeptides transporters (OATP1B1). Objective: This review article focuses on the clinical significance of statins, and their interactions in real practice. Methods: The databases like Medline/PubMed Read More

Background: Graft acceptance against immunity is one of the major challenges in solid organ transplant. Immunosuppressive medications have effectively improved the post-transplantation outcome however, it has its own limitations. Genetic polymorphisms in drug-metabolizing enzymes have been identified as the potential targets in developing a pharmacogenetic strategy, to individualize drug dose and also in preventing Read More

Background: The role of multidrug resistance-associated protein 3 (Mrp3) in the transport of bile acid (BA) in drug-induced cholestasis has not been well studied. Objective: In this study, wild type and Mrp3 knockout (Mrp3-/-) mice under normal physiological and lithocholic acid (LCA)-induced cholestatic conditions were employed to investigate the role of Mrp3 in BA transport. Methods: The levels of BA in serum, liver, gallbladd Read More

Background: Fixed-dose combination of artemisinin and naphthoquine (NQ) is a new artemisinin- based combination therapy for the treatment of uncomplicated Plasmodium falciparum. NQ absorption has been reported to be affected by food in humans. Objectives: The effect of gastric pH on NQ pharmacokinetics and antiplasmodial activity was investigated. Methods: The pharmacokinetic profiles of NQ were studied in healthy Read More

Background: Dermorphin is a heptapeptide with an analgesic potential higher than morphine that does not present the same risk for the development of tolerance. These pharmacological features make dermorphin a potential doping agent in competitive sports and it is already prohibited for racehorses. For athletes, the development of an efficient strategy to monitor for its abuse necessitates an investigation of Read More

Background: Clinical mastitis is an important production disease of dairy animals, causing significant economic losses. Objective: Disposition kinetics of ceftriaxone was conducted in healthy lactating and staphylococcal mastitic crossbred cows in field condition following single-dose intravenous administration of only ceftriaxone. Methods: A single dose of ceftriaxone at 20 mg kg-1 body weight was administered intravenously thr Read More

Background: Both clotrimazole and ketoconazole have been verified to have an inhibitory effect on CYP3A4. hCE2 is an enzyme closely related to the side effects of several anti-cancer drugs. However, the interactions between hCE2, clotrimazole, and ketoconazole remain unclear. Objective: The objective of this study was to investigate and compare the inhibition behaviors of the two antifungal agents, ketoconazole and clotri Read More

Background: Aprocitentan is an orally active, dual endothelin receptor antagonist that may offer a new therapeutic option for the treatment of difficult-to-control hypertension. Objective: To investigate safety, tolerability, mass balance, absorption, distribution, metabolism, and excretion of aprocitentan. Methods: In this single-center, open-label study, a single oral dose of 25 mg containing 3.7 MBq of 14C-radiolabeled aproci Read More