Current Drug Metabolism - Volume 23, Issue 1, 2022

Dosing time-dependency of pharmacokinetics (or chronopharmacokinetics) has been long recognized. Studies in recent years have revealed that daily rhythmicity in expression of drug-metabolizing enzymes and transporters (DMETs) are key factors determining chronopharmacokinetics. In this article, we briefly summarize current knowledge with respect to circadian mechanisms of DMETs and discuss how rhythmic DMETs are tr Read More

Background: The characteristics of pharmacokinetics and the activity and expression of drugmetabolizing enzymes and transporters significantly change under a high-altitude hypoxic environment. Gut microbiota is an important factor affecting the metabolism of drugs through direct or indirect effects, changing the bioavailability, biological activity, or toxicity of drugs and further affecting the efficacy and safety of drugs i Read More

Platycodonis Radix (Jiegeng), the dried root of Platycodon grandiflorum, is a traditional herb used as both medicine and food. Its clinical application for the treatment of cough, phlegm, sore throat, pulmonary and respiratory diseases has been thousands of years in China. Platycodin D is the main active ingredient in Platycodonis Radix, which belongs to the family of pentacyclic triterpenoid saponins because it contains an ole Read More

Background: Scutebarbatine A is a new neo-Clerodane Diterpenoid Alkaloids from Scutellaria barbata, which has many pharmacological effects, such as anti-tumor, antibacterial, and anti-inflammatory. However, there are no studies on the metabolism of Scutebarbatine A. Objective: The objective of this study is to explore the metabolism of Scutebarbatine A in the body, the bile, plasma, urine, and feces samples of rats af Read More

Background: Hypericin is the main active ingredient of St. John’s wort, a Chinese herb commonly used for treating depression. Previous studies shown that hypericin can strongly inhibit human cytochrome P450 (CYP) enzyme activities; however, its potential interactions that inhibit human carboxylesterases 2 (hCE2) are unclear. Purpose: This study aimed to investigate the inhibitory effect of hypericin on hCE2. Methods: Th Read More

Background: The effectiveness and side effects of dexmedetomidine (DEX) in combination with midazolam and propofol have not been comparatively studied in a single clinical trial as sedative agents to general anesthesia before. Objective: The objective of this study is to compare intra and post-operative sedation between DEX-Midazolam and DEX-Propofol in patients who underwent major abdominal surgery on th Read More

Objective: This study was aimed to investigate the effectiveness of dexmedetomidine (DEX) on improving the level of pain and disability to find out the possible correlation between psychological factors with pain management satisfaction and physical function in patients with femoral neck fractures. Methods: One hundred twenty-four adult patients with stable femoral neck fractures (type I and II, Garden classification) who Read More

Background: Glucuronidation is an important metabolic pathway of clozapine (CLZ), but the impact of various uridine 5'diphospho-glucuronosyltransferases (UGT) polymorphisms on the exposure and metabolism of CLZ in vivo is unclear. Objective: The objective of this study was to investigate the impact of UGT2B haplotype and UGT1A4*3 allele variants on the formation of CLZ glucuronide metabolites (5N- and N Read More

Background: Remdesivir (GS-5734) has emerged as a promising drug during the challenging times of COVID-19 pandemic. Being a prodrug, it undergoes several metabolic reactions before converting to its active triphosphate metabolite. It is important to establish the atomic level details and explore the energy profile of the prodrug to drug conversion process. Methods: In this work, Density Functional Theory (DFT) calcula Read More

Background: HER2 over-expression plays a crucial role in the cancer treatment protocol. This study evaluates the effectiveness of organic anion and cation transport inhibitors and substrate on the tumor uptake of 99mTc- HYNIC-(Ser)3-LTVPWY radiotracer in SKOV-3 tumor-bearing nude mice. Methods: Before the injection of the radiolabeled peptide, SKOV-3 tumor-bearing nude mice were treated with furosemide, cimetidine, p Read More