Population Pharmacokinetic Modelling of Acetaminophen and Ibuprofen: the Influence of Body Composition, Formulation and Feeding in Healthy Adult Volunteers
ConclusionFat mass was an important covariate to describe acetaminophen and ibuprofen pharmacokinetics. The absorption half-lives of acetaminophen and ibuprofen were increased in fed states. The delay in absorption, quantified by a lag time, was protracted for both drugs. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - April 2, 2022 Category: Drugs & Pharmacology Source Type: research

Time for Isoniazid Pharmacogenomic-Guided Therapy of Tuberculosis Based on NAT2 Acetylation Profiles in India
AbstractTuberculosis (TB), caused by a bacterial pathogenMycobacterium tuberculosis, is a highly contagious infectious disease. India ranks top in TB burden among other countries in the world. The current treatment of TB in India includes isoniazid (INH) as the first-line drug, based on the “one dose fits all’’ concept. It is widely known that INH is not equally tolerated by all patients, as the metabolization process of INH is highly dependent on the acetylation profile of an individual based on the pharmacogenomic profile of theN-acetyltransferase (NAT2) gene. Also, several experimental studies in several TB endemi...
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 28, 2022 Category: Drugs & Pharmacology Source Type: research

Characterization of Correction Factors to Enable Assessment of Clinical Risk from In Vitro CYP3A4 Induction Data and Basic Drug-Drug Interaction Models
ConclusionsThese iterative improvements, which reduce the number of false positives, could aid regulatory recommendations and limit unnecessary clinical explorations into CYP3A induction.Graphical abstract (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 28, 2022 Category: Drugs & Pharmacology Source Type: research

Time for Isoniazid Pharmacogenomic-Guided Therapy of Tuberculosis Based on NAT2 Acetylation Profiles in India
AbstractTuberculosis (TB), caused by a bacterial pathogenMycobacterium tuberculosis, is a highly contagious infectious disease. India ranks top in TB burden among other countries in the world. The current treatment of TB in India includes isoniazid (INH) as the first-line drug, based on the “one dose fits all’’ concept. It is widely known that INH is not equally tolerated by all patients, as the metabolization process of INH is highly dependent on the acetylation profile of an individual based on the pharmacogenomic profile of theN-acetyltransferase (NAT2) gene. Also, several experimental studies in several TB endemi...
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 28, 2022 Category: Drugs & Pharmacology Source Type: research

Characterization of Correction Factors to Enable Assessment of Clinical Risk from In Vitro CYP3A4 Induction Data and Basic Drug-Drug Interaction Models
ConclusionsThese iterative improvements, which reduce the number of false positives, could aid regulatory recommendations and limit unnecessary clinical explorations into CYP3A induction.Graphical abstract (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 28, 2022 Category: Drugs & Pharmacology Source Type: research

Correction to: A Phase I Study to Evaluate the Pharmacokinetics and Safety of Lorlatinib in Adults with Mild, Moderate, and Severe Renal Impairment
(Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - March 8, 2022 Category: Drugs & Pharmacology Source Type: research

Assessment of the Effects of Inhibition or Induction of CYP2C19 and CYP2C9 Enzymes, or Inhibition of OAT3, on the Pharmacokinetics of Abrocitinib and Its Metabolites in Healthy Individuals
ConclusionsIt is important to consider the effects of DDIs on the abrocitinib active moiety when making dosing recommendations. Co-administration of strong CYP2C19/2C9 inhibitors or CYP inducers impacted exposure to the abrocitinib active moiety. A dose reduction by half is recommended if abrocitinib is co-administered with strong CYP2C19 inhibitors, whereas co-administration with strong CYP2C19/2C9 inducers is not recommended. No dose adjustment is required when abrocitinib is administered with OAT3 inhibitors.Clinical Trials Registration IDsNCT03634345, NCT03637790, NCT03937258 (Source: European Journal of Drug Metabolis...
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 28, 2022 Category: Drugs & Pharmacology Source Type: research

Correction to: Effects and Mechanism of Action of Panax notoginseng Saponins on the Pharmacokinetics of Warfarin
(Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 22, 2022 Category: Drugs & Pharmacology Source Type: research

Clinical Pharmacokinetics and Pharmacodynamics of Esaxerenone, a Novel Mineralocorticoid Receptor Antagonist: A Review
AbstractEsaxerenone is a selective, nonsteroidal, high-affinity mineralocorticoid receptor antagonist recently approved in Japan for the treatment of hypertension. It has high oral biovailability, a large volume of distribution, and is primarly metabolized in liver and excreted in bile. Esaxerenone is an efficient antihypertensive, whether given alone or as add-on therapy. The antihypertensive effect is accompanied by renoprotective action, which is being further investigated in current clinical trials. Due to its relatively long half-life and high affinity for the mineralocorticoid receptor, esaxerenone is administered on...
Source: European Journal of Drug Metabolism and Pharmacokinetics - February 21, 2022 Category: Drugs & Pharmacology Source Type: research