The main part of human cytochrome P450-dependent drug metabolism is carried out by polymorphic enzymes that can cause abolished, quantitatively or qualitatively altered, or enhanced drug metabolism. Ultrarapid metabolism is due to stable duplication, multiduplication, or amplification of active genes. Several examples exist where subjects carrying certain alleles suffer from a lack of drug effi...

BACKGROUND Elimination of rosiglitazone in humans is via hepatic metabolism. The existing studies suggest that CYP2C8 is the major enzyme responsible, with a minor contribution from CYP2C9; however, other studies suggest the involvement of additional cytochrome P450 enzymes and metabolic pathways. Thus a full picture of rosiglitazone metabolism is unclear. OBJECTIVE This study aimed to improv...

The contribution of fetal metabolism to drug disposition in pregnancy is poorly understood. With maternal administration of morphine, like many drugs, steady-state concentrations in fetal plasma are less than in maternal plasma. The contribution of fetal metabolism to this difference is unknown. Morphine was used as a model drug to test the hypothesis that fetal metabolism contributes significa...

The cytochrome P450 (CYP) gene superfamily comprises a large group of hemoproteins with diverse functions in steroid, lipid, and xenobiotic metabolism. The human genome is estimated to contain 57 genes that encode functional CYP proteins, a number of which are important for the metabolism of foreign chemicals, including carcinogens and most therapeutic drugs. Given that metabolic interactions a...

Endotoxin-resistant C3H/HeJ mice were used to test the hypothesis that a macrophage product, possibly interleukin-1, might mediate the depression of liver cytochrome P-450-dependent drug metabolism in endotoxin-treated mice. Depression of liver drug metabolism by endotoxin was observed in normal mice (C3H/HeN) but not in C3H/HeJ mice. Serum transfer experiments demonstrated that a serum factor ...

Buccal patches are the types of formulations in which drug is administered through buccal mucosa. these or placed between gums and for pharmacological response. The main advantage there no first pass metabolism takes place easily absorb systemic circulation themucosa .the objective this delivery system to elevate increase bioavailability drug. review informs about steps involve preparation patc...

Purpose: Remdesivir, a drug originally developed against Ebola virus, is currently recommended for patients hospitalized with coronavirus disease of 2019 (COVID-19). In spite United States Food and Drug Administration’s recent assent remdesivir as the only approved agent COVID-19, there limited information available about physicochemical, metabolism, transport, pharmacokinetic (PK), drug-drug i...

propranolol (pl), a non-selective beta-blocker, is a cardiovascular drug widely used to treat hypertension. the present study was concerned with assessing the cytogenetic effects of this drug on chinese hamster ovary (cho) cell line. mtt assay was then carried out to determine the cytotoxicity index (ic50) of the drug. the ic50 value of pl was 0.43±0.02 mm. to investigate the clastogenic effect...

Azithromycin (AZ) is an azalide macrolide antibiotic that frequently employed for treating bacterial skin infections. It suffers from limited oral bioavailability, which results incomplete absorption or extensive first-pass metabolism. Therefore, preparing azithromycin formulations topical administration highly recommended to avoid metabolism and boost the concentration of drug on skin. The obj...