The urine levels of cortisol and 6-beta-hydroxycortisol in 30 healthy children were determined with high performance liquid chromatography. The activity of cytochrome P450 isoenzyme CYP3A4 was estimated by the ratio of 6-beta-hydroxycortisol and cortisol. Differences in the CYP3A4 activity depended on the age sex. At the age of 4 to 9 years the value of the ratio was 9.21 +/- 0.67 which in fact was statistically higher than that in the children at the age of 0 to 3 years (p<0.001). In the female children at the age of 0 to 3 years the value of the isoenzyme CYP3A4 activity was actually lower (p<0,05) vs. the female children of the higher ages and the male children at the age of 0 to 3 years. The results are useful for further researches on improvement of drugs dosing and prevention of adverse reactions.
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Pharmaceutics
December 2024
Department of Clinical Pharmacy and Biopharmacy, Poznań University of Medical Sciences, Rokietnicka 3, 60-806 Poznań, Poland.
Background: Olaparib (OLA) and regorafenib (REG) are metabolized by the CYP3A4 isoenzyme of cytochrome P450. Both drugs are also substrates and inhibitors of the membrane transporters P-glycoprotein and BCRP. Therefore, the potential concomitant use of OLA and REG may result in clinically relevant drug-drug interactions.
View Article and Find Full Text PDFInt J Mol Sci
November 2024
Department of Comparative Biomedicine and Food Science, University of Padua, 35020 Padua, Italy.
Cytochrome P450 3A (CYP3A) enzymes catalyze the metabolism of a wide range of endogenous and exogenous compounds. Genetic variations in the 3 CYP3A isoforms (CYP3A28, CYP3A74, and CYP3A76) may influence their expression and activity, leading to inter-individual differences in xenobiotic metabolism. In domestic cattle, understanding how genetic variations modulate CYP3A activity is crucial for both its therapeutic implications (clinical efficacy and adverse drug effects) and food safety (residues in foodstuff).
View Article and Find Full Text PDFMetabolites
October 2024
Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, "Iuliu Hațieganu" University of Medicine and Pharmacy, 41 Victor Babeș Street, 400012 Cluj-Napoca, Romania.
: In psychiatric disorders, antipsychotics and antidepressant medication are often administered together. Aripiprazole, a third-generation antipsychotic drug, is extensively metabolized by CYP2D6 and CYP3A4 isoenzymes, while bupropion, used in depressive disorders, is known as a moderate or strong CYP2D6 enzyme inhibitor. This in vivo experiment aimed to assess the presence of a pharmacokinetic drug interaction between aripiprazole and bupropion and its magnitude on the systemic exposure of aripiprazole.
View Article and Find Full Text PDFFed Pract
August 2024
Joint Pathology Center, Silver Spring, Maryland.
Background: Paclitaxel is an antineoplastic agent used to treat breast, lung, endometrial, cervical, pancreatic, sarcoma, and thymoma cancer. However, drugs that induce, inhibit, or are substrates of cytochrome P450 (CYP) isoenzymes 2C8 or 3A4 may alter the metabolism of paclitaxel, potentially impacting its effectiveness. The purposes of this study are to provide an overview of paclitaxel use, identify potential drugs that interact with paclitaxel, and describe their clinical manifestations.
View Article and Find Full Text PDFBiomedicines
September 2024
Department of Pharmacology and Toxicology, University of Veterinary Medicine, Hungary István utca 2, H-1078 Budapest, Hungary.
Inhibitors of the serine protease furin have been widely studied as antimicrobial agents due to their ability to block the cleavage and activation of certain viral surface proteins and bacterial toxins. In this study, the antipseudomonal effects and safety profiles of the furin inhibitors MI-1851 and MI-2415 were assessed. Fluorescence quenching studies suggested no relevant binding of the compounds to human serum albumin and α-acid glycoprotein.
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