CYP3A4 induction by xenobiotics: biochemistry, experimental methods and impact on drug discovery and development

G Luo, T Guenthner, LS Gan… - Current drug …, 2004 - ingentaconnect.com
Cytochrome P450 3A4 (CYP3A4), an enzyme that is highly expressed in the human liver
and small intestine, plays a major role in the metabolism of a large variety of xenobiotics …

Drug–drug interactions, effectiveness, and safety of hormonal contraceptives in women living with HIV

KK Scarsi, KM Darin, CA Chappell, SM Nitz… - Drug safety, 2016 - Springer
Family planning options, including hormonal contraceptives, are essential for improving
reproductive health among the more than 17 million women living with HIV worldwide. For …

Differentiation of intestinal and hepatic cytochrome P450 3A activity with use of midazolam as an in vivo probe: effect of ketoconazole

SM Tsunoda, RL Velez, LL von Moltke… - Clinical …, 1999 - Wiley Online Library
Background The cytochrome P450 3A (CYP3A) isoforms are responsible for the metabolism
of a majority of therapeutic compounds, and they are abundant in the intestine and liver …

P-glycoprotein (P-gp/MDR1)-Mediated Efflux of Sex-Steroid Hormones and Modulation of P-gp Expression In Vitro

WY Kim, LZ Benet - Pharmaceutical research, 2004 - Springer
Purpose. To determine whether female sex-steroid hormones and their metabolites can
modulate P-glycoprotein (P-gp) expression and catalytic activity and to investigate P-gp …

Hormonal regulation of hepatic drug‐metabolizing enzyme activity during adolescence

MJ Kennedy - Clinical Pharmacology & Therapeutics, 2008 - Wiley Online Library
Activities of drug‐metabolizing enzymes (DMEs) are known to change throughout the course
of physical and sexual maturation, with the greatest variability noted during infancy and …

Drug interactions between antiretrovirals and hormonal contraceptives

A Tseng, C Hills-Nieminen - Expert opinion on drug metabolism & …, 2013 - Taylor & Francis
Introduction: Significant advances in antiretroviral therapy have transformed HIV into a
chronic manageable disease, and millions of women living with HIV now have the …

Depo‐medroxyprogesterone in women on antiretroviral therapy: effective contraception and lack of clinically significant interactions

SE Cohn, JG Park, DH Watts, A Stek… - Clinical …, 2007 - Wiley Online Library
We conducted an open‐label, steady‐state pharmacokinetic (PK) study of drug interactions
among HIV‐infected women treated with depo‐medroxyprogesterone acetate (DMPA) while …

Effect of a triphasic oral contraceptive on drug‐metabolizing enzyme activity as measured by the validated Cooperstown 5+ 1 cocktail

T Shelepova, AN Nafziger, J Victory… - The Journal of …, 2005 - Wiley Online Library
The effects of a common oral contraceptive preparation on the activity of 7 drug‐
metabolizing enzymes were investigated using the validated Cooperstown 5+ 1 Cocktail. In …

The effect of atorvastatin treatment on serum oxysterol concentrations and cytochrome P450 3A4 activity

J Hukkanen, J Puurunen, T Hyötyläinen… - British Journal of …, 2015 - Wiley Online Library
Aims Atorvastatin is known to both inhibit and induce the cytochrome P450 3A4 (CYP3A4)
enzyme in vitro. Some clinical studies indicate that atorvastatin inhibits CYP3A4 but there …

Oral contraceptives

JR Oesterheld, K Cozza, NB Sandson - Psychosomatics, 2008 - Elsevier
Nearly 50 years ago, the introduction of Enovid©(norethynodrel 10 μg and mestranol 150
μg), which provided convenient and reliable contraception, revolutionized birth control …