Publications by authors named "Nadia O Bamfo"
Article Synopsis
- The study examined how the antiretroviral drug efavirenz affects the metabolism of bupropion (BUP) and its active metabolites, focusing on the role of genetic factors.
- Researchers conducted a three-phase study with healthy volunteers, comparing BUP alone, BUP with efavirenz, and BUP after chronic efavirenz treatment.
- Results indicated that efavirenz produces both acute inhibition and chronic induction of the enzyme CYP2B6, affecting BUP levels in a genotype-dependent manner, suggesting implications for personalized medicine and drug interactions.
Striking stereoselective disposition of the antidepressant and smoking cessation aid bupropion (BUP) and its active metabolites observed clinically influence patients' response to BUP therapy and its clinically important drug-drug interactions (DDI) with CYP2D6 substrates. However, understanding of the biochemical mechanisms responsible is incomplete. This study comprehensively examined hepatic and extrahepatic stereoselective metabolism of BUP Racemic-, R-, and S-BUP were incubated separately with pooled cellular fractions of human liver [microsomes (HLMs), S9 fractions (HLS9s), and cytosols (HLCs)] and intestinal [microsomes (HIMs), S9 fractions (HIS9s), and cytosols (HICs)] and cofactors.
View Article and Find Full Text PDFPurpose: A dataset of fraction excreted unchanged in the urine (fe) values was developed and used to evaluate the ability of preclinical animal species to predict high urinary excretion, and corresponding poor metabolism, in humans.
Methods: A literature review of fe values in rats, dogs, and monkeys was conducted for all Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3 and 4 drugs (n=352) and a set of Class 1 and 2 drugs (n=80). The final dataset consisted of 202 total fe values for 135 unique drugs.