Quercetin, kaempferol and myricetin inhibit CYP3A4
Genetic factors are known to make a great contribution to the variability in the CYP3A4
activity.,, Among CYP3A4
alleles identified, CYP3A4*1G (CYP3A4
SNP, rs2242480 [G/A]) is a well-known single-nucleotide polymorphism site with a high mutation frequency in Chinese population.,,, A synonymous G-A transition in exon 10 has been confirmed to be associated with CYP3A4
enzyme activity, leading to change in drug metabolism and distinct response to treatment among different patients.
Vladimir Maletic, MD, MS, explains: "Concomitant use of LATUDA with strong CYP3A4
inhibitors such as ketoconazole may increase the exposure of lurasidone compared to the use of LATUDA alone."
Suppose that a drug, X, is predominantly metabolized through CYP3A4
in humans and that it is concomitantly administered with another drug, Y, that is a strong inhibitor of CYP3A4
gene is located on chromosome 7q21.3-q22.1, is 27,592 base pairs (bp) long, and has 13 exons.
It is metabolized in the liver through CYP3A4
and CYP2D6 enzymes where it undergoes O-desmethylation and N-desmethylation as well as conjugation of O-desmethylated glucuronide derivatives.
The authors reported that significant pharmacokinetic interactions were more likely with drugs that were substrates for CYP3A4
and/or p-glycoprotein (ABCB1) and were less likely in studies that investigated SJW products with low-hyperforin content.
-- Consider the potential effects of increased plasma concentrations of midazolam or other benzodiazepines metabolized via CYP3A4
(alprazolam, triazolam) when administering with AKYNZEO.
Grapefruit inhibits cytochrome P450 3A4 (CYP3A4
), a key enzyme that breaks down many drugs in the small intestine and the liver.
As is known to all, CYP2C9 and CYP3A4
play an important role in the drug metabolism.
The risk of bleeding with rivaroxaban can be accentuated by the concomitant use of medications such as amiodarone  which compete for metabolism via the CYP3A4
hepatic pathway .
Both the systemic and pre-systemic drug dispositions are affected because of the location of CYP3A4
in the liver and small bowel.