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1576 n/a Ensembl ENSG00000160868 n/a UniProt P08684 n/a RefSeq (mRNA) NM_001202855 NM_001202856 NM_001202857 NM_017460 n/a RefSeq (protein) NP_001189784 NP_059488 n/a Location (UCSC) Chr 7: 99.76 – 99.78 Mb n/a PubMed search n/a Wikidata View/Edit Human Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14.13.97) is an important enzyme in the body, mainly found in the liver and in the intestine ...
Examples of drugs metabolized by CYP3A4 are statins (used to lower cholesterol levels), benzodiazepines (used to treat anxiety and insomnia), calcium channel blockers (used to treat high blood pressure), etc. By measuring 6β-hydroxycortisol levels in clinical trials, researchers can assess whether certain drugs affect the activity CYP3A4 which ...
"Indiana University Department of Medicine Clinical Pharmacology Drug Interactions Flockhart Table ™". "INHIBITORS, INDUCERS AND SUBSTRATES OF CYTOCHROME P450 ISOZYMES". "The Life Raft Group: Long List of Inhibitors and Inducers of CYP3A4 and CYP2D6". "DRUGBANK Online: Cytochrome P-450 Enzyme Inhibitors".
Many substrates for CYP3A4 are drugs with a narrow therapeutic index, such as amiodarone [10] or carbamazepine. [11] Because these drugs are metabolized by CYP3A4, the mean plasma levels of these drugs may increase because of enzyme inhibition or decrease because of enzyme induction.
Noroxycodone is the major metabolite of the opioid analgesic oxycodone. [1] [2] [3] It is formed from oxycodone in the liver via N-demethylation predominantly by CYP3A4.[1] [2] [3] Noroxycodone binds to and activates the μ-opioid receptor (MOR) similarly to oxycodone, although with one-third of the affinity of oxycodone and 5- to 10-fold lower activational potency.
Rifapentine induces metabolism by CYP3A4, CYP2C8 and CYP2C9 enzymes. It may be necessary to adjust the dosage of drugs metabolized by these enzymes if they are taken with rifapentine. Examples of drugs that may be affected by rifapentine include warfarin , propranolol , digoxin , protease inhibitors and birth control pills .
Nefazodone is a potent inhibitor of CYP3A4, and may interact adversely with many commonly used medications that are metabolized by CYP3A4. [ 26 ] [ 27 ] [ 28 ] Pharmacology
Theophylline, also known as 1,3-dimethylxanthine, is a drug that inhibits phosphodiesterase and blocks adenosine receptors. [1] It is used to treat chronic obstructive pulmonary disease (COPD) and asthma. [2] Its pharmacology is similar to other methylxanthine drugs (e.g., theobromine and caffeine). [1]