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Clopidogrel (top left) being activated: The first step is an oxidation mediated (mainly) by the enzyme CYP2C19, unlike the activation of the related drug prasugrel. The two structures at the bottom are tautomers of each other; and the final step is a hydrolysis.
[3] [4] CYP2C19 is a liver enzyme that acts on at least 10% of drugs in current clinical use, [5] most notably the antiplatelet treatment clopidogrel (Plavix), drugs that treat pain associated with ulcers, such as omeprazole, antiseizure drugs such as mephenytoin, the antimalarial proguanil, and the anxiolytic diazepam. [6]
Clopidogrel, unlike prasugrel, was issued a black box warning from the FDA on 12 March 2010, as the estimated 2–14% of the US population who have low levels of the CYP2C19 liver enzyme needed to activate clopidogrel may not get the full effect. Tests are available to predict if a patient would be susceptible to this problem or not.
Clopidogrel has a common drug interaction with CYP2C19 inhibitors, particularly omeprazole and esomeprazole which are indicated for treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD). As the activation of clopidogrel requires an enzyme called CYP2C19, its inhibitors should be avoided. [38]
The CYP2C19 enzyme metabolizes proton pump inhibitors (PPI) as well as clopidogrel. Various reports have stated that there is a negative clopidogrel-omeprazole drug interaction . Some studies have found that clopidogrel activity on platelets was hampered significantly by patients receiving treatment with omeprazole , a proton pump inhibitor (PPI).
Enzyme Inhibitors Inducers; CYP1A1: Certain foods (e.g., cumin, turmeric) Certain herbs/herbal teas (e.g., peppermint, German chamomile, dandelion, Kava) Amiodarone ...
A network meta-analysis of 37 studies involving 88,402 STEMI patients and 5,077 major adverse cardiac events (MACE) patients found that use of prasugrel was associated with lower mortality and MACE than other drugs in this class (clopidogrel and ticagrelor).
1559 72303 Ensembl ENSG00000138109 ENSMUSG00000067231 UniProt P11712 n/a RefSeq (mRNA) NM_000771 NM_028191 RefSeq (protein) NP_000762 n/a Location (UCSC) Chr 10: 94.94 – 94.99 Mb Chr 19: 39.05 – 39.08 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Cytochrome P450 family 2 subfamily C member 9 (abbreviated CYP2C9) is an enzyme protein. The enzyme is involved in the metabolism, by ...