Clopidogrel Essay Clopidogrel is an antiplatelet mostly sold under the name plavilex. It’s mostly used by
to treat coronary artery diseases, Peripheral vascular disease and cerebral vascular
disease. The most common brand name for clopidogrel is Plavix. Other names include
Clavix, Anpalt and Anthorel. In Canada it is mostly known as po-Clopidogre or Dom-
One other drug that could match up Plavix is Brilinta. Initial test results have termed
it more effective than Plavix because of the fact that it has a better and more efficient
metabolism process. The downside of Brilinta is that it has higher risk as compared to
Plavix and tends not to last as long as Plavix hence has to be taken twice a day.
The route of administration for clopidogrel is oral. It can taken with or without food.
They are sold in two forms 300mg that are pink, oblong and film coated. The
other are the 75 mg tablets, which are also, pink but are round.
It’s a synthetic drug that is made by condensing 220.127.116.11 -tetrahydrothienol[3,2-
c]pyridine with racemic methyl alpha-chloro-(2-chlorophenyl)acetate in the
presence of potassium carbonate
Clopidogrel works, as a P2Y12 platelet inhibitor. This means that its mechanism of
action is as P2Y12 receptor antagonist. Physiologically it works by reducing the
The most common and minor side effects of using clopidogrel include stomach
upsets, easy bleeding, purple skin patches, blood in the stool and diarrhea. At times
the drug may cause bleeding in the stomach, gut or the brain may occur.
It’s advised that a patient who is using the drugs experiences any of the mild side effects
If a patient takes a 14C-labeled clopidogrel, on average 50% of the total radioactivity
is excreted in urine and approximately 46% is excreted in the feces in the next 5 days
upon taking the dose. The half-life of 75gm oral tablet is estimated to be 6hrs while
the half-life of the metabolite is 30minutes.
When a dose of a single 75mg tablet is taken with or without food the absorption rate
of is estimated a to be at around 50% based on the urinary excretion of the
metabolites. Clopidogrel is metabolized into its active metabolite by CYP2C19.
Clopidogrel upon ingestion is readily absorbed in the intestine and activated in the
liver. This activation takes place in two oxidation steps. The first is the formation of
2-oxo-clopidogrel, which is then converted into an active metabolite in the second
step. The cytochrome P450 enzymes; CYP1A2, CYP2B6, CYP2C9, CYP2C19, and
CYP3A4/5 are involved in the metabolism of Clopidogrel.
The drug has not found to have a major effect when taken with or without food.
It is advised that a patient should take a test to determine CYP2C19 genotype. The
test is used to determine the therapeutic strategy that has to be undertaken. This is
because the effectiveness of clopidogrel is dependent on it activation to an active
metabolite via CYP2C19.
The effectiveness of the drug is very much dependent on the activation to an active
metabolite. Patients who are being treated for acute coronary syndrome (ACS) or
undergoing percutaneous coronary intervention and are poor metabolizers are at a
higher risk of of experiencing the side effects.
Ullmann's Encyclopedia of Industrial ChemistryCopyright © 1999-2014 by John
Wiley and Sons, Inc.
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