What percentage of clopidogrel is eliminated as parent or metabolite drug?
In the liver, approximately 15% of absorbed clopidogrel is metabolized by the cytochrome P450 (CYP) system to generate its active metabolite via a 2-step bioactivation process, whereas the rest 85% is hydrolyzed by carboxylesterase 1 (CES1) to an inactive carboxylic acid derivative.
How is clopidogrel eliminated?
An oral dose of radiolabelled clopidogrel is excreted 50% in the urine and 46% in the feces over 5 days. The remainder of clopidogrel is irreversibly bound to platelets for their lifetime, or approximately 8-11 days.
How is clopidogrel synthesized?
The preparation methods of Clopidogrel were reviewed and Clopidogrel was finally synthesized from 2-chlorobenzyl cyanide via bromination, condensation, hydrolyze, esterification, resolution, Finally with the sulfate, re-crystallization product of the target compound clopidogrel. The overall yield is 16%.
How do you take clopidogrel 75 mg?
You should take Clopidogrel 75mg Tablet exactly as prescribed by the doctor. You can take it with or without food, at any time of the day. However, it is important to take it regularly at the same time each day for best results.
Why is clopidogrel a prodrug?
Clopidogrel (Plavix) is a prodrug that is metabolized by cytochrome P450 in the liver to an active metabolite that specifically and irreversibly blocks the platelet ADP P2Y12 receptor (as discussed in detail in Chapter 62).
Is clopidogrel soluble?
Clopidogrel bisulfate is a white to off-white powder. It is practically insoluble in water at neutral pH but freely soluble at pH 1. It also dissolves freely in methanol, dissolves sparingly in methylene chloride, and is practically insoluble in ethyl ether.
Is clopidogrel reversible or irreversible?
There are no specific reversal agents for clopidogrel. Since its effects are irreversible, the resultant platelet inhibition lasts for the lifespan of the platelet, ∼7–9 days.
When do you take clopidogrel?
You may be given clopidogrel if you have had:
- a heart attack.
- acute coronary syndrome (minor heart attack or unstable angina)
- a stroke or transient ischaemic attack (TIA)
- a coronary stent (a device to open up a blocked artery to the heart)
- an open heart operation.
- peripheral arterial disease.
- a vascular operation.
Can clopidogrel be crushed and taken orally?
Conclusions: A 300 mg loading dose of crushed clopidogrel administered via NG tube provides faster and greater bioavailability than an equal dose taken orally as whole tablets. The clinical benefits of this strategy need to be investigated.
Where is clopidogrel metabolised?
Owing to its extensive metabolism, clopidogrel is not detected in human plasma. Clopidogrel is a prodrug that is absorbed in the intestine [3,4] and activated in the liver [5]. The conversion of clopidogrel to its active metabolite requires two sequential oxidative steps.