What is the bioavailability of clopidogrel?
Clopidogrel
Clinical data | |
---|---|
Bioavailability | >50% |
Protein binding | 94–98% |
Metabolism | Liver |
Onset of action | 2 hours |
What is the classification of clopidogrel?
Clopidogrel is in a class of medications called antiplatelet medications. It works by preventing platelets (a type of blood cell) from collecting and forming clots that may cause a heart attack or stroke.
What percentage of clopidogrel is eliminated as parent or metabolite drug?
Clopidogrel is a pro-drug and requires complex metabolic activation in the liver. Up to 85 % of the absorbed drug can be transformed by carboxyl esterases into a carboxylic acid derivative of clopidogrel (CLPM), the major metabolite circulating in the blood [5].
What is the mechanism of action of clopidogrel?
Mechanism Of Action Clopidogrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
How is clopidogrel absorbed?
After oral administration, clopidogrel is rapidly absorbed. 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].
What is the pharmacokinetics of clopidogrel?
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.
What is the trade name for clopidogrel?
Clopidogrel oral tablet is available as both a generic and brand-name drug. Brand name: Plavix. Clopidogrel only comes in the form of a tablet you take by mouth. Clopidogrel is used to prevent heart attack and stroke.
How is clopidogrel metabolized?
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).
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 long does clopidogrel stay in system?
Plavix is estimated to be cleared from your body in about 33 hours. A single, oral dose of Plavix (clopidogrel) 75 mg has a half-life of approximately 6 hours. It takes 5.5 x half-life of a medicine for a drug to leave the body, therefore most of the Plavix should be eliminated from your system in 5.5 x 6 = 33 hours.
What are the pharmacodynamics of clopidogrel?
Upon activation, clopidogrel exhibits its pharmacodynamic effect by specifically and irreversibly binding to P2Y12, a subtype of the adenosine diphosphate (ADP) receptor, on the surface of platelets [3, 31]. P2Y12 is a Gi-protein coupled receptor.
Is clopidogrel and Plavix the same?
Plavix and Brilinta are both brand-name drugs. A generic form of Plavix, called clopidogrel, is available for use. However, a generic form of Brilinta is not yet available. A generic drug is an exact copy of a brand-name medication.
What is clopidogrel metabolite?
The active metabolite of clopidogrel contains a thiol group which binds to a free cysteine on the P2RY12 receptor and irreversibly blocks ADP binding and receptor activation (Fig. 1) [1]. Once this blockage has occurred, platelets are affected for their entire lifespan of approximately 7–10 days.
Can you suddenly stop taking clopidogrel?
Do not stop taking clopidogrel without first talking to your health care professional. Suddenly stopping the use of antiplatelet medicines can put you at risk for heart attacks, strokes, and blood clots. Be aware that while taking clopidogrel you may bruise more easily, and it may take longer for any bleeding to stop.
Is it OK to take clopidogrel every other day?
Conclusions: Long term dual anti-platelet therapy with aspirin 81 mg daily and clopidogrel 75 mg every other day beyond 12 months after PCI with DES may be a safe and efficacious cost-saving strategy to prevent VLST.
How do you monitor the effects of clopidogrel?
Conclusions: VASP phosphorylation assays are reliable for quantifying clopidogrel effects. Because the VASP assay directly measures the function of the clopidogrel target, the P2Y12 receptor, the assay is selective for clopidogrel effects rather than effects of other platelet inhibitors commonly in use.
Which is better Plavix or clopidogrel?
Clopidogrel has an average rating of 7.0 out of 10 from a total of 82 ratings on Drugs.com. 62% of reviewers reported a positive effect, while 23% reported a negative effect. Plavix has an average rating of 7.6 out of 10 from a total of 57 ratings on Drugs.com.
What is an FDA black box warning?
Boxed warnings (formerly known as Black Box Warnings) are the highest safety-related warning that medications can have assigned by the Food and Drug Administration. These warnings are intended to bring the consumer’s attention to the major risks of the drug.