Only one of the eight structures is an active antiplatelet drug. This has the following configuration: Z configuration at the C3—C16 double bond, the original S configuration at C7, [30] and, although the stereocentre at C4 cannot be directly determined, as the thiol group is too reactive, work with the active metabolite of the related drug prasugrel suggests the R-configuration of the C4 group is critical for P2Y12 and platelet-inhibitory activity.
Patients with a variant allele of CYP2C19 are 1. Cmax occurs approximately 30 to 60 minutes after dosing. In the 75 to mg dose range, the pharmacokinetics of the active metabolite deviates from dose proportionality: After a single, oral dose of 75 mg, Clopidogrel has a half-life of approximately 6 hours. The half-life of the active metabolite is about 30 minutes. Concomitant use of certain inhibitors of this enzyme results in reduced plasma concentrations of the active metabolite of Clopidogrel and a reduction in platelet inhibition.
Proton Pump Inhibitors PPI The effect of proton pump inhibitors PPI on the systemic exposure to the Clopidogrel active metabolite following multiple doses of Clopidogrel 75 mg evaluated in dedicated drug interaction studies is presented in Figure 1.
Pharmacodynamic and pharmacokinetic parameters measured in these studies showed that the interaction was highest with omeprazole and least with dexlansoprazole. Effect of Clopidogrel on other drugs In vitro studies have shown that the glucuronide metabolite of Clopidogrel is a strong inhibitor of CYP2C8. Pharmacogenomics CYP2C19 is involved in the formation of both the active metabolite and the 2-oxo-Clopidogrel intermediate metabolite.
Clopidogrel active metabolite pharmacokinetics and antiplatelet effects, as measured by ex vivo platelet aggregation assays, differ according to CYP2C19 genotype.
Tests are available to identify patients who are CYP2C19 poor metabolizers. A crossover study in 40 healthy subjects, 10 each in the four CYP2C19 metabolizer groups, evaluated pharmacokinetic and antiplatelet responses using mg followed by 75 mg per day and mg followed by mg per day, each for a total of 5 days. Examples of affected drugs include dasabuvir, repaglinide , among others. Ask your pharmacist about using these products safely. Should I avoid certain foods while taking Clopidogrel?
Overdose If someone has overdosed and has serious symptoms such as passing out or trouble breathing , call Otherwise, call a poison control center right away. US residents can call their local poison control center at Canada residents can call a provincial poison control center. Notes Do not share this medication with others.
Consult your doctor for more details. Missed Dose If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip themissed dose. Take your next dose at the regular time. Do not double the dose to catch up. Storage Store at room temperature away from light and moisture. Do not store in the bathroom. Hemorrhages, including those with fatal outcome, have been reported in patients treated with Plavix.
Blood and lymphatic system disorders: Acute liver failure, hepatitis non-infectious , abnormal liver function test Immune system disorders: Hypersensitivity reactions, anaphylactoid reactions, serum sickness Musculoskeletal, connective tissue and bone disorders: Myalgia, arthralgia, arthritis Nervous system disorders: Taste disorders, headache Psychiatric disorders: Confusion, hallucinations Respiratory, thoracic and mediastinal disorders: Bronchospasm, interstitial pneumonitis, eosinophilic pneumonia Renal and urinary disorders: Increased creatinine levels Skin and subcutaneous tissue disorders: Maculopapular, erythematous or exfoliative rash, urticaria, bullous dermatitis, eczema, toxic epidermal necrolysis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis AGEP , angioedema, drug-induced hypersensitivity syndrome, drug rash with eosinophilia and systemic symptoms DRESS , erythema multiforme, lichen planus, generalized pruritus Vascular disorders: Concomitant use of drugs that inhibit the activity of this enzyme results in reduced plasma concentrations of the active metabolite of clopidogrel and a reduction in platelet inhibition [see Warnings and Precautions 5.
Omeprazole or esomeprazole Avoid concomitant use of Plavix with omeprazole or esomeprazole. In clinical studies, omeprazole was shown to reduce significantly the antiplatelet activity of Plavix when given concomitantly or 12 hours apart. A similar reduction in antiplatelet activity was observed with esomeprazole when given concomitantly with Plavix. Dexlansoprazole, lansoprazole and pantoprazole had less effect on the antiplatelet activity of Plavix than did omeprazole or esomeprazole [see Warnings and Precautions 5.
Warfarin CYP2C9 Substrates Although the administration of clopidogrel 75 mg per day did not modify the pharmacokinetics of S-warfarin a CYP2C9 substrate or INR in patients receiving long-term warfarin therapy, coadministration of Plavix with warfarin increases the risk of bleeding because of independent effects on hemostasis.
Acute coronary syndrome The CURE study included 12, patients with non-ST segment elevation acute coronary syndrome unstable angina or non-Q-wave myocardial infarction , and presenting within 24 hours of onset of the most recent episode of chest pain or symptoms consistent with ischaemia.
Patients were required to have either ECG changes compatible with new ischaemia or elevated cardiac enzymes or troponin I or T to at least twice the upper limit of normal.
Patients were treated for up to one year. In CURE, 6. The number of patients experiencing the primary endpoint [cardiovascular CV death, myocardial infarction MI , or stroke] was 9. The number of patients experiencing the co-primary endpoint CV death, MI, stroke or refractory ischaemia was 1, This benefit was mostly driven by the statistically significant reduction in the incidence of MI [ 4.
There was no observed effect on the rate of rehospitalisation for unstable angina. The results obtained in populations with different characteristics e. Moreover, the safety profile of clopidogrel in this subgroup of patients did not raise any particular concern. Thus, the results from this subset are in line with the overall trial results. The efficacy of clopidogrel was observed independently of the dose of ASA mg once daily.
The patients were followed for 30 days. The primary endpoint was the occurrence of the composite of an occluded infarct-related artery on the predischarge angiogram, or death or recurrent MI before coronary angiography.
For patients who did not undergo angiography, the primary endpoint was death or recurrent myocardial infarction by Day 8 or by hospital discharge. The patient population included A total of
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