- Present for treatment with a heart attack with ST-elevation, including
- A loading dose given in advance of percutaneous coronary intervention, followed by a full year of treatment for those receiving a vascular stent
- A loading dose given in advance of fibrinolytic therapy, continued for at least 14 days
- Present for treatment of a heart attack or unstable angina without ST-elevation .
- Including a loading dose and maintenance therapy in those receiving PCI and unable to tolerate aspirin therapy
- Maintenance therapy for up to 12 months in those at medium to high risk for which a non-invasive treatment strategy is chosen
- In those with stable ischemic heart disease, treatment with clopidogrel is described a a "reasonable" option for monotherapy in those who cannot tolerate aspirin, as is treatment with clopidogrel in combination with aspirin in certain high risk patients.
- Severe neutropenia (low white blood cells) (incidence: one in 2,000)
- Thrombotic thrombocytopenic purpura (incidence: four per million patients treated)
- Hemorrhage - the annual incidence of hemorrhage may be increased by the coadministration of aspirin.
- Gastrointestinal hemorrhage (incidence: 2.0% annually)
- Cerebral hemorrhage (incidence: 0.1 to 0.4% annually)
- Use of nonsteroidal anti-inflammatory drugs is discouraged in those taking clopidogrel due to increased risk of digestive tract hemorrhage
- Bleeding in the postoperative period is especially problematic for patients after heart surgery, where clopidogrel is associated with a more than double the take-back for bleeding rate, as well as other complications. The take-back for bleeding occurs when chest tube clogging occurs in the setting of ongoing bleeding in early postoperative period. Often, if chest tube clogging can be avoided, and the chest tubes drain, the patient can be given platelets until the platelet defect is corrected and the bleeding ceases. But, if the bleeding continues, and the chest tubes occlude, then the patient will become hemodynamically unstable and may require an emergency take-back to the operating room. This affects outcomes and costs of care.
- Most studies researching clopidogrel do not compare patients on clopidogrel to patients taking placebo; rather, clopidogrel use is compared to aspirin use. Thus, attributing side effects directly to clopidogrel is difficult. Other side effects may include:
- Other gastrointestinal side effects
- Upper GI discomfort (27% vs 29% in patients taking aspirin alone)
- Gastric or duodenal ulcer, gastritis
- Diarrhea (4.5% of patients in the CAPRIE trial)
- Rash (6% overall, 0.33% severe)
- Respiratory (infrequent)
- Upper respiratory infections, rhinitis, shortness of breath, cough
- chest pain
- edema (generalized swelling)
- Thrombocytopenia (reduction of platelets, 0.2% severe cases as compared to 0.1% under aspirin)
|Systematic (IUPAC) name|
|Licence data||US FDA:|
|Pregnancy cat.||B1 (AU) B (US)|
|Legal status||Prescription Only (S4) (AU)POM (UK) ℞-only (US)|
|Half-life||7–8 hours (inactive metabolite)|
|Mol. mass||321.82 g/mol|
Pharmacokinetics and metabolism
- Effect of food: Administration of clopidogrel bisulfate with meals did not significantly modify the bioavailability of clopidogrel as assessed by the pharmacokinetics of the main circulating metabolite.
- Absorption and distribution: Clopidogrel is rapidly absorbed after oral administration of repeated doses of 75-milligram clopidogrel (base), with peak plasma levels (about 3 mg/l) of the main circulating metabolite occurring around one hour after dosing. The pharmacokinetics of the main circulating metabolite are linear (plasma concentrations increased in proportion to dose) in the dose range of 50 to 150 mg of clopidogrel. Absorption is at least 50% based on urinary excretion of clopidogrel-related metabolites.
- Metabolism and elimination: In vitro and in vivo, clopidogrel undergoes rapid hydrolysis into its carboxylic acid derivative. In plasma and urine, the glucuronide of the carboxylic acid derivative is also observed.
Marketing and litigation
Use in cat
Racemic Synthesis 1
Racemic Synthesis 2
Asymmetric Synthesis 1
Asymmetric Synthesis 2
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