clopidogrel bisulfate


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Related to clopidogrel bisulfate: amlodipine besylate, atorvastatin, Plavix, Rosuvastatin, metoprolol tartrate

clopidogrel bisulfate

Plavix

Pharmacologic class: Platelet aggregation inhibitor

Therapeutic class: Antiplatelet drug

Pregnancy risk category B

FDA Box Warning

• Effectiveness of clopidogrel depends on activation to an active metabolite by the cytochrome P(CYP) 450 system, principally CYP2C19.

• Patients identified as CYP2C19 poor metabolizers treated with clopidogrel at recommended dosages exhibit higher cardiovascular event rates following acute coronary syndrome or percutaneous coronary intervention than patients with normal CYP2C19 function.

• Tests are available to identify a patient's CYP2C19 genotype and can be used as an aid in determining therapeutic strategy.

• Consider alternative treatment or treatment strategies in patients identified as CYP2C19 poor metabolizers.

Action

Inhibits platelet aggregation by blocking binding of adenosine diphosphate to platelets, thereby preventing thrombus formation

Availability

Tablets: 75 mg, 300 mg

Indications and dosages

Recent myocardial infarction (MI) or stroke or established peripheral arterial disease

Adults: 75 mg/day P.O.

Acute coronary syndrome (ACS)

Adults: 300 mg P.O. as a loading dose, then 75 mg/day P.O. in combination with aspirin (75 to 325 mg once daily) for patients with non-ST-segment elevation ACS (unstable angina, non-ST-elevation MI)

Adults: 75 mg P.O. once daily in combination with aspirin (75 to 325 mg once daily), with or without a loading dose and with or without thrombolytics for patients with ST-elevation MI

Contraindications

• Hypersensitivity to drug
• Active pathologic bleeding

Precautions

Use cautiously in:
• thrombotic thrombocytopenic purpura
• increased risk of bleeding
• concomitant use of drugs that inhibit CYP2C19 (such as esomeprazole, omeprazole)
• concomitant use of aspirin in patients with recent transient ischemic attack or cerebrovascular accident
• premature discontinuation of drug
• pregnant or breastfeeding patients
• children (safety and efficacy not established).

Administration

• Give with or without food.
• Know that drug may need to be discontinued 5 days before surgery.

Adverse reactions

CNS: depression, dizziness, fatigue, headache

CV: chest pain, hypertension

EENT: epistaxis, rhinitis

GI: diarrhea, abdominal pain, dyspepsia, gastritis, GI bleeding

Hematologic: bleeding, neutropenia, thrombotic thrombocytopenic purpura

Metabolic: hypercholesterolemia, gout

Musculoskeletal: joint pain, back pain

Respiratory: cough, dyspnea, bronchitis, upper respiratory tract infection, bronchospasm

Skin: pruritus, rash, angioedema

Other: hypersensitivity reactions, anaphylactic reactions

Interactions

Drug-drug.Abciximab, aspirin, eptifibatide, heparin, heparinoids, nonsteroidal anti-inflammatory drugs (NSAIDs), thrombolytics, ticlopidine, tirofiban, warfarin: increased risk of bleeding

CYP2C19 inhibitors (such as esomeprazole, omeprazole): significantly reduced clopidogrel antiplatelet activity

Fluvastatin, many NSAIDs, phenytoin, tamoxifen, tolbutamide, torsemide: interference with metabolism of these drugs

Drug-diagnostic tests.Bilirubin, hepatic enzymes, nonprotein nitrogen, total cholesterol, uric acid: increased levels

Platelets: decreased count

Drug-herbs.Anise, arnica, chamomile, clove, fenugreek, feverfew, garlic, ginger, ginkgo, ginseng: increased risk of bleeding

Patient monitoring

• Monitor hemoglobin and hematocrit periodically.
• Monitor patient for unusual bleeding or bruising; drug significantly increases risk of bleeding.
• Assess for occult GI blood loss if patient is receiving naproxen concurrently with clopidogrel.

Patient teaching

• Tell patient to take tablets with or without food.

Advise patient to immediately report unusual or acute chest pain, respiratory difficulty, rash, purplish bruises on skin or in mouth, purple skin patches, unusual fatigue, fast heart rate, confusion, signs and symptoms of stroke (including weakness on one side, speech changes), low urine output, unresolved bleeding, diarrhea, GI distress, nosebleed, or acute headache.

Instruct patient not to discontinue drug without consulting prescriber.
• Instruct patient to tell all health care providers that he's taking clopidogrel, especially if surgery is scheduled or new drugs are prescribed.
• Advise patient to contact prescriber before taking over-the-counter products, particularly nonsteroidal anti-inflammatory drugs.
• Tell patient drug may cause headache and dizziness. Caution him to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Advise patient to minimize adverse GI effects by eating small, frequent meals or chewing gum.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

References in periodicals archive ?
For international and China market analysis, the report analyzes Clopidogrel Bisulfate Market in China and other countries or regions (such as US, Europe, Japan, etc) by presenting research on global products of different types and applications, developments and trends of market, technology, competitive landscape, and leading suppliers' and countries' 2010-2015 capacity, production, cost, price, profit, production value, and gross margin.
For technical data and manufacturing plants analysis, the report analyzes Clopidogrel Bisulfate leading suppliers on capacity, commercial production date, manufacturing plants distribution, R&D status, technology sources, and raw materials sources.
2 billion in the second quarter of 2007 compared to the same period in 2006, due to continued growth of key products and sales of newer products BARACLUDE(R), ORENCIA(R) and SPRYCEL(TM), partially offset by the impact of generic clopidogrel bisulfate and increased generic competition for PRAVACHOL(R).
The company estimated the impact of the at- risk launch of generic clopidogrel bisulfate to be in the range of $50 million to $100 million for the second quarter of 2007 as inventory of generic clopidogrel bisulfate in the distribution channels was substantially depleted at June 30, 2007.
These risks and uncertainties include risks that may arise from the outcome of any appeal, the adverse impact of generic product distributed into the market by Apotex, the potential launch of a generic clopidogrel bisulfate product by other entities, as well as those discussed or identified in the public filings with the SEC and the AMF made by sanofi-aventis, including those listed under "Risk Factors" and "Cautionary Statement Regarding Forward-Looking Statements" in sanofi-aventis' annual report on Form 20-F for the year ended December 31, 2006.
While the company expects generic clopidogrel bisulfate inventory in the market to have a continued residual impact on 2007 PLAVIX(R) net sales, the company does expect PLAVIX(R) net sales and earnings growth in 2007, assuming the absence of renewed or additional generic competition.
The at-risk launch of generic clopidogrel bisulfate continued to have a significant adverse effect on sales in the fourth quarter, which the company estimates to be in the range of $700 million to $750 million.
These risks and uncertainties include risks that may arise from the Department of Justice's criminal investigation on the Plavix(R) proposed settlement with Apotex, the adverse impact of Apotex's launch and generic product distributed into the market prior to the Court's injunction, the potential launch of a generic clopidogrel bisulfate product by other entities, as well as those discussed or identified in the public filings with the SEC and the AMF made by sanofi-aventis, including those listed under "Risk Factors" and "Cautionary Statement Regarding Forward- Looking Statements" in sanofi-aventis' annual report on Form 20-F for the year ended December 31, 2005.
On August 8, 2006, Apotex announced that it had launched a generic version of clopidogrel bisulfate 75 mg tablets in competition with Plavix(R).
Apotex) and the announcement on August 8, 2006 by Apotex that it had launched a generic clopidogrel bisulfate product that competes with PLAVIX(R).
These factors include, among other things, the unpredictability of the ultimate outcome of any litigation matter, including whether the appellate court in the Plavix litigation will, on appeal, rule in the company's favor and maintain interim relief pending trial, any risks associated with the criminal investigation conducted by the Department of Justice in connection with the proposed settlement with Apotex, and the launch of a generic clopidogrel bisulfate product by Apotex, including the amount of generic product distributed prior to the Court's injunction.
These risks and uncertainties include the outcome of the Plavix litigation, the adverse impact of generic product distributed into the market prior to the Court's injunction, the Department of Justice's criminal investigation and the launch of a generic clopidogrel bisulfate and the potential launch of generic clopidogrel bisulfate product by other generic companies.