pharmacopeia
GET
/api/v1/drug/clopidogrel

Boxed warning

DIMINISHED ANTIPLATELET EFFECT IN PATIENTS WITH TWO LOSS-OF-FUNCTION ALLELES OF THE CYP2C19 GENE The effectiveness of clopidogrel results from its antiplatelet activity, which is dependent on its conversion to an active metabolite by the cytochrome P450 (CYP) system, principally CYP2C19 [ see Warnings and Precautions ( 5.1 ), Clinical Pharmacology ( 12.3 ) ]. Clopidogrel at recommended doses forms less of the active metabolite and so has a reduced effect on platelet activity in patients who are homozygous for nonfunctional alleles of the CYP2C19 gene, (termed “CYP2C19 poor metabolizers”). Tests are available to identify patients who are CYP2C19 poor metabolizers [ see Clinical Pharmacology ( 12.5 ) ]. Consider use of another platelet P2Y 12 inhibitor in patients identified as CYP2C19 poor metabolizers. WARNING: DIMINISHED ANTIPLATELET EFFECT IN PATIENTS WITH TWO LOSS-OF-FUNCTION ALLELES OF THE CYP2C19 GENE See full prescribing information for complete boxed warning. • Effectiveness of clopidogrel depends on conversion to an active metabolite by the cytochrome P450 (CYP) system, principally CYP2C19. ( 5.1 , 12.3 ) • Tests are available to identify patients who are CYP2C19 poor metabolizers. ( 12.5 ) • Consider use of another platelet P2Y 12 inhibitor in patients identified as CYP2C19 poor metabolizers. ( 5.1 )

2D structure
methyl (2S)-2-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetate
SMILES COC(=O)[C@H](C1=CC=CC=C1Cl)N2CCC3=C(C2)C=CS3
InChIKey GKTWGGQPFAXNFI-HNNXBMFYSA-N

Mechanism of action

Sourced from openFDA

Clopidogrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y 12 class of ADP receptors on platelets.

Cytochrome P450 2C8P2Y12 Receptor

Indications

Sourced from openFDA
  • & USAGE Clopidogrel is a P2Y 12 platelet inhibitor indicated for: • Acute coronary syndrome -For patients with non-ST-segment elevation ACS (unstable angina [UA]/non-ST-elevation myocardial infarction [NSTEMI]), clopidogrel has been shown to reduce the rate of myocardial infarction (MI) and stroke. ( 1.1 ) - For patients with ST-elevation myocardial infarction (STEMI), clopidogrel has been shown to reduce the rate of MI and stroke.ICD-10: I20.9, I21.9, I63.9

Contraindications

Sourced from openFDA
  • • Active pathological bleeding, such as peptic ulcer or intracranial hemorrhage ( 4.1 ) • Hypersensitivity to clopidogrel or any component of the product ( 4.2 ) 4.1 Active Bleeding Clopidogrel tablets are contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage. 4.2 Hypersensitivity Clopidogrel tablets are contraindicated in patients with hypersensitivity (e.g., anaphylaxis) to clopidogrel or any component of the product [see Adverse Reactions ( 6.2 )] .contraindicated

Dosage & administration

Sourced from openFDA

DOSAGE & ADMINISTRATION • Acute coronary syndrome ( 2.1 ) - Initiate clopidogrel with a single 300 mg oral loading dose and then continue at 75 mg once daily. - Initiating clopidogrel without a loading dose will delay establishment of an antiplatelet effect by several days. • Recent MI, recent stroke, or established peripheral arterial disease: 75 mg once daily orally without a loading dose. ( 2.2 ) 2.1 Acute Coronary Syndrome In patients who need an antiplatelet effect within hours, initiate clopidogrel with a single 300 mg oral loading dose and then continue at 75 mg once daily. Initiating clopidogrel without a loading dose will delay establishment of an antiplatelet effect by several days [ see Clinical Pharmacology ( 12.3 ) and Clinical Studies ( 14.1 ) ]. 2.2 Recent MI, Recent Stroke, or Established Peripheral Arterial Disease 75 mg once daily orally without a loading dose [ see Clinical Pharmacology ( 12.3 ) and Clinical Studies ( 14.2 ) ].

Warnings & precautions

Sourced from openFDA

• CYP2C19 inhibitors: Avoid concomitant use of omeprazole or esomeprazole. ( 5.1 ) • Bleeding: Clopidogrel increases risk of bleeding. ( 5.2 ) • Discontinuation: Premature discontinuation increases risk of cardiovascular events. Discontinue 5 days prior to elective surgery that has a major risk of bleeding. ( 5.3 ) • Thrombotic thrombocytopenic purpura (TTP) has been reported. ( 5.4 ) • Cross-reactivity among thienopyridines has been reported. ( 5.5 ) 5.1 Diminished Antiplatelet Activity in Patients with Impaired CYP2C19 Function Clopidogrel is a prodrug. Inhibition of platelet aggregation by clopidogrel is achieved through an active metabolite. The metabolism of clopidogrel to its active metabolite can be impaired by genetic variations in CYP2C19 [ see Boxed Warning ]. The metabolism of clopidogrel can also be impaired by drugs that inhibit CYP2C19, such as omeprazole or esomeprazole. Avoid concomitant use of clopidogrel with omeprazole or esomeprazole because both significantly reduce the antiplatelet activity of clopidogrel [ see Drug Interactions ( 7.2 ) ]. 5.2 General Risk of Bleeding P2Y12 inhibitors (thienopyridines), including clopidogrel, increase the risk of bleeding. P2Y12 inhibitors (thienopyridines), inhibit platelet aggregation for the lifetime of the platelet (7 to 10 days). Because the half-life of clopidogrel’s active metabolite is short, it may be possible to restore hemostasis by administering exogenous platelets; however, platelet transfusions within 4 hours of the loading dose or 2 hours of the maintenance dose may be less effective.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are discussed below and elsewhere in the labeling: • Bleeding [see Warnings and Precautions ( 5.2 )] • Thrombotic thrombocytopenic purpura [see Warnings and Precautions ( 5.4 )] Bleeding, including life-threatening and fatal bleeding, is the most commonly reported adverse reaction. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Macleods Pharma USA, Inc. at 1-888-943-3210 or 1-855-926-3384 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions and durations of follow-up, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Clopidogrel has been evaluated for safety in more than 54,000 patients, including over 21,000 patients treated for one year or more. The clinically important adverse reactions observed in trials comparing clopidogrel plus aspirin to placebo plus aspirin and trials comparing clopidogrel alone to aspirin alone are discussed below. Bleeding CURE In CURE, clopidogrel use with aspirin was associated with an increase in major bleeding (primarily gastrointestinal and at puncture sites) compared to placebo with aspirin (see Table 1). The incidence of intracranial hemorrhage (0.1%) and fatal bleeding (0.2%) were the same in both groups. Other bleeding events that were reported more frequently in the clopidogrel group were epistaxis, hematuria, and bruise.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary Available data from cases reported in published literature and postmarketing surveillance with clopidogrel use in pregnant women have not identified any drug-associated risks for major birth defects or miscarriage [see Data]. There are risks to the pregnant woman and fetus associated with myocardial infarction and stroke [ see Clinical Considerations ]. No evidence of fetotoxicity was observed when clopidogrel was administered to pregnant rats and rabbits during organogenesis at doses corresponding to 65 and 78 times the recommended daily human dose [ see Data ]. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Myocardial infarction and stroke are medical emergencies. Therapy for the pregnant woman should not be withheld because of potential concerns regarding the effects of clopidogrel on the fetus. Labor or delivery Clopidogrel use during labor or delivery will increase the risk of maternal bleeding and hemorrhage.

Pharmacokinetics

Sourced from openFDA
Metabolism
Clopidogrel is a prodrug and is metabolized to a pharmacologically active metabolite and inactive metabolites. Absorption After single and repeated oral doses of 75 mg per day, clopidogrel is rapidly absorbed.

Overdosage

Sourced from openFDA

Platelet inhibition by clopidogrel is irreversible and will last for the life of the platelet. Overdose following clopidogrel administration may result in bleeding complications. A single oral dose of clopidogrel at 1500 or 2000 mg/kg was lethal to mice and to rats and at 3000 mg/kg to baboons. Symptoms of acute toxicity were vomiting, prostration, difficult breathing, and gastrointestinal hemorrhage in animals. Based on biological plausibility, platelet transfusion may restore clotting ability.

Approval history

Sourced from openFDA
  • Nov 17, 1997NDANDA020839Sanofi Aventis Us
  • Jan 14, 2008ANDAANDA076273Dr Reddys
  • May 17, 2012ANDAANDA076999Teva
  • May 17, 2012ANDAANDA090494Sun Pharm
  • May 17, 2012ANDAANDA090844Torrent Pharms Ltd
  • May 17, 2012ANDAANDA076274Apotex Inc
  • May 17, 2012ANDAANDA090540Aurobindo Pharma Ltd
  • May 17, 2012ANDAANDA091023Dr Reddys Labs Ltd

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
208,712 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea10,7835.2%
  2. 2Myocardial Infarction10,1884.9%
  3. 3Fatigue9,2804.4%
  4. 4Gastrointestinal Haemorrhage8,7124.2%
  5. 5Nausea8,5614.1%
  6. 6Dizziness8,3834.0%
  7. 7Diarrhoea8,0313.8%
  8. 8Drug Ineffective7,9473.8%
  9. 9Asthenia7,3313.5%
  10. 10Fall7,1173.4%
  11. 11Cerebrovascular Accident6,7873.3%
  12. 12Anaemia6,6683.2%
  13. 13Death6,5033.1%
  14. 14Headache5,9402.8%
  15. 15Pain5,8782.8%

Literature

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Recent PubMed references pinned to Clopidogrel as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 1,270 ClinicalTrials.gov registrations naming Clopidogrel as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Clopidogrel. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Clopidogrel work?
Clopidogrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y 12 class of ADP receptors on platelets.
What is Clopidogrel used for?
According to FDA labeling, Clopidogrel carries indications including: & USAGE Clopidogrel is a P2Y 12 platelet inhibitor indicated for: • Acute coronary syndrome -For patients with non-ST-segment elevation ACS (unstable angina [UA]/non-ST-elevation myocardial infarction [NSTEMI]), clopidogrel has been shown to reduce the rate of myocardial infarction (MI) and stroke. ( 1.1 ) - For patients with ST-elevation myocardial infarction (STEMI), clopidogrel has been shown to reduce the rate of MI and stroke.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Clopidogrel?
Clopidogrel is classified as Platelet aggregation inhibitors excl. heparin, P2Y12 Platelet Inhibitor, Cytochrome P450 2C8 Inhibitors, P2Y12 Receptor Antagonists, Decreased Platelet Aggregation, Hemorrheologic Alteration.
What are the brand names for Clopidogrel?
Clopidogrel is marketed under brand names including Plavix.
What are the contraindications for Clopidogrel?
Clopidogrel labeling lists contraindications including: • Active pathological bleeding, such as peptic ulcer or intracranial hemorrhage ( 4.1 ) • Hypersensitivity to clopidogrel or any component of the product ( 4.2 ) 4.1 Active Bleeding Clopidogrel tablets are contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage. 4.2 Hypersensitivity Clopidogrel tablets are contraindicated in patients with hypersensitivity (e.g., anaphylaxis) to clopidogrel or any component of the product [see Adverse Reactions ( 6.2 )] .. Always consult the full prescribing information and a clinician.
Note. Data for clopidogrel is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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