pharmacopeia
GET
/api/v1/drug/prasugrel

Boxed warning

BLEEDING RISK Prasugrel can cause significant, sometimes fatal, bleeding [see Warnings and Precautions (5.1 , 5.2) and Adverse Reactions (6.1) ] . Do not use prasugrel in patients with active pathological bleeding or a history of transient ischemic attack (TIA) or stroke [see Contraindications (4.1 , 4.2) ] . In patients ≥75 years of age, prasugrel is generally not recommended, because of the increased risk of fatal and intracranial bleeding and uncertain benefit, except in high-risk situations (patients with diabetes or a history of prior myocardial infarction [MI]) where its effect appears to be greater and its use may be considered [see Use in Specific Populations (8.5) ] . Do not start prasugrel in patients likely to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue prasugrel at least 7 days prior to any surgery [see Warnings and Precautions (5.2) ] . Additional risk factors for bleeding include: body weight <60 kg, propensity to bleed, concomitant use of medications that increase the risk of bleeding (e.g., warfarin, heparin, fibrinolytic therapy, chronic use of nonsteroidal anti-inflammatory drugs [NSAIDs]) [see Warnings and Precautions (5.1) ] .

2D structure
[5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-2-yl] acetate
SMILES CC(=O)OC1=CC2=C(S1)CCN(C2)C(C3=CC=CC=C3F)C(=O)C4CC4
InChIKey DTGLZDAWLRGWQN-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Prasugrel 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.

P2Y12 Receptor

Indications

Sourced from openFDA
  • Prasugrel tablets are a P2Y 12 platelet inhibitor indicated for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with percutaneous coronary intervention (PCI) as follows: Patients with unstable angina or non-ST-elevation myocardial infarction (NSTEMI) (1.1) . Patients with ST-elevation myocardial infarction (STEMI) when managed with either primary or delayed PCI (1.1) .ICD-10: I20.9, I21.9

Contraindications

Sourced from openFDA
  • Active pathological bleeding (4.1) Prior transient ischemic attack or stroke (4.2) Hypersensitivity to prasugrel or any component of the product (4.3) 4.1 Active Bleeding Prasugrel tablets are contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage (ICH) [see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ] . 4.2 Prior Transient Ischemic Attack or Stroke Prasugrel tablets are contraindicated in patients with a history of prior transient ischemic attack (TIA) or stroke.contraindicated

Dosage & administration

Sourced from openFDA

Initiate prasugrel tablets treatment as a single 60 mg oral loading dose and then continue at 10 mg orally once daily. Patients taking prasugrel tablets should also take aspirin (75 mg to 325 mg) daily [see Drug Interactions (7.4) and Clinical Pharmacology (12.3) ] . Prasugrel tablets may be administered with or without food [see Clinical Pharmacology (12.3) and Clinical Studies (14) ] . Timing of Loading Dose In the clinical trial that established the efficacy and safety of prasugrel tablets, the loading dose of prasugrel tablets was not administered until coronary anatomy was established in UA/NSTEMI patients and in STEMI patients presenting more than 12 hours after symptom onset. In STEMI patients presenting within 12 hours of symptom onset, the loading dose of prasugrel tablets was administered at the time of diagnosis, although most received prasugrel tablets at the time of PCI [see Clinical Studies (14) ] . For the small fraction of patients that required urgent CABG after treatment with prasugrel tablets, the risk of significant bleeding was substantial. Although it is generally recommended that antiplatelet therapy be administered promptly in the management of ACS because many cardiovascular events occur within hours of initial presentation, in a trial of 4033 NSTEMI patients, no clear benefit was observed when prasugrel tablets loading dose was administered prior to diagnostic coronary angiography compared to at the time of PCI; however, risk of bleeding was increased with early administration in patients undergoing PCI or early CABG.

Warnings & precautions

Sourced from openFDA

CABG-related bleeding: Risk increases in patients receiving prasugrel who undergo CABG (5.2) . Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death (5.3) . Thrombotic thrombocytopenic purpura (TTP): TTP has been reported with prasugrel (5.4) . Hypersensitivity: Hypersensitivity including angioedema has been reported with prasugrel including in patients with a history of hypersensitivity reaction to other thienopyridines (5.5) . 5.1 General Risk of Bleeding Thienopyridines, including prasugrel, increase the risk of bleeding. With the dosing regimens used in TRITON-TIMI 38, TIMI (Thrombolysis in Myocardial Infarction) Major (clinically overt bleeding associated with a fall in hemoglobin ≥5 g/dL, or intracranial hemorrhage) and TIMI Minor (overt bleeding associated with a fall in hemoglobin of ≥3 g/dL but <5 g/dL), bleeding events were more common on prasugrel than on clopidogrel [see Adverse Reactions (6.1) ] . The bleeding risk is highest initially, as shown in Figure 1 (events through 450 days; inset shows events through 7 days). Figure 1: Non-CABG-Related TIMI Major or Minor Bleeding Events Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, PCI, CABG, or other surgical procedures even if the patient does not have overt signs of bleeding. Do not use prasugrel in patients with active bleeding, prior TIA or stroke [see Contraindications (4.1 , 4.2) ] . Other risk factors for bleeding are: Age ≥75 years.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are also discussed elsewhere in the labeling: Bleeding [see Boxed Warning and Warnings and Precautions (5.1 , 5.2) ] Thrombotic Thrombocytopenic Purpura [see Warnings and Precautions (5.4) ] Hypersensitivity Including Angioedema [see Warnings and Precautions (5.5) ] Bleeding, including life-threatening and fatal bleeding, is the most commonly reported adverse reaction (6.1) . To report SUSPECTED ADVERSE REACTIONS, contact Aurobindo Pharma USA, Inc. at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Safety in patients with ACS undergoing PCI was evaluated in a clopidogrel-controlled study, TRITON-TIMI 38, in which 6741 patients were treated with prasugrel (60 mg loading dose and 10 mg once daily) for a median of 14.5 months (5802 patients were treated for over 6 months; 4136 patients were treated for more than 1 year). The population treated with prasugrel was 27 to 96 years of age, 25% female, and 92% Caucasian. All patients in the TRITON-TIMI 38 study were to receive aspirin. The dose of clopidogrel in this study was a 300 mg loading dose and 75 mg once daily. Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with the rates observed in other clinical trials of another drug and may not reflect the rates observed in practice. Drug Discontinuation The rate of study drug discontinuation because of adverse reactions was 7.2% for prasugrel and 6.3% for clopidogrel.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary There are no data with prasugrel use in pregnant women to inform a drug-associated risk. No structural malformations were observed in animal reproductive and developmental toxicology studies when rats and rabbits were administered prasugrel during organogenesis at doses of up to 30 times the recommended therapeutic exposures in humans [see Data] . Due to the mechanism of action of prasugrel, and the associated identified risk of bleeding, consider the benefits and risks of prasugrel and possible risks to the fetus when prescribing prasugrel to a pregnant woman [see Boxed Warning and Warnings and Precautions (5.1 , 5.3) ]. The background risk of major birth defects and miscarriage for the indicated population is unknown. The background risk in the U.S. general population of major birth defects is 2 to 4% and of miscarriage is 15 to 20% of clinically recognized pregnancies. Data Animal Data In embryo-fetal developmental toxicology studies, pregnant rats and rabbits received prasugrel at maternally toxic oral doses equivalent to more than 40 times the human exposure. A slight decrease in fetal body weight was observed, but there were no structural malformations in either species.

Pharmacokinetics

Sourced from openFDA
Metabolism
Prasugrel is a prodrug and is rapidly metabolized to a pharmacologically active metabolite and inactive metabolites. The active metabolite has an elimination half-life of about 7 hours (range 2 to 15 hours).

Overdosage

Sourced from openFDA

10.1 Signs and Symptoms Platelet inhibition by prasugrel is rapid and irreversible, lasting for the life of the platelet, and is unlikely to be increased in the event of an overdose. In rats, lethality was observed after administration of 2000 mg/kg. Symptoms of acute toxicity in dogs included emesis, increased serum alkaline phosphatase, and hepatocellular atrophy. Symptoms of acute toxicity in rats included mydriasis, irregular respiration, decreased locomotor activity, ptosis, staggering gait, and lacrimation. 10.2 Recommendations about Specific Treatment Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.

Approval history

Sourced from openFDA
  • Jul 10, 2009NDANDA022307Cosette
  • Jul 12, 2017ANDAANDA205927Mylan
  • Oct 16, 2017ANDAANDA205888Aurobindo Pharma
  • Oct 16, 2017ANDAANDA205897Panacea
  • Feb 2, 2018ANDAANDA205987Accord Hlthcare
  • Jun 19, 2018ANDAANDA205913Amneal Pharms
  • Aug 28, 2023ANDAANDA213315Unichem

FAERS reports

View JSON
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.
12,294 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. 1Myocardial Infarction6755.5%
  2. 2Chest Pain5474.4%
  3. 3Dyspnoea5414.4%
  4. 4Gastrointestinal Haemorrhage5344.3%
  5. 5Haemorrhage5094.1%
  6. 6Contusion4493.7%
  7. 7Off Label Use4133.4%
  8. 8Fatigue3993.2%
  9. 9Nausea3983.2%
  10. 10Dizziness3773.1%
  11. 11Drug Ineffective3192.6%
  12. 12Acute Myocardial Infarction3152.6%
  13. 13Epistaxis3102.5%
  14. 14Headache3032.5%
  15. 15Thrombosis In Device3032.5%

Literature

View JSON

Recent PubMed references pinned to Prasugrel 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 270 ClinicalTrials.gov registrations naming Prasugrel as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Prasugrel work?
Prasugrel 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 Prasugrel used for?
According to FDA labeling, Prasugrel carries indications including: Prasugrel tablets are a P2Y 12 platelet inhibitor indicated for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with percutaneous coronary intervention (PCI) as follows: Patients with unstable angina or non-ST-elevation myocardial infarction (NSTEMI) (1.1) . Patients with ST-elevation myocardial infarction (STEMI) when managed with either primary or delayed PCI (1.1) .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Prasugrel?
Prasugrel is classified as Platelet aggregation inhibitors excl. heparin, P2Y12 Platelet Inhibitor, P2Y12 Receptor Antagonists, Decreased Platelet Aggregation.
What are the brand names for Prasugrel?
Prasugrel is marketed under brand names including Effient.
What are the contraindications for Prasugrel?
Prasugrel labeling lists contraindications including: Active pathological bleeding (4.1) Prior transient ischemic attack or stroke (4.2) Hypersensitivity to prasugrel or any component of the product (4.3) 4.1 Active Bleeding Prasugrel tablets are contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage (ICH) [see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ] . 4.2 Prior Transient Ischemic Attack or Stroke Prasugrel tablets are contraindicated in patients with a history of prior transient ischemic attack (TIA) or stroke.. Always consult the full prescribing information and a clinician.
Note. Data for prasugrel 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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