Prasugrel

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Efient; Belgium: Efient; Bulgaria: Efient; Czech Republic: Efient; Denmark: Efient; Estonia: Efient; Finland: Efient; France: Efient; Germany: Efient; Greece: Efient; Hungary: Efient; Ireland: Efient; Italy: Efient; Latvia: Efient; Lithuania: Efient; Luxembourg: Efient; Malta: Efient; Netherlands: Efient; Poland: Efient; Portugal: Efient; Romania: Efient; Slovakia: Efient; Slovenia: Efient; Spain: Efient; Sweden: Efient; UK: Efient.

North America

Canada: Effient; USA: Effient.

Latin America

Argentina: Effient, Nefagrel, Procardia-Roemmers, Trocal.

Drug combinations

Chemistry

Prasugrel Hydrochloride: C~20~H~21~ClFNO~3~S. Mw: 409.90. (1) 5-[(1RS)-2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate hydrochloride. (2) 2-[2-(Acetyloxy)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl)ethanone hydrochloride. CAS – 389574-19-0.

Pharmacologic Category

Antithrombotic Agents; Platelet-aggregation Inhibitors; Thienopyridines. (ATC-Code: B01AC22).

Mechanism of action

Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.

Therapeutic use

Reduces rate of thrombotic cardiovascular events (e.g. stent thrombosis) in patients with unstable angina, non-ST-segment elevation MI, or ST-elevation MI (STEMI) managed with percutaneous coronary intervention (PCI).

Pregnancy and lactiation implications

Not recommended during pregnancy or lactation.

Unlabeled use

Contraindications

Active pathological bleeding. Prior transient ischemic attack or stroke.

Warnings and precautions

Risk increases in patients receiving prasugrel who undergo coronary artery bypass graft surgery (CABG)(do not start prasugrel in patients likely to undergo urgent CABG; suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, PCI, CABG, or other surgical procedures in the setting of prasugrel). Premature discontinuation of prasugrel increases risk of stent thrombosis, MI, and death (if possible, manage bleeding without discontinuing treatment). Do not use prasugrel in patients with active pathological bleeding or history of transient ischemic attack or stroke. In patients ≥75 years of age, prasugrel is generally not recommended because of the increased risk of intracranial and fatal bleeding and uncertain benefit, except in high-risk patients (diabetes or prior MI), where its effect appears to be greater and its use may be considered. When possible, discontinue treatment at least 7 days prior to any surgery. Additional risk factors for bleeding include body weight <60 kg, propensity to bleed, and concomitant use of medications that increase risk of bleeding. Thrombotic thrombocytopenic purpura (TTP) has been reported with the use of other thienopyridines, sometimes after a brief exposure (<2 weeks).

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