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ФАРМАКОЛОГИЧЕСКАЯ СОВМЕСТИМОСТЬ

Metabolization of Prasugrel

The drug prasugrel is an antiplatelet agent belonging to the thienopyridines group, such as ticlopidine and clopidogrel. Prasugrel inhibits platelet aggregation and activation through irreversible binding of its active metabolite to the P2Y12 platelet ADP receptors, reducing rate of cardiovascular events such as death, myocardial infarction or stroke.

The prescription of prasugrel is contraindicated in cases of hypersensitivity to the drug, when the patient suffers from active pathological hemorrhage or presents a clinical history of stroke or transient ischemic attack and when the patient has a history of severe hepatic insufficiency.

CAUTION

Before prescribing prasugrel caution should be taken in patients with renal failure or moderate hepatic impairment.

It is recommended to stop the treatment at least seven days before the scheduled surgery. In patients with acute coronary syndrome caution with scheduled withdrawal of the medication because of the risk of thrombosis, myocardial infarction or death (a minimum treatment of up to 12 months is recommended).

Extreme precautions in patients with unstable angina (UA) or non-T-segment elevation myocardial infarction (NTSEMI) undergoing coronary angiography within 48 hours post hospital admission, loading dose of prasugrel should only be given at the time of percutaneous coronary intervention (PCI) to reduce the risk of bleeding.

There is an increased risk of bleeding in: patients over 75 years old (evaluate benefit / risk), patients with propensity for bleeding (recent trauma, surgery, active peptic ulcer or recent / recurrent gastrointestinal bleeding); patients with body weight less than 60 kg; concomitant use with oral anticoagulants (warfarin, clopidogrel), NSAIDs (non-steroidal anti-inflammatory drugs) and fibrinolytic drugs.

Caution should be exercised in patients at risk of thrombotic thrombocytopenic purpura and hypersensitivity including angioedema.

SIDE EFFECTS

Common adverse effects: anemia, hematoma, epistaxis, digestive hemorrhage, hematuria, hematoma and/or haemorrhage in the puncture place. Eruption, ecchymosis, anemia, contusion.

Less common adverse effect: ocular haemorrhage, haemoptysis, hematochezia, retroperitoneal, rectal or vaginal haemorrhage. Postintervention bleeding, hypersensitivity (including angioedema).

PHARMACOLOGICAL INTERACTIONS

Intake of prasugrel decreases the bioavailability of drugs metabolised by CYP2B6 (such as cyclophosphamide, efavirenz, etc.).

BRAND NAME

  • Effient ®

GENE OR REGION STUDIED


  • CYP2C19

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