Prasugrel

Indications

Prasugrel is used for: Acute coronary syndromes, thrombotic cardiovascular (CV) events, stent thrombosis, unstable angina (UA), non-ST-elevation myocardial infarction (NSTEMI), ST-elevation myocardial infarction (STEMI), Stroke

Adult Dose

Oral Acute coronary syndrome Adult: 60 mg as loading dose, followed by 10 mg once daily for up to 12 mth, given in combination w/ aspirin. Elderly: >75 yr Maintenance: 5 mg once daily. Patient w/ low body wt (<60 kg): 5 mg once daily as maintenance dose. Hepatic impairment: Severe (Child-Pugh class C): Contraindicated.

Child Dose

Renal Dose

Renal impairment Dose adjustment not necessary

Administration

May be taken with or without food.

Contra Indications

Active pathological bleeding such as peptic ulcer or intracranial hamorrhage. Patient with a history of prior transient ischemic attack or stroke

Precautions

Patient w/ propensity to bleed, low body wt (<60 kg). Patient who will undergo CABG and other surgical procedure; coronary angiography in UA/NSTEMI patients. Elderly (>75 yr). Pregnancy and lactation. Monitoring Parameters Monitor Hb and haematocrit periodically; may consider platelet function testing.

Pregnancy-Lactation

Pregnancy There are no data with prasugrel use in pregnant women to inform a drug-associated risk Due to the mechanism of action, and the associated identified risk of bleeding, consider the benefits and possible risks to the fetus when prescribing prasugrel to a pregnant woman Lactation There is no information regarding the presence of prasugrel in human milk, the effects on the breastfed infant, or the effects on milk production Metabolites of prasugrel were found in rat milk Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for prasugrel and any potential adverse effects on the breastfed child from prasugrel or from the underlying maternal condition

Interactions

Increased risk of bleeding w/ oral anticoagulants (e.g. warfain), clopidogrel, NSAIDs and fibrinolytics.

Adverse Effects

Side effects of Prasugrel : 1-10% Bleeding, Anemia, Atrial fibrillation, Back pain, Bradycardia, Dizziness, Dyspnea, Headache, Hypertension, Nausea <1% Thrombotic thrombocytopenic purpura, Abnormal hepatic function, Angioedema, Hematoma, Hemolysis, Hemorrhage, Abnormal liver function

Mechanism of Action

Prasugrel is a prodrug that inhibits platelet activation and aggregation. The active metabolite irreversibly blocks the P2Y12 component of adenosine diphosphate (ADP) receptors on the platelet, which prevents activation of the GPIIb/IIIa receptor complex, thereby reducing platelet activation and aggregation.