Prasugrel Hydrochloride

Indications

Prasugrel is indicated to reduce the rate of thrombotic cardiovascular (CV) events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows:

Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI).
Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.

* রেজিস্টার্ড চিকিৎসকের পরামর্শ মোতাবেক ঔষধ সেবন করুন'

Pharmacology

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.

Dosage & Administration

Treatment should be initiated with a single 60 mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily.

* রেজিস্টার্ড চিকিৎসকের পরামর্শ মোতাবেক ঔষধ সেবন করুন'

Interaction

Coadministration of Prasugrel and warfarin increases the risk of bleeding.
Coadministration of Prasugrel and NSAIDs (used chronically) may increase the risk of bleeding.
Prasugrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasugrel can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.

Contraindications

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

Side Effects

Bleeding
Thrombotic thrombocytopenic purpura
Other side effects (Headache, back pain, dyspnea, nausea, hypertension, bradycardia, rash etc)

Pregnancy & Lactation

There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response.

It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.

Precautions & Warnings

CABG-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG.
Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death

Use in Special Populations

Pediatric Use: Safety and effectiveness in pediatric patients have not been established.

Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).

Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.

Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.

Overdose Effects

In rats, lethality was observed after administration of 2000 mg/kg. Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.