Prasurel 10-MG Tablet

Prasurel 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.

Prasugrel is an thienopyridine and a prodrug which inhibits ADP receptors by irreversibly acting on the P2Y12 receptor on platelets. The active metabolite of prasugrel prevents binding of adenosine diphosphate (ADP) to its platelet receptor, impairing the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. Prasugrel is proposed to have a similar mechanism of action to clopidogrel.

Adults: Prasugrel should be initiated with a single 60mg loading dose and then continued at 10 mg once a day. Patients taking Prasugrel should also take ASA daily (75 mg to 325 mg). In patients with acute coronary syndrome (ACS) who are managed with PCI, premature discontinuation of any antiplatelet agent, including Prasugrel, could result in an increased risk of thrombosis, myocardial infarction or death due to the patient’s underlying disease. A treatment of up to 12 months is recommended, unless the discontinuation of Prasugrel is clinically indicated.

Patients ≥75 years old: The use of Prasugrel in patients ≥75 years of age is generally not recommended. If, after a careful individual benefit/risk evaluation by the prescribing physician, treatment is deemed necessary in the patients age group ≥75 years, then following a 60mg loading dose a reduced maintenance dose of 5 mg should be prescribed. Patients ≥75 years of age have greater sensitivity to bleeding and higher exposure to the active metabolite of prasugrel.

Patients weighing <60 kg: Prasugrel should be given as a single 60mg loading dose and then continued at a 5mg once-daily dose. The 10mg maintenance dose is not recommended. This is due to an increase inexposure to the active metabolite of prasugrel, and an increased risk of bleeding in patients with body weight <60 kg when given a 10mg once-daily dose, compared with patients <60 kg.

Renal impairment: No dose adjustment is necessary for patients with renal impairment, including patients with end-stage renal disease.

Hepatic impairment: No dose adjustment is necessary in subjects with mild to moderate hepatic impairment (Child-Pugh class A and B). There is limited therapeutic experience in patients with mild and moderate hepatic dysfunction.

Children and adolescents: Prasugrel is not recommended for use in children below age 18 due to a lack of data on safety and efficacy.

Warfarin: Coadministration of Prasurel and warfarin increases the risk of bleeding.

Non-Steroidal Anti-Inflammatory Drugs: Coadministration of Prasurel and NSAIDs (used chronically) may increase the risk of bleeding.

Other Concomitant Medications: Prasurel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasurel can be administered with aspirin (75mg to 325mg per day), heparin, GPIIb/IIIa inhibitors, statins, digoxin, and drugs that elevate gastric pH, including proton pump inhibitors and H2.

Prasugrel is contraindicated in patients with Hypersensitivity to the active substance or to any of the excipients, active pathological bleeding, history of stroke or transient ischaemic attack (TIA), severe hepatic impairment (Child-Pugh class C)

Common: Anaemia, Haematoma, Epistaxis, Gastrointestinal haemorrhage, Rash, Ecchymosis, Haematuria, Vessel puncture site haematoma, Puncture site haemorrhage, Contusion.

Uncommon: Hypersensitivity including angioedema, Eye haemorrhage, Haemoptysis, Retroperitoneal haemorrhage, Rectal haemorrhage, Haematochezia, Gingival bleeding, Post-procedural haemorrhage.

Rare: Thrombocytopaenia, Subcutaneous haematoma.

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.

Bleeding risk: In the phase 3 clinical trial, key exclusion criteria included an increased risk of bleeding; anaemia; thrombocytopaenia; a history of pathological intracranial findings. Patients with acute coronary syndromes undergoing PCI treated with Prasurel and ASA showed an increased risk of major and minor bleeding according to the TIMI classification system. Therefore, the use of Prasurel in patients at increased risk of bleeding should only be considered when the benefits in terms of prevention of ischaemic events are deemed to outweigh the risk of serious bleedings. This concern applies especially to patients:

• Age ≥75 years.
• With a propensity to bleed (e.g., due to recent trauma, recent  surgery, recent or recurrent gastrointestinal bleeding, or active  peptic ulcer disease).
• With body weight <60 kg. In these patients the 10mg  maintenance dose is not recommended. A 5mg maintenance  dose should be used.
• With concomitant administration of medicinal products that  may increase the risk of bleeding, including oral anticoagulants,  clopidogrel, non-steroidal anti-inflammatory drugs (NSAIDs), and  fibrinolytics.

Surgery: Patients should be advised to inform physicians and dentists that they are taking prasugrel before any surgery is scheduled, and before any new medicinal product is taken. If a patient is to undergo elective surgery, and an antiplatelet effect is not desired, Prasurel should be discontinued at least 7 days prior to surgery. Increased frequency (3-fold) and severity of bleeding may occur in patients undergoing CABG surgery within 7 days of discontinuation of prasugrel . The benefits and risks of prasugrel should be carefully considered in patients in whom the coronary anatomy has not been defined, and urgent CABG is a possibility.

Overdose of Prasurel may lead to prolonged bleeding time and subsequent bleeding complications. No data are available on the reversal of the pharmacological effect of prasugrel; however, if prompt correction of prolonged bleeding time is required, platelet transfusion and/or other blood products may be considered. Pharmaceutical precautions Store in a cool and dry place, protected from light.

Anti-platelet drugs

Keep in dry place and away from light and heat. Keep out of the reach of children.