Prasugrel


Generic Medicine Info
Indications and Dosage
Oral
Prevention of atherothrombotic events
Adult: In combination with aspirin (75-325 mg daily) in patients with acute coronary syndrome (ST-elevation myocardial infarction [STEMI], NSTEMI, or unstable angina) undergoing primary or delayed percutaneous coronary intervention (PCI): Initially, 60 mg as a single loading dose. Maintenance: 10 mg once daily for up to 12 months. In patients weighing <60 kg: Reduce the maintenance dose to 5 mg once daily. For patients with unstable angina or NSTEMI who have had coronary angiography within 48 hours after hospital admission, the loading dose must be given only at the time of PCI.
Elderly: ≥75 years Use in this patient age group is generally not recommended but may be considered in high-risk situations (patients with diabetes or history of MI). Recommended dose: Initially, 60 mg as a single loading dose, then 5 mg once daily for up to 12 months.
Hepatic Impairment
Severe (Child-Pugh class C): Contraindicated.
Administration
May be taken with or without food.
Contraindications
Active pathological bleeding (e.g. intracranial haemorrhage, peptic ulcer), history of stroke or TIA. Severe hepatic impairment (Child-Pugh class C).
Special Precautions
Patient with increased risk of bleeding (e.g. body weight <60 kg, recent trauma or surgery, recent or recurrent gastrointestinal bleeding, concomitant use of oral anticoagulants, clopidogrel, NSAIDs, or fibrinolytics), history of thienopyridine hypersensitivity. Patients who will undergo CABG or other surgical procedures (discontinue treatment at least 7 days before surgery if possible). Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, PCI, CABG, or other surgeries. Renal (including ESRD) and moderate hepatic impairment. Elderly (particularly ≥75 years of age). Pregnancy and lactation.
Adverse Reactions
Significant: Hypersensitivity reactions (e.g. angioedema, anaphylaxis).
Blood and lymphatic system disorders: Anaemia, leucopenia.
Cardiac disorders: Atrial fibrillation, bradycardia.
Eye disorders: Eye haemorrhage.
Gastrointestinal disorders: Haematochezia, rectal haemorrhage, gingival bleeding, nausea, diarrhoea.
General disorders and administration site conditions: Vessel puncture haematoma, peripheral oedema, fatigue, fever, noncardiac chest pain.
Injury, poisoning and procedural complications: Contusion, post-procedural haemorrhage.
Metabolism and nutrition disorders: Hypercholesterolaemia, hyperlipidaemia.
Musculoskeletal and connective tissue disorders: Back pain, limb pain.
Nervous system disorders: Headache, dizziness.
Renal and urinary disorders: Haematuria.
Respiratory, thoracic and mediastinal disorders: Epistaxis, haemoptysis, dyspnoea, cough.
Skin and subcutaneous tissue disorders: Rash, ecchymosis.
Vascular disorders: Haematoma, hypertension, hypotension.
Potentially Fatal: Bleeding (e.g. gastrointestinal, intracranial, retroperitoneal, or puncture site haemorrhage), thrombotic thrombocytopenic purpura (TTP).
Monitoring Parameters
Monitor Hb and haematocrit periodically; signs and symptoms of bleeding.
Overdosage
Symptoms: Prolonged bleeding time and subsequent bleeding complications. Management: Platelet transfusion and/or other blood products may be considered if prompt correction of prolonged bleeding time is needed.
Drug Interactions
Decreased therapeutic efficacy with morphine and other opioid agonists. May increase the risk of bleeding with NSAIDs (including COX-2 inhibitors), warfarin, clopidogrel, and fibrinolytics.
Action
Description:
Mechanism of Action: Prasugrel, a thienopyridine antiplatelet agent, is a prodrug that inhibits platelet activation and aggregation. It is metabolised to an active metabolite which irreversibly blocks the P2Y12 class of adenosine diphosphate (ADP) receptors on the platelet, preventing the activation of the glycoprotein IIb/IIIa (GPIIb/IIIa) receptor complex, thereby reducing platelet activation and aggregation.
Onset: Inhibition of platelet aggregation: Dose-dependent; <30 minutes (loading dose).
Duration: Return of platelet aggregation to baseline: 5-9 days after discontinuation.
Pharmacokinetics:
Absorption: Rapidly absorbed. Time to peak plasma concentration: Approx 30 minutes (active metabolite).
Distribution: Volume of distribution: 44-68 L (active metabolite). Plasma protein binding: Approx 98% (active metabolite), mainly to albumin.
Metabolism: Rapidly metabolised in the intestine via esterase-mediated hydrolysis to thiolactone intermediate (inactive), which is then converted to an active metabolite (R-138727) via oxidation by CYP450 isoenzymes (primarily CYP3A4 and CYP2B6).
Excretion: Via urine (approx 68% as inactive metabolites); faeces (27% as inactive metabolites). Elimination half-life: Approx 7.4 hours (active metabolite).
Chemical Structure

Chemical Structure Image
Prasugrel

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6918456, Prasugrel. https://pubchem.ncbi.nlm.nih.gov/compound/Prasugrel. Accessed Feb. 27, 2023.

Storage
Store between 15-30°C. Protect from moisture.
MIMS Class
Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics)
ATC Classification
B01AC22 - prasugrel ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
References
Anon. Prasugrel. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 28/11/2022.

Anon. Prasugrel. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 28/11/2022.

Buckingham R (ed). Prasugrel Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/11/2022.

Effient 5 mg Film-coated Tablets; Effient 10 mg Film-coated Tablets (Daiichi Sankyo [Thailand] Ltd.). MIMS Thailand. http://www.mims.com/thailand. Accessed 28/11/2022.

Effient Tablet, Coated (Cosette Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 28/11/2022.

Efient 5 mg Film-coated Tablets (Vygoris Limited). MHRA. https://products.mhra.gov.uk. Accessed 28/11/2022.

Joint Formulary Committee. Prasugrel. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/11/2022.

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