Prasugrel


Concise Prescribing Info
Indications/Uses
Acute coronary syndrome.
Dosage/Direction for Use
Adult : PO Loading dose: 60 mg. Maintenance: 10 mg once daily up to 12 mth, w/ aspirin.
Dosage Details
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.
Special Patient Group
Patient w/ low body wt (<60 kg): 5 mg once daily as maintenance dose.
Hepatic Impairment
Severe (Child-Pugh class C): Contraindicated.
Administration
May be taken with or without food.
Contraindications
Active pathological bleeding, history of stroke or transient ischaemic attack. Severe hepatic impairment (Child-Pugh class C).
Special 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.
Adverse Reactions
Angioedema, anaphylaxis, HTN, hyperlipidaemia, headache, back pain, dyspnoea, nausea, dizziness, cough, hypotension, fatigue, non-cardiac chest pain, AF, bradycardia, leucopenia, rash, pyrexia, peripheral oedema, extremity pain, diarrhoea.
Potentially Fatal: Serious bleeding, thrombotic thrombocytopenic purpura.
MonitoringParameters
Monitor Hb and haematocrit periodically; may consider platelet function testing.
Overdosage
Symptoms: Prolonged bleeding time and subsequent bleeding complications. Management: Platelet transfusion and/or other blood products may be considered.
Drug Interactions
Increased risk of bleeding w/ oral anticoagulants (e.g. warfain), clopidogrel, NSAIDs and fibrinolytics.
Action
Description: 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.
Onset: Inhibition of platelet aggregation: <30 min (dose-dependent).
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Time to peak plasma concentration: Approx 30 min.
Distribution: Plasma protein binding: Approx 98%.
Metabolism: Undergoes hydrolysis in the intestines before being metabolised by CYP450 isoenzymes to the active metabolite (R-138727) which is further metabolised to 2 inactive compounds.
Excretion: Via urine (approx 68%) and faeces (approx 27%). Elimination half-life: Approx 7.4 hr.
Storage
Store at 25°C.
References
Anon. Prasugrel. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/08/2014.

Buckingham R (ed). Prasugrel Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/08/2014.

Effient (prasugrel hydrochloride) 5 mg and 10 mg Tablets. U.S. FDA. https://www.fda.gov/. Accessed 06/08/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Prasugrel Hydrochloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/08/2014.

Disclaimer: This information is independently developed by MIMS based on Prasugrel from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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