Asurel Tablet

Asurel is a thienopyridine derivative which is formulated as a hydrochloride salt. Asurel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y 12 class of ADP receptors on platelets. Since platelets participate in the initiation and/or evolution of thrombotic complications of atherosclerotic disease, inhibition of platelet function can result in the reduction of the rate of cardiovascular events such as death, myocardial infarction or stroke.

Uses

Asurel is used 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.

Asurel is also used to associated treatment for these conditions: Cardiovascular Events

Trade Name Asurel
Generic Prasugrel
Other Names Prasugrel
Weight 5mg, 10mg
Type Tablet
Formula C20H20FNO3S
Weight Average: 373.441
Monoisotopic: 373.114792406
Protein binding

Approximately 98% of the active metabolite was bound to human serum albumin in a 4% buffered solution. The major inactive metabolites are also highly bound to human plasma proteins.

Therapeutic Class Anti-platelet drugs
Manufacturer Navana Pharmaceuticals Ltd
Available Country Bangladesh
Last Updated: June 23, 2021 at 11:24 am

Dosage

Asurel dosage

Asurel should be initiated with a single 60 mg loading dose and then continued at 10 mg once a day. Patients taking Asurel should also take aspirin (75 mg to 325 mg) daily. Asurel may be administered with or without food.

In patients with acute coronary syndrome (ACS) who are managed with PCI, premature discontinuation of any antiplatelet agent, including Asurel, 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 Asurel is clinically indicated.

In case of patients weighing ≤ 60 kg or patient’s ≥ 75 years old, Asurel should be given as a single 60 mg loading dose and then continued at a 5 mg once-daily dose.

Precaution

General Risk of Bleeding: Thienopyridines, including Asurel, increase the risk of bleeding. Asurel should not be used in patients with active bleeding, prior TIA or stroke

Age ≥ 75 years: Because of the risk of bleeding (including fatal bleeding) and uncertain effectiveness in patients ≥ 75 years of age, use of Asurel is generally not recommended in these patients, except in high-risk situations (patients with diabetes or history of myocardial infarction) where its effect appears to be greater and its use may be considered.

Propensity to bleed (e.g., recent trauma, recent surgery, recent or recurrent gastrointestinal (GI) bleeding, active peptic ulcer disease, or severe hepatic impairment): Asurel should be used with caution.

Coronary Artery Bypass Graft surgery related bleeding: The risk of bleeding is increased in patients receiving Asurel who undergo CABG. If possible, Asurel should be discontinued at least 7 days prior to CABG. Do not start Asurel in patients likely to undergo urgent CABG.

Discontinuation of Asurel: Discontinue thienopyridines, including Asurel, for active bleeding, elective surgery, stroke, or TIA.

Interaction

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

Food Interaction

  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • Take with or without food.

Volume of Distribution

44-68L

Half Life

The active metabolite has an elimination half-life of about 7.4 hours (range 2-15 hours).

Clearance

Apparent clearance = 112 - 166 L/hr

Pregnancy & Breastfeeding use

Pregnancy Category B. There are no adequate and well-controlled studies of Asurel use in pregnant women. Asurel should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

It is not known whether Asurel 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.

Contraindication

Asurel should be avoided in case of hypersensitivity to the active substance or to any of the excipients, active pathological bleeding, and history of stroke or transient ischaemic attack (TIA), severe hepatic impairment.

Special Warning

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

Geriatric Use: The use of Asurel in patients ≥75 years of age is generally not recommended because these patients are at greater risk of bleeding, including fatal bleeding, compared to patients <75 years of age. If prescribed, a lower maintenance dose of 5 mg should be used.

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.

Acute Overdose

Overdose of Asurel may lead to prolonged bleeding time and subsequent bleeding omplications. 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.

Storage Condition

Store in a dry & cool place. Protect from light & moisture. Keep out of the reach of children.

Asurel contains Prasugrel see full prescribing information from innovator Monograph