Apagrel is a thienopyridine derivative which is formulated as a hydrochloride salt. Apagrel 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.
Apagrel 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.
Apagrel is also used to associated treatment for these conditions: Cardiovascular Events
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||Intas Pharmaceuticals Ltd, Healthcare Pharmacuticals Ltd|
|Available Country||India, Bangladesh|
|Last Updated:||June 23, 2021 at 9:10 am|
Table Of contents
Apagrel should be initiated with a single 60 mg loading dose and then continued at 10 mg once a day. Patients taking Apagrel should also take aspirin (75 mg to 325 mg) daily. Apagrel 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 Apagrel, 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 Apagrel is clinically indicated.
In case of patients weighing ≤ 60 kg or patient’s ≥ 75 years old, Apagrel should be given as a single 60 mg loading dose and then continued at a 5 mg once-daily dose.
General Risk of Bleeding: Thienopyridines, including Apagrel, increase the risk of bleeding. Apagrel 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 Apagrel 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): Apagrel should be used with caution.
Coronary Artery Bypass Graft surgery related bleeding: The risk of bleeding is increased in patients receiving Apagrel who undergo CABG. If possible, Apagrel should be discontinued at least 7 days prior to CABG. Do not start Apagrel in patients likely to undergo urgent CABG.
Discontinuation of Apagrel: Discontinue thienopyridines, including Apagrel, for active bleeding, elective surgery, stroke, or TIA.
Coadministration of prasugrel and warfarin increases the risk of bleeding. Coadministration of Apagrel and NSAIDs (used chronically) may increase the risk of bleeding. Apagrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Apagrel 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.
- 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
The active metabolite has an elimination half-life of about 7.4 hours (range 2-15 hours).
Apparent clearance = 112 - 166 L/hr
Pregnancy & Breastfeeding use
Pregnancy Category B. There are no adequate and well-controlled studies of Apagrel use in pregnant women. Apagrel 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 Apagrel 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.
Apagrel 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.
Pediatric use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: The use of Apagrel 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.
Overdose of Apagrel 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.
Store in a dry & cool place. Protect from light & moisture. Keep out of the reach of children.