Prasugrel

Registered South African indications:

• Acute coronary syndrome undergoing percutaneous coronary intervention

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Severe hepatic impairment (Child Pugh Class C)
• Active pathological bleeding
• History of stroke or transient ischaemic attack

Cautions

• History of hypersensitivity to clopidogrel and thienopyridines
• Pregnancy
• Breastfeeding
• Moderate to severe renal impairment (including ESRD)
• Mild to moderate hepatic impairment (Child Pugh Class A & B)
• Elderly (>75 years)
• Increased risk of bleeding
• Recent surgery or dental procedure
• Recent trauma
• Recent or recurrent gastrointestinal bleeding
• Active peptic ulcer disease
• Weight <60kg
• Lactose allergy
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption

Forms avail. in SA and covered in this monograph: tab

Risk reduction in atherothrombotic events in patients with acute coronary syndrome undergoing percutaneous coronary intervention (PCI) as follows:
- Patients with unstable angina or non-ST segment elevation myocardial infarction treated with PCI
- Patients with ST-segment elevation myocardial infarction treated with primary or delayed PCI

<60kg

• Oral (tab): Loading dose: 60mg, immediately; Maintenance: 5mg, dly; Treatment duration: 12 months

>60kg

• Oral (tab): Loading dose: 60mg, immediately; Maintenance: 10mg, dly; Treatment duration: 12 months

Must be administered with aspirin (75-325mg) daily

May be taken with or without food. Loading dose in the fasted state may provide the most rapid onset of action

Do not crush or break the tablet

For oral use only

See Additional Prescribing Points

Not established for use in children below 18 years

Pregnancy

• Caution; not recommended
• No clinical study has been conducted in pregnant women
• Animal studies do not indicate direct harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development
• Because animal reproduction studies are not always predictive of a human response, prasugrel should only be used during pregnancy if the potential benefit to the mother justifies the potential risk to the foetus

Breastfeeding

• Caution; not recommended
• No clinical study has been conducted in breastfeeding women
• It is unknown whether prasugrel is excreted in human breast milk. Animal studies have shown excretion of prasugrel in breast milk
• The use of prasugrel during breastfeeding is not recommended

Fertility

• Prasugrel had no effect on fertility of male and female rats at oral doses up to an exposure of 240 times the recommended daily human maintenance dose (based on mg/m²)

Renal Impairment

• Caution; no dose adjustment recommended

Hepatic Impairment

• Mild to moderate (Child Pugh Class A & B): No dose adjustment recommended 
• Severe (Child Pugh Class C): Contraindicated

Elderly

• Caution; dose adjustment recommended
  Use of prasugrel in patients >75 years of age is generally not recommended
  If treatment is deemed necessary, then: Loading dose: 60mg, immediately; Maintenance: 5mg, dly

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted

Cardiovascular Disorders

• Haematoma

Respiratory Disorders

• Epistaxis
• Haemoptysis

Gastrointestinal Disorders

• Gastrointestinal haemorrhage
• Retroperitoneal haemorrhage
• Rectal haemorrhage
• Haematochezia
• Gingival bleeding

Genitourinary Disorders

• Haematuria

Skin and Subcutaneous Tissue Disorders

• Rash
• Ecchymosis
• Vessel puncture site haematoma
• Puncture site haemorrhage
• Contusion
• Post-procedural haemorrhage
• Subcutaneous haematoma

Immune, Blood and Lymphatic System Disorders

• Anaemia
• Thrombocytopaenia
• Thrombotic thrombocytopaenic purpura
• Hypersensitivity reactions
• Angioedema
  

Sensory Disorders

• Eye haemorrhage

• Agents that increase the risk of bleeding
• Warfarin
• Coumarin derivatives
• Non-steroidal anti-inflammatory drugs
• CYP2B6 substrates
• Efavirenz
• Cyclophosphamide
• Morphine
• Opioids

• Haemoglobin
• Haematocrit

Premature discontinuation

• In patients with acute coronary syndrome 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

Coadministration with aspirin

• Prasugrel is to be administered concomitantly with aspirin. Although a pharmacodynamic interaction with aspirin leading to an increased risk of bleeding is possible, the demonstration of the efficacy and safety of prasugrel comes from patients concomitantly treated with aspirin
• Patients should be told that it might take longer than usual to stop bleeding when they take prasugrel with aspirin, and that they should report any unusual bleeding (site or duration) to their doctor

Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of adenosine diphosphate (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.

Tablet 5mg

• Efient (Eli Lilly) originator

Tablet 10mg

• Efient (Eli Lilly) originator