EFIENT 10MG TABLETS 28`S

EFIENT contains prasugrel, a third-generation thienopyridine prodrug that irreversibly inhibits the platelet ADP receptor (P2Y12). After oral administration, prasugrel is rapidly converted to its active metabolite which blocks platelet aggregation. Unlike clopidogrel (Plavix), prasugrel's conversion is more predictable and less dependent on CYP2C19 genetic polymorphisms, making it a more consistent antiplatelet agent.

EFIENT is used, in combination with aspirin, for the prevention of atherothrombotic events in patients with acute coronary syndrome (ACS — unstable angina, NSTEMI, or STEMI) who are managed with percutaneous coronary intervention (PCI).

The TRITON-TIMI 38 trial demonstrated that prasugrel 10 mg significantly reduced the composite endpoint of cardiovascular death, non-fatal MI, and non-fatal stroke compared to clopidogrel.

EFIENT is not indicated for patients managed medically without PCI. It has a superior anti-ischaemic effect compared to clopidogrel but carries a higher bleeding risk, making careful patient selection essential.

EFIENT is given as a loading dose followed by a daily maintenance dose, always in combination with aspirin (75–100 mg daily).

Standard Dosing (Body weight 60 kg and above)

•       Loading dose: 60 mg as a single oral dose, as early as possible before or at the time of PCI.

•       Maintenance dose: 10 mg once daily if >60kg.

Low Body Weight (under 60 kg)

•       Loading dose: 60 mg (same loading dose).

•       Maintenance dose: 5 mg once daily (not the 10 mg tablet — use the 5 mg tablet if available, or consider alternative agent).

Tablets may be taken with or without food. Do not crush or chew the tablet — swallow whole.

Duration of Therapy

•       For patients with bare metal stent (BMS): minimum 4 weeks dual antiplatelet therapy (DAPT).

•       For patients with drug-eluting stent (DES): minimum 12 months DAPT (or longer depending on ischaemic/bleeding risk balance).

•       Do not discontinue EFIENT without consulting a cardiologist — premature discontinuation carries a significant risk of stent thrombosis.

Most Important Side Effect — Bleeding

Bleeding is the most common and serious side effect of EFIENT. Major bleeding events occur more frequently with prasugrel than with clopidogrel.

•       Minor bleeding: bruising easily, bleeding gums, prolonged bleeding from cuts, nosebleeds.

•       Serious bleeding: gastrointestinal bleeding (black tarry stools, blood in vomit), haematuria (blood in urine), severe headache (could indicate intracranial haemorrhage).

Other Common Side Effects

•       Anaemia (low haemoglobin).

•       Dyspnoea (shortness of breath — usually due to underlying cardiac condition).

•       Hypotension (low blood pressure), oedema.

•       Rash.

Rare but Serious

•       Thrombotic thrombocytopenic purpura (TTP) — fever, low platelets, renal failure, neurological symptoms: seek immediate medical care.

Bleeding Risk Factors — Avoid or Use 5mg in High-Risk Patients

Three patient groups have significantly higher bleeding risk and are generally not recommended for EFIENT 10 mg: (1) Age 75 years or older — net clinical benefit is uncertain due to excess intracranial haemorrhage risk; (2) Body weight under 60 kg — use 5 mg maintenance dose; (3) History of stroke or TIA — absolute contraindication.

Perioperative Management

EFIENT must be stopped 7 days before elective surgery that carries significant bleeding risk (including CABG). Stopping earlier is associated with rebound platelet reactivity and stent thrombosis risk if within the DAPT window. Discuss with the cardiologist before any surgical procedure.

Premature Discontinuation

Stopping EFIENT prematurely (especially within the first year after DES placement) risks acute stent thrombosis — a potentially fatal complication. Any decision to stop therapy must be made in consultation with the interventional cardiologist.

Renal Impairment

No dose adjustment is required for renal impairment. However, patients with severe renal impairment have higher baseline bleeding risk and should be monitored closely.

•       Warfarin and other anticoagulants — significantly increased bleeding risk; co-prescribing requires careful haematological monitoring and should be avoided unless clearly indicated (e.g., AF + ACS post-PCI).

•       NSAIDs (ibuprofen, diclofenac, naproxen) — additive antiplatelet and GI bleeding risk; avoid if possible. If NSAID needed, use lowest dose for shortest time and add proton pump inhibitor cover.

•       Aspirin — intentionally co-administered (75–100 mg daily) as dual antiplatelet therapy. Higher aspirin doses increase bleeding risk without additional ischaemic benefit.

•       Other antiplatelet agents (dipyridamole, cilostazol) — additive bleeding risk; avoid triple antiplatelet therapy.

•       Fibrinolytics (alteplase, streptokinase) — additive bleeding risk during acute treatment phases.

•       Store below 30 degrees Celsius.

•       Store in original blister packaging — protect from moisture.

•       Keep out of reach of children.

•       Do not use after the expiry date.

EFIENT is a prescription-only medicine (POM) in Kenya, regulated by the Pharmacy and Poisons Board (PPB). It must be prescribed by a cardiologist or specialist physician with expertise in acute coronary syndrome management.

Due to the specialist nature of its use, it is typically initiated in hospital settings post-PCI and continued on outpatient prescriptions thereafter.

Prescribing Guidance

•       EFIENT is indicated only for ACS managed by PCI — do not use in ACS managed medically without PCI.

•       Absolute contraindication: prior stroke or TIA — document this in the patient record.

•       Relative contraindication in patients aged 75 years or older and/or body weight under 60 kg — use 5 mg maintenance dose if EFIENT is still selected, or consider alternative (ticagrelor or clopidogrel).

Monitoring

•       FBC at baseline and periodically — detect anaemia due to occult bleeding.

•       Renal function at baseline.

•       Check for any new bleeding symptoms at each clinic visit.

PPI Co-prescription

Co-prescribe a proton pump inhibitor (omeprazole, pantoprazole) to reduce gastrointestinal bleeding risk. Unlike clopidogrel, prasugrel's antiplatelet efficacy is not significantly affected by PPIs.

Switching from EFIENT to Ticagrelor or Clopidogrel

Switching is sometimes required due to bleeding, tolerability, or cost. Consult with the cardiologist before switching — the timing and loading strategy during switch must be carefully managed to avoid periods of inadequate platelet inhibition.

How is EFIENT different from clopidogrel?

EFIENT (prasugrel) is a more potent and faster-acting antiplatelet medicine than clopidogrel. It does not depend on genetic variation in the CYP2C19 enzyme for its activation, so its antiplatelet effect is more consistent. It reduces the risk of heart attacks in ACS patients treated with stenting, but it also has a higher risk of bleeding compared to clopidogrel.

What should I do if I need surgery while on EFIENT?

Do not stop EFIENT on your own. Contact your cardiologist immediately if surgery is planned. For elective surgery, EFIENT is usually stopped 7 days before the procedure. For urgent or emergency surgery, a platelet transfusion may be needed as there is no antidote to reverse its effect.

Why do I need to take aspirin alongside EFIENT?

EFIENT and aspirin work through different mechanisms to block platelet aggregation. When used together (dual antiplatelet therapy), they provide more complete protection against blood clots in coronary stents than either drug alone. The standard dose of aspirin used alongside EFIENT is 75–100 mg daily.