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UNIGRILIN (EPTIFIBATIDE) 75MG/100ML INJ VIAL

Ksh 19,499

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What is this medicine and what is it used for?

Eptifibatide is a cyclic heptapeptide that reversibly inhibits the platelet glycoprotein IIb/IIIa receptor — the final common pathway for platelet aggregation. By blocking fibrinogen and von Willebrand factor from binding to this receptor, eptifibatide prevents platelets from clumping together to form dangerous clots in coronary arteries.

It is used in hospital settings for:

       Non-ST-elevation acute coronary syndrome (NSTE-ACS) — unstable angina or NSTEMI — in patients scheduled for early percutaneous coronary intervention (PCI), in combination with unfractionated heparin and aspirin.

       Prevention of early thrombotic complications during and after elective or urgent PCI, including patients undergoing intracoronary stent placement.

How this medicine is given

Eptifibatide is administered exclusively by trained medical staff in a hospital or cardiac catheterisation suite. It is given intravenously as:

       A bolus injection (180 mcg/kg IV bolus from the 2 mg/mL vial — not this 0.75 mg/mL infusion vial), followed immediately by:

       A continuous IV infusion at 2 mcg/kg/min (from this 0.75 mg/mL vial) for up to 72 hours (NSTE-ACS) or up to 18–24 hours post-PCI.

The 75 mg/100 mL (0.75 mg/mL) concentration is specifically designed for the maintenance infusion. Dosing is weight-based — the clinical pharmacist or cardiologist calculates the infusion rate based on patient weight.

HOSPITAL ONLY — must be administered under continuous cardiac monitoring with resuscitation facilities available.

Renal dose adjustment: reduce infusion rate to 1 mcg/kg/min if creatinine clearance < 50 mL/min. Contraindicated if creatinine > 4 mg/dL or dialysis-dependent.

Possible side effects

Frequency

Side Effect

What to Do

Very Common (>10%)

Bleeding at puncture sites

Apply firm manual or mechanical compression. Use radial access when possible to reduce access site bleeding.

Common (1–10%)

Major bleeding (GI, genitourinary, retroperitoneal)

Stop infusion immediately; apply pressure; assess haemoglobin; notify physician.

Common (1–10%)

Thrombocytopenia (low platelets)

Platelet count monitored at baseline, 6 hours post-bolus, and daily. If severe thrombocytopenia (<100,000/mcL), stop immediately.

Uncommon

Hypotension

Monitor blood pressure continuously during infusion.

Rare

Intracranial haemorrhage

Screen all patients with contraindication checklist before administration.

Seek help urgently

Signs of major bleeding: sudden haemodynamic instability, drop in haemoglobin, neurological change

Stop infusion immediately; initiate bleeding management protocol.

ABSOLUTE CONTRAINDICATIONS to Eptifibatide:

Active internal bleeding or bleeding diathesis within 30 days.

History of stroke within 30 days or any history of haemorrhagic stroke.

Major surgery or severe trauma within 6 weeks.

Severe hypertension (SBP > 200 mmHg or DBP > 110 mmHg despite therapy).

Intracranial neoplasm, arteriovenous malformation or aneurysm.

Current or planned use of another parenteral GP IIb/IIIa inhibitor.

Creatinine > 4 mg/dL (354 mcmol/L) or dialysis-dependence.

Platelet count < 100,000/mm3.

Drug interactions

       Other antiplatelet agents (aspirin, clopidogrel, ticagrelor, prasugrel): additive bleeding risk — routinely co-administered per ACS protocol under specialist supervision.

       Thrombolytics (alteplase, streptokinase): significantly increased bleeding risk — generally contraindicated with GP IIb/IIIa inhibitors.

       Anticoagulants (UFH, LMWH, warfarin, NOACs): co-administration increases bleeding risk — monitor closely; UFH co-administration is standard per protocol.

       NSAIDs: additive platelet inhibition — avoid.

Storage

Store at 2–8°C (refrigerate). Protect from light. Do not freeze. The infusion solution is for single use only. Once opened/connected, use within 24 hours. Inspect visually — discard if discoloured or particulate matter visible. Dispose of unused solution per hospital hazardous waste protocol.

Prescription requirement

PRESCRIPTION ONLY MEDICINE (POM) — Cardiology / interventional cardiology specialist use only.

Monitoring: Continuous cardiac monitoring; platelet count at baseline, 6 hours, and daily; aPTT if using concomitant UFH; haematocrit/haemoglobin.

Guidance for patients & caregivers

Eptifibatide is given to you in hospital to prevent further clot formation in the arteries supplying your heart during or after a heart attack or coronary procedure. The most important risk is bleeding — you will be closely monitored throughout the infusion. Let your nurse know immediately if you notice unusual bruising, bleeding gums, blood in your urine, black stools, or any sudden headache or vision change.

After the infusion is stopped, its platelet-inhibiting effect wears off within 4 hours because eptifibatide reversibly binds to its receptor, unlike some other antiplatelet agents.

Pharmacist & prescriber notes

The 75 mg/100 mL (0.75 mg/mL) vial is the maintenance infusion concentration. The separate 2 mg/mL vial is used to prepare the initial 180 mcg/kg IV bolus.

Do not confuse concentrations. Infusion rate: 2 mcg/kg/min for standard renal function; 1 mcg/kg/min if CrCl 10–50 mL/min.

Maximum duration: 72 hours (NSTE-ACS) or 18–24 hours post-PCI. Platelet count must be checked at baseline; if thrombocytopenia develops (< 100,000/mcL), immediately discontinue.

Post-procedure: leave arterial sheath in place and do not remove until aPTT < 45 seconds or ACT < 150 seconds to minimise access-site bleeding.

Frequently asked questions (clinical)

Can eptifibatide be reversed if there is serious bleeding?

There is no specific antidote. Management involves stopping the infusion, applying compression, and — in extreme cases — platelet transfusion (though eptifibatide rapidly dissociates from transfused platelets given its reversible binding).

Can eptifibatide be used with low molecular weight heparin?

Yes — enoxaparin is an acceptable alternative to UFH with eptifibatide in NSTE-ACS, with last dose > 8 hours before PCI requiring a UFH supplement per protocol. Consult current ACS guidelines for specific co-administration recommendations.

Why is eptifibatide contraindicated in renal failure?

Eptifibatide and its metabolite are primarily renally excreted. In severe renal failure (creatinine > 4 mg/dL or dialysis), drug accumulation leads to markedly prolonged platelet inhibition and prohibitive bleeding risk.

Does eptifibatide work better than newer antiplatelet agents?

Eptifibatide is most valuable in the PCI setting where rapid, reversible, potent platelet inhibition is needed during the procedure. For long-term secondary prevention, oral P2Y12 inhibitors (ticagrelor, clopidogrel) are used.

What are the signs of thrombocytopenia to watch for?

Unusual bruising (petechiae, purpura), unexplained bleeding from skin or mucous membranes, blood in urine or stools. A blood test confirms the diagnosis — your team will check platelet counts regularly during the infusion.


 

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