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Cardiovascular Emergency Pregnancy: There are no or limited data from use in pregnant women and animal studies are insufficient with respect to reproductive toxicity — not recommended during pregnancy unless clearly necessary. Breastfeeding: it is unknown whether tirofiban is excreted in human milk; excretion has been shown in animal milk and a risk to the newborn cannot be excluded — decide whether to discontinue breastfeeding or therapy taking the benefits into account.

Tirofiban

Brand names: Aggrastat

Tirofiban is an intravenous glycoprotein IIb/IIIa receptor antagonist used as an antiplatelet adjunct in acute coronary syndromes and percutaneous coronary intervention. This page covers its emergency cardiology use.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: Two regimens by clinical setting. (1) NSTE-ACS managed with an early invasive strategy but not planned to undergo angiography for at least 4 hours and up to 48 hours after diagnosis: initial infusion rate of 0.4 microgram/kg/min for 30 minutes, then a maintenance infusion rate of 0.1 microgram/kg/min. (2) NSTE-ACS planned to undergo PCI within the first 4 hours of diagnosis, or acute myocardial infarction intended for primary PCI: initial bolus of 25 microgram/kg given over a 3 minute period, followed by a continuous infusion at a rate of 0.15 microgram/kg/min for 12-24, and up to 48 hours
Route: Intravenous only — the concentrate must be diluted before use (draw 50 ml from a 250 ml container of sterile 0.9% saline or 5% glucose and replace with 50 ml of concentrate to make 50 microgram/ml); administer with a calibrated infusion set; may be given with unfractionated heparin through the same infusion tube
Frequency: Continuous infusion — loading/bolus then maintenance as above
Max: For the 0.4 microgram/kg/min loading regimen the entire duration of treatment should not exceed 108 hours
Hospital use only, by specialist physicians experienced in the management of acute coronary syndromes. CONCURRENT THERAPY: must be given with unfractionated heparin (usually an intravenous bolus of 50-60 units/kg simultaneously with the start of tirofiban, then approximately 1,000 U per hour, titrated on the basis of the APTT, which should be about twice the normal value) and oral antiplatelet therapy including but not limited to ASA, unless contraindicated; administration of tirofiban alone without unfractionated heparin is not recommended. DURATION: for the 0.4 microgram/kg/min regimen, initiate upon diagnosis; recommended duration of the maintenance infusion is at least 48 hours; infusion of tirofiban and heparin may be continued during coronary angiography and should be maintained for at least 12 hours and not more than 24 hours after angioplasty/atherectomy, then discontinued once the patient is clinically stable and no coronary intervention is planned. For the 25 microgram/kg bolus regimen, initiate at the start of PCI (or as soon as possible after diagnosis in AMI intended for primary PCI). If PCI is performed, heparin should be stopped after PCI and sheaths withdrawn once coagulation has returned to normal (e.g. ACT < 180 seconds, usually 2-6 hours after stopping heparin). ELDERLY: no dosage adjustment necessary. §4.2 also provides a ml/hr dosing table by weight band (30-153 kg) for both regimens, including severe kidney failure columns. PAEDIATRIC: safety and efficacy in children aged < 18 years have not been established; no data are available; use is not recommended. Stop the infusion immediately if thrombolytic therapy, emergency CABG or an intra-aortic balloon pump becomes necessary. US labelling differs: 25 mcg/kg IV within 5 minutes then 0.15 mcg/kg/min for up to 18 hours (0.075 mcg/kg/min if CrCl <= 60 mL/min). NOTE ON SOURCES: eMC §4.5 was not captured in the fetched bundle — the interactions listed are drawn from §4.4 (which cross-refers §4.5) and from the US label §7; clinician to check the full §4.5.

Dose adjustments

Renal

In severe kidney failure (creatinine clearance < 30 ml/min) the dosage should be reduced by 50%; §4.2 provides a corresponding ml/hr dosing table for severe kidney failure. (US labelling uses a different threshold: for CrCl <= 60 mL/min, 25 mcg/kg intravenously within 5 minutes then 0.075 mcg/kg/min.)

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to tirofiban or to any of the excipients
  • Thrombocytopenia developed during earlier use of a GP IIb/IIIa receptor antagonist
  • History of stroke within 30 days, or any history of haemorrhagic stroke
  • Known history of intracranial disease (e.g. neoplasm, arteriovenous malformation, aneurysm)
  • Active or recent (within the previous 30 days) clinically relevant bleeding, e.g. gastro-intestinal bleeding
  • Malignant hypertension
  • Relevant trauma or major surgical intervention within the past six weeks
  • Thrombocytopenia (platelet count < 100,000/mm3) or disorders of platelet function
  • Clotting disturbances (e.g. prothrombin time > 1.3 times normal or INR > 1.5)
  • Severe liver failure

Side effects

  • Bleeding — the most common adverse reaction, usually mild mucocutaneous or catheterisation-site bleeding; gastro-intestinal, retro-peritoneal, intracranial, haemorrhoidal and post-operative bleeding, spinal epidural haematoma, haemopericardium and pulmonary (alveolar) haemorrhage have also been reported. Fatal bleeding was the most serious adverse reaction
  • Thrombocytopenia — platelet count < 90,000/mm3 in 1.5% of patients treated with tirofiban and heparin; severe thrombocytopenia (< 50,000/mm3) in 0.3%; acute and/or severe (< 20,000/mm3) decreases in platelet counts also reported
  • Common non-bleeding reactions: nausea (1.7%), fever (1.5%), headache (1.1%)
  • Common: haematoma, ecchymosis, haematuria, haemoptysis, epistaxis, oral and gingival haemorrhage, vessel puncture site haemorrhage, occult blood in stool or urine, decreases in haematocrit
  • Not known: severe allergic reactions including anaphylactic reactions; intracranial bleeding; spinal epidural haematoma; retroperitoneal bleeding

Interactions

  • Thrombolytic therapy — there is no therapeutic experience in patients for whom thrombolytic therapy is indicated; use of tirofiban is not recommended in combination with thrombolytics, and the infusion should be stopped immediately if thrombolysis becomes necessary (§4.4, cross-referring §4.5)
  • Drugs that increase the risk of bleeding to a relevant degree — concurrent use is not recommended (§4.4, cross-referring §4.5)
  • Enoxaparin — limited experience; associated with a higher frequency of cutaneous and oral bleeding events than concomitant unfractionated heparin, and efficacy of the combination has not been established; safety and efficacy with other low molecular weight heparins has not been investigated (§4.4)
  • Fibrinolytics, anticoagulants and antiplatelet agents — coadministration increases the risk of bleeding (US label §7)

Clinical monograph

How it works

It reversibly blocks the platelet glycoprotein IIb/IIIa receptor, preventing fibrinogen-mediated platelet aggregation, the final common step of thrombus formation.

Prescribing in practice

  • Bleeding is the dominant risk — it is contraindicated in active bleeding, recent stroke, major surgery or trauma and other conditions predisposing to haemorrhage.
  • Thrombocytopenia can occur, sometimes severely, so check platelet counts before and during therapy.
  • Reduce the maintenance infusion rate in significant renal impairment as clearance is reduced.

Monitoring

Monitor for bleeding, full blood count including platelets, and renal function during the infusion.

Counselling the patient

  • Explain this drip helps keep the blood from clotting in the heart's arteries.
  • Report any unusual bruising, bleeding or blood in urine or stool.

Evidence & guidelines

Use in acute coronary syndromes and PCI is supported by randomised trials and reflected in cardiology guidelines.

Reference: ESC NSTE-ACS Guidelines 2020; PRISM-PLUS trial NEJM 1998; 338(21):1488-1497; NICE NG185; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.