Tirofiban

Indications
 Intravenous
Acute coronary syndrome
Adult: Loading dose: 0.4 mcg/kg/minute for 30 minutes followed by 0.1 mcg/kg/minute. Patients undergoing percutaneous coronary intervention (PCI): Loading dose: 0.4 mcg/kg/minute for 30 minutes followed by 0.1 mcg/kg/minute given during angiography and for 12-24 hr after angioplasty or atherectomy. Patients who require CABG: Discontinue tirofiban at least 4-6 hr before CABG. All patients should receive aspirin before start of tirofiban therapy and unfractionated heparin simultaneously with the start of tirofiban therapy, unless contra-indicated. Max duration of treatment: 108 hr.
CrCl (ml/min)Dosage Recommendation
<30Reduce dose by 50%.


Special Populations: Severe renal impairment (CrCl <30 mL/min): 1/2 the usual dose.

Reconstitution: Preparing inj concentrate for infusion: Withdraw and discard 50-100 ml of solution from a 250 or 500 ml bag, respectively, of 0.9% sodium chloride or 5% dextrose inj and replace this volume with 50 ml (12.5 mg of tirofiban) or 100 mL (25 mg of tirofiban) of tirofiban inj to achieve a final tirofiban concentration of 50 mcg/ml.
Incompatibility: Do not admin diazepam in the same IV line.
Contraindications
 History of thrombocytopenia with glycoprotein IIb/IIIa receptor antagonist. Active internal bleeding. Active peptic ulcer within the past 3 mth. History of bleeding diathesis within the previous 30 days; history of stroke within 30 days or history of intracranial haemorrhage; history or findings suggestive of aortic dissection; intracranial neoplasm, arteriovenous malformation, or aneurysm; acute pericarditis; vasculitis; haemorrhagic retinopathy; uncontrolled hypertension >180/110 mm Hg; anaemia. Recent major surgery or severe trauma. Traumatic or protracted CPR, organ biopsy or lithotripsy within the past 2 wk. Serious hepatic impairment.
Warnings / Precautions
 Anaemia, thrombocytopenia or known history of platelet function disturbance. Puncture of a non-compressible vessel within 24 hr, recent epidural procedure, severe CHF, cardiogenic shock. Discontinue in case of uncontrolled bleeding or require emergency surgery or thrombolytic therapy. Severe renal impairment. Monitor platelet counts, haematocrit and haemoglobin before and periodically (e.g. within the first 6 hr of the loading infusion and daily thereafter). Monitor activated clotting time (ACT) or aPTT if on concurrent heparin therapy. Defer PCI for at least 4 hr after initiation of therapy. Elderly, females, patients with low body weight.
Adverse Reactions
 Bleeding, thrombocytopenia, bradycardia, dissection of the coronary artery, dizziness, oedema, pelvic pain, sweating, nausea, fever, headache, rashes.
Potentially Fatal: Anaphylaxis.
Overdose Reactions
 Bleeding, usually mucosal and localised bleeding at the arterial puncture site for cardiac catheterisation. In severe cases, intracranial haemorrhages and retroperitoneal bleeding. Management: Discontinue infusion and transfusions of blood and/or thrombocytes if required. Tirofiban can be removed by haemodialysis.
Drug Interactions
 Potentially Fatal: Increased risk of bleeding with drugs that affect haemostasis including anticoagulants, thrombolytics, other glycoprotein IIb/IIIa inhibitors, platelet aggregation inhibitors (e.g. iloprost).
See Below for More tirofiban Drug Interactions
Mechanism of Actions
 Tirofiban, a synthetic nonpeptide tyrosine derivative, is a platelet glycoprotein (GP IIb/IIIa)-receptor inhibitor. It reversibly inhibits binding of fibrinogen to the glycoprotein IIb/IIIa receptors of platelets.
Duration: 4-8 hr.
Distribution: Plasma half-life: 2 hr. Protein-binding: 65%. Volume of distribution: 22-42 L.
Metabolism: Limited metabolism.
Excretion: Eliminated largely unchanged in the urine, with some biliary excretion in the faeces.
Storage Conditions
 Intravenous: Store between 15-30°C. Protect from light. Avoid freezing. Discard unused portions.
ATC Classification
 B01AC17 - tirofiban ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
Storage
 Intravenous: Store between 15-30°C. Protect from light. Avoid freezing. Discard unused portions.
Available As
  • Tirofiban 5 mg

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