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Tirofiban information from DrugsUpdate  

See Available Brands of Tirofiban in India

Tirofiban is an antiplatelet drug. It belongs to a class of anticoagulants named glycoprotein IIb/IIIa inhibitors. Tirofiban is the first drug candidate whose origins can be traced to a pharmacophore-based virtual screening lead.

Pharmacodynamics

Pharmacokinetics

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 hours.

Distribution
Plasma half-life: 2 hours. 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.

Tirofiban Indications / Tirofiban Uses

Information Not Available

Tirofiban Adverse Reactions / Tirofiban Side Effects

Bleeding, thrombocytopenia, bradycardia, dissection of the coronary artery, dizziness, oedema, pelvic pain, sweating, nausea, fever, headache, rashes.

Potentially Fatal: Anaphylaxis.

Precautions

Monitor
Monitor for bleeding. Monitor platelet counts, hemoglobin, and hematocrit prior to treatment, 6 hours following loading infusion, and at least daily thereafter during treatment. APTT should be determined prior to treatment and anticoagulant effects of heparin should be carefully monitored by repeated determinations of APTT.

Overdosage

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.

Special Precautions

Anaemia, thrombocytopenia or known history of platelet function disturbance. Puncture of a non-compressible vessel within 24 hours, 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 hours 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 hours after initiation of therapy. Elderly, females, patients with low body weight.

Other Drug Interactions

Information Not Available

Other Interactions

Information Not Available

Dosage

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 hours after angioplasty or atherectomy. Patients who require CABG: Discontinue tirofiban at least 4–6 hours 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 hours.
CrCl (ml/min)    Dosage Recommendation
<30                  Reduce dose by 50%.


Reconstitution
Preparing injection 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 injection and replace this volume with 50 ml (12.5 mg of tirofiban) or 100 mL (25 mg of tirofiban) of tirofiban injection to achieve a final tirofiban concentration of 50 mcg/ml.

Incompatibility
Do not admin diazepam in the same IV line.

Food(before/after)

Information Not Available

List of Contraindications

Tirofiban and Pregnancy

Information Not Available

Tirofiban and Lactation

Information Not Available

Tirofiban and Children

Safety and efficacy not established

Tirofiban and Geriatic

Information Not Available

Tirofiban and Other Contraindications

History of thrombocytopenia with glycoprotein IIb/IIIa receptor antagonist. Active internal bleeding. Active peptic ulcer within the past 3 months. 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 weeks. Serious hepatic impairment.

Storage

Intravenous
Store between 15-30°C. Protect from light. Avoid freezing. Discard unused portions.

Lab interference

Intravenous
Store between 15-30°C. Protect from light. Avoid freezing. Discard unused portions.

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