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Tirofiban Hydrochloride

Pronunciation: TYE-roe-FYE-ban HYE-droe-KLOR-ide
Class: Antiplatelet agent

Trade Names

- Injection 50 mcg/mL
- Injection, concentrate 250 mcg/mL


Reversible antagonist of fibrinogen binding to glycoprotein IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation.

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Vd ranges from 22 to 42 L. Not highly bound to plasma protein (35% present in plasma as unbound drug).


Excreted 65% in urine and approximately 25% in feces, both primarily as unchanged drug. The t ½ is approximately 2 h.

Special Populations

Renal Function Impairment

Plasma Cl is significantly decreased (more than 50%) in patients with CrCl less than 30 mL/min.

Hepatic Function Impairment

Plasma Cl in mild to moderate hepatic function impairment is not significantly different from healthy patients.


Plasma Cl is about 19% to 26% lower.

Indications and Usage

In combination with heparin for treatment of acute coronary syndrome, including percutaneous coronary transluminal angioplasty (PCTA) or atherectomy.


Patients with active internal bleeding or a history of bleeding diathesis within the previous 30 days; a history of intracranial hemorrhage, intracranial neoplasm, arteriovenous malformation, or aneurysm; history of stroke within 30 days or any history of hemorrhagic stroke; major surgical procedure or severe physical trauma within the previous month; history, symptoms, or findings suggestive of aortic dissection; severe hypertension (systolic BP above 180 mm Hg and/or diastolic BP above 110 mm Hg); concomitant use of another parenteral glycoprotein IIb/IIIa inhibitor; acute pericarditis; history of thrombocytopenia following prior exposure to the product; known hypersensitivity to any component of the product.

Dosage and Administration


IV 0.4 mcg/kg/min for 30 min, then continue at 0.1 mcg/kg/min.

Severe Renal Function Impairment (CrCl less than 30 mL/min)

IV 0.2 mcg/kg/min for 30 min, then 0.05 mcg/kg/min.

General Advice

  • Prior to administration, dilute tirofiban injection (250 mcg/mL) to same strength as tirofiban injection premixed (ie, 50 mcg/mL) using sodium chloride 0.9% or dextrose 5% in water.
  • Mix well prior to administration.
  • Do not use unless the solution is clear.
  • Do not administer in the same IV line as diazepam.


Store at 59° to 86°F. Do not freeze. Protect from light during storage.

Drug Interactions

Aspirin, heparin

Risk of bleeding is increased.

Drugs that affect hemostasis (eg, warfarin)

Use with caution, risk of bleeding may be increased.

Levothyroxine, omeprazole

Tirofiban clearance may be increased; however, the clinical importance is not known.

Adverse Reactions

The following adverse reactions were reported with combined use of tirofiban and heparin.


Coronary artery dissection (5%); bradycardia (4%).


Dizziness (3%); headache (greater than 1%).


Sweating (2%).


Increased blood in feces (18%); nausea (greater than 1%).


Increase blood in urine (11%).


Thrombolysis in MI (TIMI) major bleeding in patients undergoing coronary artery bypass graft (25%); minor bleeding (11%); TIMI following PCTA (3%); TIMI following angiography, major bleeding (1%); bleeding, emopericardium, fatal bleeding, intracranial bleeding, pulmonary (alveolar) hemorrhage, retroperitoneal bleeding, spinal-epidural hemorrhage, severe decreases in platelet count associated with chills, low-grade fever, or bleeding complications (postmarketing).

Lab Tests

Decreased hemoglobin and hematocrit, platelet count below 90,000/mm 3 (2%).


Leg pain (3%).


Pelvic pain (6%); edema/swelling, vasovagal reaction (2%); fever (greater than 1%); allergic reactions, including anaphylaxis (postmarketing).



Monitor for bleeding. Monitor platelet counts, hemoglobin, and hematocrit prior to treatment, 6 h 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.


Category B .




Safety and efficacy not established.

Renal Function

Reduce dose in severe renal function impairment (eg, CrCl less than 30 mL/min).


Bleeding is the most common complication. Use with caution in patients with platelet count below 150,000/mm 3 .

IV coronary intervention

Care should be taken when attempting vascular access to ensure that only the anterior wall of the femoral artery is punctured.

Vascular and other trauma

Minimize other arterial and venous punctures, epidural procedures, IM injections, and use of urinary catheters, nasotracheal intubation, and nasogastric tubes.



Bleeding, primarily minor mucocutaneous bleeding events and minor bleeding at the site of cardiac catheterization.

Patient Information

  • Advise patient to report any bleeding or bruising to health care provider immediately.

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