Tirofiban Hydrochloride

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

Trade Names

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

Pharmacology

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

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Pharmacokinetics

Distribution

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

Elimination

Excreted 65% in urine and approximately 25% in feces, both primarily as unchanged drug. The t _½ is approximately 2 h.

Special Populations

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

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.

Contraindications

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.

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.

Storage/Stability

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

Drug Interactions

Risk of bleeding is increased.

Use with caution, risk of bleeding may be increased.

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.

Cardiovascular

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

CNS

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

Dermatologic

Sweating (2%).

GI

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

Genitourinary

Increase blood in urine (11%).

Hematologic-Lymphatic

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%).

Musculoskeletal

Leg pain (3%).

Miscellaneous

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

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

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

Bleeding

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.

Overdosage

Symptoms

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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