Tirofiban – Aggrastat ®

Tirofiban (Aggrastat ®)

Usual Diluents

Standard Dilutions   [Amount of drug] [Infusion volume] [Infusion rate]

DOSAGE FORMS AND STRENGTHS

Injection: 5 mg/100mL (50 mcg/mL) in 100 mL bag
Injection: 12.5 mg/250mL (50 mcg/mL) in 250 mL bag
Injection: 5 mg/100mL (50 mcg/mL) in 100 mL vial
Injection: 3.75 mg/15mL (250 mcg/mL) in 15 mL bolus vial

WARNINGS 

DESCRIPTION 

Tirofiban hydrochloride monohydrate is chemically described as N(butylsulfonyl)-O-[4-(4-piperidinyl)butyl]-L-tyrosine monohydrochloride monohydrate.

CLINICAL PHARMACOLOGY:

When given according to the PRISM-PLUS regimen of 0.4 mcg/kg/min over 30 minutes followed by a 0.1 mcg/kg/min maintenance infusion, >90% inhibition of platelet aggregation is attained by the end of the 30-minute infusion. When given according to the recommended regimen of 25 mcg/kg followed by a 0.15 mcg/kg/min maintenance infusion, >90% inhibition of platelet aggregation is attained within 10 minutes. Platelet aggregation inhibition is reversible following cessation of the infusion of AGGRASTAT.

INDICATIONS AND USAGE 

USE IN SPECIFIC POPULATIONS
Renal Insufficiency: Reduce the dose in patients with severe renal insufficiency.

CONTRAINDICATIONS

PRECAUTIONS

1.  AGGRASTAT can cause serious bleeding. If bleeding cannot be controlled discontinue AGGRASTAT.
2. Thrombocytopenia: Discontinue AGGRASTAT and heparin.

ADVERSE REACTIONS

• Bleeding is the most commonly reported adverse reaction. (6.1)

  To report SUSPECTED ADVERSE REACTIONS, contact Medicure at 1-800-509-0544 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
  DRUG INTERACTIONS

  Coadministration of fibrinolytics, anticoagulants and antiplatelet agents, increases the risk of bleeding.

See PACKAGE INSERT for PATIENT COUNSELING INFORMATION and Medication Guide.

DOSAGE AND ADMINISTRATION 

2.1 Recommended Dosage

The recommended dosage is 25 mcg/kg administered intravenously within 5 minutes and then 0.15 mcg/kg/min for up to 18 hours.

2.2 Administration

For intravenous use only. Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.

Do not use plastic INTRAVIA bags in series connections; such use can result in air embolism by drawing air from the first bag if it is empty of solution.

To open the INTRAVIA bag, first tear off its foil overpouch. The plastic may be somewhat opaque because of moisture absorption during sterilization; the opacity will diminish gradually. Check for leaks by squeezing the inner bag firmly; if any leaks are found or sterility is suspect then the solution should be discarded. Do not use unless the solution is clear and the seal is intact.

Administration Instructions

Withdraw the bolus dose of AGGRASTAT from the 15 mL premixed bolus vial into a syringe. Alternatively, the bolus dose of AGGRASTAT may be administered from the 100 mL premixed vial or from the premixed bags. Do not dilute. Administer the bolus dose within 5 minutes via a syringe or IV pump.
Immediately following the bolus dose administration, administer the maintenance infusion from the 100 mL premixed vial or bags via an IV pump.
Discard any unused portion left in the vial or bag.

The recommended bolus volume using the 15 mL premixed bolus vial can be calculated using the following equation:

Bolus volume (mL) = [25 mcg/kg x body weight (kg)] / 250 mcg/mL

The recommended bolus volume using the 100 mL premixed vial or premixed bags can be calculated using the following equation:

Bolus volume (mL) = [25 mcg/kg x body weight (kg)] / 50 mcg/mL

The recommended infusion rate for patients with CrCl (Creatinine Clearance) >60 mL/min using the 100 mL premixed vial or premixed bags can be calculated using the following equation:

Infusion rate for CrCl > 60 mL/min (mL/hr) = [0.15 mcg/kg/min x body weight (kg) x 60 min/hr] / 50 mcg/mL

Drug Compatibilities
AGGRASTAT can be administered in the same intravenous line as heparin, atropine sulfate, dobutamine, dopamine, epinephrine hydrochloride (HCl), famotidine injection, furosemide, lidocaine, midazolam HCl, morphine sulfate, nitroglycerin, potassium chloride, and propranolol HCl. Do not administer AGGRASTAT through the same IV line as diazepam. Do not add other drugs or remove solution directly from the INTRAVIA bag with a syringe.

2.3 Dose Adjustment for Renal Impairment

The recommended dosage in patients with CrCl </=60 mL/min is 25 mcg/kg intravenously within 5 minutes and then 0.075 mcg/kg/min, for up to 18 hours.

The recommended infusion rate for patients with CrCl </=60 mL/min using the 100 mL premixed vial or premixed bags can be calculated using the following equation:

Infusion rate for CrCl </= 60 mL/min (mL/hr) = [0.075 mcg/kg/min x body weight (kg) x 60 min/hr] / 50 mcg/mL

HOW SUPPLIED 

Injection: 5 mg/100mL (50 mcg/mL) in 100 mL bag
Injection: 12.5 mg/250mL (50 mcg/mL) in 250 mL bag
Injection: 5 mg/100mL (50 mcg/mL) in 100 mL vial
Injection: 3.75 mg/15mL (250 mcg/mL) in 15 mL bolus vial

Storage and Stability

Store AGGRASTAT at controlled room temperature, 25°C (77°F) with excursions permitted between 15-30°C (59-86°F) [see USP]. Do not freeze. Protect from light during storage.