Tirofiban

What is Tirofiban?

• Tirofiban (Aggrastat) is a platelet aggregation inhibitor, a non-peptide antagonist of the platelet GP IIb/IIIa receptor used to reduce the rate of thrombotic cardiovascular events (combined endpoint of death, myocardial infarction, or refractory ischemia/repeat cardiac procedure) in patients with non-ST elevation acute coronary syndrome.

Tirofiban

Tirofiban Structural Formulae

Tirofiban ball-and-stick

What are the uses of this medicine?

• Tirofiban (Aggrastat) is used to reduce the rate of thrombotic cardiovascular events (combined endpoint of death, myocardial infarction, or refractory ischemia/repeat cardiac procedure) in patients with non-ST elevation acute coronary syndrome.

How does this medicine work?

• Tirofiban - a non peptide tyrosine derivative, with anticoagulant activity.
• Upon administration, tirofiban antagonizes fibrinogen binding to the platelet cell surface receptor, glycoprotein (gp) iib/iiia complex, one of the two purinergic receptors activated by adp.
• This prevents the gp iib/iiia receptor complex mediated activation of adenylyl cyclase.
• This results in decreased levels of camp, interferes with the platelet membrane function and subsequent platelet platelet interaction, prevents the release of platelet granule constituents and prolongs bleeding time.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Severe hypersensitivity reaction to Aggrastat (i.e., anaphylactic reactions).
• A history of thrombocytopenia following prior exposure to Aggrastat.
• Active internal bleeding or a history of bleeding diathesis, major surgical procedure or severe physical trauma within the previous month.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to tell your doctor or pharmacist if you are taking the following medications or have stopped taking them within the past two weeks:

• fibrinolytics
• anticoagulants
• antiplatelet drugs

Is this medicine FDA approved?

• According to the US Orange Book, it was first approved in the US on 20 April 2000.
• Tirofiban has been available as a generic medication in the United States since April 2021.

How should this medicine be used?

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.
• In patients with creatinine clearance ≤60 mL/min, give 25 mcg/kg within 5 minutes and then 0.075 mcg/kg/min.

Administration:

• For intravenous use only.
• Administer the bolus dose within 5 minutes via a syringe or IV pump.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection: 12.5 mg/250mL (50 mcg/mL) in 250 mL bag.
• Injection: 5 mg/100mL (50 mcg/mL) in 100 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.

This medicine is available in fallowing brand namesː

• Aggrastat

What side effects can this medication cause?

The most common side effects of this medicine include:

• Bleeding
• Edema/swelling
• pelvic Pain
• vasovagal Reaction
• [[Bradycardia
• coronary artery Dissection
• Dizziness
• Sweating
• Thrombocytopenia

What special precautions should I follow?

• Bleeding is the most common complication encountered during therapy with Aggrastat. Concomitant use of fibrinolytics, anticoagulants and antiplatelet drugs increases the risk of bleeding. If bleeding cannot be controlled discontinue Aggrastat.
• Profound thrombocytopenia has been reported with Aggrastat. Monitor platelet counts beginning about 6 hours after treatment initiation and daily thereafter. If thrombocytopenia is confirmed, discontinue Aggrastat and heparin. Previous exposure to a glycoprotein (GP) IIb/IIIa receptor antagonist may increase the risk of developing thrombocytopenia.
• Advise patients to discuss with their health care provider their use of any other medications, including over-the-counter or herbal products prior to Aggrastat use.
• There is no data on the presence of tirofiban in human milk, the effects of the drug on the breastfed infant, or the effects of the drug on human milk production.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• bleeding
• primarily minor mucocutaneous bleeding events
• minor bleeding at the sites of cardiac catheterization

Management of overdosage:

• Overdosage of Aggrastat should be treated by assessment of the patient’s clinical condition and cessation or adjustment of the drug infusion as appropriate.
• Aggrastat can be removed by hemodialysis.

Can this medicine be used in pregnancy?

• Untreated myocardial infarction can be fatal to the pregnant woman and fetus.
• Available published case reports have not established an association with tirofiban use during pregnancy and major birth defects, miscarriage, or adverse maternal or fetal outcomes.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredients:

• TIROFIBAN HYDROCHLORIDE

Inactive Ingredients:

• ANHYDROUS CITRIC ACID
• TRISODIUM CITRATE DIHYDRATE
• SODIUM CHLORIDE
• WATER

Who manufactures and distributes this medicine?

Aggrastat is manufactured for:

• MEDICURE INTERNATIONAL, INC.

by:

• EMERGENT BIOSOLUTIONS
• Baltimore, Maryland USA

And

• LABORATORIOS GRIFOLS S.A
• Parets del Vallès (Barcelona), Spain

Distributed by:

• MEDICURE PHARMA, INC.
• Princeton, NJ USA

What should I know about storage and disposal of this medication?

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

• Dailymed label info on Tirofiban
• FDA Tirofiban