Acute coronary syndrome:
Note: Initial therapy for acute coronary syndrome (ACS) typically includes oral antiplatelet therapy (eg, aspirin plus a P2Y12 inhibitor) and an IV anticoagulant (eg, bivalirudin or heparin). A glycoprotein (GP) IIb/IIIa inhibitor is not routinely used due to limited benefit on ischemic outcomes and more bleeding complications. However, use may be considered in high-risk patients (eg, significant thrombus burden) when percutaneous coronary intervention (PCI) is planned (Ref).
Non-ST elevation acute coronary syndrome:
IV: Loading dose: 25 mcg/kg administered over ≤5 minutes beginning after diagnostic coronary angiography, just before PCI; maintenance infusion: 0.15 mcg/kg/minute continued for up to 18 hours (Ref).
ST-elevation myocardial infarction (off-label use):
IV: Loading dose: 25 mcg/kg administered over ≤5 minutes beginning after diagnostic coronary angiography, just before PCI; maintenance infusion: 0.15 mcg/kg/minute continued for up to 18 hours (Ref).
Note : If CABG is performed, discontinue tirofiban ≥4 hours before surgery (Ref).
Note: Renal function may be estimated using the Cockcroft-Gault formula using actual body weight.
CrCl >60 mL/minute: No dosage reduction necessary.
CrCl ≤60 mL/minute: IV Loading dose: 25 mcg/kg administered over ≤5 minutes; Maintenance infusion: 0.075 mcg/kg/minute continued for up to 18 hours.
Hemodialysis: Dialyzable: Yes (Ref).
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults and may include incidence in combination with heparin.
>10%: Hematologic & oncologic: Hemorrhage (11%; major hemorrhage: 1%)
1% to 10%:
Cardiovascular: Bradycardia (4%), coronary artery dissection (5%), edema (≤2%), vasodepressor syncope (2%)
Dermatologic: Diaphoresis (2%)
Genitourinary: Pelvic pain (6%)
Hematologic & oncologic: Thrombocytopenia (≤2%)
Nervous system: Dizziness (3%)
Neuromuscular & skeletal: Lower extremity pain (3%)
Miscellaneous: Swelling (≤2%)
Postmarketing:
Hematologic & oncologic: Severe anemia (Sakellariou 2009)
Hypersensitivity: Anaphylaxis, severe hypersensitivity reaction
Severe hypersensitivity reaction (ie, anaphylactic reaction) to tirofiban or any component of the formulation; history of thrombocytopenia following prior exposure to tirofiban; active internal bleeding or a history of bleeding diathesis, major surgical procedure, or severe physical trauma within the previous month
Canadian labeling: Additional contraindications (not in US labeling): History of thrombocytopenia following prior exposure to any other GPIIb/IIIa inhibitor; recent (within the previous 30 days) internal bleeding; history of intracranial hemorrhage or neoplasm, arteriovenous malformation, or aneurysm; history, symptom or findings suggestive of aortic dissection; known coagulopathy, platelet disorder or history of thrombocytopenia; stroke within 30 days prior to hospitalization or any history of hemorrhagic stroke; major surgical procedure or relevant trauma within the previous 6 weeks; malignant or severe uncontrolled hypertension (>180 mmHg/110 mmHg); current use with other GP IIb/IIIa inhibitors; acute pericarditis; cirrhosis or clinically significant liver disease; angina precipitated by obvious provoking factors (eg, arrhythmia, severe anemia, hyperthyroidism, hypotension); recent epidural procedure.
Concerns related to adverse effects:
• Bleeding: The most common complication is bleeding, including retroperitoneal, pulmonary, and spontaneous GI and/or GU bleeding; watch closely for bleeding, especially the arterial access site for the cardiac catheterization. Fatal bleeding has been reported. Use with extreme caution in patients with platelet counts <150,000/mm3, patients with hemorrhagic retinopathy, previous history of GI disease, recent thrombolytic therapy and in chronic dialysis patients. Use caution with administration of other drugs affecting hemostasis. Minimize other procedures including arterial and venous punctures, IM injections, nasogastric tubes, etc.
• Thrombocytopenia: Profound thrombocytopenia has been reported with use of tirofiban. If during therapy platelet count decreases to <90,000/mm3, monitor platelet counts to exclude pseudothrombocytopenia. If thrombocytopenia is confirmed, discontinue tirofiban and heparin if administered concurrently. Platelet counts should recover rapidly (within 1 to 5 days) after discontinuation. Previous exposure to a glycoprotein IIb/IIIa inhibitor may increase the risk of thrombocytopenia. Use is contraindicated in patients with a history of thrombocytopenia following exposure to tirofiban. Specific management guidelines for GP IIb/IIIa induced thrombocytopenia have been published (Huxtable 2006; Llevadot 2000).
Disease-related concerns:
• Renal impairment: Dosage reduction of the maintenance infusion rate is necessary in patients with CrCl ≤60 mL/minute.
Other warnings/precautions:
• Percutaneous coronary intervention: Sheath removal: Prior to pulling the sheath, ACT should be <180 seconds or aPTT <50 seconds. Use standard compression techniques after sheath removal. Watch the site closely afterwards for further bleeding.
• Surgery: Discontinue at least 4 hours prior to coronary artery bypass graft surgery (ACC/AHA [Lawton 2022]).
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Concentrate, Intravenous:
Aggrastat: 3.75 mg/15 mL (15 mL)
Solution, Intravenous:
Aggrastat: 5 mg/100 mL in NaCl 0.9% (100 mL); 12.5 mg/250 mL in NaCl 0.9% (250 mL)
Solution, Intravenous [preservative free]:
Generic: 12.5 mg/250 mL in NaCl 0.9% (250 mL); 5 mg/100 mL in NaCl 0.9% (100 mL)
May be product dependent
Concentrate (Aggrastat Intravenous)
3.75 mg/15 mL (per mL): $4.69
Solution (Aggrastat Intravenous)
5 mg/100 mL 0.9% (per mL): $0.65
12.5MG/250ML 0.9% (per mL): $0.51
Solution (Tirofiban HCl in NaCl Intravenous)
5 mg/100 mL 0.9% (per mL): $1.05
12.5MG/250ML 0.9% (per mL): $0.77 - $1.09
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous:
Aggrastat: 12.5 mg/250 mL in NaCl 0.9% (250 mL)
IV: Administer loading dose over 5 minutes or less, followed by a continuous infusion. Note: Clinical trials administered tirofiban loading dose over a period of 3 minutes (Ref).
Non-ST elevation acute coronary syndromes: To decrease the rate of thrombotic cardiovascular events (combined end point of death, MI, or refractory ischemia/repeat cardiac procedure) in patients with non-ST-elevation acute coronary syndrome (unstable angina/non-ST-elevation myocardial infarction).
ST-elevation myocardial infarction
Aggrastat may be confused with Aggrenox, argatroban
The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes (glycoprotein IIb/IIIa inhibitor) which have a heightened risk of causing significant patient harm when used in error (High-Alert Medications in Acute Care Settings).
Tirofiban is identified in the Screening Tool of Older Person's Prescriptions (STOPP) criteria as a potentially inappropriate medication in older adults (≥65 years of age) at increased risk of bleeding (eg, gastric antral vascular ectasia, recent significant spontaneous bleeding, severe uncontrolled hypertension, bleeding diathesis) or as use for stroke prevention in patients with chronic atrial fibrillation (other agents preferred) (O’Mahony 2023).
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Abrocitinib: Therapeutic Antiplatelets may increase antiplatelet effects of Abrocitinib. Management: Do not use antiplatelet drugs with abrocitinib during the first 3 months of abrocitinib therapy. The abrocitinib prescribing information lists this combination as contraindicated. This does not apply to low dose aspirin (81 mg/day or less). Risk X: Avoid
Acalabrutinib: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Aducanumab: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Agents with Antiplatelet Effects: May increase antiplatelet effects of Glycoprotein IIb/IIIa Inhibitors. Risk C: Monitor
Anagrelide: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Anticoagulants (Miscellaneous Agents): Therapeutic Antiplatelets may increase anticoagulant effects of Anticoagulants (Miscellaneous Agents). Risk C: Monitor
Antiplatelet Agents (P2Y12 Inhibitors): Therapeutic Antiplatelets may increase antiplatelet effects of Antiplatelet Agents (P2Y12 Inhibitors). Risk C: Monitor
Caplacizumab: May increase antiplatelet effects of Therapeutic Antiplatelets. Management: Avoid this combination if possible. If coadministration is required, monitor closely for bleeding. Interrupt caplacizumab if clinically significant bleeding occurs and administer von Willebrand factor concentrate to rapidly correct hemostasis, if needed. Risk D: Consider Therapy Modification
Collagenase (Systemic): Therapeutic Antiplatelets may increase adverse/toxic effects of Collagenase (Systemic). Specifically, the risk of injection site bruising and or bleeding may be increased. Risk C: Monitor
Dasatinib: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Deoxycholic Acid: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Desirudin: Therapeutic Antiplatelets may increase anticoagulant effects of Desirudin. Risk C: Monitor
Direct Oral Anticoagulants (DOACs): Glycoprotein IIb/IIIa Inhibitors may increase anticoagulant effects of Direct Oral Anticoagulants (DOACs). Risk C: Monitor
Donanemab: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Fondaparinux: Glycoprotein IIb/IIIa Inhibitors may increase anticoagulant effects of Fondaparinux. Management: Discontinue antiplatelet agents, such as glycoprotein IIb/IIIa inhibitors, prior to fondaparinux therapy, if possible. If co-administration is required, use caution and monitor patients closely for signs and symptoms of bleeding. Risk D: Consider Therapy Modification
Glycoprotein IIb/IIIa Inhibitors: Therapeutic Antiplatelets may increase anticoagulant effects of Glycoprotein IIb/IIIa Inhibitors. Risk C: Monitor
Heparin: Glycoprotein IIb/IIIa Inhibitors may increase anticoagulant effects of Heparin. Risk C: Monitor
Heparins (Low Molecular Weight): Glycoprotein IIb/IIIa Inhibitors may increase anticoagulant effects of Heparins (Low Molecular Weight). Risk C: Monitor
Herbal Products with Anticoagulant/Antiplatelet Effects: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Ibritumomab Tiuxetan: Therapeutic Antiplatelets may increase antiplatelet effects of Ibritumomab Tiuxetan. Risk C: Monitor
Ibrutinib: Therapeutic Antiplatelets may increase adverse/toxic effects of Ibrutinib. Specifically, the risks of bleeding and hemorrhage may be increased. Risk C: Monitor
Icosapent Ethyl: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Inotersen: Therapeutic Antiplatelets may increase adverse/toxic effects of Inotersen. Specifically, the risk of bleeding may be increased. Risk C: Monitor
Lecanemab: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Limaprost: May increase adverse/toxic effects of Therapeutic Antiplatelets. Specifically, the risk of bleeding may be increased. Risk C: Monitor
Lipid Emulsion (Fish Oil Based): May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Miscellaneous Antiplatelets: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Multivitamins/Fluoride (with ADE): May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Multivitamins/Minerals (with ADEK, Folate, Iron): May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Multivitamins/Minerals (with AE, No Iron): May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Obinutuzumab: Therapeutic Antiplatelets may increase adverse/toxic effects of Obinutuzumab. Specifically, the risk of bleeding may be increased. Management: Consider avoiding coadministration of obinutuzumab and therapeutic antiplatelets, especially during the first cycle of obinutuzumab therapy. Risk D: Consider Therapy Modification
Omega-3 Fatty Acids: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Pentosan Polysulfate Sodium: Therapeutic Antiplatelets may increase adverse/toxic effects of Pentosan Polysulfate Sodium. Specifically, the risk of hemorrhage may be increased. Risk C: Monitor
Pirtobrutinib: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Selumetinib: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Therapeutic Antiplatelets: May increase anticoagulant effects of Glycoprotein IIb/IIIa Inhibitors. Risk C: Monitor
Thrombolytic Agents: Therapeutic Antiplatelets may increase adverse/toxic effects of Thrombolytic Agents. Specifically, the risk of bleeding may be increased. Risk C: Monitor
Tipranavir: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Vitamin E (Systemic): May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Vitamin K Antagonists: Glycoprotein IIb/IIIa Inhibitors may increase anticoagulant effects of Vitamin K Antagonists. Risk C: Monitor
Volanesorsen: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Zanubrutinib: May increase antiplatelet effects of Therapeutic Antiplatelets. Risk C: Monitor
Information related to use in pregnancy is limited (Boztosun 2008; Hajj-Chahine 2010).
It is not known if tirofiban is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Platelet count (baseline; 6 hours after initiation and daily thereafter during therapy). Monitor platelet counts more closely in patients who have had previous exposure to glycoprotein IIb/IIa antagonists. Persistent reductions of platelet counts <90,000/mm3 may require interruption or discontinuation of infusion; hemoglobin and hematocrit; signs of bleeding.
Standard post-PCI assessment if patient undergoes PCI (eg, monitoring vascular access site, monitoring for chest pain and signs of bleeding)
A reversible antagonist of fibrinogen binding to the glycoprotein (GP) IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation. When administered intravenously, it inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner. When given according to the recommended regimen, >90% inhibition is attained within 10 minutes after initiation. Platelet aggregation inhibition is reversible following cessation of the infusion.
Onset: >90% inhibition of platelet aggregation (reversible after discontinuation) seen within 10 minutes
Distribution: Vdss: 22 to 42 L
Protein Binding: 65% (concentration dependent)
Metabolism: Negligible
Half-life elimination: 2 hours; Note: In ~90% of patients, ex vivo platelet aggregation returns to near baseline in 4 to 8 hours after discontinuation.
Excretion: Urine (65%) and feces (25%) primarily as unchanged drug
Altered kidney function: Plasma clearance is decreased by ~40% in patients with CrCl <60 mL/minute and more than 50% in patients with CrCl <30 mL/minute (including those requiring hemodialysis).