Version May 2024
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): $4.48
Solution (Aggrastat Intravenous)
5 mg/100 mL 0.9% (per mL): $1.10
12.5MG/250ML 0.9% (per mL): $1.15
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 drugs which have a heightened risk of causing significant patient harm when used in error.
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 Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Abrocitinib: Agents with Antiplatelet Properties may enhance the antiplatelet effect 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 combination
Acalabrutinib: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): May enhance the antiplatelet effect of other Agents with Antiplatelet Properties. Risk C: Monitor therapy
Anagrelide: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Anticoagulants: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants. Risk C: Monitor therapy
Apixaban: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Apixaban. Specifically, the risk for bleeding may be increased. Management: Carefully consider risks and benefits of this combination and monitor closely. Risk C: Monitor therapy
Bemiparin: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Bemiparin. Management: Avoid concomitant use of bemiparin with antiplatelet agents. If concomitant use is unavoidable, monitor closely for signs and symptoms of bleeding. Risk D: Consider therapy modification
Caplacizumab: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Caplacizumab. Specifically, the risk of bleeding may be increased. Management: Avoid coadministration of caplacizumab with antiplatelets if possible. If coadministration is required, monitor closely for signs and symptoms of bleeding. Interrupt use of caplacizumab if clinically significant bleeding occurs. Risk D: Consider therapy modification
Cephalothin: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Cephalothin. Specifically, the risk for bleeding may be increased. Risk C: Monitor therapy
Collagenase (Systemic): Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Collagenase (Systemic). Specifically, the risk of injection site bruising and or bleeding may be increased. Risk C: Monitor therapy
Dabigatran Etexilate: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Dabigatran Etexilate. Agents with Antiplatelet Properties may increase the serum concentration of Dabigatran Etexilate. This mechanism applies specifically to clopidogrel. Management: Carefully consider risks and benefits of this combination and monitor closely; Canadian labeling recommends avoiding prasugrel or ticagrelor. Risk C: Monitor therapy
Dasatinib: May enhance the anticoagulant effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Deoxycholic Acid: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Deoxycholic Acid. Specifically, the risk for bleeding or bruising in the treatment area may be increased. Risk C: Monitor therapy
Edoxaban: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Edoxaban. Specifically, the risk of bleeding may be increased. Risk C: Monitor therapy
Enoxaparin: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Enoxaparin. Management: Discontinue antiplatelet agents prior to initiating enoxaparin whenever possible. If concomitant administration is unavoidable, monitor closely for signs and symptoms of bleeding. Risk D: Consider therapy modification
Heparin: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Heparin. Management: Decrease the dose of heparin or agents with antiplatelet properties if coadministration is required. Risk D: Consider therapy modification
Herbal Products with Anticoagulant/Antiplatelet Effects (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Bleeding may occur. Risk C: Monitor therapy
Ibritumomab Tiuxetan: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Ibritumomab Tiuxetan. Both agents may contribute to impaired platelet function and an increased risk of bleeding. Risk C: Monitor therapy
Ibrutinib: May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Icosapent Ethyl: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Inotersen: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Lecanemab: May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Specifically, the risk of hemorrhage may be increased. Risk C: Monitor therapy
Limaprost: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Lipid Emulsion (Fish Oil Based): May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Multivitamins/Fluoride (with ADE): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Multivitamins/Minerals (with ADEK, Folate, Iron): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Multivitamins/Minerals (with AE, No Iron): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Obinutuzumab: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Obinutuzumab. Specifically, the risk of serious bleeding-related events may be increased. Risk C: Monitor therapy
Omega-3 Fatty Acids: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Pentosan Polysulfate Sodium: May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Specifically, the risk of bleeding may be increased by concurrent use of these agents. Risk C: Monitor therapy
Pentoxifylline: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Pirtobrutinib: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Rivaroxaban: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Rivaroxaban. Management: Carefully consider risks and benefits of this combination and monitor closely; Canadian labeling recommends avoiding prasugrel or ticagrelor. Risk C: Monitor therapy
Selumetinib: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Thrombolytic Agents: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents. Risk C: Monitor therapy
Tipranavir: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Urokinase: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Urokinase. Risk X: Avoid combination
Vitamin E (Systemic): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
Zanubrutinib: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Risk C: Monitor therapy
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).
آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟
