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Medically reviewed by Fedorchenko Olga Valeryevna, PharmD. Last updated on 24.05.2022
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Intravenous
Acute coronary syndrome
Adult: Loading dose: 0.4 mcg/kg/minute for 30 minutes followed by 0.1 mcg/kg/minute.
Patients undergoing percutaneous coronary intervention (PCI): Loading dose: 0.4 mcg/kg/minute for 30 minutes followed by 0.1 mcg/kg/minute given during angiography and for 12-24 hr after angioplasty or atherectomy. Patients who require CABG: Discontinue Tirofiban at least 4-6 hr before CABG. All patients should receive aspirin before start of Tirofiban therapy and unfractionated heparin simultaneously with the start of Tirofiban therapy, unless contra-indicated. Max duration of treatment: 108 hr.
Tirofiban injection is used to prevent blood clots from forming in the arteries of the heart after certain types of chest pain and heart attacks. It may also be used in patients who are having certain heart and blood vessel procedures.
Tirofiban is an antiplatelet medicine. It reduces the chance that a harmful clot will form by preventing certain cells in the blood from clumping together.
Tirofiban is to be given only by or under the direct supervision of your doctor.
The vial of Tirofiban (concentrate) must be diluted prior to administration.
Tirofiban is for IV use only using sterile equipment. Tirofiban may be co-administered with heparin through the same line.
Tirofiban is recommended for use with a calibrated infusion device. Care should be taken to avoid a prolonged loading infusion. Care should also be taken in calculating the bolus dose and infusion rates based on patient weight.
In clinical studies, patients received aspirin, unless contraindicated.
Unstable Angina Pectoris or Non-Q-Wave Myocardial Infarction: Tirofiban should be administered IV, in combination with heparin, at the initial infusion rate of 0.4 mcg/kg/min for 30 min. Upon completion of the initial infusion, Tirofiban should be continued at a maintenance infusion rate of 0.1 mcg/kg/min. Table 1 is provided as a guide to dosage adjustment by weight.
In the study that demonstrated efficacy, Tirofiban, in combination with heparin was generally continued for a minimum of 48 hrs and up to 108 hrs on average, patients received Tirofiban for 71.3 hrs. This infusion can be continued through angiography and should be continued up to 12-24 hrs post-angioplasty/atherectomy. Arterial sheaths should be removed when the patient's activated clotting time is <180 sec or 2-6 hrs following cessation of heparin.
Angioplasty/Atherectomy: In patients in whom Tirofiban is initiated in the setting of angioplasty/atherectomy, Tirofiban should be administered IV, in combination with heparin, as an initial bolus of 10 mcg/kg administered over 3 min followed by a maintenance infusion rate of 0.15 mcg/kg/min. Table 2 is provided as a guide to dosage adjustment by weight.
The Tirofiban maintenance infusion should be administered for 36 hrs. Upon completion of the procedure, heparin should be discontinued and arterial sheaths should then be removed when the patient's activated clotting time is <180 sec.
Patients with Severe Renal Insufficiency: As specified in Tables 1 and 2, the dosage of Tirofiban should be decreased by 50% in patients with severe renal insufficiency [creatinine clearance (CrCl) <30 mL/min].
Other Patient Populations: No dosage adjustment is recommended for elderly patients or female patients.
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What is the most important information I should know about Tirofiban?
Do not receive this medication if you are allergic to Tirofiban, or to similar drugs such as abciximab (ReoPro) or eptifibatide (Integrilin).
Do not receive this medication if you have a stomach ulcer or ulcerative colitis, severe liver disease, severe high blood pressure, a bleeding or blood clotting disorder, a history of head injury, brain tumor, or blood clot in the brain (aneurysm), a stroke or any type of bleeding within the past 30 days, or any type of surgery, injury, or medical emergency within the past 6 weeks.
Tirofiban is not expected to be harmful to an unborn baby. However, aspirin is sometimes given with Tirofiban, and aspirin can cause bleeding when it is taken during the last 3 months of pregnancy. Aspirin can also cause side effects in a newborn baby.
Tell your doctor if you are pregnant or plan to become pregnant during treatment with Tirofiban and aspirin.
Because Tirofiban keeps your blood from coagulating (clotting) to prevent unwanted blood clots, it can also make it easier for you to bleed, even from a minor injury. Contact your doctor or seek emergency medical attention if you have bleeding that will not stop.
Use Tirofiban as directed by your doctor. Check the label on the medicine for exact dosing instructions.
- Tirofiban is usually administered as an injection at your doctor's office, hospital, or clinic. If you are using Tirofiban at home, carefully follow the injection procedures taught to you by your health care provider.
- If Tirofiban contains particles or is discolored, or if the vial is cracked or damaged in any way, do not use it.
- Tirofiban is only to be injected into the vein or artery.
- Keep this product, as well as syringes and needles, out of the reach of children and away from pets. Do not reuse needles, syringes, or other materials. Dispose of properly after use. Ask your doctor or pharmacist to explain local regulations for proper disposal.
- If you miss a dose of Tirofiban, contact your doctor immediately.
Ask your health care provider any questions you may have about how to use Tirofiban.
There are specific as well as general uses of a drug or medicine. A medicine can be used to prevent a disease, treat a disease over a period or cure a disease. It can also be used to treat the particular symptom of the disease. The drug use depends on the form the patient takes it. It may be more useful in injection form or sometimes in tablet form. The drug can be used for a single troubling symptom or a life-threatening condition. While some medications can be stopped after few days, some drugs need to be continued for prolonged period to get the benefit from it.Use: Labeled Indications
Unstable angina/non-ST-elevation myocardial infarction: 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 [UA/NSTEMI]).
Off Label Uses
To support PCI (administered at the time of PCI) for ST-elevation myocardial infarction (STEMI)
Data from one double-blinded, randomized, controlled trial and one open-label, randomized, controlled trial supports the use of high-bolus dose Tirofiban in the management of patients with STEMI undergoing primary PCI. Additional trials may be necessary to further define the role of Tirofiban in this setting.
Based on the American College of Cardiology Foundation/American Heart Association/Society for Cardiovascular Angiography and Interventions (ACCF/AHA/SCAI) guidelines for PCI, a glycoprotein IIb/IIIa inhibitor including Tirofiban (high-bolus dose) given to support elective PCI is effective and recommended in the management of patients with stable ischemic heart disease and high risk features undergoing PCI.
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What other drugs will affect Tirofiban?
Tirofiban has been studied on a background of aspirin and heparin.
The use of Tirofiban, in combination with heparin and aspirin, has been associated with an increase in bleeding compared to heparin and aspirin alone. Caution should be employed when Tirofiban is used with other drugs that affect hemostasis (eg, warfarin).
Tirofiban has been used concomitantly in clinical studies with β-blockers, calcium-channel blockers, nonsteroidal anti-inflammatory agents (NSAIDs) and nitrate preparations without evidence of clinically significant adverse interactions.
In a subset of patients (n=762) in the PRISM study, the plasma clearance of Tirofiban in patients receiving one of the following drugs was compared to that in patients not receiving that drug. There were no clinically significant interactions of these drugs on the plasma clearance of Tirofiban: Acebutolol, acetaminophen, alprazolam, amlodipine, aspirin preparations, atenolol, bromazepam, captopril, diazepam, digoxin, diltiazem, docusate sodium, enalapril, furosemide, glyburide, heparin, insulin, isosorbide, levothyroxine, lorazepam, lovastatin, metoclopramide, metoprolol, morphine, nifedipine, nitrate preparations, omeprazole, oxazepam, potassium chloride, propranolol, ranitidine, simvastatin, sucralfate and temazepam.
See also:
What are the possible side effects of Tirofiban?
Clinical Trial Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
In the PRISM (Platelet Receptor Inhibition for Ischemic Syndrome Management), PRISM-PLUS (Platelet Receptor Inhibition for Ischemic Syndrome Management — Patients Limited by Unstable Signs and Symptoms) and RESTORE (Randomized Efficacy Study of Tirofiban for Outcomes and Restenosis) trials, 1946 patients received Tirofiban in combination with heparin and 2002 patients received Tirofiban alone for about 3 days. Forty-three percent of the population was >65 years of age and approximately 30% of patients were female. In clinical studies with the recommended regimen (25 mcg/kg bolus followed by a 0.15 mcg/kg/min maintenance infusion), Tirofiban was administered in combination with aspirin, clopidogrel and heparin or bivalirudin to over 8000 patients for typically ≤24 hours. Approximately 30% of the population was >65 years of age and approximately 25% were female.
Bleeding
PRISM-PLUS Regimen
The incidences of major and minor bleeding using the TIMI criteria in the PRISM-PLUS study are shown below.
The incidence rates of TIMI major bleeding in patients undergoing percutaneous procedures in PRISM-PLUS are shown below.
The incidence rates of TIMI major bleeding in patients undergoing coronary artery bypass graft surgery (CABG) in PRISM-PLUS within one day of discontinuation of Tirofiban were 17% on Tirofiban plus heparin (N=29) and 35% on heparin alone (N=31).
Recommended (“High-Dose Bolus”) Regimen
Rates of major bleeds (including any intracranial, intraocular or retroperitoneal hemorrhage, clinically overt signs of hemorrhage associated with a drop in hemoglobin of >3 g/dL or any drop in hemoglobin by 4g/dL, bleeding requiring transfusion of >2U blood products, bleeding directly resulting in death within 7 days or hemodynamic compromise requiring intervention) were consistent with the rates observed in subjects administered the PRISM-PLUS regimen of Tirofiban. There was a trend toward greater bleeding in ST segment elevation myocardial infarction (STEMI) patients treated with fibrinolytics prior to administration of Tirofiban using the recommended regimen during rescue PCI.
Non-Bleeding
The incidences of non-bleeding adverse events that occurred at an incidence of >1% and numerically higher than control, regardless of drug relationship, are shown below:
Thrombocytopenia
Patients treated with Tirofiban plus heparin, were more likely to experience decreases in platelet counts than were those on heparin alone. These decreases were reversible upon discontinuation of Tirofiban. The percentage of patients with a decrease of platelets to <90,000/mm3 was 1.5%, compared with 0.6% in the patients who received heparin alone. The percentage of patients with a decrease of platelets to <50,000/mm3 was 0.3%, compared with 0.1% of the patients who received heparin alone.
Post-Marketing Experience
The following additional adverse reactions have been identified during post-approval use of Tirofiban. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to the drug exposure.
Hypersensitivity: Severe allergic reactions including anaphylactic reactions have occurred during the first day of Tirofiban infusion, during initial treatment, and during readministration of Tirofiban. Some cases have been associated with severe thrombocytopenia (platelet counts <10,000/mm3). No information is available on the formation of antibodies to Tirofiban.
Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide reversible antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation.