Tirofiban


Generic Medicine Info
Indications and Dosage
Intravenous
Acute coronary syndrome
Adult: In combination with unfractionated heparin and oral antiplatelet therapy, including aspirin: For patients with non-ST-elevation MI (NSTEMI) or unstable angina undergoing percutaneous coronary intervention (PCI) within 4 hours of diagnosis or patients with ST-elevation MI (STEMI) undergoing primary PCI: Initially, 25 mcg/kg given as IV bolus over 3-5 minutes, followed by continuous maintenance infusion rate of 0.15 mcg/kg/min. Initiate treatment at the time of PCI, or it may be given at the time of diagnosis in STEMI, and continue for 12-24 hours. Max treatment duration: 48 hours. For patients with NSTEMI or unstable angina who are managed with early invasive strategy but not planned to undergo angiography for at least 4 hours and up to 48 hours after diagnosis: Initially, 0.4 mcg/kg/min for 30 minutes, followed by continuous maintenance infusion rate of 0.1 mcg/kg/min. Initiate treatment at the time of diagnosis and continue for at least 48 hours. Infusion may be continued during coronary angiography and maintained for 12-24 hours following angioplasty or atherectomy. Max treatment duration: 108 hours. Dosage and treatment recommendations may vary among countries (refer to local guidelines).
Renal Impairment
CrCl (mL/min) Dosage
<30 Reduce dose by 50%.
Dosage recommendations may vary among countries and individual products (refer to specific product guidelines).
Hepatic Impairment
Severe hepatic failure: Contraindicated.
Reconstitution
Inj concentrate for infusion: Aspirate and discard 50 mL or 100 mL of solution from 250 mL or 500 mL bag, respectively, of NaCl 0.9% or dextrose 5% inj and replace this volume with 50 mL (12.5 mg) or 100 mL (25 mg) of tirofiban to achieve a final concentration of 0.05 mg/mL. Mix well before infusion.
Incompatibility
Incompatible with diazepam; do not administer in the same IV line.
Contraindications
History of thrombocytopenia after prior exposure to tirofiban; history of stroke within 30 days or history of haemorrhagic stroke; history of intracranial haemorrhage, intracranial neoplasm, aneurysm, or arteriovenous malformation; active or recent (within the last 30 days) clinically relevant bleeding (e.g. gastrointestinal bleeding); malignant hypertension; relevant trauma or major surgery within the last 6 weeks; thrombocytopenia (platelet count <100,000/mm3) or other platelet disorders, clotting disturbances. Severe hepatic failure.
Special Precautions
Patient with platelet count <150,000/mm3; known history of thrombocytopenia or platelet function disturbance; recent clinically relevant bleeding (<1 year); Hb concentration <11 g/dL or haematocrit <34%, severe acute or chronic heart failure, cardiogenic shock, suspected aortic dissection, acute pericarditis, uncontrolled hypertension; active peptic ulcer (within the last 3 months), haemorrhagic retinopathy, organ biopsy or lithotripsy (within the last 2 weeks), low body weight, active or history of vasculitis, history of cerebrovascular disease (within 1 year). Severe trauma or major surgery >6 weeks but <3 months; traumatic or protracted CPR; puncture of a non-compressible vessel (within 24 hours before tirofiban administration), recent epidural procedure. Discontinue treatment at least 4 hours before CABG surgery. Concomitant use with thrombolytic therapy is not recommended. Female patients. Chronic haemodialysis patients. Renal and mild to moderate hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Profound thrombocytopenia.
Blood and lymphatic system disorders: Anaemia.
Cardiac disorders: Bradycardia, coronary artery dissection.
Gastrointestinal disorders: Nausea, gingival haemorrhage, oral haemorrhage.
General disorders and administration site conditions: Swelling or oedema, fever.
Immune system disorders: Severe hypersensitivity reactions (including anaphylactic reactions).
Injury, poisoning and procedural complications: Postoperative haemorrhage (mainly related to catheterisation sites), vessel puncture site haemorrhage.
Investigations: Occult blood in stool, decreased haematocrit and Hb.
Musculoskeletal and connective tissue disorders: Lower extremity pain.
Nervous system disorders: Headache, dizziness.
Renal and urinary disorders: Haematuria, pelvic pain.
Respiratory, thoracic and mediastinal disorders: Epistaxis, haemoptysis.
Skin and subcutaneous tissue disorders: Ecchymosis, diaphoresis.
Vascular disorders: Haematoma, vasodepressor syncope.
Potentially Fatal: Major bleeding episodes including intracranial, pulmonary (alveolar), or retroperitoneal haemorrhage.
IV/Parenteral: B
Monitoring Parameters
Monitor platelet count, haematocrit and Hb before treatment and within 6 hours after initiating treatment and at least once daily thereafter. Consider earlier monitoring (e.g. within the 1st hour of administration) of platelet count in patients who have previously received glycoprotein IIb/IIIa receptor antagonists. Obtain aPTT before and during treatment to monitor the anticoagulant effects of heparin. Closely monitor for bleeding, particularly in the arterial access site for cardiac catheterisation.
Overdosage
Symptoms: Bleeding, usually mucocutaneous bleeding and localised bleeding at the arterial puncture site for cardiac catheterisation; intracranial haemorrhages and retroperitoneal bleeding have also been reported. Management: Transfusion of blood and/or thrombocytes may be considered. Treatment must be based on patient's condition and assessment of the clinician. Tirofiban may be removed by haemodialysis.
Drug Interactions
Increased risk of bleeding with anticoagulants, thrombolytics, and other antiplatelet agents.
Action
Description:
Mechanism of Action: Tirofiban, a non-peptide tyrosine derivative, is a selective, competitive inhibitor of platelet glycoprotein (GP) IIb/IIIa receptor, which is the major platelet surface receptor involved in platelet aggregation. It blocks the binding of fibrinogen to GP IIb/IIIa receptor, thus inhibiting platelet cross-linking and platelet aggregation.
Onset: >90% inhibition of platelet aggregation (regimen of 25 mcg/kg followed by 0.15 mcg/kg/min infusion): Within 10 minutes.
Pharmacokinetics:
Distribution: Plasma protein binding: 65%.
Excretion: Via urine (approx 65%) and faeces (approx 25%), mainly as unchanged drug. Elimination half-life: Approx 2 hours (range: 1.7-2 hours).
Chemical Structure

Chemical Structure Image
Tirofiban

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 60947, Tirofiban. https://pubchem.ncbi.nlm.nih.gov/compound/Tirofiban. Accessed Jan. 24, 2024.

Storage
Store between 15-30°C. Protect from light. Do not freeze.
MIMS Class
Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics)
ATC Classification
B01AC17 - tirofiban ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
References
Aggrastat Concentrate for Infusion (Aspen Medical Products Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 30/05/2023.

Aggrastat Injection, Solution (Medicure International Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 30/11/2023.

Anon. Tirofiban. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 30/05/2023.

Anon. Tirofiban. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/11/2023.

Buckingham R (ed). Tirofiban Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/05/2023.

Joint Formulary Committee. Tirofiban. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/05/2023.

Tirofiban 50 micrograms/mL Solution for Infusion (Kent Pharma UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 30/11/2023.

Tirofiban. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 30/05/2023.

Disclaimer: This information is independently developed by MIMS based on Tirofiban from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Already a member? Sign in
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Already a member? Sign in