Tirofiban


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Acute coronary syndrome
Adult: In combination w/ unfractioned heparin and oral antiplatelet therapy, including aspirin: Patients w/ ST-elevation MI (STEMI) undergoing primary PCI or patients w/ non-ST-elevation MI (NSTEMI) undergoing PCI w/in 4 hr of diagnosis: Initially, 25 mcg/kg bolus over 3 min followed by a continuous infusion of 0.15 mcg/kg/min for 12-24 hr. Max duration: 48 hr. Patients w/ NSTEMI undergoing PCI >4 hr after diagnosis: Initially, 0.4 mcg/kg/min for 30 min followed by 0.1 mcg/kg/min, started at the time of diagnosis and continued for at least 48 hr. Infusion may be continued during coronary angiography and maintained for 12-24 hr after angioplasty or atherectomy. Max duration: 108 hr.
Renal Impairment
CrCl (mL/min) Dosage
<30 Reduce dose by 50%.
Hepatic Impairment
Severe: Contraindicated.
Hướng dẫn pha thuốc
Aspirate and discard 50 or 100 mL of soln from a 250 or 500 mL bag, respectively, of NaCl 0.9% or dextrose 5% inj and replace this volume w/ 50 mL (12.5 mg) or 100 mL (25 mg) of tirofiban inj to achieve a final concentration of 50 mcg/mL.
Tương kỵ
Y-site admin: Incompatible w/ diazepam.
Chống chỉ định
History of thrombocytopenia during earlier use of GP IIb/IIIa receptor antagonist; history of stroke w/in 30 days or history of haemorrhagic stroke; history of intracranial disease (e.g. neoplasm, aneurysm); active or recent (w/in 30 days) clinically relevant bleeding (e.g. GI bleeding); malignant HTN; relevant trauma or major surgery (w/in the past 6 wk); thrombocytopenia (platelet count <100,000/mm3), disorders of platelet function; clotting disturbances. Severe hepatic failure.
Thận trọng
Patient w/ anaemia, active peptic ulcer (w/in the past 3 mth), uncontrolled HTN, acute pericarditis, active or history of vasculitis, suspected aortic dissection, haemorrhagic retinopathy, occult blood in stool or haematuria, thrombocytopenia (platelet count <150,000/mm3) or known history of platelet function disturbance, recent bleeding (<1 yr), severe CHF, cardiogenic shock. Severe trauma or surgery (>6 wk but <3 mth previously); traumatic or protracted CPR, organ biopsy or lithotripsy (w/in the past 2 wk), puncture of a non-compressible vessel (w/in 24 hr), recent epidural procedure. Renal and mild to moderate hepatic impairment. Pregnancy and lactation.
Phản ứng phụ
Nausea, headache, fever, rashes and other hypersensitivity reactions, thrombocytopenia, anaemia, minor bleeding (e.g. mild mucocutaneous bleeding).
Potentially Fatal: Major bleeding (e.g. intracranial or retroperitoneal haemorrhage).
IV/Parenteral: B
MonitoringParameters
Monitor signs of bleeding, platelet counts, activated thromboplastin time (aPTT), haematocrit and Hb before and periodically (e.g. w/in the first 6 hr of the loading infusion and daily thereafter).
Quá liều
Symptoms: Bleeding, usually at mucocutaneous and cardiac catheterisation sites. Intracranial haemorrhage and retroperitoneal bleeding may also occur. Management: Transfusion of blood and/or thrombocytes may be considered if treatment for haemorrhage is necessary.
Tương tác
Increased risk of bleeding w/ drugs that affect haemostasis including anticoagulants, thrombolytics, other glycoprotein IIb/IIIa inhibitors, platelet aggregation inhibitors.
Tác dụng
Description: Tirofiban is a non-peptide tyrosine derivative that prevents fibrinogen binding to the glycoprotein (GP) IIb/IIIa receptor, leading to inhibition of platelet function, evidenced by its ability to inhibit ex vivo ADP-induced platelet aggregation and prolong bleeding time.
Onset: Inhibition of platelet aggregation: W/in 10 min.
Pharmacokinetics:
Distribution: Volume of distribution: 22-42 L. Plasma protein binding: 65%.
Excretion: Via urine (65%) and faeces (25%) primarily as unchanged drug. Elimination half-life: Approx 2 hr.
Đặc tính

Chemical Structure Image
Tirofiban

Source: National Center for Biotechnology Information. PubChem Database. Tirofiban, CID=60947, https://pubchem.ncbi.nlm.nih.gov/compound/Tirofiban (accessed on Jan. 23, 2020)

Bảo quản
Store between 15-30°C. Protect from light. Do not freeze.
Phân loại ATC
B01AC17 - tirofiban ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
References
Aggrastat Inj, Solution (Medicure International Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 01/07/2016.

Anon. Tirofiban. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/07/2016.

Buckingham R (ed). Tirofiban Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/07/2016.

Joint Formulary Committee. Tirofiban. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/07/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Tirofiban. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/07/2016.

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