Argatroban


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Treatment and prophylaxis of thrombosis in patients with heparin-induced thrombocytopenia
Adult: Initially, 2 mcg/kg/min by continuous infusion. Check aPTT after 2 hr and adjust dose until steady-state aPTT is 1.5-3 times the initial baseline value, not exceeding 100 seconds. Max: 10 mcg/kg/min. Patients who has undergone cardiac surgery, critically ill patients/intensive care unit patients w/ multiple organ failure: Initially, 0.5 mcg/kg/min, then adjust to the target aPTT range.

Intravenous
Anticoagulant in percutaneous coronary intervention
Adult: Initially, 25 mcg/kg/min by infusion and 350 mcg/kg by bolus inj given simultaneously over 3-5 min. Check activated clotting time (ACT) 5-10 min after the bolus dose is completed, procedure may proceed if ACT is >300 seconds; if ACT is <300 seconds, an additional bolus dose of 150 mcg/kg may be given, adjust infusion rate to 15-40 mcg/kg/min then check ACT after 5-10 min.
Hepatic Impairment
Treatment and prophylaxis of thrombosis in patients w/ heparin-induced thrombocytopenia:
Moderate: Initially, 0.5 mcg/kg/min. Severe: Contraindicated.
Hướng dẫn pha thuốc
Dilute in NaCl 0.9%, dextrose 5% or lactated Ringer’s inj to a final concentration of 1 mg/mL.
Tương kỵ
Incompatible w/ amiodarone.
Chống chỉ định
Active major bleeding. Severe hepatic impairment.
Thận trọng
Disease states and other circumstances in which there is an increased risk of haemorrhage (e.g. severe HTN, major surgery). Critically ill patients. Moderate hepatic impairment. Childn. Pregnancy and lactation.
Phản ứng phụ
Haemorrhagic effects (e.g. GI bleeding, haematuria, hemoptysis), hypotension, fever, dyspnoea, diarrhoea, sepsis, nausea, cardiac arrest, ventricular tachycardia, pain, UTI, vomiting, infection, pneumonia, AF, cough, abnormal renal function, abdominal pain, cerebrovascular disorder, chest and back pain, headache, MI, bradycardia.
IV/Parenteral: B
MonitoringParameters
Monitor Hb, haematocrit, signs/symptoms of bleeding; aPTT, ACT.
Quá liều
Symptoms: Excessive anticoagulation w/ or w/o bleeding. Management: Symptomatic and supportive treatment.
Tương tác
Increased risk of bleeding w/ antiplatelet agents, thrombolytics and other anticoagulants. Increased INR and prothrombin time w/ warfarin.
Tác dụng
Description: Argatroban is a synthetic direct thrombin inhibitor which reversibly binds to the active thrombin site of free and clot-associated thrombin. It exerts its anticoagulant effects by inhibiting thrombin-catalysed or -induced reactions, e.g. fibrin formation; activation of coagulation factors V, VIII, and XIII; activation of protein C; and platelet aggregation.
Onset: Immediate.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Steady-state: 1-3 hr.
Distribution: Distributed mainly in the extra-cellular fluid. Volume of distribution: 174 mL/kg. Plasma protein binding: 20% (albumin); 34% (α1-acid glycoprotein).
Metabolism: Undergoes hepatic metabolism mainly via hydroxylation and aromatisation; also metabolised by CYP3A4/5 isoenzymes to form 4 known metabolites.
Excretion: Primarily in the faeces via the bile, as metabolites and at least 14% as unchanged drug; via urine (approx 16% as unchanged drug). Terminal elimination half-life: 39-51 min.
Đặc tính

Chemical Structure Image
Argatroban

Source: National Center for Biotechnology Information. PubChem Database. Argatroban, CID=92722, https://pubchem.ncbi.nlm.nih.gov/compound/Argatroban (accessed on Jan. 21, 2020)

Bảo quản
Store between 20-25°C. Do not freeze. Protect from light.
Phân loại ATC
B01AE03 - argatroban ; Belongs to the class of direct thrombin inhibitors. Used in the treatment of thrombosis.
References
Anon. Argatroban . Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/01/2016.

Argatroban Injection, Solution (Teva Parenteral Medicines, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/01/2016.

Buckingham R (ed). Argatroban. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/01/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Argatroban. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 05/01/2016.

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