1. Brief Introduction of Argatroban

Argatroban (CAS No. 74863-84-6) is an anticoagulant that is a small molecule direct thrombin inhibitor and the molecular formula of argatroban is C₂₃H₃₆N₆O₅S•H₂O. Its chemical name is 1-[5-[(aminoiminomethyl) amino]-1-oxo2[[(1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2- piperidinecarboxylic acid, monohydrate. Argatroban Injection is a white, non-pyrogenic, clear, colorless to pale yellow, aqueous solution.

2. Argatroban Dose

Each 50 mL glass Vial contains 50 mg argatroban (1 mg/mL); and, as supplied, is ready for intravenous infusion. Dilution is not required. The argatroban dose in different diseases is not the same.

1) Argatroban Dose in Patients with Heparin-Induced Thrombocytopenia

Initial Dosage: Before administering argatroban, discontinue heparin therapy and obtain a baseline aPTT. The recommended initial argatroban dose for adult patients without hepatic impairment is 2 mcg/kg/min, administered as a continuous infusion.

Dosage Adjustment: After the initiation of Argatroban Injection, adjust the argatroban dose (not to exceed 10 mcg/kg/min) as necessary to obtain a steady state aPTT in the target range.

2) Argatroban Dose in Patients Undergoing Percutaneous Coronary Intervention

Initial Dosage: Initiate an infusion of Argatroban Injection at 25 mcg/kg/min and administer a bolus of 350 mcg/kg via a large bore intravenous line over 3 to 5 minutes. Check an activated clotting time (ACT) 5 to 10 minutes after the bolus dose is completed. The PCI procedure may proceed if the ACT is greater than 300 seconds.

Dosage Adjustment: If the ACT is less than 300 seconds, an additional intravenous bolus dose of 150 mcg/kg should be administered, the infusion dose increased to 30 mcg/kg/min, and the ACT checked 5 to 10 minutes later.

Except for the two circumstances above, Hangzhou Holypharm biotech Co.,Ltd., a professional supplier of active pharmaceutical ingredients and intermediates showed there were other conditions, such as in patients with Hepatic Impairment, Thrombosis Syndrome and so on.

3. Storage And Handling of Argatroban

Argatroban Injection is supplied in a single use vial containing 50 mg argatroban in 50 mL of aqueous solution (1 mg/mL). Store the Vials in original cartons at 20°– 25° C (68°– 77° F) (see USP Controlled Room Temperature). Do not freeze. Retain in the original carton to protect from light.