Argatroban Monohydrate

What it is and how it works

Mechanism of Action Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban does not require the co-factor antithrombin III for antithrombotic activity. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or –induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; activation of protein C; and platelet aggregation. Argatroban inhibits thrombin with an inhibition constant (K i ) of 0.04 μM. At therapeutic concentrations, argatroban has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein).

Mechanism class: Thrombin Inhibitors

Indications

Argatroban in Sodium Chloride injection is a direct thrombin inhibitor indicated: For prophylaxis or treatment of thrombosis in adult patients with heparin-induced thrombocytopenia (HIT) As an anticoagulant in adult patients with or at risk for HIT undergoing percutaneous coronary intervention (PCI) Heparin-Induced Thrombocytopenia Argatroban in Sodium Chloride Injection is indicated for prophylaxis or treatment of thrombosis in adult patients with heparin-induced thrombocytopenia (HIT). Percutaneous Coronary Intervention Argatroban in Sodium Chloride Injection is indicated as an anticoagulant in adult patients with or at risk for HIT undergoing percutaneous coronary intervention (PCI).

Dosage and administration (summary)

Heparin-Induced Thrombocytopenia The dose for heparin-induced thrombocytopenia without hepatic impairment is 2 mcg/kg/min administered as a continuous infusion Percutaneous Coronary Intervention The dose for patients with or at risk for heparin-induced thrombocytopenia undergoing percutaneous coronary intervention is started at 25 mcg/kg/min and a bolus of 350 mcg/kg administered via a large bore intravenous line over 3 to 5 minutes Preparation for Intravenous Administration Each 50 mL glass vial contains 50 mg of argatroban (1 mg/mL); and, as supplied, is ready for intravenous infusion. Dilution is not required.

Contraindications

Argatroban is contraindicated in: Patients with major bleeding . Patients with a history of hypersensitivity to argatroban. Airway, skin, and generalized hypersensitivity reactions have been reported . Major bleeding History of hypersensitivity to this product

Warnings and precautions

Risk of hemorrhage: Hemorrhage at any site can occur (unexplained fall in hematocrit or blood pressure or other unexplained symptom may indicate hemorrhage). Use with caution in patients at risk, including those receiving antiplatelet agents, thrombolytics, or other anticoagulants Use in hepatic impairment: Adjust starting dose and titrate carefully in patients with HIT who have moderate or severe hepatic impairment.

Pregnancy

Pregnancy Risk Summary Limited data from published literature and postmarketing reports do not suggest an association between argatroban and adverse fetal outcomes. There are risks to the mother associated with untreated thrombosis in pregnancy and a risk of hemorrhage in the mother and fetus associated with the use of anticoagulants (see Clinical …

Storage and supply

Storage Store the vials in original cartons at 20ºC to 25ºC (68ºF to 77°F) : excursion permitted between 15°C to 30°C (59°F to 86°F). Do not refrigerate or freeze. Protect from light and store in carton. Do not use if solution is cloudy or contains a precipitate.

Source: Argatroban (Argatroban) — US FDA prescribing information, 2026-05-21, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.