argatroban

High Alert

Prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT).
As an anticoagulant in patients with or at risk for heparin-induced thrombocytopenia who are undergoing percutaneous coronary intervention (PCI).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Major bleeding;
Hypersensitivity.

Use Cautiously in:

Hepatic impairment (↓ initial infusion rate recommended);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension

GI: diarrhea, nausea, vomiting

Hemat: BLEEDING

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Risk of bleeding may be ↑ by concurrent use of antiplatelet agents, thrombolytic agents, or other anticoagulants.

Drug-Natural Products:

↑bleeding risk with anise, arnica, chamomile, clove, feverfew, garlic, ginger, ginkgo, Panax ginseng, and others.

Availability ⬆ ⬇

(Generic available)

Premixed infusion: 50 mg/50 mL
Solution for injection: 100 mg/mL

Route/Dosage ⬆ ⬇

IV (Adults ): 2 mcg/kg/min as a continuous infusion; adjust infusion rate on the basis of activated partial thromboplastin time (aPTT). Patients undergoing PCI: 350 mcg/kg bolus followed by infusion at 25 mcg/kg/min, activated clotting time (ACT) should be assessed 5–10 min later. If ACT is 300–450 sec, procedure may be started. If ACT <300 sec, give additional bolus of 150 mcg/kg and ↑ infusion rate to 30 mcg/kg/min. If ACT is >450 sec infusion rate should be ↓ to 15 mcg/kg/min and ACT rechecked after 5–10 min. If thrombotic complications occur or ACT drops to <300 sec, an additional bolus of 150 mcg/kg may be given and the infusion rate ↑ to 40 mcg/kg/min followed by ACT monitoring. If anticoagulation is required after surgery, lower infusion rates should be used.

Hepatic Impairment

IV (Adults ): 0.5 mcg/kg/min as a continuous infusion; adjust infusion rate on the basis of aPTT.

Action ⬆ ⬇

Inhibits thrombin by binding to its receptor sites. Inhibition of thrombin prevents activation of factors V, VIII, and XII; the conversion of fibrinogen to fibrin; platelet adhesion and aggregation.

Therapeutic effects:

Decreased thrombus formation and extension with decreased sequelae of thrombosis (emboli, postphlebitic syndromes).

Classifications ⬆ ⬇

Therapeutic Classification: anticoagulants

Pharmacologic Classification: thrombin inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Mostly metabolized by the liver; excreted primarily in feces via biliary excretion. 16% excreted unchanged in urine, 14% excreted unchanged in feces.

Half-Life: 39–51 min (↑ in hepatic impairment).

Time/Action Profile ⬆ ⬇

(anticoagulant effect)

ROUTE	ONSET	PEAK	DURATION
IV	immediate	1–3 hr	2–4 hr

Patient/Family Teaching ⬆ ⬇

Explain the purpose of argatroban to patient.
Advise patient to avoid other products known to affect bleeding.
Instruct patient to notify health care professional immediately if any bleeding or signs and symptoms of allergic reaction is noted.
Rep: Advise females or reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇