Classifications: anticoagulant; thrombin inhibitor; Therapeutic: anticoagulant; thrombin inhibitor
Pregnancy Category: C
250 mg/2.5 mL vials
Synthetic derivative of arginine that is a direct thrombin inhibitor. Capable of inhibiting the action of both free and clot-bound
Reversibly binds to the thrombin active site, thereby blocking clot-forming activity of thrombin.
Prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT); prophylaxis or treatment
of coronary artery thrombosis during percutaneous coronary interventions (PCI) in patients at risk for HIT.
Treatment of disseminated intravascular coagulation (DIC).
Hypersensitivity to argatroban; lactation. Any bleeding including intracranial bleeding, GI bleeding, retroperitoneal bleeding,
pregnancy (category C); severe hepatic impairment.
Diseased states with increased risk of hemorrhaging; severe hypertension; GI ulcerations, hepatic impairment; spinal anesthesia,
stroke, surgery, trauma. Safety and effectiveness in children <18 y are not established.
Route & Dosage
|Prevention & Treatment of Thrombosis
Adult: IV 2 mcg/kg/min, may be adjusted to maintain an aPTT of 1.53 times baseline (max: 10 mcg/kg/min)
0.5 mcg/kg/min, may be adjusted to maintain an aPTT of 1.53 times baseline (max: 10 mcg/kg/min)
Prophylaxis or Treatment of Coronary Thrombosis during PCI
Adult: IV Initiate at 25 mcg/kg/min, then bolus of 350 mcg/kg administered via a large bore IV line over 35 min, then 25 mcg/kg/min
by continuous infusion; maintain activated clotting time (ACT) 300450 sec; if ACT below 300 sec, increase infusion
to 30 mcg/kg/min; if ACT over 450 sec, decrease infusion to 15 mcg/kg/min
Note: Argatroban is supplied in 100 mg/mL vials which must be diluted 100-fold prior to infusion.
PREPARE: Continuous: Dilute each 2.5 mL vial by mixing with 250 mL of D5W, NS, or RL to yield 1 mg/mL. Mix by repeated inversion of the diluent
bag for 1 min.
ADMINISTER: Continuous for Heparin-Induced Thrombocytopenia (HIT/HITTS): Before administration, discontinue heparin and obtain a baseline aPTT. Give at a rate of 2 mcg/kg/min, or as ordered. Lower
initial doses are required with hepatic impairment. Check aPTT 2 h after initiation of therapy. After the initial dose, adjust
dose (not to exceed 10 mcg/kg/min) until the steady-state aPTT is 1.5 to 3 times baseline (not to exceed 100 sec). Adjust
dose to maintain aPTT at 1.53 times baseline, but not >100 sec. Check aPTT 2 h after initiation of therapy to confirm
desired therapeutic range. Continuous for Percutaneous Coronary Intervention: Start an infusion at 25 mcg/kg/min and give a bolus of 350 mcg/kg, via a large bore IV line, over 35 min. Check ACT
510 min after the bolus dose. If the ACT is >450 sec, decrease infusion rate to 15 mcg/kg/min. If ACT is <300 sec,
give an additional bolus of 150 mcg/kg and increase infusion to 30 mcg/kg/min. Check ACT q510min to maintain an ACT
level 300450 sec.
- Diluted solutions are stable for 24 h at 25° C (77° F) in ambient indoor light. Protect from direct sunlight. Store
solutions refrigerated at 2°8° C (36°46° F) in the dark.
Adverse Effects (≥1%)Body as a Whole:
Fever, sepsis, pain, allergic reactions (rare). CV:
Hypotension, cardiac arrest,
ventricular tachycardia. GI:
Diarrhea, nausea, vomiting, coughing, abdominal pain. Hematologic: Major GI bleed, minor GI bleeding, hematuria, decrease Hgb/Hct,
groin bleed, hemoptysis, brachial bleed. Respiratory:
results in increased bleeding; may prolong PT with warfarin;
may increase risk of bleeding with thrombolytics
. Herbal: Feverfew, garlic, ginger, ginkgo
may increase potential for bleeding.
13 h. Distribution:
In extracellular fluid; 54% protein bound. Metabolism:
In liver by CYP3A4/5. Elimination:
Primarily in bile (78%). Half-Life:
Assessment & Drug Effects
- Heparin-Induced Thrombocytopenia: Monitor aPTT. Dose adjustment may be needed to reach the target aPTT. Check aPTT 2 h after initiation of therapy. After
the initial dose, adjust dose (not to exceed 10 mcg/kg/min), until the steady-state aPTT is 1.5 to 3 times baseline (not
to exceed 100 sec).
- Monitor cardiovascular status carefully during therapy.
- Monitor for and report S&S of bleeding: Ecchymosis, epistaxis, GI bleeding, hematuria, hemoptysis.
- Note: Patients with history of GI ulceration, hypertension, recent trauma, or surgery are at increased risk for bleeding.
- Monitor neurologic status and report immediately focal or generalized deficits.
- Lab tests: Baseline and periodic ACT (activated clotting time), thrombin time (TT), platelet count, Hgb & Hct; daily INR
when argatroban and warfarin are co-administered; periodic stool test for occult blood; urinalysis.
Patient & Family Education
- Report immediately any of the following to physician: Unexplained back or stomach pain; black, tarry stools; blood in urine,
coughing up blood; difficulty breathing; dizziness or fainting spells; heavy menstrual bleeding; nosebleeds; unusual bruising
or bleeding at any site.