Classifications: anticoagulant; direct thrombin inhibitor; Therapeutic: antithrombotic; anticoagulant
Pregnancy Category: B
50 mg powder for injection
Highly specific direct inhibitor of thrombin, including thrombin entrapped within established clots. One molecule of lepirudin
binds to one molecule of thrombin and thereby blocks the thrombogenic activity of thrombin. Increases PT/INR and aPTT values
in relation to the dose given.
Has antithrombotic activity; its effectiveness is indicated by aPTT ratio in target range of 1.5 to 2.5.
Anticoagulation in patients with heparin-induced thrombocytopenia (HIT).
Hypersensitivity to lepirudin; intracranial bleeding; patients with increased risk of bleeding (e.g., recent surgery, CVA,
advanced kidney impairment); lactation. Safety and efficacy in children not established.
Serious liver injury (e.g., cirrhosis); concomitant administration with streptokinase; renal impairment; pregnancy (category
Route & Dosage
Adult: IV 0.4 mg/kg initial bolus (max: 44 mg) followed by 0.15 mg/kg/h (max: 16.5 mg/h) for 210 d, adjust rate to maintain
aPTT of 1.52.5
Clcr 4560 mL/min: initial dose 0.2 mg/kg, then 0.075 mg/kg/h; 3044 mL/min: initial dose 0.2 mg/kg then 0.045 mg/kg/h;
1529 mL/min: initial dose 0.2 mg/kg, then 0.0225 mg/kg/h; <15 mL/min: do not use
PREPARE: Direct: Reconstitute by adding 1 mL of sterile water for injection or NS to the 50-mg vial. To prepare bolus dose, withdraw reconstituted
solution into a 10-cc syringe and dilute to 10 mL with sterile water for injection, NS or D5W to yield 5 mg/mL. Continuous: Transfer the contents of two reconstituted vials into 250 or 500 mL of D5W or NS to yield of 0.4 or 0.2 mg/mL, respectively.
ADMINISTER: Direct: Give over 1520 sec. Continuous: Give at a rate determined by body weight.
- Diluted solution is stable for 24 h during infusion. Store unopened vials at 2°25° C (36°77°
Adverse Effects (≥1%) CNS: Intracranial bleeding. CV:
Heart failure, ventricular fibrillation, pericardial effusion, MI. GI:
Abnormal LFTs. Hematologic:
Bleeding from injection site, anemia, hematoma, bleeding, hematuria, GI and rectal bleeding, epistaxis, hemothorax, vaginal
bleeding. Respiratory: Pneumonia
, cough, bronchospasm, stridor, dyspnea. Skin:
Allergic skin reactions. Body as a Whole:
Sepsis, abnormal kidney function, multiorgan failure.
Interactions Drug: Warfarin, nsaids
, antiplatelet agents
increases risk of bleeding. Herbal: Feverfew, ginkgo, ginger, valerian
may potentiate bleeding.
Distributed primarily to extracellular compartment. Metabolism:
By catabolic hydrolysis in serum. Elimination:
48% in urine. Half-Life:
Assessment & Drug Effects
- Lab tests: Baseline PT/INR and aPTT prior to initiation of therapy (withhold therapy and notify physician if baseline aPTT
ratio ≥2.5); aPTT 4 h after start of therapy and at least once daily (more
often with renal or hepatic impairment) thereafter.
- Give with extreme caution to those at increased risk for bleeding.
- Monitor carefully for bleeding events (e.g., from puncture wounds, hematoma, hematuria); and report immediately.
- Do not give oral anticoagulants until lepirudin dose has been reduced and aPTT ratio lowered to just above 1.5.