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Bivalirudin- specific and reversible direct thrombin inhibitor.

Bivalirudin is a specific and reversible direct thrombin inhibitor. Chemically, it is a synthetic congener of the naturally occurring drug hirudin. More

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Description

Bivalirudin is a specific and reversible direct thrombin inhibitor. Chemically, it is a synthetic congener of the naturally occurring drug hirudin.

Generic Name

Bivalirudin- specific and reversible direct thrombin inhibitor.

Chemical names

Bivalirudin; Angiomax; Hirulog; Hirulog-1

Brand names

Angiomax, Bivaflo, Bivasave, Bivastat

IUPAC name

(4S)-4-[(2S)-2-[(2S)-2-[(2S)-2-{2-[(2S)-2-(2-{2-[2-(2-{[(2S)-1-[(2S)-2-{[(2S)-1[(2R)-2-amino-3-phenylpropanoyl]pyrrolidin-2-yl]formamido}-5-carbamimidamidopentanoyl]pyrrolidin-2-yl]formamido}acetamido)acetamido]acetamido}a

Pharmacokinetics

Actions

Bivalirudin directly and reversibly inhibits thrombin by specifically binding to the anion-binding exosite of circulating and clot-bound thrombin and to the catalytic site. The action of bivalirudin is reversible because thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.

Dosage/Dosage form

750 mcg/kg by IV injection followed by an infusion of 1.75 mg/kg/hr during procedure and up to 4 hr post procedure.

Therapeutic uses

For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. 

Adverse effects/Side effects

Bleeding, hypersensitivity reactions. Hypertension, hypotension, bradycardia, nausea, dyspepsia, vomiting, urinary retention, headache, back pain, pain at injection site and anxiety. Severe anaphylactic reactions which may lead to death.

Interaction

May increase risk of bleeding when used with oral anticoagulants, thrombolytic, or drugs that affect platelet function.

Contraindications

Active major bleeding. CrCl <30 ml/min and dialysis-dependent patients

Storage

Unopened vials stored at 15-30°C whereas reconstituted vials stored at 2-8°C.

Information

Molecular weight

2180.2853

Molecular formula

C98H138N24O33

CAS number

128270-60-0

Precautions

  • Hepatic or renal impairment.
  • Patients at risk of serious recent major surgery, bleeding, organ biopsy, puncture of large vessels.