bivalirudin, Angiomax

 Indications

Used in conjunction with aspirin in patients with unstable

angina who are undergoing percutaneous transluminal

angioplasty (PTCA). Used in conjunction with aspirin

in patients with or at risk of heparin-induced

thrombocytopenia (HIT) or heparin-induced thrombocytopenia

and thrombosis syndrome (HITTS) who are

undergoing percutaneous coronary intervention (PCI).

Used in conjunction with aspirin and with provisional

glycoprotein IIb/IIIa inhibitor therapy in patients who

are undergoing PCI.

Action

Specifically and reversibly 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 acute ischemic

complications in patients with unstable angina (death,

MI, or the urgent need for revascularization procedures).

Pharmacokinetics

Absorption: IV administration results in complete

bioavailability.

Distribution: Unknown.

Metabolism and Excretion: Cleared from plasma

by a combination of renal mechanisms and proteolytic

breakdown.

Half-life: 25 min (qin renal impairment).

TIME/ACTION PROFILE (anticoagulant effect)

ROUTE ONSET PEAK DURATION

IV immediate unknown 1–2 hr

Contraindications/Precautions

Contraindicated in: Active major bleeding; Hypersensitivity.

Use Cautiously in: Any disease state associated with

anqrisk of bleeding; Heparin-induced thrombocytopenia

or heparin-induced thrombocytopenia-thrombosis

syndrome; Patients with unstable angina not undergoing

PTCA; Patients with other acute coronary syndromes;

Concurrent use with other platelet aggregation

inhibitors (safety not established); Renal impairment

(pinfusion rate if CCr 30 mL/min); Lactation, Pedi:

Safety not established; OB: Use only if clearly needed.

Adverse Reactions/Side Effects

CNS: headache, anxiety, insomnia, nervousness. CV:

ACUTE STENT THROMBOSIS (especially in patients with STsegment

elevation MI undergoing PCI), hypotension,

bradycardia, hypertension. GI: nausea, abdominal

pain, dyspepsia, vomiting. Hemat: BLEEDING. Local:

injection site pain. MS: back pain. Misc: pain, fever,

pelvic pain.

Interactions

Drug-Drug: Risk of bleeding may beqby concurrent

use of abciximab, heparin, low molecular

weight heparins, clopidogrel, thrombolytics, or

any other drugs that inhibit coagulation.

Drug-Natural Products:qrisk of bleeding with

arnica, chamomile, clove, dong quai, feverfew,

garlic, ginger, gingko, Panax ginseng, and others.

Route/Dosage

IV (Adults): 0.75 mg/kg as a bolus injection, followed

by an infusion at a rate of 1.75 mg/kg/hr for the duration

of the PCI/PTCA procedure. For patients without

HIT/HITTS, an activated clotting time (ACT) should be

performed 5 min after bolus dose and an additional bolus

dose of 0.3 mg/kg may be administered if needed.

Continuation of the infusion (at a rate of 1.75 mg/kg/

hr) for up to 4 hr post-procedure is optional (should

be considered in patients with ST-segment elevation

MI). If needed, the infusion may be continued beyond

this initial 4 hr at a rate of 0.2 mg/kg/hr for up to 20 hr.

Therapy should be initiated prior to the procedure and

given in conjunction with aspirin.

Renal Impairment

IV (Adults): Nopin the bolus dose is needed in any

patient with renal impairment. GFR 10–29 mL/min—

pinfusion rate to 1 mg/kg/hr; Dialysis-dependent patients

(off dialysis)—pinfusion rate to 0.25 mg/kg/

hr. ACT should be monitored in all patients with renal

impairment.

Availability (generic available)

Powder for injection: 250 mg/vial.