protamine sulfate

Indications: 1) reversal of severe heparin overdose - most cases are managed by stopping heparin administration 2) reversal of LMW heparin toxicity 3) reversal of heparin effects after surgery or dialysis Contraindications: - fondaparinux toxicity Pregnancy category: C) Safety in lactation: ? Dosage: 1) 10-50 mg IV over 10 minutes 2) 1 mg antagonizes approximately a) 100 U of heparin, b) 100 U of dalteparin c) 100 U of tinzaparin d) 1 mg of enoxaparin 3) doses > 100 mg produce paradoxical anticoagulation 4) for subcutaneous heparin overdose, dosage may need to be repeated Injection: 10 mg/mL (5 mL, 25 mL). Pharmacokinetics: 1) elimination: plasma 2) neutralization of heparin occurs within 5 minutes of IV administration 4) duration of action: 2 hours (dependent upon body temperature) Adverse effects: 1) common (> 10%) - hypotension, dyspnea, bradycardia 2) less common (1-10%) - hemorrhage 3) uncommon (< 1%) - flushing, lassitude, nausea/vomiting, pulmonary hypertension, hypersensitivity reactions Mechanism of action: 1) binds to heparin forming a stable salt which has no anticoagulant activity 2) protamine given in excess has anticoagulant properties

General

hematologic agent antidote

References

The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
Kaiser Permanente Northern California Regional Drug Formulary, 1998

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