protamine

REMS

Acute management of severe heparin overdosage.
Used to neutralize heparin received during dialysis, cardiopulmonary bypass, and other procedures.

Unlabeled Use:

Management of overdose of heparin-like compounds.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to protamine or fish
.

Use Cautiously in:

Patients who have received previous protamine-containing insulin or vasectomized men (↑ risk of hypersensitivity reactions)
;
OB: Safety not established in pregnancy; use during pregnancy only if clearly needed;
Lactation: Safety not established in breastfeeding; use while breastfeeding only if clearly needed.

Adv. Reactions/Side Effects ⬆ ⬇

CV: bradycardia, hypertension, hypotension

Derm: flushing

GI: nausea, vomiting

Hemat: bleeding

MS: back pain

Resp: dyspnea, pulmonary edema, pulmonary hypertension

Misc: HYPERSENSITIVITY REACTIONS(INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

None reported.

Availability ⬆ ⬇

(Generic available)

Solution for injection: 10 mg/mL

Route/Dosage ⬆ ⬇

IV (Adults and Children ): Heparin overdose: 1 mg of protamine/100 units of heparin. If given >30 min after heparin, give 0.5 mg of protamine/100 units of heparin (not to exceed 100 mg/2 hr). Further doses should be determined by coagulation tests. If heparin was administered subcutaneously, use 1–1.5 mg of protamine per 100 units of heparin (give 25–50 mg of the protamine dose slowly followed by a continuous infusion over 8–16 hr). Enoxaparin overdose (unlabeled use): 1 mg of protamine/1 mg of enoxaparin. Dalteparin overdose (unlabeled use): 1 mg of protamine/100 anti-Xa units of dalteparin. If required, a 2nd dose of 0.5 mg of protamine/100 anti-Xa units of dalteparin may be given 2–4 hr later if laboratory assessment indicates need.

Action ⬆ ⬇

A strong base that forms a complex with heparin (an acid).

Therapeutic effects:

Inactivation of heparin.

Classifications ⬆ ⬇

Therapeutic Classification: antidotes

Pharmacologic Classification: antiheparins

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Metabolic fate not known. Protamine-heparin complex eventually degrades.

Half-Life: 7 min.

Time/Action Profile ⬆ ⬇

(reversal of heparin effect)

ROUTE	ONSET	PEAK	DURATION
IV	30 sec–1 min	unknown	2 hr‡

‡Depends on body temperature.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of protamine. Advise patient to read Medication Guide before starting and periodically during therapy in case of changes.
Tell patient to report and seek treatment for signs and symptoms of bleeding (weakness; fast heartbeat; trouble breathing; dizziness; pale skin; tiredness; obvious bleeding in urine, stool, mouth, or nose).
Advise patient to avoid activities that may result in bleeding (shaving, brushing teeth, receiving injections or rectal temperatures, ambulating) until risk of hemorrhage has passed.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇