Protamine Sulfate

Protamine Sulfate Injection is indicated in the treatment of heparin overdosage.

Protamine sulfate is prepared from the sperm or mature testes of salmon or related species and is composed of arginine, proline, serine and valine. It combines with strongly acidic heparin to form a stable complex, neutralising the anticoagulant activity of both drugs.

Each mg of Protamine Sulfate will neutralize approximately 90 units of heparin activity derived from beef lung tissue or about 115 units of heparin activity derived from porcine intestinal mucosa.

Protamine Sulfate Injection, should be given by very slow intravenous injection in doses not to exceed 50 mg of Protamine Sulfate in any 10 minute period.

Protamine Sulfate is intended for injection without further dilution; however,if further dilution is desired, 5% Dextrose Injection,or 0.9% Sodium Chloride Injection may be used. Diluted solutions should not be stored since they contain no preservative.

Protamine Sulfate should not be mixed with other drugs without knowledge of their compatibility, because Protamine Sulfate has been shown to be incompatible with certain antibiotics,including several of the cephalosporins and penicillins.

Because heparin disappears rapidly from the circulation, the dose of Protamine Sulfate required also decreases rapidly with the time elapsed following intravenous injection of heparin.For example, if the Protamine Sulfate is administered 30 minutes after the heparin, one-half the usual dose may be sufficient.

The dosage of Protamine Sulfate should be guided by blood coagulation studies.Parenteral drug products should be visually inspected for particulate matter and discolouration prior to administration, whenever solution and container permit.

Protamine sulfate has been shown to be incompatible with certain antibiotics, including several of the cephalosporins and penicillins.

Protamine sulfate is contraindicated in patients who have shown previous intolerance to the drug.

Intravenous injections of Protamine sulfate may cause a sudden fall in blood pressure, bradycardia, pulmonary hypertension, dyspnea, or transitory flushing and a feeling of warmth. There have been reports of anaphylaxis that resulted in respiratory embarrassment. Other reported adverse reactions include systemic hypertension, nausea, vomiting and lassitude. Back pain has been reported rarely in conscious patients undergoing such procedures as cardiaccatheterization. Because fatal reactions often resembling anaphylaxis have been reported after administration of Protamine sulfate, the drug should be given only when resuscitation techniques and treatment of anaphylactoid shock are readily available.

Usage in Pregnancy: Animal reproduction studies have not been conducted with Protamine sulfate . It is also not known whether Protamine sulfate can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Protamine sulfate should be given to a pregnant woman only if clearly needed.

Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Protamine sulfate is administered to a nursing woman.

Patient at risk of developing hypersensitivity to protamine (e.g. previous history of procedures such as coronary angioplasty or cardiopulmonary bypass surgery where protamine is frequently used, diabetics using protamine insulin, allergy to fish, vasectomised or infertile males who may have antibodies to protamine). Pregnancy and lactation.

Because of the anticoagulant effect of Protamine sulfate , overdosage of this drug may theoretically result in hemorrhage. However, in one study, overdosage of 600 to 800 mg of intravenous Protamine sulfate had only minimal, transient effects on blood coagulation tests.The patient should be followed with coagulation studies and treated symptomatically. The LD50 of Protamine sulfate is 100 mg/kg in mice.

Antidote preparations.

Usage in Children: Safety and effectiveness in children have not been established.

Store between 20-25° C. Do not freeze.