Protamin sulfate

General characteristics. Structure:

Active ingredient - protamin sulfate - 10 mg.

Excipients: water for injections to 1 ml.

Pharmacological properties:

Pharmacodynamics. Protamin sulfate is a specific antagonist of heparin. 1 mg of protamin of sulfate neutralizes 80 - 120 PIECES of heparin in blood. The complex formation is caused by abundance of cationic groups (at the expense of an arignin) which contact the anion centers of heparin. Effect of drug after intravenous administration comes instantly and continues within 2 hours. After intravenous administration the complex protamin-heparin which can collapse with heparin release is formed. At overdose can reduce coagulability of blood since sulfate of protamin shows anticoagulating activity.

Pharmacokinetics. Researches of pharmacokinetics were not conducted.

Indications to use:

- bleedings owing to heparin overdose;

- before operation at patients who accept heparin with the medical purpose;

- after heart operations and blood vessels with extracorporal blood circulation;

- hyperheparinemia.

Route of administration and doses:

Solution of protamin of sulfate is entered slowly intravenously struyno or kapelno. Rate of administering should not exceed 5 mg a minute (for example, to enter 50 mg of drug within 10 minutes) as more bystry introduction can cause anaphylactoid reaction. The dose of drug depends on a way of administration of heparin. The calculated dose dissolve 0,9% of solution of sodium of chloride in 300-500 ml. It is not necessary to enter more than 150 mg of protamin of sulfate within 1 hour.

1. At bolyusny injections of heparin the dose of protamin of sulfate decreases depending on time which passed from administration of heparin as the last continuously leaves from an organism.

 

Time which passed after a heparin injection	Sulfate protamin dose counting on 100 ME heparins
15-30 minutes	1-1,5 mg
30 - 60 minutes	0,5 - 0,75 mg
Over 2 hours	0,25-0,375 mg

2. If heparin was entered intravenously kapelno, it is necessary to stop its infusion and to enter 25-30 mg of protamin of sulfate.

Features of use:

Introduction is carried out under control of coagulability of blood. Before introduction it is necessary to be convinced of adequacy of volume of blood of the patient (the hypovolemia increases risk of a collapse).

Side effects:

From cardiovascular system: lowering of arterial pressure, bradycardia.

From the alimentary system: nausea, vomiting.

From immune system: skin rash, itch, development of anaphylactoid reactions.

Others: feeling of heat, a dermahemia, feeling of shortage of air (at excessively bystry introduction).

Interaction with other medicines:

It is incompatible with cephalosporins and penicillin. Is an antagonist of low molecular heparins. Can increase intensity and duration of action of not depolarizing muscle relaxants.

Contraindications:

- the increased sensitivity to drug components;

- an idiopathic or inborn hyperheparinemia (in such cases drug is not effective and can strengthen bleeding);

- the expressed arterial hypotension;

- thrombocytopenia;

- insufficiency of bark of adrenal glands;

- reception by patients of the insulin containing protamin sulfate and also other medicines containing protamin sulfate;

- allergic reactions to fish in the anamnesis.

Experience of a medical use at children is limited.

Overdose:

Can be followed by bleeding since protamin has own anticoagulating activity. Treatment - symptomatic.

Storage conditions:

In the place protected from light, at a temperature from 4 ºС to 10 ºС. To store in the place, unavailable to children. Not to allow freezing.

 

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous administration of 10 mg/ml on 2 ml or 5 ml in ampoules. 5 ampoules place in a blister strip packaging from a film polyvinyl chloride.

1 or 2 blister strip packagings together with the application instruction and the scarificator ampoule or a knife ampoule place in a pack from a cardboard.

5 or 10 ampoules together with the application instruction and the scarificator ampoule or a knife ampoule place in a box from a cardboard with a corrugated insert.

When using ampoules with a point or a ring of a break the scarificator or a knife ampoule do not put.