Epsilcapramine

Uses

Epsilcapramine used to treat excessive postoperative bleeding, especially after procedures in which a great amount of bleeding is expected, such as cardiac surgery. It can be given orally or intravenously. A meta-analysis found that lysine analogs like Epsilcapramine significantly reduced blood loss in patients undergoing coronary artery bypass grafting. Epsilcapramine can also be used to treat the overdose and/or toxic effects of the thrombolytic pharmacologic agents tissue plasminogen activator and streptokinase.

Epsilcapramine is also used to associated treatment for these conditions: Bleeding, Bleeding caused by thrombocytopenia, Bleeding of the oral, Hemorrhage, Secondary subarachnoid hemorrhage

How Epsilcapramine works

Epsilcapramine binds reversibly to the kringle domain of plasminogen and blocks the binding of plasminogen to fibrin and its activation to plasmin. With NO activation of plasmin, there is a reduction in fibrinolysis. This consequently will reduce the amount of bleeding post surgery. Elevated plasma levels of lipoprotein(a) have been shown to increase the risk of vascular disease. Lipoprotein 9a)a has two components, apolipoprotein B-100, linked to apolipoprotein (a). Epsilcapramine may change the conformation of apoliprotein (a), changing its binding properties and potentially preventing the formation of lipoprotein (a).

Dosage

Epsilcapramine dosage

Dosage of Epsilcapramine must be adjusted to individual cases according to the severity of the hemmohagic event. It must however born in mind that Epsilcapramine cleared rapidly by renal rough, so that administration must be repeated every 4-6 hours. The average dose is 8-16 gm a day.i.e. 1 ampule of Epsilcapramine according to the case, every 6 hours.

Epsilcapramine is equally effective by mouth and intarvenous injection. In cases of particular severity, or when it is sought to obtain a high blood concentration quickly it is advisable to start treatment by intravenous rough, with slow injection of two Epsilcapramine ampules with an interval of 30-60 minutes between them, continuing with divided doses until a dosage of 20-25 grams in the 24 hour is reached.

In any case, administration of the drug must be continued until complete cessation of all symptoms. Epsilcapramine could be intravenously administered, following suitable dilution in Physiological solution.

Side Effects

Mild muscle pain or weakness; headache, tired feeling; nausea, vomiting, stomach pain, diarrhea; (in men) decreased amount of semen when having an orgasm; stuffy nose, watery eyes; vision problems, ringing in your ears; or Mild skin rash.

Toxicity

A few cases of acute overdosage with intravenous administration have been reported. The effects have ranged from no reaction to transient hypotension to severe acute renal failure leading to death. The intravenous and oral LD₅₀ were 3.0 and 12.0 g/kg respectively in the mouse and 3.2 and 16.4 g/kg respectively in the rat. An intravenous infusion dose of 2.3 g/kg was lethal in the dog.

Precaution

Safety and efficacy have not been established in patients younger than 18 years.

Food Interaction

• Take with or without food. The absorption is unaffected by food.

Volume of Distribution

• 23.1 ± 6.6 L

Elimination Route

Absorbed rapidly following oral administration. In adults, oral absorption appears to be a zero-order process with an absorption rate of 5.2 g/hr. The mean lag time in absorption is 10 minutes. After a single oral dose of 5 g, absorption was complete (F=1).

Half Life

The terminal elimination half-life is approximately 2 hours.

Clearance

• 169 mL/min

Elimination Route

Renal excretion is the primary route of elimination, whether aminocaproic acid is administered orally or intravenously.

Pregnancy & Breastfeeding use

Pregnancy Category C. Animal reproduction studies have not been conducted with aminocaproic acid. It is also not known whether aminocaproic acid can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Aminocaproic Acid Injection should be given to a pregnant woman only if clearly needed.

Contraindication

• Epsilcapramine should not be used when there is evidence of an active intravascular clotting process.
• When there is uncertainty as to whether the cause of bleeding is primary fibrinolysis or disseminated intravascular coagulation (DIC), this distinction must be made before administering Epsilcapramine Injection.
• The following tests can be applied to differentiate the two conditions:
• Platelet count is usually decreased in DIC but normal in primary fibrinolysis.
• Protamine paracoagulation test is positive in DIC; a precipitate forms when protamine sulfate is dropped into citrated plasma. The test is negative in the presence of primary fibrinolysis.
• The euglobulin clot lyses test is abnormal in primary fibrinolysis but normal in DIC.
• Epsilcapramine Injection must not be used in the presence of DIC without concomitant heparin.

Storage Condition

Store in a cool, dry place, protected from light. Store the suspension below 30° C. Keep out of reach of children.

Innovators Monograph

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