AMINOCAPROIC ACID

Chemistry - An inhibitor of fibrinolysis, aminocaproic acid is a synthetic monamino carboxylicacid occurring as a fine, white crystalline powder. It is slightly soluble in alcohol and freely solublein water and has pKa's of 4.43 and 10.75. The injectable product has its pH adjusted to approximately 6.8. Aminocaproic acid may also be known by the acronym EACA.

Storage, Stability, Compatibility

Products should be stored at room temperature. Avoid freezing liquid preparations. Discoloration will occur if aldehydes or aldehydic sugars are present.
When given as an intravenous infusion, normal saline, D5W and Ringer's Injection have beenrecommended to be used as the infusion diluent.

Pharmacology - AMINOCAPROIC ACID

Aminocaproic acid inhibits fibrinolysis via its inhibitory effects on plasminogenactivator substances and also via some antiplasmin action.
Aminocaproic acid is thought to affect degenerative myelopathy by its antiprotease activity, therebyreducing the activation of inflammatory enzymes that damage myelin.

Uses, Indications

Aminocaproic acid has been used as a treatment to degenerative myelopathy(seen primarily in German shepherds). In humans, it is primarily used for treating hyperfibrinolysis-induced hemorrhage.

Pharmacokinetics - AMINOCAPROIC ACID

In humans, the drug is rapidly and completely absorbed after oral administration. The drug is well distributed in both intravascular and extravascular compartments andpenetrates cells (including red blood cells). It unknown if the drug enters maternal milk. It does notbind to plasma proteins. Terminal half life is about 2 hours in humans and the drug is primarilyrenally excreted as unchanged drug.

Contraindications, Precautions, Reproductive Safety

Aminocaproic acid is contraindicated inpatients with active intravascular clotting. It should be used when the benefits outweigh the risks inpatients with preexisting cardiac, renal or hepatic disease. Some, but not all, animal studies havedemonstrated teratogenicity; use when risk to benefit ratio merits.

Adverse Effects, Warnings

In dogs treated, about 1% exhibit symptoms of GI irritation.

Overdosage, Acute Toxicity

There is very limited information on overdoses with aminocaproicacid. The IV lethal dose in dogs is reportedly 2.3 g/kg. At lower IV overdosages, tonic-clonicseizures were noted in some dogs. There is no known antidote, but the drug is dialyzable.

Drug Interactions

Hypercoagulation states may occur in patients receiving estrogens.
Laboratory Considerations - Serum potassium may be elevated by aminocaproic acid especially in patients with preexisting renal failure.