Tetracosactide acetate

Absorption

Rapidly absorbed following intramuscular administration.

Description

Cosyntropin is a synthetic polypeptide that consists of amino acid residues 1 through 24 of human ACTH, but that has the full biological activity of its parent. Because it is of synthetic origin, it is less allergenic than ACTH of natural origin. Cosyntropin is used as a diagnostic agent in the screening of patients suspected of having adrenocortical insufficiency. Normally, parenteral administration of cosyntropin acts rapidly on the adrenal cortex to effect release of plasma hydrocortisone; when performing the test, the hydrocortisone levels are compared to a control blood sample taken earlier.

The Uses of Tetracosactide acetate

Hormone (adrenocorticotropic).

Indications

For use as a diagnostic agent in the screening of patients presumed to have adrenocortical insufficiency.

Background

Tetracosactide (also known as Cosyntropin) is a synthetic peptide that is identical to the 24-amino acid segment (sequence: SYSMEHFRWGKPVGKKRRPVKVYP) at the N-terminal of adrenocorticotropic hormone. ACTH (1-24), a segment similar in all species, contains the biological activity that stimulates production of corticosteroids in the adrenal cortex. Tetracosactide exhibits the same activity as natural ACTH with regard to all its biological activities. The complex results in a product whose absorption in man is effected over a longer period of time as compared to corticotropin. Therefore, therapy may be maintained with less frequent administration.

Pharmacokinetics

Cosyntropin exhibits the full corticosteroidogenic activity of natural ACTH. Various studies have shown that the biologic activity of ACTH resides in the N- terminal portion of the molecule and that the 1-20 amino acid residue is the minimal sequence retaining full activity. Partial or complete loss of activity is noted with progressive shortening of the chain beyond 20 amino acid residue. For example, the decrement from 20 to 19 results in a 70% loss of potency. The pharmacologic profile of Cosyntropin is similar to that of purified natural ACTH. It has been established that 0.25 mg of Cosyntropin will stimulate the adrenal cortex maximally and to the same extent as 25 units of natural ACTH. Cosyntropin has less immunogenic activity than ACTH because the amino acid sequence having most of the antigenic activity of ACTH, i.e., amino acids 25-39, is not present in cosyntropin. The extra-adrenal effects which natural ACTH and Cosyntropin have in common include increased melanotropic activity, increased growth hormone secretion and an adipokinetic effect. These are considered to be without physiological or clinical significance.

Metabolism

Not Available