Corticotropin (ACTH, Acthar, Cortrophin Gel) is an open-chain polypeptide that consists of 39 amino acid residues, the first 24 of which are essential for its biological activity. The remainder of the amino acids are also clinically important, since they may be involved in stimulating antibody formation and causing allergic reactions. This is true especially when corticotropin of animal origin is injected into humans. Commercially available corticotropin is prepared from animal pituitary glands.
Absorption, Metabolism, Excretion
Corticotropin is rapidly inactivated by gastrointestinal proteolytic enzymes and therefore must be administered parenterally. It is rapidly removed from the circulation (T1/2,15 minutes) and is probably inactivated in body tissues, since no intact compound is found in the urine.
The rationale for using corticotropin instead of pharmacological concentrations of glucocorticoids stems from the fact that corticotropin provides enhanced amounts of all endogenously secreted adrenocortical hormones, including androgens. However, obvious disadvantages are associated with the use of this polypep-tide: (1) It must be given daily parenterally. (2) It is quite expensive. (3) It is antigenic and thus can produce resistance and hypersensitivity reactions. Corticotropin is used as a diagnostic tool for the identification of primary adrenal insufficiency or as a method for evaluating the hypothalamic-pituitary-adrenal axis before surgery in patients previously treated with glucocorticoids.
Aside from hypersensitivity and allergic reactions, cor-ticotropin administration has been associated with electrolyte disturbances and masculinization in women.
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