Primary information |
---|
ThPP ID | Th1103 |
Therapeutic Peptide/Protein Name | Cosyntropin |
Sequence | ACTH(1-24)SYSMEHFRWGKPVGKKRRPVKVYP view full sequnce in fasta |
Functional Classification | IV |
Molecular Weight | 2933.437 |
Chemical Formula | C136H210N40O31S |
Isoelectric Point | N.A. |
Hydrophobicity | N.A. |
Melting Point (℃) | N.A. |
Half Life | 15 minutes (IV adminstration) |
Description | A synthetic peptide identical to the 24-amino acid N-terminal segment of adrenocorticotropic hormone. ACTH. This segment is similar in all species and responsible for biological activity. |
Indication/Disease | For use as a diagnostic agent in the screening of patients presumed to have adrenocortical insufficiency. |
Pharmacodynamics | 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. |
Mechanism of Action | Cosyntropin combines with a specific receptor in the adrenal cell plasma membrane and, in patients with normal adrenocortical function, stimulates the initial reaction involved in the synthesis of adrenal steroids (including cortisol, cortisone, weak androgenic substances, and a limited quantity of aldosterone) from cholesterol by increasing the quantity of the substrate within the mitochondria. Cosyntropin does not significantly increase plasma cortisol concentration in patients with primary or secondary adrenocortical insufficiency. |
Toxicity | N.A. |
Metabolism | N.A. |
Absorption | Rapidly absorbed following intramuscular administration. |
Volume of Distribution | N.A. |
Clearance | N.A. |
Categories | Hormones and Diagnostic Agents |
Patents Number | N.A. |
Date of Issue | N.A. |
Date of Expiry | N.A. |
Drug Interaction | N.A. |
Target | Adrenocorticotropic hormone receptor |
Information of corresponding available drug in the market |
---|
Brand Name | Cortrosyn |
Company | Amphastar Pharmaceuticals |
Brand Discription | CORTROSYN (cosyntropin) for Injection is a sterile Iyophilized powder in vials containing 0.25 mg of CORTROSYN (cosyntropin) and 10 mg of mannitol to be reconstituted with 1 mL of 0.9% Sodium Chloride Injec-tion, USP. Administration is by intravenous or intramuscular injection. Cosyntropin is α1 - 24 corticotropin, a synthetic subunit of ACTH. It is an open chain polypeptide containing, from the N terminus, the first 24 of the 39 amino acids of natural ACTH |
Prescribed for | CORTROSYN (cosyntropin) for Injection is intended for use as a diagnostic agent in the screening of patients presumed to have ad-renocortical insufficiency. Because of its rapid effect on the adrenal cortex it may be utilized to perform a 30-minute test of adrenal func-tion (plasma cortisol response) as an office or outpatient procedure, using only 2 venipuncture |
Chemical Name | N.A. |
Formulation | Box of 10 vials of CORTROSYN (cosyntropin) for Injection 0.25 mg without antimicrobial preservatives |
Physcial Appearnce | N.A. |
Route of Administration | Intravenous, Intravenous infusion, Intramuscular |
Recommended Dosage | CORTROSYN (cosyntropin) for Injection may be administered intramuscularly or as a direct Intravenous infusion when used as a rapid screening test of adrenal function. It may also be given as an Intravenous infusion over a 4 to 8 hour period to provide a greater stimulus to the adrenal glands. Doses of CORTROSYN (cosyntropin) 0.25 to 0.75 mg have been used in clinical studies and a maximal response noted with the smallest dose. |
Contraindication | The only contraindication to CORTROSYN (cosyntropin) for Injec-tion is a history of a previous adverse reaction to it. |
Side Effects | Since CORTROSYN (cosyntropin) for Injection is intended for diag-nostic and not therapeutic use. A rare hypersensitivity reaction usually associated with a pre-existing allergic disease and/or a previous reaction to natural ACTH is possible. Symptoms may include slight whealing with splotchy erythema at the injection site. The other effects such as bradycardia, tachycardia, hypertension, peripheral edema. |
Useful Link | N.A. |
PubMed ID | 20841313 |
3-D Structure | Th1103 (View) or (Download) |