Octreotide
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| Octreotide
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| Systematic (IUPAC) name | |
| (4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19- [[(2R)-2-amino-3-phenyl-propanoyl]amino]-16- benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7- (1-hydroxyethyl)-13-(1H-indol-3-ylmethyl)-6,9,12, 15,18-pentaoxo-1,2-dithia-5,8,11,14,17- pentazacycloicosane-4-carboxamide | |
| Identifiers | |
| CAS number | |
| ATC code | H01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C49H66N10O10S2 |
| Mol. mass | 1019.24 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 100%; I.M: 60% to 63% of subcutaneous dose |
| Protein binding | 65% |
| Metabolism | Hepatic |
| Half life | 1.7-1.9 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
B(US) |
| Legal status | |
| Routes | Intramuscular, intravenous |
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Ongoing Trials on Octreotide at Clinical Trials.gov Clinical Trials on Octreotide at Google
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Octreotide (brand name Sandostatin, Novartis Pharmaceuticals) is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was first synthesized in 1979 by the chemist Wilfried Bauer.
Effects
Somatostatin has numerous physiological effects:
- It inhibits secretion of many hormones, such as gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, TSH, and vasoactive intestinal peptide.
- It reduces secretion of fluids by the intestine and pancreas.
- It reduces gastrointestinal motility and inhibits contraction of the gallbladder.
- It inhibits the secretion of certain hormones from the anterior pituitary.
Uses
The Food and Drug Administration (FDA) has approved the usage of a salt form of this peptide, octreotide acetate, as an injectable depot formulation for the treatment of acromegaly, the treatment of diarrhea and flushing episodes associated with carcinoid syndrome, and treatment of diarrhea in patients with vasoactive intestinal peptide-secreting tumors (VIPomas).
Octreotide has also been used off-label for the treatment of severe, refractory diarrhea from other causes. It is used in toxicology for the treatment of prolonged recurrent hypoglycemia after sulfonylurea overdose.
Octreotide has also been used with varying degrees of success in infants with nesidioblastosis to help decrease insulin hypersecretion.
In patients with suspected esophageal varices, octreotide can be given to help decrease bleeding.
Octreotide has been investigated for patients with pain from chronic pancreatitis.[1]
References
- (2004) in Katzung, Bertram G. (ed.): Basic and Clinical Pharmacology. Stamford, Conn: Lange Medical Books/McGraw Hill. ISBN 0-07-141092-9.
External links
Pituitary and hypothalamic hormones and analogues (H01) | |
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| Anterior pituitary | Adrenocorticotropic hormone (Corticotropin, Tetracosactide) - Thyrotropin - Somatropin/agonists (Somatrem, Mecasermin, Sermorelin) - other (Pegvisomant) |
| Posterior pituitary | Vasopressin (Desmopressin, Lypressin, Terlipressin, Ornipressin, Argipressin) - Oxytocin (Demoxytocin, Carbetocin) |
| Hypothalamic | gonadotropin-releasing hormones (Gonadorelin, Nafarelin, Histrelin) - antigrowth hormone (Somatostatin, Octreotide, Lanreotide) - anti-gonadotropin-releasing hormones (Ganirelix, Cetrorelix) |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
