Octreotide
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| Image:Octreotide.svg | |
| Image:Octreotide3d.png | |
| Octreotide
| |
| 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 | 83150-76-9 |
| ATC code | H01CB02 |
| PubChem | 54373 |
| DrugBank | BTD00088 |
| Chemical data | |
| Formula | C49H66N10O10S2 |
| Mol. weight | 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 |
Octreotide (brand name Sandostatin, Novartis Pharmaceuticals) is an octapeptide that mimics natural somatostatin pharmacologically, though is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone.
Contents |
[edit] Effects
Somatostatin has numerous physiological effects:
- It inhibits secretion of many hormones, such as gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, 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.
[edit] 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.
In patients with liver cirrhosis, octreotide is used to help stop actively bleeding blood vessels.
[edit] References
- (2004) Katzung, Bertram G. (ed.): Basic and Clinical Pharmacology. Stamford, Conn: Lange Medical Books/McGraw Hill. ISBN 0-07-141092-9.
