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 |
83150-76-9 |
| ATC code |
H01CB02 |
| PubChem |
54373 |
| DrugBank |
BTD00088 |
| 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)
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| Legal status |
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| Routes |
Intramuscular, intravenous |
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:
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]
Octreotide may be useful in the treatment of thymic neoplasms.
References
- ^ Uhl W, Anghelacopoulos SE, Friess H, Büchler MW (1999). "The role of octreotide and somatostatin in acute and chronic pancreatitis". Digestion 60 Suppl 2: 23-31. PMID 10207228.
- (2004) in Katzung, Bertram G. (ed.): Basic and Clinical Pharmacology. Stamford, Conn: Lange Medical Books/McGraw Hill. ISBN 0-07-141092-9.
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Pituitary and hypothalamic hormones and analogues (H01) |
| 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) |
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