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Octreotide



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. 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

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.

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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 stion 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]

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.

v • d • e 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)

Category: Hormonal agents

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Octreotide". A list of authors is available in Wikipedia.