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 Octreotide

octreotide acetate is the acetate salt of a synthetic long-acting cyclic octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin. Octreotide is a more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Similar to somatostatin, this agent also suppresses the luteinizing hormone response to gonadotropin-releasing hormone, decreases splanchnic blood flow, and inhibits the release of serotonin, gastrin, vasoactive intestinal peptide (VIP), secretin, motilin, pancreatic polypeptide, and thyroid stimulating hormone. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

DRUG DESCRIPTION

Sandostatin® (octreotide acetate) Injection, a cyclic octapeptide prepared as a clear sterile solution of octreotide, acetate salt, in a buffered lactic acid solution for administration by deep subcutaneous (intrafat) or intravenous injection. Octreotide acetate, known chemically as L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]-, cyclic (2→7)-disulfide; [R-(R*, R*)] acetate salt, is a long-acting octapeptide with pharmacologic actions mimicking those of the natural hormone somatostatin.

Sandostatin Injection is available as: sterile 1-mL ampuls in 3 strengths, containing 50, 100, or 500 mcg octreotide (as acetate), and sterile 5-mL multi-dose vials in 2 strengths, containing 200 and 1000 mcg/mL of octreotide (as acetate).

Each ampul also contains:

lactic acid, USP............................................. 3.4 mg
mannitol, USP................................................ 45 mg
sodium bicarbonate, USP .............................. qs to pH 4.2 ±0.3
water for injection, USP...................................qs to 1 mL

Each mL of the multi-dose vials also contains:

lactic acid, USP ............................................. 3.4 mg
mannitol, USP................................................. 45 mg
phenol, USP....................................................5.0 mg
sodium bicarbonate, USP ............................... qs to pH 4.2 ±0.3
water for injection, USP...................................qs to 1 mL

Lactic acid and sodium bicarbonate are added to provide a buffered solution, pH to 4.2 ±0.3.  The molecular weight of octreotide acetate is 1019.3 (free peptide, C49H66N10O10S2)

CLINICAL PHARMACOLOGY

Sandostatin® (octreotide acetate) exerts pharmacologic actions similar to the natural hormone, somatostatin. It is an even more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Like somatostatin, it also suppresses LH response to GnRH, decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide. By virtue of these pharmacological actions, Sandostatin has been used to treat the symptoms associated with metastatic carcinoid tumors (flushing and diarrhea), and Vasoactive Intestinal Peptide (VIP) secreting adenomas (watery diarrhea). Sandostatin substantially reduces growth hormone and/or IGF-I (somatomedin C) levels in patients with acromegaly. Single doses of Sandostatin have been shown to inhibit gallbladder contractility and to decrease bile secretion in normal volunteers. In controlled clinical trials the incidence of gallstone or biliary sludge formation was markedly increased (see WARNINGS). Sandostatin suppresses secretion of thyroid stimulating hormone (TSH).

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