醋酸奥曲肽

Name: Octreotide acetate
Synonyms: C07306; D00442; D02XIY; L000453; AC1L8LCD; AN-15653; gtpl2055; AM034456; DR003664; drg-0115; STL483734; LS-177735; sm 201-995; octreotide; sandostatin; san 201-995; sms-201-995; longastatin; sms 201,995; CHEMBL262746; sandostatine; NCI60_025753; c5h12o2.c4h10; AKOS026750549; SCHEMBL678434; octreotide-lar; sandoz 201-995; sandostatin (tn); octreotidum [latin]; octreotida [spanish]; octreotide (usan/inn); octreotide acetate salt; octreotide [usan:inn:ban]; pentaazacycloicosane-4-carboxamide; zacycloicosane-4-carboxamide acetate; 2: PN: EP1358890 TABLE: A claimedprotein; 1: PN: EP1118336 SEQID: 1claimed protein; 14: PN: DE10147056 PAGE: 40 claimedprotein; 17: PN: US6268342 SEQID: 18 claimed protein; 1: PN: WO2005007122 TABLE: 22 claimed protein; 25: PN:WO2007081792 SEQID: 40 claimed protein; 11: PN:US20030229017 PAGE: 13 claimed protein
CAS Registry number: 83150-76-9
Molecular Formula: C₄₉H₆₆N₁₀O₁₀S₂
Boiling Point: 1447.228°C at 760 mmHg
Flash Point: 829.053°C
Refractive index: 1.673
Density: 1.395
Appearance: white powder

Description: Octreotide is a long-acting somatostatin analog indicated for symptomatic control in acromegaly and gastroenteropancreatic tumors. Other potential uses under investigation include diabetes, psoriasis and Alzheimer's disease.

Uses: Antisecretory (gastric).

Biological Function: Octreotide acetate, a long-acting octapeptide analogue of somatostatin, has a half-life of approximately 100 minutes. A comparison of the primary structures of octreotide and somatostatin suggests little similarity, but from earlier work at the Salk Institute it was known that not all the residues in somatostatin were necessary to elicit its full biological activity. Other studies suggested that the essential fragment for its activity was the tetrapeptide Phe7-Trp8- Lys9-Thr10. These earlier studies helped in the design of the potent drug now known as octreotide acetate. This drug suppresses the secretion of gastroenteropancreatic peptides, such as gastrin, vasoactive intestinal peptide (VIP), insulin, and glucagon, as well as pituitary GH. Furthermore, it is more potent than natural somatostatin in inhibiting the release of glucagon, insulin, and GH.

Clinical Use: Octreotide acetate is used by SC injection in the palliative treatment of patients with metastatic carcinoid tumors, which are tumors of the endocrine system, GI tract, and lung (gastroenteropancreatic). Carcinoid tumors secrete increasing amounts of vasoactive substances, including histamine, serotonin, bradykinin, and prostaglandins. Octreotide acetate inhibits or suppresses the release of these vasoactive substances and, thus, is useful in treating the severe diarrhea, facial flushing, and wheezing episodes that accompany carcinoid tumors. In addition, it finds use in the palliative management of VIP-secreting tumors (VIPomas, usually pancreatic tumors). Patients with VIPomas suffer a profuse, watery diarrhea syndrome, and octreotide acetate is able to help by decreasing the release of damaging intestinal tumor cell secretions. Octreotide also helps to reduce hypokalemia by correcting electrolyte imbalances.

An excessive secretion of GH from the pituitary can cause the disorder known as acromegaly, which is characterized by a progressive enlargement of the head, face, hands, feet, and thorax. Inasmuch as octreotide acetate is able to decrease the secretion of GH from the pituitary, it is used in treating patients with acromegaly who are unresponsive to previous pituitary radiation therapy or surgery. It is used in the treatment of acromegaly, because it reduces the blood levels of both GH and insulin-like growth factor-I (IGF-I). The long-acting repository form of octreotide acetate also is used in treating acromegaly, carcinoid tumors, and VIPomas, but in monthly depot injections.
Octreotide for IV injection is used in the treatment of acute bleeding from esophageal varices. Variceal bleeding occurs in about half the patients with cirrhosis of the liver and is responsible for about one-third of deaths in these patients. Octreotide is a potent vasoconstrictor that reduces portal and collateral blood flow by constricting visceral vessels, which leads to reduced portal blood pressure and decreases the bleeding.

Veterinary Drugs and Treatments: Octreotide may be useful in the adjunctive treatment of hyperinsulinemia in patients with insulinomas (especially dogs, ferrets). Response is variable, presumably dependent on whether the tumor cells have receptors for somatostatin. Octreotide may also be useful in the diagnosis and symptomatic treatment of gastrinomas in dogs or cats. It may be of use in the treatment of acute pancreatitis, but more research is needed before it can be recommended for this use in veterinary patients.