Octreotide
- Atc Codes:H01CB02
- CAS Codes:79517-01-4
- PHARMGKB ID:79517-01-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Sandostatin, Siroctid; Belgium: Octreotide, Sandostatine; Bulgaria: Sandostatin; Cyprus: Sandostatin; Czech Republic: Sandostatin; Denmark: Octreotide, Sandostatin; Estonia: Sandostatin; Finland: Octreotide, Sandostatin; France: Sandostatine; Germany: Bendatreotid, Octreotid, Octreotidacetat, Sandostatin, Sandostatine; Greece: Sandostatin; Hungary: Sandostatin; Ireland: Octreotide, Sandostatin; Italy: Longastatina, Octreotide, Samilstin, Sandostatina; Lithuania: Sandostatin; Netherlands: Octreotide, Sandostatin, Sandostatine; Poland: Sandostatin; Portugal: Octreotida, Octreotido Color, Sandostatina, Siroctid; Romania: Sandostatin; Slovakia: Sandostatin; Slovenia: Sandostatin; Spain: Octeotrida, Sandostatin; Sweden: Octreotide, Sandostatin, Sandostatina; UK: Octreotide, Sandostatin.
North America
Canada: Octreotide, Sandostatin; USA: Octreotide, Sandostatin.
Latin America
Argentina: Sandostatin; Brazil: Sandostatin; Mexico: Cryostatin, Octeotrida, Proclose, Sandostatina.
Asia
Japan: Sandostatin.
Drug combinations
Chemistry
Octreotide Acetate: C~49~H~66~N~10~O~10~S~2~ xC~2~H~4~O~2~. (1) L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]-, cyclic (2→7)-disulfide, [R-(R*,R*)]-, acetate; (2) D-Phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-[(1R,2R)-2-hydroxy-1-(hydroxymethyl)propyl]-L-cysteinamide cyclic (2→7)-disulfide acetate. CAS-79517-01-4 (1990).
Pharmacologic Category
Other Miscellaneous Therapeutic Agents. Antidiarrheal. Antidote. Somatostatin Analog. (ATC-Code: H01CB02).
Mechanism of action
A synthetic polypeptide which mimics natural somatostatin by inhibiting serotonin release, and secretion of gastrin, vasoactive intestinal peptide, insulin, glucagon, secretin, motilin, thyrotropin, cholecystokinin, serotonin, and pancreatic polypeptide. Decreases GI motility, inhibits intestinal secretion of water and electrolytes, and decreases splanchnic blood flow. Decreases growth hormone and IGF-1 in acromegaly. Also suppresses LH response to GnRH, and secretion of thyroid-stimulating hormone.
Therapeutic use
Control of symptoms in metastatic carcinoid and vasoactive intestinal peptide-secreting tumors (VIPomas). Acromegaly.
Pregnancy and lactiation implications
Teratogenic effects not observed in animal studies. Octreotide crosses human placenta. Data concerning use in pregnancy limited. In case reports of acromegalic women who received normal doses of octreotide during pregnancy, no congenital malformations reported. Excretion in breast milk unknown (use caution).
Unlabeled use
AIDS-associated secretory diarrhea (including cryptosporidiosis). Control of bleeding of esophageal varices. Second-line treatment for thymic malignancies. Cushing’s syndrome (ectopic). Insulinomas. Glucagonoma. Small bowel fistulas. Pancreatic tumors. Gastrinoma. Postgastrectomy dumping syndrome. Chemotherapy-induced diarrhea. Graft-vs-host disease-induced diarrhea. Zollinger-Ellison syndrome. Congenital hyperinsulinism. Hypothalamic obesity. Hypoglycemia secondary to sulfonylurea poisoning (as an adjunct to dextrose).
Contraindications
Hypersensitivity to octreotide or any component of the formulation.
Warnings and precautions
Chronic treatment associated with abnormal Schillings test. May impair gallbladder function (inhibits gallbladder contractility and decreases bile secretion). Suppresses secretion of TSH. May alter absorption of dietary fats. Use with caution in heart failure or concomitant medications which alter heart rate or rhythm (bradycardia, conduction abnormalities, and arrhythmia observed in acromegalic and carcinoid syndrome patients). Somatostatin analogs may affect glucose regulation (in type I diabetes, severe hypoglycemia may occur; in type II diabetes or patients without diabetes, hyperglycemia may occur). May reduce excessive fluid loss in conditions that cause such a loss. Use caution in hepatic and renal impairment. Depot formulation should not be used for treatment of sulfonylurea-induced hypoglycemia. Vehicle used in depot injection (polylactide-co-glycolide microspheres) rarely associated with retinal artery occlusion in abnormal arteriovenous anastomosis (e.g. patent foramen ovale). Increases in elimination half-life observed in older adults. Therapy may restore fertility.