Control of symptoms (diarrhea and flushing) in patients with metastatic carcinoid tumors; treatment of watery diarrhea associated with vasoactive intestinal peptide-secreting tumors (VIPomas); treatme tof acromegaly.
藥理
Octreotide is a synthetic octapeptide derivative of naturally occurring somatostatin with similar pharmacological effects, but with a considerably prolonged duration of action. It inhibits pathologically increased secretion of growth hormone (GH) and of peptides and serotonin produced within the gastro-entero-pancreatic (GEP) endocrine system.
藥動學
Bioavailability: (subcutaneous, long-acting), 60% to 63% compared to immediate-release form; Protein binding: about 65%; Renal excretion: about 32% unchanged; Elimination Half Life: 1.7 hr, prolonged in renal impairment(2.4-3.1 hr), liver cirrhosis(3.7 hr) and the elderly( increased by 46%).
禁忌症
Known hypersensitivity to octreotide or any of its components
懷孕分類
B
哺乳分類
Excretion in breast milk unknown/use caution
副作用
injection site localized pain; gastrointestinal disorders such as diarrhea, constipation, abdominal pain, nausea; headache, dizziness, hepatobiliary disorders, hyperglycemia, anorexia.
劑量和給藥方法
50-100 mcg SC BID or TID. Repeated injections at the same site in short periods of time should be avoided. Continuous I.V. infusion rates (unlabeled administration rate) have ranged from 25-50 mcg/hour for the treatment of esophageal variceal bleeding (unlabeled use); continuous I.V. infusion rates of 100-125 mcg/hour have been used for the treatment of sulfonylurea-induced hypoglycemia.