Overview
11 DESCRIPTION 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 or intravenous injection. Octreotide acetate, known chemically as L-Cysteinamide,...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Octreotide acetate injection exerts pharmacologic actions similar to the natural hormone, somatostatin. It is an even more potent inhibitor of GH, glucagon, and insulin than somatostatin. Like somatostatin, it also suppresses luteinizing hormone (LH) response to gonadotropin releasing hormone (GnRH), decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, VIP, secretin, motilin, and pancreatic polypeptide. By virtue of these pharmacological actions, octreotide has been used to treat the symptoms associated with metastatic carcinoid tumors (flushing and diarrhea), and VIP secreting adenomas (watery diarrhea). 12.
Indications
- 1 INDICATIONS AND USAGE Octreotide Acetate Injection is a somatostatin analogue indicated: Acromegaly : To reduce blood levels of growth hormone (GH) and insulin growth factor-1 (IGF-1; somatomedin C) in acromegaly patients who have had inadequate response to or cannot be treated with surgical resection, pituitary irradiation, and bromocriptine mesylate at maximally tolerated doses. ( 1.1 ) Carcinoid Tumors : For the symptomatic treatment of patients with metastatic carcinoid tumors where it suppresses or inhibits the severe diarrhea and flushing episodes associated with the disease. ( 1.
Common Doses
- 50 mcg
- 100 mcg
- 500 mcg
- 600 mcg
Dosage
2 DOSAGE AND ADMINISTRATION Octreotide Acetate injection may be administered subcutaneously or intravenously. ( 2.1 ) Acromegaly : Recommended initial Octreotide Acetate injection dosage is 50 mcg three times daily during the initial 2 weeks of therapy. Maintenance dose 100 mcg to 500 mcg three times daily. ( 2.2 ) Carcinoid Tumors : Recommended dosage range of 100 mcg to 600 mcg daily in two to four divided doses during the initial 2 weeks of therapy. ( 2.3 ) VIPomas : Recommended dosage range of 200 mcg to 300 mcg daily in two to four divided doses during the initial 2 weeks of therapy. ( 2.
Contraindications
- 4 CONTRAINDICATIONS Sensitivity to this drug or any of its components. Sensitivity to this drug or any of its components. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Complete Atrioventricular Block [see Warnings and Precautions (5.1)] Cholelithiasis and Complications of Cholelithiasis [see Warnings and Precautions (5.2)] Hyperglycemia and Hypoglycemia [see Warnings and Precautions (5.3)] Thyroid Function Abnormalities [see Warnings and Precautions (5.4)] Steatorrhea and Malabsorption of Dietary Fats [see Warnings and Precautions (5.5)] Changes in Vitamin B12 Levels [see Warnings and Precautions (5.
Interactions
- 7 DRUG INTERACTIONS The following drugs require monitoring and possible dose adjustment when used with octreotide acetate injection : cyclosporine, insulin, oral hypoglycemic agents, beta-blockers, and bromocriptine. ( 7 ) Lutetium Lu 177 Dotatate Injection : Discontinue octreotide acetate injection at least 24 hours prior to each lutetium Lu 177 dotatate dose. ( 7.6 ) 7.1 Cyclosporine Octreotide has been associated with alterations in nutrient absorption, so it may have an effect on absorption of orally administered drugs.