Warnings and Precautions Gallbladder abnormalities may occur. There have been postmarketing reports of cholelithiasis (gallstones) resulting in complications, including cholecystitis, cholangitis, ...
Mechanism of Action
About Sandostatin LAR Depot
Sandostatin® LAR Depot (octreotide acetate) for injectable suspension for treatment of the severe diarrhea and flushing associated with metastatic carcinoid tumors
Sandostatin LAR Depot has been designed to target somatostatin receptors.1,2
Sandostatin LAR Depot inhibits hormone secretions
- When carcinoid tumors metastasize to the liver, elevated levels of serotonin and other hormones that are secreted by the carcinoid tumors are able to reach systemic circulation and can cause severe diarrhea and flushing3
- The severe diarrhea associated with metastatic carcinoid tumors is related to elevated levels of serotonin and its metabolite, 5-HIAA4,5
- Octreotide acetate is a naturally occurring inhibitory hormone that suppresses the release of exocrine and endocrine secretions1,2
- Sandostatin LAR Depot is a somatostatin analogue and is a more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin1
- Octreotide is a synthetic octapeptide that has pharmacologic properties similar to those of somatostatin, but with a longer half-life1,3
Sandostatin LAR Depot provides somatostatin receptor–targeted inhibition
Octreotide binds to somatostatin receptors that are highly expressed on the surface of carcinoid tumors, where it inhibits the release of gastrin, vasoactive intestinal peptide, secretin, motilin, and serotonin1-3,6
5-HIAA, 5-hydroxyindoleacetic acid.
References: 1. Sandostatin LAR Depot [prescribing information]. East Hanover, NJ: Novartis Pharmaceuticals Corp; 2019. 2. Susini C, Buscail L. Rationale for the use of somatostatin analogs as antitumor agents. Ann Oncol. 2006;17(12):1733-1742. 3. Rubin J, Ajani J, Schirmer W, et al. Octreotide acetate long-acting formulation versus open-label subcutaneous octreotide acetate in malignant carcinoid syndrome. J Clin Oncol. 1999;17(2):600-606. 4. Öberg K, Kvols L, Caplin M, et al. Consensus report on the use of somatostatin analogs for the management of neuroendocrine tumors of the gastroenteropancreatic system. Ann Oncol. 2004;15(6):966-973. 5. Davis Z, Moertel CG, McIlrath DC. The malignant carcinoid syndrome. Surg Gynecol Obstet. 1973;137:637-644. 6. Chaudhri O, Small C, Bloom S. Gastrointestinal hormones regulating appetite. Philos Trans R Soc Lond B Biol Sci. 2006;361(1471):1187-1209.
IMPORTANT SAFETY INFORMATION
Warnings and Precautions
- Gallbladder abnormalities may occur. There have been postmarketing reports of cholelithiasis (gallstones) resulting in complications, including cholecystitis, cholangitis, pancreatitis, and requiring cholecystectomy in patients taking Sandostatin LAR Depot. Patients should be monitored periodically. If complications of cholelithiasis are suspected, discontinue Sandostatin LAR Depot and treat appropriately
- Glucose Metabolism: Hypoglycemia or hyperglycemia may occur. Blood glucose levels should be monitored when Sandostatin LAR Depot treatment is initiated or when the dose is altered. Antidiabetic treatment should be adjusted accordingly
- Thyroid Function: Hypothyroidism may occur. Baseline and periodic assessment of thyroid function (TSH, total and/or free T4) is recommended
- Cardiac Function: Bradycardia, arrhythmia, conduction abnormalities, and other ECG changes may occur. The relationship of these events to octreotide acetate is not established because many of these patients have underlying cardiac disease. Use with caution in at-risk patients
- Nutrition: Octreotide may alter absorption of dietary fats. Monitoring of vitamin B12 levels is recommended during therapy with Sandostatin LAR Depot. Patients on total parenteral nutrition (TPN) and octreotide should have periodic monitoring of zinc levels
- The following drugs require monitoring and possible dose adjustment when used with Sandostatin LAR Depot: cyclosporine, insulin, oral hypoglycemic agents, beta-blockers, and bromocriptine. Octreotide has been associated with alterations in nutrient absorption, so it may have an effect on absorption of orally administered drugs. Drugs mainly metabolized by CYP3A4 and which have a low therapeutic index should be used with caution
- The most common adverse reactions occurring in patients receiving Sandostatin LAR Depot were biliary abnormalities (62%), injection-site pain (20%-50%), nausea (24%-41%), abdominal pain (10%-35%), fatigue (8%-32%), headache (16%-30%), hyperglycemia (27%), back pain (8%-27%), constipation or vomiting (15%-21%), dizziness (18%-20%), sinus bradycardia (19%), pruritus (18%), upper respiratory tract infection (10%-18%), myalgia (4%-18%), flatulence (9%-16%), arthropathy (8%-15%), rash (15%), generalized pain (4%-15%), sinusitis (5%-12%), conduction abnormalities (9%), hypoglycemia (4%), and arrhythmia (3%)
Please see full Prescribing Information.
Indications and Usage
Sandostatin® LAR Depot (octreotide acetate) for injectable suspension is indicated for patients in whom initial treatment with immediate-release Sandostatin® (octreotide acetate) Injection has been shown to be effective and tolerated for
- Long-term treatment of the severe diarrhea and flushing episodes associated with metastatic carcinoid tumors
- Long-term treatment of the profuse watery diarrhea associated with VIP-secreting tumors
In patients with carcinoid syndrome and VIPomas, the effect of Sandostatin Injection and Sandostatin LAR Depot on tumor size, rate of growth, and development of metastases has not been determined.