Mechanism of Action

Sandostatin^® LAR Depot (octreotide acetate for injectable suspension) is a
somatostatin analogue. Its effects in the body are similar to those of the naturally occurring hormone, except that Sandostatin^® LAR Depot remains active much longer than somatostatin¹.

Sandostatin^® LAR Depot binds to the somatostatin receptors, and thereby suppresses the release of the peptides and amines from the tumor and inhibits their action, suppressing the severe diarrhea and flushing associated with this disease¹.

MOA of Sandostatin^® LAR Depot Slows Intestinal Transport

• Rapid gastrointestinal (GI) transit leads to accumulation of fluid in the colon and profuse volumes of watery stool²
• Sandostatin^® slows GI transit and increases fluid absorption by over 300%³

Animation

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See how Sandostatin^® LAR Depot works to suppress the overproduction of certain peptides and amines associated with carcinoid syndrome. You will need the Macromedia Flash Player to view the animation.

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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 maintenance therapy in acromegalic patients who have had inadequate response to surgery and/or radiotherapy or for whom surgery and/or radiotherapy is not an option (the goal of treatment in acromegaly is to reduce GH and IGF-1 levels to normal).
• 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.

IMPORTANT SAFETY INFORMATION

Warnings and Precautions:

• Gallbladder abnormalities may occur: Patients should be monitored periodically.
• 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 EKG 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.

Drug Interactions: The following drugs require monitoring and possible dose adjustment when used with Sandostatin LAR Depot: cyclosporine, insulin, oral hypoglycemic agents, beta-blockers, 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.

Adverse Reactions: The most common adverse reactions occurring in patients receiving Sandostatin LAR Depot are:

• Acromegaly: biliary abnormalities (52%), diarrhea (36-48%), cholelithiasis (13-38%), abdominal pain or discomfort (11-29%), flatulence (26%), influenza-like symptoms (20%), constipation (19%), headache (15%), anemia (15%), hyperglycemia (15%), injection site pain (2-14%), hypertension (13%), dizziness (12%), fatigue (11%), nausea (10%), vomiting (7%), hypothyroidism (2%), hypoglycemia (2%), and goiter (2%).
• Carcinoid Tumors and VIPomas: 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%), URTI (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%).

References