Octreotide

What it is and how it works

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).

Indications

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. • 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. • Vasoactive Intestinal Peptide Tumors (VIPomas) : For the treatment of profuse watery diarrhea associated with VIP-secreting tumors. Limitations of Use Improvement in clinical signs and symptoms, or reduction in tumor size or rate of growth, were not shown in clinical trials performed with octreotide acetate injection; these trials were not optimally designed to detect such effects. Acromegaly Octreotide acetate injection is indicated to reduce blood levels of growth hormone (GH) and insulin growth factor-1 (IGF-1.

Dosage and administration (summary)

• Octreotide acetate injection may be administered subcutaneously or intravenously. • 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. • 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. • VIPomas : Recommended dosage range of 200 mcg to 300 mcg daily in two to four divided doses during the initial 2 weeks of therapy. Dosage and Administration Overview • Octreotide acetate injection may be administered subcutaneously or intravenously.

Contraindications

Sensitivity to this drug or any of its components. Sensitivity to this drug or any of its components.

Warnings and precautions

• Cardiac Function Abnormalities : Increased risk for higher degree of atrioventricular blocks. Consider cardiac monitoring in patients receiving Octreotide acetate injection intravenously. Bradycardia, arrhythmias, or conduction abnormalities may occur. Use with caution in at-risk patients. Dosage adjustment of cardiac medications may be necessary. • Cholelithiasis and Complications of Cholelithiasis : Monitor periodically. Discontinue if complications of cholelithiasis are suspected. • Glucose Metabolism : Hypoglycemia or hyperglycemia may occur.

Pregnancy

Pregnancy Risk Summary The limited data with octreotide acetate injection in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage.

Storage and supply

How Supplied Octreotide Acetate Injection is available in a 1 mL single-dose syringe with a fixed 27 gauge ½ inch needle as follows: NDC 67457-239-01 octreotide acetate equivalent to octreotide 50 mcg/mL, carton of 10. NDC 67457-245-01 octreotide acetate equivalent to octreotide 100 mcg/mL, carton of 10.

Source: Octreotide Acetate (Octreotide Acetate) — US FDA prescribing information, 2024-07-15, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.