How Do Somatostatin Analogs Work?

Somatostatin analogs are a synthetic form of somatostatin hormone and are used to reduce the production of various hormones in the body, particularly hormones produced by tumors. The U.S. Food and Drug Administration approved three drugs, namely, octreotide, Ianreotide, and pasireotide in this drug class. 

Somatostatin is a hormone produced by several tissues in the body, but it is mainly found in the nervous and digestive systems. It inhibits the secretion of several other hormones in the body and also acts as a neurotransmitter.

Octreotide is a synthetic octapeptide analog of somatostatin. It binds to somatostatin receptors (SSTR) subtypes 2 and 3 found in the pancreas and subtype 5 found in the intestine and inhibits the blood flow, gastric secretions, splanchnic hemodynamics, pancreatic secretions, intestinal motility, and all gastroenteropancreatic (GEP) endocrine secretions; suppresses luteinizing hormone response to gonadotropin-releasing hormone secretion, and decreases growth hormone (GH) and insulin-like growth factor 1 (IGF-I). It is used to treat acromegaly, diarrhea, variceal bleeding, and GEP neuroendocrine tumors.

Lanreotide is a synthetic octapeptide analog of somatostatin that works by binding specifically to SSTR-2 and SSTR-5 with a lesser affinity. Lanreotide inhibits multiple endocrine, neuroendocrine, and exocrine mechanisms such as decreasing circulating total and free IGF-I and treats neuroendocrine tumors that secrete excessive amount of growth hormone (acromegaly) or other active hormones or neuropeptides. Lanreotide is used for the treatment of acromegaly and to relieve the symptoms of neuroendocrine tumors.

Pasireotide is a synthetic long-acting cyclic peptide that binds to human somatostatin receptors 1, 2, 3, 4, and 5 and inhibits the release of human GH, glucagon, and insulin. Pasireotide is used for the treatment of Cushing’s disease and acromegaly. It also acts as an antineoplastic agent.

Somatostatin analogs are given as intramuscular and subcutaneous injections and oral tablets to treat the following:

• Acromegaly
• Carcinoid tumor
• VIPoma (a type of pancreatic neuroendocrine tumor)
• GEP neuroendocrine tumors
• Carcinoid syndrome
• Cushing’s disease
• Diarrhea 
• Variceal bleeding

Side effects of somatostatin analogs may include:

• Nausea and vomiting
• Injection site reactions
• Diarrhea
• Headache
• Dizziness 
• Weakness
• Fatigue 
• Sweating
• Cholelithiasis 
• Abdominal discomfort
• Indigestion
• Constipation
• Flatulence 
• Upper respiratory tract infections
• Hyperglycemia (high sugar levels)
• Hypertension (high blood pressure)
• Arrhythmias (irregular heartbeats)
• Conduction abnormalities
• Biochemical hypothyroidism
• Elevated liver enzymes
• Pancreatitis 
• Muscle and joint pains
• Anaphylaxis (life-threatening allergic reactions)

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of somatostatin analogs include:

• Bynfezia Pen
• lanreotide
• Mycapssa
• Octreotide
• Pasireotide
• Sandostatin
• Sandostatin LAR
• Signifor
• Signifor LAR
• Somatuline Depot