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Pharmacology of Octreotide (Sandostatin) ; Mechanism of action, Pharmacokinetics, Uses, Effects
Pharmacology of Octreotide
Octreotide is a synthetic analog of somatostatin, a naturally occurring growth hormone inhibiting peptide. It is primarily used to treat certain hormonal disorders and symptoms associated with certain types of tumors2.
Mechanism of Action
Octreotide mimics the action of natural somatostatin but has a longer duration of effect. It binds to somatostatin receptors (SSTR2 and SSTR5) and inhibits the secretion of several hormones, including:
Growth hormone (GH)
Glucagon
Insulin
By binding to these receptors, octreotide helps regulate the hormonal imbalances in conditions like acromegaly and certain types of neuroendocrine tumors.
Pharmacokinetics
Absorption: Octreotide can be administered via subcutaneous (SC), intramuscular (IM), or intravenous (IV) routes. The bioavailability of octreotide is approximately 100% for SC administration and 60% for IM administration1.
Distribution: It is widely distributed throughout the body and binds to plasma proteins at a rate of 40-65%.
Metabolism: Octreotide is metabolized primarily by the liver.
Elimination: It has a half-life of approximately 1.7-1.9 hours and is excreted mainly through the urine.
Clinical Uses
Acromegaly: Used to reduce growth hormone levels.
Neuroendocrine Tumors: Helps manage symptoms such as diarrhea and flushing associated with carcinoid syndrome and vasoactive intestinal peptide (VIP)-secreting tumors (VIPomas).
Variceal Bleeding: Octreotide is used in the management of esophageal varices secondary to portal hypertension.
Adverse Effects
Some common side effects of octreotide include:
Gastrointestinal disturbances (such as nausea, vomiting, and abdominal pain)
Altered blood glucose levels (both hyperglycemia and hypoglycemia)
Gallbladder issues, including gallstones
Octreotide plays a crucial role in managing hormone-related conditions, but it requires careful monitoring due to its potential side effects.
#Octreotide
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