For treatment of acromegaly and reduction of side effects from cancer chemotherapy
Octreotide binds to somatostatin receptors. These receptors are coupled via pertussis toxin sensitive G proteins which lead to inhibition of adenylyl cyclase. Octreotide binding to these receptors also stimulates phosphotyrosine phosphatase and activation of the Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.
About 32% of the dose is excreted unchanged into the urine.
* 13.6 L [healthy volunteers] * 21.6±8.5 L [patients with acromegaly]
* 7 – 10 L/hr [healthy after 100-mcg SC injection] * 18 L/hr [patients with acromegaly after 100-mcg SC injection] * 8.8 L/hr [mild renal impairment after 100-mcg SC injection] * 7.3 L/hr [moderate renal impairment after 100-mcg SC injection] * 7.6 L/hr [severe renal impairment after 100-mcg SC injection] * 4.5 L/hr [severe renal failure requiring dialysis after 100-mcg SC injection] * 5.9 L/hr [Patients with liver cirrhosis after 100-mcg SC injection] * 8.2 L/hr [patients with fatty liver disease after 100-mcg SC injection]