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Lanreotide
Information about Lanreotide
Lanreotide is a synthetic polypeptide analogue of somatostatin that resembles the native hormone in its ability to suppress levels and activity of growth hormone, insulin, glucagon and many other gastrointestinal peptides. Because its half-life is longer than somatostatin, lanreotide can be used clinically to treat neuroendocrine tumors that secrete excessive amounts of growth hormone (acromegaly) or other active hormones or neuropeptides.
Liver safety of Lanreotide
Lanreotide has many side effects including suppression of gall bladder contractility and bile production, and maintenance therapy may cause cholelithiasis and pancreatitis as well accompanying liver injury.
Mechanism of action of Lanreotide
Lanreotide (lan ree' oh tide) is a synthetic octapeptide and analogue of somatostatin that is used for its ability to suppress levels and activities of hormones (growth hormone, insulin, gastrin, secretin, glucagon) or active neuropeptides (serotonin, vasoactive intestinal polypeptide [VIP]). Natural somatostatin is produced in the hypothalamus and acts to suppress growth hormone release from the pituitary. Somatostatin is also found in other neurons throughout the body and particularly in intestinal and pancreatic neurons, where it is active in suppressing release of hormones and neuropeptides such as insulin, glucagon, gastrin, secretin, motilin, VIP, serotonin and cholecystokinin. Because of its short half-life (~3 minutes), somatostatin is impractical as a therapeutic agent, and analogues have been developed that have a more favorable pharmacological profile such as octreotide, pasireotide and lanreotide, all three of which have been marketed in long acting release (LRA) forms to allow once weekly or monthly administration. Lanreotide appears to interact largely with the somatostatin subtype 2 and possibly subtype 5 receptors, with little effect on subtypes 1, 3 and 4, but otherwise acts in a similar manner to somatostatin. Lanreotide therapy has been shown to improve symptoms and complications of several neuroendocrine tumors including abnormal growth in acromegaly due to growth hormone-secreting pituitary tumors, diarrhea due to VIP-secreting intestinal tumors, and flushing due to serotonin-producing carcinoid tumors.
FDA approval information for Lanreotide
Lanreotide was approved for use in the United States in 2007 and current listed indications include acromegaly and unresectable, locally advanced or metastatic gastroenteropancreatic neuroendocrine tumors. Lanreotide has been used off label for polycystic liver and kidney disease.
Dosage and administration for Lanreotide
A long acting form of lanreotide is available under the brand name Somatuline Depot in prefilled syringes of 60 mg in 0.2 mL, 90 mg in 0.3 mL or 120 mcg in 0.5 mL (240 mg/mL). Lanreotide depot is administered as a deep subcutaneous injection every 4 weeks in doses of 60 to 120 mg each.
Side effects of Lanreotide
Side effects are common. Adverse events from single injections include influenza-like symptoms of fatigue, headache, nausea and vomiting and local injection reactions. With continued therapy, common adverse events include diarrhea, abdominal pain, back pain, headache, dizziness, hypothyroidism, hypo- and hyperglycemia, arrhythmias and gallbladder disease.
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