Longastatin
Longastatin - General Information
Longastatin is the acetate salt of a cyclic octapeptide. It is a long-acting octapeptide with pharmacologic properties mimicking those of the natural hormone somatostatin.
Pharmacology of Longastatin
Longastatin exerts pharmacologic actions similar to the natural hormone, somatostatin. It is an even more potent inhibitor of growth hormone, glucagon, and insulin than somatostatin. Like somatostatin, it also suppresses leuteinizing hormone (LH) response to GnRH, decreases splanchnic blood flow, and inhibits release of serotonin, gastrin, vasoactive intestinal peptide, secretin, motilin, and pancreatic polypeptide. Longastatin has been used to treat the symptoms associated with metastatic carcinoid tumors (flushing and diarrhea), and Vasoactive Intestinal Peptide (VIP) secreting adenomas (watery diarrhea). Longastatin substantially reduces and in many cases can normalize growth hormone and/or IGF-1 (somatomedin C) levels in patients with acromegaly.
Longastatin for patients
Longastatin Interactions
Octreotide has been associated with alterations in nutrient absorption, so it may have an effect on absorption of orally administered drugs. Concomitant administration of octreotide injection with cyclosporine may decrease blood levels of cyclosporine and result in transplant rejection.
Patients receiving insulin, oral hypoglycemic agents, beta-blockers, calcium channel blockers, or agents to control fluid and electrolyte balance, may require dose adjustments of these therapeutic agents.
Concomitant administration of octreotide and bromocriptine increases the availability of bromocriptine. Limited published data indicate that somatostatin analogs might decrease the metabolic clearance of compounds known to be metabolized by cytochrome P450 enzymes, which may be due to the suppression of growth hormones. Since it cannot be excluded that octreotide may have this effect, other drugs mainly metabolized by CYP3A4 and which have a low therapeutic index (e.g., quinidine, terfenadine) should therefore be used with caution.
Drug Laboratory Test Interactions
No known interference exists with clinical laboratory tests, including amine or peptide determinations.
Longastatin Contraindications
Sensitivity to this drug or any of its components.
Additional information about Longastatin
Longastatin Indication: For treatment of acromegaly and reduction of side effects from cancer chemotherapy
Mechanism Of Action: Longastatin binds to somatostatin receptors. These receptors are coupled via pertussis toxin sensitive G proteins which lead to inhibition of adenylyl cyclase. Longastatin binding to these receptors also stimulates phosphotyrosine phosphatase and activation of the Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Octreotide
Synonyms: Octreotide acetate; Octreotidum [Latin]; Octreotida [Spanish]; Octrotide
Drug Category: Anabolic Agents; Hormone Replacement Agents; Gastrointestinal Agents; Antineoplastic Agents, Hormonal
Drug Type: Biotech; Approved; Investigational
Other Brand Names containing Octreotide: Sandostatin LAR (Novartis); Longastatin; Sandostatin; Sandostatin LAR; Atrigel;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: Not Available
Dosage Forms of Longastatin: Powder Intramuscular
Solution Intravenous
Chemical IUPAC Name: 10-(4-aminobutyl)-19-[(2-amino-3-phenylpropanoyl)amino]-N-(1,3-dihydroxybutan-2-yl)-7-(1-hydroxyethyl)-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-16-(phenylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
Chemical Formula: C49H66N10O10S2
Octreotide on Wikipedia: https://en.wikipedia.org/wiki/Octreotide
Organisms Affected: Humans and other mammals