Octreotide

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Octreotide
Systematic (IUPAC) name
(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19- [[(2R)-2-amino-3-phenyl-propanoyl]amino]-16- benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7- (1-hydroxyethyl)-13-(1H-indol-3-ylmethyl)-6,9,12, 15,18-pentaoxo-1,2-dithia-5,8,11,14,17- pentazacycloicosane-4-carboxamide
Identifiers
CAS number	83150-76-9
ATC code	H01CB02
PubChem	54373
DrugBank	BTD00088
Chemical data
Formula	C49H66N10O10S2
Mol. mass	1019.24 g/mol
Pharmacokinetic data
Bioavailability	100%; I.M: 60% to 63% of subcutaneous dose
Protein binding	65%
Metabolism	Hepatic
Half life	1.7-1.9 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	B(US)
Legal status
Routes	Intramuscular, intravenous

Octreotide (brand name Sandostatin, Novartis Pharmaceuticals) is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was first synthesized in 1979 by the chemist Wilfried Bauer.

Contents 1 Pharmaceutical Effects 2 Adverse Effects 3 Uses 4 References 5 External links

[edit] Pharmaceutical Effects

Since Octreotide resembles Somatostatin in physiological activities, it can:

• Inhibit secretion of many hormones, such as gastrin, cholecystokinin, glucagon, growth hormone, insulin, secretin, pancreatic polypeptide, TSH, and vasoactive intestinal peptide.
• Reduce secretion of fluids by the intestine and pancreas.
• Reduce gastrointestinal motility and inhibits contraction of the gallbladder.
• Inhibit the action of certain hormones from the anterior pituitary.
• Cause vasoconstriction in the blood vessels.

[edit] Adverse Effects

Some of the formulations of this drug show some adverse effects, most important of which is the QT-Interval prolonging. As a rule, a drug that causes prolonged QT-Interval shall have Drug-Drug Interaction possibilities. This indicates that giving such drug shall be of care so that no severe interactions can occur. Octreotide usually shows certain commonly observed adverse effects that differ in the frequency from patient to another:

Most Frequent Adverse Effects: Abdominal Pain with Cramps, Bradycardia, Conduction Disorder of the Heart, Constipation, Diarrhea, Disorder of the Digestive System, Injection Site Sequelae, Nausea, Vomiting

Less Frequent Adverse Effects: Discolored Feces, Dyspepsia, Flatulence, Hypothyroidism, Steatorrhea, Tenesmus

Rare Adverse Effects: Acute Pancreatitis, Alopecia, Biliary Calculus, Disease of Liver, Dizziness, Edema, Fatigue, Fever, Flushing, General Weakness, Headache Disorder, Hepatitis, Hyperbilirubinemia, Hyperglycemia, Hypoglycemic Disorder, Prolonged QT Interval

Keep in mind that this drug can cause diarrhea despite the fact of being used in the treatment of diarrhea!

[edit] Uses

The Food and Drug Administration (FDA) has approved the usage of a salt form of this peptide, octreotide acetate, as an injectable depot formulation for the treatment of acromegaly, the treatment of diarrhea and flushing episodes associated with carcinoid syndrome, and treatment of diarrhea in patients with vasoactive intestinal peptide-secreting tumors (VIPomas).

Octreotide has also been used off-label for the treatment of severe, refractory diarrhea from other causes. It is used in toxicology for the treatment of prolonged recurrent hypoglycemia after sulfonylurea overdose.

Octreotide has also been used with varying degrees of success in infants with nesidioblastosis to help decrease insulin hypersecretion.

In patients with suspected esophageal varices, octreotide can be given to help decrease bleeding.

Octreotide has been investigated for patients with pain from chronic pancreatitis.^[1]

Octreotide may be useful in the treatment of thymic neoplasms.

Octreotide has been used as an unlicensed drug, injected sub-cutaneously in the management of hypertrophic pulmonary osteoarthropathy (HPOA), secondary to non-small cell lung carcinoma. Although its mechanism is not known it appears to reduce the pain associated with HPOA

[edit] References

1. ^ Uhl W, Anghelacopoulos SE, Friess H, Büchler MW (1999). "The role of octreotide and somatostatin in acute and chronic pancreatitis". Digestion 60 Suppl 2: 23-31. doi:10.1159/000051477. PMID 10207228. 

• (2004) in Katzung, Bertram G. (ed.): Basic and Clinical Pharmacology. Stamford, Conn: Lange Medical Books/McGraw Hill. ISBN 0-07-141092-9. 

[edit] External links

• Caring for Carcinoid Foundation
• Sandostatin (Octreotide) brand homepage
• [1] Indevus Pharma and Octreotide

v • d • e Pituitary and hypothalamic hormones and analogues (H01) Anterior pituitary Adrenocorticotropic hormone (Corticotropin, Tetracosactide) - Thyrotropin - Somatropin/agonists (Somatrem, Mecasermin, Sermorelin) - other (Pegvisomant) Posterior pituitary Vasopressin (Desmopressin, Lypressin, Terlipressin, Ornipressin, Argipressin) - Oxytocin (Demoxytocin, Carbetocin) Hypothalamic gonadotropin-releasing hormones (Gonadorelin, Nafarelin, Histrelin) - antigrowth hormone (Somatostatin, Octreotide, Lanreotide) - anti-gonadotropin-releasing hormones (Ganirelix, Cetrorelix)