      Document 0132
 DOCN  DRG0132
 UNIQUE IDENTIFIER        DRG-0115
 NAME OF SUBSTANCE        Octreotide acetate [USAN 1996]
 REGISTRY NUMBER          79517-01-4
 STANDARD CHEMICAL NAME   L-cysteinamide,
                          D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-
                          tryptophyl-L-lysyl-L-threonyl-N-(2-hydroxy-1-
                          (hydroxymethyl)propyl)- cyclic
                          (2->7)-disulfide, (R-(R*,R*))-, acetate [USAN
                          1996]
 SYNONYMS                 Sandostatin [PDR 1995]
 PROTOCOL ID NUMBERS      FDA 102A
 PROTOCOL ID NUMBERS      FDA 102B
 SECONDARY SOURCE ID      SMS-201-995ac [USAN 1993]
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Suppresses secretion of
                          serotonin and the gastroenteropancreatic
                          peptides: gastrin, vasoactive intestinal
                          peptide, insulin, glucagon, secretin,
                          motilin, and pancreatic polypeptide.
                          Suppresses growth hormone. Enhances water and
                          electrolyte absorption. [PDR 1995]
 DISEASES STUDIED/TREATED Under investigation for the treatment of
                          cryptosporidiosis and HIV-related diarrhea
                          [AmFAR Tx Dir 1995;7(4)]
 CLASSIFICATION CODE      Antidiarrheal [USAN 1996]
 OTHER MAJOR USES         Metastatic carcinoid and vasoactive
                          intestinal peptide-secreting tumors and
                          acromegaly [PDR 1995]
 SUBSTANCE INTERACTIONS   May interfere with drugs affecting glucose
                          metabolism such as insulin, and the dosage of
                          these drugs may need to be adjusted. May
                          interfere with the absorption of any orally
                          administered drug and they should be
                          carefully monitored. May decrease
                          cyclosporine blood levels, resulting in
                          transplant rejection. [PDR 1995]
 ADVERSE EFFECTS          Adverse effects include nausea, injection
                          site pain, diarrhea, abdominal
                          pain/discomfort, loose stools, vomiting, and
                          gallbladder abnormalities. [PDR 1995]
 CONTRAINDICATIONS        Contraindicated in patients with known
                          sensitivity to the drug or any of its
                          components. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Long-acting synthetic
                          octapeptide analog of somatostatin that
                          mimics the inhibitory action of the naturally
                          occurring hormone somatostatin [PDR 1995]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C49H66N10O10S2.xC2H4O2
                          [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 1019.24 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   ELEMENTAL COMPOSITION: C57.74%, H6.53%,
                          N13.74%, O15.70%, S6.29% [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: Clear solution [PDR
                          1995]
 CHEMICAL/PHYSICAL DATA   STABILITY: Stable for 14 days at room
                          temperature if protected from light [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: Ampules (50, 100, 500 mcg/ml);
                          vials (200 and 1,000 mcg/ml). [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Subcutaneous injection or
                          intravenous infusion. [PDR 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: For prolonged storage, ampules
                          should be stored in the refrigerator at 2-8 C
                          (36-46 F) and protected from light [PDR 1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Ampules can be stored at room
                          temperature (20-30C or 70-86F) for the day
                          they will be used. [PDR 1995]
 MANUFACTURERS            Sandoz
 REFERENCES               Simon DM, Cello JP, Valenzuela J, Levy R,
                          Dickerson G, Goodgame R, Brown M, Lyche K,
                          Fessel WJ, Grendell J, et al. Multicenter
                          trial of octreotide in patients with
                          refractory acquired immunodeficiency
                          syndrome-associated diarrhea [see comments].
                          Gastroenterology. 1995 Jun;108(6):1753-60.
 REFERENCES               Garcia Compean D, Ramos Jimenez J, Guzman de
                          la Garza F, Saenz C, Maldonado H, Barragan
                          RF, Michel H. Octreotide therapy of
                          large-volume refractory AIDS-associated
                          diarrhea: a randomized controlled trial.
                          AIDS. 1994 Nov;8(11):1563-7.
 REFERENCES               Miranda-Ruiz R, Feregrino-Goyos M, Alvarado
                          Diez R, Castanon GJ, Gallegos-Perez H,
                          Eid-Lidt G. Experience of two years in
                          therapy of AIDS hypersecretory diarrhea with
                          octreotide. Int Conf AIDS. 1994 Aug
                          7-12;10(1):187 (abstract no. PB0177).
 REFERENCES               Mosdell KW, Visconti JA. Emerging indications
                          for octreotide therapy, Part 1. Am J Hosp
                          Pharm. 1994 May 1;51(9):1184-92.
 REFERENCES               Manfredi R, Vezzadini P, Costigliola P,
                          Ricchi E, Fanti MP, Chiodo F. Elevated plasma
                          levels of vasoactive intestinal peptide in
                          AIDS patients with refractory idiopathic
                          diarrhoea. Effects of treatment with
                          octreotide. AIDS. 1993 Feb;7(2):223-6.
 REFERENCES               Moroni M, Esposito R, Cernuschi M, Franzetti
                          F, Carosi GP Fiori GP. Treatment of
                          AIDS-related refractory diarrhoea with
                          octreotide. Digestion. 1993;54 Suppl 1:30-2.
 REFERENCES               Beaugerie L, Baumer P, Berard H, Rozenbaum W,
                          Pialoux G, Lecomte JM. Treatment of
                          refractory diarrhea in AIDS with acetorphan
                          and octreotide: a randomized cross over
                          study. Int Conf AIDS. 1993 Jun 6-11;9(1):64
                          (abstract no. WS-B21-6).
 REFERENCES               Liberti A, Bisogno A, Izzo E. Octreotide
                          treatment in secretory and cryptosporidial
                          diarrhea in patients with acquired
                          immunodeficiency syndrome (AIDS): clinical
                          evaluation. J Chemother. 1992 Oct;4(5):303-5.
 REFERENCES               Harris AG, Ambrus K, Boerlin V. Effect of the
                          somatostatin analog, octreotide, in
                          AIDS-related refractory diarrhea. The
                          International AIDS-Diarrhea Study Group. Int
                          Conf AIDS. 1992 Jul 19-24;8(3):88 (abstract
                          no. PuB 7234).
 REFERENCES               Cello JP, Grendell JH, Basuk P, Simon D,
                          Weiss L, Wittner M, Rood RP, Wilcox CM,
                          Forsmark CE, Read AE, et al. Effect of
                          octreotide on refractory AIDS-associated
                          diarrhea. A prospective, multicenter clinical
                          trial. Ann Intern Med. 1991 Nov
                          1;115(9):705-10.
 ENTRY MONTH              9105
 LAST REVISION DATE       951213
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
