Ondansetron hydrochloride

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H301：Giftig bei Verschlucken.

  H318：Verursacht schwere Augenschäden.

  H410：Sehr giftig für Wasserorganismen mit langfristiger Wirkung.

• Sicherheit

  P273：Freisetzung in die Umwelt vermeiden.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

Ondansetron hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R25:Giftig beim Verschlucken.
  R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.

• S-Sätze Betriebsanweisung:

  S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
  S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.

• Beschreibung

  Ondansetron hydrochloride is a selective 5HT3-antagonist approved for the management of nausea and vomiting induced by cancer chemotherapy and radiotherapy. It is reported to have a superior side-effect profile compared with metoclopramide, representing an important advance in the treatment of nausea and vomiting associated with chemotherapy. Ondansetron hydrochloride is the first specific 5HT3-antagonist to reach the market. It is also under investigation for a number of other indications, including anxiety and schizophrenia.

• Chemische Eigenschaften

  White or almost white powder.

• Originator

  Glaxo (United Kingdom)

• Verwenden

  These Secondary Standards are qualified as Certified Reference Materials. These are suitable for use in several analytical applications including but not limited to pharma release testing, pharma method development for qualitative and quantitative analyses, food and beverage quality control testing, and other calibration requirements.

• Verwenden

  Ondansetron hydrochloride dihydrate has been used as a 5-HT₃ antagonist to attenuate rostro ventromedial medulla (RVM)/cholecystokinin (CCK)-induced mechanical hypersensitivity and to block the effects of trichostatin A (TSA) on 5-HT₃ protein.

• Verwenden

  A serotonin type 3 receptor antagonist.

• Verwenden

  Antiemetic;Serotonergic receptor antagonist

• Definition

  ChEBI: Ondansetron hydrochloride is a member of carbazoles.

• Manufacturing Process

  Preparation of 3-ethoxalyl-9-methyl-1,2,3,9-tetrahydro-4H-carbozol-4-one 3.0 g (0.13 mole) of sodium metal are portionwise added to a stirred mixture containing 19.93 g (0.1 mole) of 9-methyl-1,2,3,9-tetrahydro-4H-carbazol-4one, 19.0 g (0.13 mole) of diethyl oxalate, 2 g of ethanol and 200 ml of dioxane. The slightly warming reaction mixture is stirred at 40° to 50°C for 4 hours, then 16 g of glacial acetic acid and finally 200 ml of water are added thereto at room temperature. After filtering off the yellow crystalline suspension, the precipitate is washed with water and dried to give the title compound in a yield of 24 g (80.2%), m.p. 118°-120°C
  Preparation of 3-hydroxymethyl-9-methyl-1,2,3,9-tetrahydro-4H-carbazol-4one-3-glyoxylic acid lacton
  After adding 0.1 g of triethylamine to a stirred suspension containing 3.00 g (0.01 mole) of the 3-ethoxalyl-9-methyl-1,2,3,9-tetrahydro-4H-carbazol-4 2512 one, in 20 ml of acetone, 1.13 g (0.015 mole) of formol solution are dropwise added to the mixture. The suspension becomes clear within 1 to 2 minutes and crystals begin to precipitate. After further stirring at 35° to 40°C for one hour, the reaction mixture is cooled down to room temperature, filtered off, the precipitate is washed with 50% acetone and dried to give 2.10 g (74.2%) of the title compound, m.p. 242°-244°C.
  Preparation of ondansetron base (chemically 9-methyl-3-[(2-methyl-1-Himidazol-1-yl)methyl]-1,2,3,9-tetrahidro-4-H-carbazol-4-one)
  A mixture containing 2.83 g (0.01 mole) of 3-hydroxymethyl-9-methyl-2,3,9tetrahydro-4H-carbazol-4-one-3-glyoxylic acid lactone, 15 ml of dioxane, 1.32 g of triethylamine, 1.0 g of ethanol and 1.64 g (0.02 mole) of 2methylimidazole is boiled under reflux while stirring for 5 hours. Thereafter, the reaction mixture is diluted with 45 ml of water and cooled down. The precipitate is filtered off, washed with aqueous dioxane and dried to obtain 2.56 g (87.3%) of the title compound, m.p. 220°-223°C.
  Preparation of 9-methyl-3-[(2-methyl-1-H-imidazol-1-yl)methyl]-1,2,3,9tetrahydro-4H-carbazol-4-one hydrochloride dihydrate The process above described is followed, except that after cooling down the reaction mixture to room temperature after boiling, 20 ml of 37% aqueous hydrochloric acid are added thereto. Then, the precipitate is filtered off, washed with isopropanol and dried to obtain 2.40 g (65.6%) of the title salt, m.p. 178°-180°C. The active agent content of the product was found to be 100.3% based on potentiometric titration with sodium hydroxide solution. The theoretical water content is 9.85% (calculated for C18H19N3OHCl2H2O).The water content measured is 10.03%.

• Trademarks

  Zofran (GlaxoSmithKline);Zophran.

• Therapeutic Function

  Serotonin antagonist

• Allgemeine Beschreibung

  Ondansetron Hydrochloride acts as a 5HT3 (serotonin) antagonist and is a powerful antiemetic drug. It is widely used for the prevention and treatment of nausea and vomiting related to post-operative states, cancer chemotherapy and radiotherapy, and chronic medical illness. It has been found to exhibit inconsistent bioavailability resulting from its poor aqueous solubility and high first-pass hepatic metabolism.
  Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.

• Biologische Aktivität

  Selective 5-HT 3 receptor antagonist (K i = 6.16 nM). Antiemetic; prevents emesis induced by cytotoxic drugs and radiation.

• Biochem/physiol Actions

  5-HT3 serotonin receptor antagonist

• Lager

  Room temperature

Ondansetron hydrochloride Upstream-Materialien And Downstream Produkte

Ondansetron hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(467)Suppliers

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