Dolasetron mesylate

Bezeichnung:Dolasetron mesylate

CAS-Nr115956-13-3

Englisch Name:Dolasetron mesylate

CBNumberCB8341693

SummenformelC20H26N2O7S

Molgewicht438.49

MOL-Datei115956-13-3.mol

Dolasetron mesylate physikalisch-chemischer Eigenschaften

Schmelzpunkt	278°
storage temp.	Sealed in dry,2-8°C
Löslichkeit	H2O: >30mg/mL
Aggregatzustand	powder
Farbe	white to off-white
CAS Datenbank	115956-13-3(CAS DataBase Reference)

Sicherheit

WGK Germany

Gefahreninformationscode (GHS)

Dolasetron mesylate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Dolasetron was launched as Anzemet in Australia and the US for the prevention of nausea and vomiting in chemotherapy patients. It is a highly potent and very selective antagonist of 5-HT3 receptors ; it is the sixth in this class of compounds to be marketed for the treatment of chemotherapy-induced emesis. The last two approved in this class were Nazasetron (1994) and Ramosetron (1996). Anzemet was prepared by a seven step sequence from a cyclopentenecarboxylic ester via a Robinson-Schopf cyclisation of a dialdehyde into a key 9-azabicyclo[3.3.l]nonan-3-one. In a clinical study with 164 cancer patients treated with Dolasetron mesylate prior to Cisplatin, single doses of 10- 50 mg achieved major control of nausea and emesis in 73% of subjects and were well tolerated. Results from pharmacokinetic studies in humans showed that the clinical effects and duration of action seem to be due mainly to a major plasma metabolite rapidly formed and very potent itself, the (+) enantiomeric alcohol obtained by enzymatic reduction of the cyclic ketone.
Originator
Hoechst Marion Roussel (Germany)
Verwenden
Dolasetron Mesylate acts as a bridged pseudopelletierine derivative; specific serotonin (5HT3) receptor antagonist. Antiemetic.
Verwenden
Antidepressant
Verwenden
Nausea in chemotherapy;5-HT3 antagonist
Trademarks
Anzemet (Sanofi Aventis.
Veterinary Drugs and Treatments
Dolasetron may be effective in treating severe nausea and vomiting in dogs and cats, particularly if caused by cancer chemotherapy drugs. Because it is given once a day, the injectable form of dolasetron is often preferred over ondansetron, a similarly effective antiemetic. However, for oral use in small animals, dolasetron tablets are too large (50 and 100 mg) to be practically administered.

Dolasetron mesylate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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