Zofran
AKOS NCG1-0013 · ondansetron hyd · OndansetronHclUsp28 · Ondansetron hydrochl · ODANSETRON HYDROCHLORIDE · Ondansetron hydrochlorid · OndansetronHClmonohydrate · Ondansetron hydrochloride
Identifikatoren & physikalische Daten
| CAS No. | 103639-04-9 |
|---|---|
| Summenformel | C18H24ClN3O3 |
| Durchschnittliche Molmasse | 365,9 g/mol |
| Monoisotopische Masse | 365,15061931 g/mol |
| SMILES | Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O.Cl.O.O |
| InChIKey | VRSLTNZJOUZKLX-UHFFFAOYSA-N |
| PubChem CID | 59774 |
| ChEBI | CHEBI:7774 |
| EC No. | 600-465-5 |
| DTXSID | DTXSID9048857 |
Chemische & physikalische Eigenschaften
| Polarare Oberfläche (TPSA) | 41,8 |
|---|---|
| H-Brücken-Donoren | 3 |
| H-Brücken-Akzeptoren | 4 |
| Frei drehbare Bindungen | 2 |
| Schwere Atome | 25 |
| Formalladung | 0 |
| Komplexität | 440 |
| Human Drugs | Breast FeedingLactationMilk, HumanAntiemeticsGastrointestinal AgentsSerotonin AntagonistsSerotonin 5-HT3 Receptor Antagonists |
| Schmelzpunkt | 231-232 C |
| Lagerbedingungen | -20°C |
| Löslichkeit | H2O: >5mg/mL |
| Aggregatzustand | powder |
| Farbe | white |
| InChI | InChI=1S/C18H19N3O.ClH.H2O/c1-12-19-9-10-21(12)11-13-7-8-16-17(18(13)22)14-5-3-4-6-15(14)20(16)2/h3-6,9-10,13H,7-8,11H2,1-2H3 |
| InChIKey | FELGMEQIXOGIFQ-ZDUSSCGKSA-N |
| SMILES | O=C1C(CCC2N(C)C3=CC=CC=C3C1=2)CN1C=CN=C1C.Cl.O |
| CAS Datenbank | 103639-04-9(CAS DataBase Reference) |
Sicherheit & Vorschriften
| GHS-Einstufung | DangerH301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]P264, P264+P265, P270, P273, P280, P301+P316, P305+P351+P338, P305+P354+P338, P317, P321, P330, P337+P317, P391, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 117 reports by companies from 16 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. |
|---|---|
| Hazard Classes and Categories | Acute Tox. 3 (100%) |
| Treatment | There is no specific antidote for ondansetron overdose. Patients should be managed with appropriate supportive therapy. (L1712) |
| Expositionspfade | Ondansetron is well absorbed after oral administration and undergoes limited first-pass metabolism. |
| Toxizitätsübersicht | Ondansetron is a selective serotonin 5-HT<sub>3</sub> receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT<sub>3</sub> receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT<sub>3</sub> receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. |
| Signs and Symptoms | Low blood pressure and fainting, sudden blindness, severe constipation |
| Carcinogen Classification | No indication of carcinogenicity to humans (not listed by IARC). |
| Effects During Pregnancy and Lactation | ◉ Summary of Use during Lactation |
| Wassergefährdungsklasse (WGK) | 3 |
| UN-Transportnummer | UN 2811 |
| Zollcode | 2933290000 |
| RTECS-Nr. | FE6375500 |
| R-Sätze (R) | 25-36/37/38-50/53-41 |
Anwendungen & Verwendung
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.
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.