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Dolasetron
drug data and news
Dolasetron drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Dolasetron | ||
| Brand Names/Synonyms | Anzemet; CHEMBANK1627; Dolasetron; Dolasetronum [Inn-Latin]; Dolasteron | ||
| Indication | For the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy, including initial and repeat courses and prevention of postoperative nausea and vomiting | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Dolasetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. | ||
| Mechanism Of Action | Dolasetron is a selective serotonin 5-HT3 receptor antagonist. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine, and that the released serotonin then activates 5-HT3 receptors located on vagal efferents to initiate the vomiting reflex. Therefore Dolasetron works by blocking the reception of serotonin at these 5-HT3 receptors. | ||
| Dolasetron News (When available) |
Subcutaneous Amifostine Feasible During Radiotherapy for Head and ... Mar 1, 2006 FDA Approves EMEND(R) (aprepitant), in Combination with Other ... Jan 11, 2006 Genta Appoints Seasoned Pharma Executive, Lloyd Sanders, as Vice ... Jan 17, 2006 Organon Enters into Distribution Agreement for Anzemet(R) Dec 5, 2005 Delayed Nausea After Chemotherapy Poses Treatment Challenge Sep 20, 2005 Antiemetics of the 5-Hydroxytryptamine 3A Antagonist Class Inhibit ... Aug 22, 2005 Pharmacokinetics of Palonosetron in Combination With Aprepitant in ... Jun 8, 2005 Helsinn’s New Antiemetic Drug Aloxi(R) Receives Marketing ... Apr 4, 2005 News For Your Web Site Apr 19, 2005 Helsinn’s New Antiemetic Drug Aloxi(R) Receives Marketing ... Apr 4, 2005 | ||
| Dosage Forms | Intravenous injection; Tablet | ||
| Drug_Category | Antiemetics; Serotonin Antagonists; ATC:A04AA04 | ||
| Absorption | Orally-administered dolasetron is well absorbed | ||
| Interactions | Interactions for Dolasetron: The potential for clinically significant drug-drug interactions posed by dolasetron and hydrodolasetron appears to be low for drugs commonly used in chemotherapy or surgery, because hydrodolasetron is eliminated by multiple routes. Blood levels of hydrodolasetron increased 24% when dolasetron was coadministered with cimetidine (nonselective inhibitor of cytochrome P-450) for 7 days, and decreased 28% with coadministration of rifampin (potent inducer of cytochrome P-450) for 7 days. Dolasetron has been safely coadministered with drugs used in chemotherapy and surgery. As with other agents which prolong ECG intervals, caution should be exercised in patients taking drugs which prolong ECG intervals, particularly QTc. In patients taking furosemide, nifedipine, diltiazem, ACE inhibitors, verapamil, glyburide, propranolol, and various chemotherapy agents, no effect was shown on the clearance of hydrodolasetron. Clearance of hydrodolasetron decreased by about 27% when dolasetron mesylate was administered intravenously concomitantly with atenolol. Dolasetron does not influence anesthesia recovery time in patients. Dolasetron mesylate did not inhibit the antitumor activity of four chemotherapeutic agents (cisplatin, 5-fluorouracil, doxorubicin, cyclophosphamide) in four murine models. | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | Not Available | ||
| Chemical Formula | C19H20N2O3 | ||
| Molecular Weight | 324.374 g/mol | ||
| Smiles String | C1C2CC3CC(CC1N3CC2=O)OC(=O)C4=CNC5=CC=CC=C54 | ||
| Melting Point | 278 °C | ||
| Water Solubility | Freely soluble in water | ||
| State | Solid | ||
| LogP/Hphobicity | 2.347 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 8.1 hours | ||
| Protein Binding [%] | 69-77% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Dolasetron.html http://www.rxlist.com/cgi/generic2/dolaset.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00518 | ||
| CAS Registry Number | 115956-12-2 | ||
| KEGG Compound ID | C07866 | ||
| PubChem ID | SID:210767 | ||
| PharmGKB ID | PA449390 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2231380 |
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