Dolasetron

Dolasetron
(IUPAC) ime
	(3R)-10-oxo-8-azatricyclo[5.3.1.03,8]undec-5-yl 1H-indole-3-carboxylate
Klinički podaci
Identifikatori
CAS broj	115956-12-2
ATC kod	A04AA04
PubChem	60654
DrugBank	APRD00518
ChemSpider	16736416
Hemijski podaci
Formula	C19H20N2O3
Mol. masa	324.374 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H20N2O3/c22-18-10-21-12-5-11(18)6-13(21)8-14(7-12)24-19(23)16-9-20-17-4-2-1-3-15(16)17/h1-4,9,11-14,20H,5-8,10H2/t11-,12+,13-,14- ; Key: UKTAZPQNNNJVKR-YXSUXZIUSA-N
Farmakokinetički podaci
Vezivanje za proteine plazme	69 to 77%
Poluvreme eliminacije	8.1 sati
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	Rx samo
Način primene	Intravenozno, oralno

Dolasetron (trgovačko ime Anzemet) je serotonin 5-HT₃ receptor antagonist^[4] korišćen u tretmanu mučnine i povraćanja nakon hemoterapije. Njegov glavni efekat je smanjenje aktivnosti Vagus nerva, koji je nerv što aktivira centar za povraćanje u medulla oblongata. On nema primetan antiemetički efekt kad su simptomi uzrokovani morskom bolešću. Ovaj lek nema efekta na dopamin receptore, nit na muskarinske receptore.

Dolasetron se sporo razlaže, i zadržava se u telu dogo vremena. Jedna doza obično traje 4 do 9 sati. On se normalno administrira jednom ili dva puta dnevno. Ovaj lek se odstranjuje is tela putem jetre i bubrega.

Klinička upotreba

Hemoterapijom prouzrokovana mučnina i povraćanje
- 5-HT₃ receptor antagonisti su primarni lekovi korišćeni u tretmanu hemoterapijom prouzrokovane mučnine i povraćanja. Oni se uglavnom daju intravenozno oko 30 minuta pre hemoterapije.^[5]
Postoperativna i postradijaciona mučnina i povraćanje^[6]^[7]
On je moguća terapija za mučninu i povraćanje prouzrokovanu akutnim ili hroničnim gastroenteritisom
Za razliku od mnogih drugih 5HT3 antagonista, podaci nisu dostupni za upotrebu dolasetrona sa aprepitantom u hemoterapijom izazvanoj mučnini i povraćanju (CINV).

Nuspojave

Dolasetron je dobro podnošen lek sa malo nuspojava. Glavobolja, vrtoglavica, i konstipacija su najčešće pominjane nuspojave njegove upotrebe. Nisu poznate značajne interakcije lekove sa anzemetom. On se razlaže u jetri putem citohrom P450 sistema^[8], i on ima malo efekta na metabolizam drugih lekova razlaganih ovim sistemom.

Povezano

5-HT₃ receptor antagonist: Otkriće i razvoj lekova
DrugBank
Anzemet
Drugs.com

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Katzung BG, Masters S, Trevor A (2009). Basic and Clinical Pharmacology (11 izd.). McGraw-Hill. ISBN 0071604057.
↑ Fauser AA, Dornoff W, Briese V, Knutzen B, Herzog G, Schultze W, Nowicki J (1999). [content.karger.com/ProdukteDB/produkte.asp?Doi=26933 „The Anti-Emetic Efficiacy of Intravenous Dolasetron Mesilate plus Dexamethasone versus Intravenous Dolasetron Mesilate Alone in Patients Receiving Fractionated Chemotherapy”]. Onkologie 22 (2): 140-144. DOI:10.1159/000026933.
↑ Janicki PK, Schuler HG, Jarzembowski TM, Rossi M (2006). [www.anesthesia-analgesia.org/content/102/4/1127.full „Prevention of Postoperative Nausea and Vomiting with Granisetron and Dolasetron in Relation to CYP2D6 Genotype”]. Anasthesia & Analgesia 102 (4): 1127-1133. DOI:10.1213/01.ane.0000200364.5579.
↑ Walker B (2001). „Efficacy of single-dose intravenous dolasetron versus ondansetron in the prevention of postoperative nausea and vomiting”. Clinical Therapeutics 23 (6): 932-938. DOI:10.1016/S0149-2918(01)80080-1.
↑ Sanwald P, David M, Dow J (1996). „Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of dolasetron. Comparison with other indole-containing 5-HT3 antagonists”. Drug metabolism and disposition 24 (5): 602-609.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[Katzung-4] Katzung BG, Masters S, Trevor A (2009). Basic and Clinical Pharmacology (11 izd.). McGraw-Hill. ISBN 0071604057.

[Fauser-5] Fauser AA, Dornoff W, Briese V, Knutzen B, Herzog G, Schultze W, Nowicki J (1999). [content.karger.com/ProdukteDB/produkte.asp?Doi=26933 „The Anti-Emetic Efficiacy of Intravenous Dolasetron Mesilate plus Dexamethasone versus Intravenous Dolasetron Mesilate Alone in Patients Receiving Fractionated Chemotherapy”]. Onkologie 22 (2): 140-144. DOI:10.1159/000026933.

[Janicki-6] Janicki PK, Schuler HG, Jarzembowski TM, Rossi M (2006). [www.anesthesia-analgesia.org/content/102/4/1127.full „Prevention of Postoperative Nausea and Vomiting with Granisetron and Dolasetron in Relation to CYP2D6 Genotype”]. Anasthesia & Analgesia 102 (4): 1127-1133. DOI:10.1213/01.ane.0000200364.5579.

[Walker-7] Walker B (2001). „Efficacy of single-dose intravenous dolasetron versus ondansetron in the prevention of postoperative nausea and vomiting”. Clinical Therapeutics 23 (6): 932-938. DOI:10.1016/S0149-2918(01)80080-1.

[Sanwald-8] Sanwald P, David M, Dow J (1996). „Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of dolasetron. Comparison with other indole-containing 5-HT3 antagonists”. Drug metabolism and disposition 24 (5): 602-609.

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