Desloratadin

Desloratadin
(IUPAC) ime
	8-hloro-6,11-dihidro-11-(4-piperdiniliden)- 5H-benzo[5,6]ciklohepta[1,2-b]piridin
Klinički podaci
Robne marke	Klarineks
AHFS/Drugs.com	Monografija
MedlinePlus	a602002
Identifikatori
CAS broj	100643-71-8
ATC kod	R06AX27
PubChem	124087
DrugBank	DB00967
ChemSpider	110575
UNII	FVF865388R
KEGG	D03693
ChEBI	CHEBI:291342
ChEMBL	CHEMBL1172
Hemijski podaci
Formula	C19H19ClN2
Mol. masa	310,82
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2 ; Key: JAUOIFJMECXRGI-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	Brzo se apsorbuje
Vezivanje za proteine plazme	85%
Metabolizam	Jetra
Poluvreme eliminacije	27 sata
Izlučivanje	40% kao conugovani metaboliti u urin
Farmakoinformacioni podaci
Licenca	EU EMEA:link, US FDA:link
Trudnoća	B1(AU) C(US)
Pravni status	POM (UK) ℞-only (SAD)
Način primene	oralno

Desloratadin je lek koji se koristi za tretiranje alergija. On je uprodaji pod imenima NeoClarityn, Claramax, Clarinex, Larinex, Aerius, Dazit, Azomyr, Deselex, Delot, Dasselta i Deslordis. On je aktivni metabolit loratadina, koji je isto tako u prodaji.

Dostupne forme

Desloratadin je dostupan u obliku tableta (uključujući oralno dizintegrirajuće i produženo otputajuće) i kao sirupa.^[6]

Mehanizam dejstva

Desloratadin je triciklični antihistaminik, koji deluje kao selektivni i periferni H₁ antagonist. On je isto tako antagonist na svim tipovima muskarinskog acetilholinskog receptora. On ima dugotrajno dejstvo u umerenim i niskim dozama, i ne uzrokuje somnolenciju jer u maloj meri dospeva u centralni nervni sistem.^[7] Za razliku od drugih antihistaminika, desloratadin je isto tako efektivan u olakšavanju nazalne kongestije, posebno kod pacijenata sa alergijskim rinitisom.^[8]

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
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ FDA Electronic Orange Book
↑ Mann R, Pearce G, Dunn N, Shakir S (2000). „Sedation with "non-sedating" antihistamines: four prescription-event monitoring studies in general practice”. BMJ 320 (7243): 1184–6. DOI:10.1136/bmj.320.7243.1184. PMC 27362. PMID 10784544.
↑ Horak F, Stübner UP, Zieglmayer R, Harris AG (June 2002). „Effect of desloratadine versus placebo on nasal airflow and subjective measures of nasal obstruction in subjects with grass pollen-induced allergic rhinitis in an allergen-exposure unit”. J. Allergy Clin. Immunol. 109 (6): 956–61. PMID 12063524.

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

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[6] FDA Electronic Orange Book

[7] Mann R, Pearce G, Dunn N, Shakir S (2000). „Sedation with "non-sedating" antihistamines: four prescription-event monitoring studies in general practice”. BMJ 320 (7243): 1184–6. DOI:10.1136/bmj.320.7243.1184. PMC 27362. PMID 10784544.

[8] Horak F, Stübner UP, Zieglmayer R, Harris AG (June 2002). „Effect of desloratadine versus placebo on nasal airflow and subjective measures of nasal obstruction in subjects with grass pollen-induced allergic rhinitis in an allergen-exposure unit”. J. Allergy Clin. Immunol. 109 (6): 956–61. PMID 12063524.

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