desloratadine

Desloratadine
Systematic (IUPAC) name
	8-chloro-6,11-dihydro-11-(4-piperdinylidene)- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Clinical data
Trade names	Clarinex
AHFS/Drugs.com	monograph
MedlinePlus	a602002
Licence data	EMA:Link, US FDA:link
Pregnancy; category	AU: B1; US: C (Risk not ruled out);
Legal status	AU: Pharmacy Only (S2); CA: OTC; UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	oral
Pharmacokinetic data
Bioavailability	Rapidly absorbed
Protein binding	85%
Metabolism	Liver
Half-life	27 hours
Excretion	40% as conjugated metabolites into urine; Similar amount into the feces
Identifiers
CAS Registry Number	100643-71-8
ATC code	R06AX27
PubChem	CID: 124087
IUPHAR ligand	7157
DrugBank	DB00967
ChemSpider	110575
UNII	FVF865388R
KEGG	D03693
ChEBI	CHEBI:291342
ChEMBL	CHEMBL1172
Chemical data
Formula	C19H19ClN2
Molecular mass	310.82
	SMILES Clc4cc2c(C(/c1ncccc1CC2)=C3/CCNCC3)cc4;
	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 ;
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同: Clarinex

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/06/17 19:38:14」(JST)

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[Wiki en表示]

Desloratadine is a drug used to treat allergies. It is an active metabolite of loratadine.

Use

Desloratadine is used to treat allergic rhinitis and nasal congestion.^[1] It is the major metabolite of loratadine and the two drugs are similar in safety and effectiveness.^[1]

Side effects

Most common side-effects are fatigue, dry mouth, headache, and gastrointestinal disturbances.^[1]

Mechanism of action

Desloratadine is a tricyclic antihistamine, which has a selective and peripheral H₁-antagonist action. It is an antagonist at histamine H1 receptors, and an antagonist at all subtypes of the muscarinic acetylcholine receptors. It has a long-lasting effect and in moderate and low doses, does not cause drowsiness because it does not readily enter the central nervous system.^[2]

Society and culture

Desloratadine is available in many dosage forms and under many trade names worldwide.^[3]

References

^ ^a ^b ^c See S (2003). "Desloratadine for allergic rhinitis". Am Fam Physician 68 (10): 2015–6. PMID 14655812.
^ 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.
^ Drugs.com Desloratadine entry at drugs.com international Page accessed May 4, 2015

UpToDate Contents

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1. 寒冷蕁麻疹 cold urticaria
2. アレルギー性鼻炎の薬物療法 pharmacotherapy of allergic rhinitis
3. アレルギー性結膜炎：マネージメント allergic conjunctivitis management
4. 慢性蕁麻疹：標準的なマネージメントおよび患者教育 chronic urticaria standard management and patient education
5. 物理性蕁麻疹 physical urticarias

English Journal

Tap water nasal irrigation in adults with seasonal allergic rhinitis: a randomized double-blind study.

Xiong M1, Fu X, Deng W, Lai H, Yang C.
European archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery.Eur Arch Otorhinolaryngol.2014 Jun;271(6):1549-52. doi: 10.1007/s00405-013-2741-4. Epub 2013 Oct 4.
Saline nasal irrigation is effective in the treatment of seasonal allergic rhinitis, and sodium chloride itself has no antiallergic effects. The mechanism of saline nasal irrigation depends mainly on washing away allergens and inflammatory mediators induced by allergic reactions. Tap water has the s
PMID 24091560

Utility of Cerebrospinal Fluid Drug Concentration as a Surrogate for Unbound Brain Concentration in Nonhuman Primates.

Nagaya Y1, Nozaki Y, Kobayashi K, Takenaka O, Nakatani Y, Kusano K, Yoshimura T, Kusuhara H.
Drug metabolism and pharmacokinetics.Drug Metab Pharmacokinet.2014 May 6. [Epub ahead of print]
In the central nervous system drug discovery, cerebrospinal fluid (CSF) drug concentration (CCSF) has been widely used as a surrogate for unbound brain concentrations (Cu,brain). However, previous rodent studies demonstrated that when drugs undergo active efflux by transporters, such as P-glycopr
PMID 24806821