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Wikipedia - Desloratadine

Desloratadine


Systematic (IUPAC) name
8-chloro-6,11-dihydro-11-(4-piperdinylidene)- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Identifiers
CAS number	100643-71-8
ATC code	R06AX27
PubChem	CID 124087
DrugBank	APRD00324
ChemSpider	110575
Chemical data
Formula	C₁₉H₁₉Cl N₂
Mol. mass	310.82
SMILES	eMolecules & PubChem
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
Therapeutic considerations
Licence data	EU EMA:link, US FDA:link
Pregnancy cat.	B1(AU) C(US)
Legal status	POM (UK) ?-only (US)
Routes	oral
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Desloratadine is a drug used to treat allergies. It is marketed under several trade names such as NeoClarityn, Claramax, Clarinex, Aerius and Delot ( by Apex Pharma Ltd. in Bangladesh). It is an active metabolite of loratadine, which is also on the market.

1 Available forms
2 Mechanism of action
3 Side effects
4 Desloratadine vs. loratadine
5 References

[edit] Available forms

Desloratadine is available as tablets (including orally disintegrating and extended release) and as syrup. ^[1]

[edit] Mechanism of action

Desloratadine is a tricyclic antihistamine, which has a selective and peripheral H₁-antagonist action. It has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.^[2]

[edit] Side effects

Most common side-effects are fatigue, dry mouth, headache, and gastrointestinal disturbances.

[edit] Desloratadine vs. loratadine

Desloratadine is the major metabolite of loratadine. There are no head-to-head randomised controlled trials of the two drugs. A survey of patients dissatisfied with loratadine published in August 2003 reported equal or better satisfaction with desloratadine^[3], concluding:

When severity of disease was controlled for in the analysis, a pattern emerged suggesting greater levels of satisfaction amongst loratadine dissatisfied patients who converted to desloratadine. Point estimates suggest a consistent pattern favoring desloratadine patient satisfaction, with statistically significant results reported for sum of adverse effects, nighttime awakening due to symptoms, symptom severity just prior to the next dose, and overall satisfaction (p < 0.05).

A November 2003 article published in the journal American Family Physician about the safety, tolerability, effectiveness, price, and simplicity of desloratadine concluded the following:^[4]

Desloratadine is similar in effectiveness to fexofenadine and would be expected to produce results similar to loratadine and other nonsedating antihistamines. There is no clinical advantage to switching a patient from loratadine to desloratadine. However, it may be an option for patients whose medical insurance no longer covers loratadine if the co-pay is less than the cost of the over-the-counter product.

[edit] References

^ FDA Electronic Orange Book http://www.fda.gov/cder/ob/default.htm
^ 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. PMID 10784544. PMC 27362. http://bmj.bmjjournals.com/cgi/content/full/320/7243/1184.
^ Glass D, Harper A (August 13, 2003). "Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine". BMC Fam Pract 4: 10. doi:10.1186/1471-2296-4-10. PMID 12917016. PMC 194638. http://www.pubmedcentral.gov/articlerender.fcgi?tool=pubmed&pubmedid=12917016.
^ See S (2003). "Desloratadine for allergic rhinitis". Am Fam Physician 68 (10): 2015–6. PMID 14655812. http://www.aafp.org/afp/20031115/steps.html.

Histaminergics

Receptor
Ligands

H₁	Agonists: 2-Pyridylethylamine • Betahistine • Histamine • HTMT • UR-AK49 Antagonists: 1st Generation: 4-Methyldiphenhydramine • Alimemazine • Antazoline • Azatadine • Bamipine • Benzatropine (Benztropine) • Bepotastine • Bromazine • Brompheniramine • Buclizine • Captodiame • Carbinoxamine • Chlorcyclizine • Chloropyramine • Chlorothen • Chlorpheniramine • Chlorphenoxamine • Cinnarizine • Clemastine • Clobenzepam • Clocinizine • Cyclizine • Cyproheptadine • Dacemazine • Deptropine • Dexbrompheniramine • Dexchlorpheniramine • Dimenhydrinate • Dimetindene • Diphenhydramine • Diphenylpyraline • Doxylamine • Embramine • Etybenzatropine (Ethylbenztropine) • Etymemazine • Histapyrrodine • Homochlorcyclizine • Hydroxyethylpromethazine • Hydroxyzine • Isopromethazine • Isothipendyl • Meclizine • Mepyramine (Pyrilamine) • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • Phenindamine • Pheniramine • Phenyltoloxamine • Pimethixene • Piperoxan • Promethazine • Propiomazine • Pyrrobutamine • Talastine • Thenalidine • Thenyldiamine • Thiazinamium • Thonzylamine • Tolpropamine • Tripelennamine • Triprolidine; 2nd Generation: Acrivastine • Astemizole • Azelastine • Cetirizine • Clemizole • Clobenztropine • Ebastine • Emedastine • Epinastine • Ketotifen • Latrepirdine • Levocabastine • Loratadine • Mebhydrolin • Mizolastine • Olopatadine • Rupatadine • Setastine • Terfenadine; 3rd Generation: Desloratadine • Fexofenadine • Levocetirizine; Miscellaneous: Tricyclic Antidepressants (Amitriptyline, Doxepin, Trimipramine, etc) • Tetracyclic Antidepressants (Mianserin, Mirtazapine, etc) • Serotonin Antagonists and Reuptake Inhibitors (Trazodone, Nefazodone) • Typical Antipsychotics (Chlorpromazine, Thioridazine, etc) • Atypical Antipsychotics (Clozapine, Olanzapine, Quetiapine, etc)

H₂	Agonists: Amthamine • Betazole • Dimaprit • Histamine • HTMT • Impromidine • UR-AK49 Antagonists: Cimetidine • Famotidine • Lafutidine • Lavoltidine • Metiamide • Niperotidine • Nizatidine • Ranitidine • Roxatidine

H₃	Agonists: a-Methylhistamine • Cipralisant • Histamine • Imetit • Immepip • Immethridine • Methimepip • Proxyfan Antagonists: A-349,821 • A-423,579 • ABT-239 • Betahistine • Burimamide • Ciproxifan • Clobenpropit • Conessine • GSK-189,254 • Impentamine • Iodophenpropit • JNJ-5,207,852 • MK-0249 • NNC-38-1,049 • SCH-79,687 • Thioperamide • Tiprolisant • VUF-5,681

H₄	Agonists: 4-Methylhistamine • Histamine • VUF-8,430 Antagonists: JNJ-7,777,120 • Thioperamide • VUF-6,002

Reuptake
Inhibitors

Plasmalemmal

.....

Vesicular

VMAT Inhibitors

Ibogaine • Reserpine • Tetrabenazine

Enzyme
Inhibitors

Anabolism

HDC Inhibitors

a-FMH • Brocresine • Catechin • Cyanidanol-3 • McN-A-1293 • ME • Meciadanol • Naringenin • Thiazol-4-yimethoxyamine • Tritoqualine • Zy-15,029

Catabolism

HNMT Inhibitors	Amodiaquine • BW-301U • Diphenhydramine • Harmaline • Metoprine • Quinacrine • SKF-91,488 • Tacrine

DAO Inhibitors	1,4-Diamino-2-butyne • Aminoguanidine

Others

Precursors	L-Histidine

Cofactors	Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal ? Pyridoxal Phosphate)

v • d • e Tricyclics

Classes	Acridine • Anthracene • Dibenzazepine • Dibenzocycloheptene • Dibenzodiazepine • Dibenzothiazepine • Dibenzothiepin • Dibenzoxazepine • Dibenzoxepin • Phenothiazine • Pyridazinobenzoxazine • Pyridinobenzodiazepine • Thioxanthene

Antidepressants	7-OH-Amoxapine • Amineptine • Amitriptyline • Amitriptylinoxide • Amoxapine • Azepindole • Butriptyline • Cianopramine • Ciclazindol • Clomipramine • Cotriptyline • Cyanodothiepin • Demexiptiline • Desipramine • Dibenzepine • Dimetacrine • Dosulepin/Dothiepin • Doxepin • Esmirtazapine • Fluotracen • Hepzidine • Homopipramol • Imipramine • Imipraminoxide • Intriptyline • Iprindole • Ketipramine • Litracen • Lofepramine • Lortalamine • Losindole • Loxapine • Maprotiline • Mariptiline • Mazindol • Melitracen • Metapramine • Mezepine • Mianserin • Mirtazapine • Naranol • Nitroxazepine • Nortriptyline • Noxiptiline • Octriptyline • Opipramol • Oxaprotiline • Pipofezine • Pirandamine • Propizepine • Protriptyline • Quinupramine • Setiptiline/Teciptiline • Tandamine • Tampramine • Tianeptine • Tienopramine • Trimipramine

Antihistamines	Alimemazine • Azatadine • Clobenzepam • Cyproheptadine • Dacemazine • Deptropine • Desloratadine • Epinastine • Etymemazine • Hydroxyethylpromethazine • Isopromethazine • Isothipendyl • Ketotifen • Latrepirdine • Loratadine • Mebhydrolin • Mequitazine • Methdilazine • Olopatadine • Oxomemazine • Phenindamine • Pimethixene • Promethazine • Propiomazine • Rupatadine • Thiazinamium

Antipsychotics	Acetophenazine • Amoxapine • Asenapine • Butaclamol • Butaperazine • Carphenazine • Carpipramine • Chlorpromazine • Chlorprothixene • Ciclindole • Clocapramine • Clomacran • Clotiapine • Clozapine • Flucindole • Fluotracen • Flupentixol • Fluphenazine • Gevotroline • Homopipramol • Levomepromazine/Methotrimeprazine • Loxapine • Maroxepin • Mesoridazine • Metitepine/Methiothepin • Mosapramine • Naranol • Olanzapine • Perazine • Perphenazine • Periciazine • Piperacetazine • Pipotiazine • Piquindone • Prochlorperazine • Promazine • Prothipendyl • Quetiapine • Sulforidazine • Thiethylperazine • Thiopropazate • Thioridazine • Thiothixene • Trifluoperazine • Triflupromazine • Zotepine • Zuclopenthixol

Others	Atiprosin • Carbamazepine • Carvedilol • Cyclobenzaprine • Licarbazepine • Methylene Blue • Monatepil • Oxcarbazepine • Pirenzepine • Pirolate • Pitrazepin • Pizotifen • Profenamine