Azelastine

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Azelastine
Systematic (IUPAC) name

4-[(4-chlorophenyl)methyl]-2- (1-methylazepan-4-yl)-phthalazin-1-one
Identifiers
CAS number	58581-89-8
ATC code	R01AC03 R06AX19, S01GX07
PubChem	2267
DrugBank	APRD00813
ChemSpider	2180
Chemical data
Formula	C₂₂H₂₄Cl N₃O
Mol. mass	381.898 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	40% (intranasal)
Metabolism	?
Half life	22 hours
Excretion	?
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status	Rx Only (US)
Routes	intranasal, ocular
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Azelastine is an antihistamine and mast cell stabilizer available as a nasal spray (Astelin or Astepro) for hay fever and as eye drops (Optivar) for allergic conjunctivitis.

1 Side effects
- 1.1 Nasal spray
2 External links
3 References

[edit] Side effects

[edit] Nasal spray

Side effects of azelastine nasal spray vary somewhat depending on the condition being treated. The most common side effects include bitter taste, headache, rhinitis, nose bleed, and somnolence. Adults being treated for vasomotor rhinitis may also experience dysesthesia and sinusitis. Additional side effects experienced by adults being treated for seasonal allergies include nasal burning, pharyngitis, dry mouth, paroxysmal sneezing, nausea, fatigue, dizziness, and weight gain.^[1] Additional side effect can include a slight mind alertness.^{[citation needed]}

[edit] External links

[edit] References

This article includes a list of references, related reading or external links, but its sources remain unclear because it lacks inline citations. Please improve this article by introducing more precise citations where appropriate. (June 2009)

^ Astelin prescribing information

Decongestants and other nasal preparations (R01)

Topical

Sympathomimetics, plain	Cyclopentamine • Ephedrine • Phenylephrine • Oxymetazoline • Tetryzoline • Xylometazoline • Naphazoline • Tramazoline • Metizoline • Tuaminoheptane • Fenoxazoline • Tymazoline • Epinephrine

Antiallergic agents, excluding corticosteroids	Spaglumic acid histamine antagonists (Levocabastine, Antazoline, Thonzylamine) mast cell stabilizer (some are also antihistamines) (Cromoglicic acid, Nedocromil, Azelastine, Olopatadine)

Corticosteroids	Beclometasone • Prednisolone • Dexamethasone • Flunisolide • Budesonide • Betamethasone • Tixocortol • Fluticasone • Mometasone furoate • Triamcinolone • Ciclesonide

Other nasal preparations	Calcium hexamine thiocyanate • Retinol • Ipratropium bromide • Ritiometan • Mupirocin • Hexamidine • Framycetin • Hyaluronic acid • Eucalyptus oil

Systemic use:
Sympathomimetics

Phenylpropanolamine • Pseudoephedrine • Phenylephrine • Phenylpropylamine

Histaminergics

Receptor
Ligands

H₁	Agonists: 2-Pyridylethylamine • Betahistine • Histamine • HTMT • UR-AK49 Antagonists: 1st Generation: Alimemazine • Azatadine • Bamipine • Bepotastine • Bromazine • Brompheniramine • Buclizine • Carbinoxamine • Chlorcyclizine • Chloropyramine • Chlorothen • Chlorpheniramine • Chlorphenoxamine • Cinnarizine • Clemastine • Clobenzepam • Clocinizine • Cyclizine • Cyproheptadine • Dacemazine • Deptropine • Dexbrompheniramine • Dexchlorpheniramine • Dimetindene • Diphenhydramine • Diphenylpyraline • Doxylamine • Embramine • Etymemazine • Histapyrrodine • Hydroxyethylpromethazine • Hydroxyzine • Iproheptine • Isopromethazine • Isothipendyl • Meclizine • Mepyramine (Pyrilamine) • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • p-Methyldiphenhydramine • Pheniramine • Phenyltoloxamine • Promethazine • Pyrrobutamine • Setastine • Talastine • Thenalidine • Thenyldiamine • Thiazinamium • Thonzylamine • Tolpropamine • Tripelennamine • Triprolidine; 2nd Generation: Acrivastine • Antazoline • Astemizole • Azatadine • Azelastine • Bamipine • Cetirizine • Clemizole • Clobenztropine • Deptropine • Dimebon • Ebastine • Emedastine • Epinastine • Ketotifen • Levocabastine • Loratadine • Mebhydrolin • Mizolastine • Olopatadine • Phenindamine • Pimethixene • Pyrrobutamine • Rupatadine • Terfenadine • Thenalidine • Tritoqualine; 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 • Metiamide • Niperotidine • Nizatidine • Ranitidine • Roxatidine

H₃	Agonists: α-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

α-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