Azelastine

Brand names: Astelin®Optivar®

Chemical formula:

Drug Forms:
• Azelastine eye solution (below)
• Azelastine Hydrochloride Ophthalmic drops, solution
• Azelastine Hydrochloride Nasal spray, solution
• Azelastine Nasal spray, solution

Español:
• Solución ocular de azelastina
• Clorhidrato de Azelastina, Solución para gotas oftálmicas
• Clorhidrato de Azelastina, Solución para aerosol nasal
• Azelastina, Aerosal Nasal, solución

Azelastine eye solution

What is azelastine eye solution?

AZELASTINE (Optivar™) is an antihistamine. It reduces itching of eyes associated with hay fever or other allergies (allergic conjunctivitis). Generic azelastine eye solution is not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• any other medical problems
• wear contact lenses
• an unusual or allergic reaction to azelastine, other medicines, foods, dyes, or preservatives
• pregnant or trying to become pregnant
• breast-feeding

How should I use this medicine?

Azelastine eye solution is only for use in the eye. Do not take by mouth. Follow the directions on the prescription label. Wash hands before and after use. Tilt the head back slightly and pull down the lower eyelid with your index finger to form a pouch. Try not to touch the tip of the dropper to your eye, fingertips, or any other surface. Squeeze the prescribed number of drops (usually 1 drop) into the pouch. Close the eye gently; do not blink for a minute or two. Use your doses at regular intervals. Do not use your medicine more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed. Azelastine eye solution may be used in children 3 years of age and older.

What if I miss a dose?

What drug(s) may interact with azelastine eye solution?

There are no drug interactions known with azelastine eye solution. If you use other eye drops or ointments, you should use one product, then wait 5—10 minutes before using the next product. Eye ointments should be applied last when several eye medicines are used together.

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking azelastine?

Tell your prescriber or health care professional if your symptoms do not start to improve in 2 or 3 days.

If you wear contact lenses, do not wear them if your eyes are red. Azelastine ophthalmic solution should not be used to treat contact lens-related irritation. If you wear soft contact lenses, you should wait at least 10 minutes after instilling azelastine ophthalmic solution before inserting your contact lenses.

Report any serious side effects promptly. Stop using azelastine if your eyes get inflamed, painful, or have a discharge and see your prescriber or health care professional as soon as you can.

Be careful not to touch the tip of the dispensing container onto the eye, or any other surface. Eye infections can result from contamination of eye drops.

What side effects may I notice from using azelastine?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• skin rash, hives, or itching
• swelling of the lips, tongue or face

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
More common:
• bitter taste
• blurred vision
• eye burning or stinging
• headache
Less common:
• eye pain
• fatigue

Where can I keep my medicine?

Keep out of the reach of children.

Keep container tightly closed when not in use. Store upright between 2—25°C (36—77°F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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	C22H24ClN3O
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.

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

Side effects

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]}

External links

• Official Astelin Website
• Official Astepro Website
• Official Optivar Website
• Manufacturer's Website

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)

1. ^ Astelin prescribing information

v • d • e 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

v • d • e 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 • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • p-Methyldiphenhydramine • Pheniramine • Phenyltoloxamine • Promethazine • Pyrilamine • 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 Others Precursors L-Histidine Cofactors Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal → Pyridoxal Phosphate)

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