azelastine


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Related to azelastine: Azelastine hydrochloride

azelastine

 [ah-zel´as-tēn″]
an antihistamine used intranasally as the hydrochloride salt in treatment of hay fever and topically to the conjunctiva in treatment of allergic conjunctivitis.

azelastine

Astelin, Astepro, Optivar

Pharmacologic class: Histamine 1 (H1)-receptor antagonist

Therapeutic class: Respiratory inhalant, ophthalmologic agent

Pregnancy risk category C

Action

Selectively antagonizes H1 and inhibits release of histamine and other mediators from cells (such as mast cells) involved in allergic response. Based on in vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (such as leukotrienes and platelet-aggregating factor) has also been demonstrated. Decreased chemotaxis and activation of eosinophils has also been demonstrated.

Availability

Nasal spray (Astepro): 0.15% (205.5 mcg in each 0.137-ml spray)

Nasal spray, metered (Astelin): 137-mcg spray

Ophthalmic solution (Optivar): 0.05%

Indications and dosages

Seasonal and allergic rhinitis

Adults and children age 12 and older: 1 or 2 sprays (Astelin, Astepro) per nostril b.i.d. or 2 sprays (Astepro) per nostril once daily

Children ages 5 to 11: 1 spray (Astelin) per nostril b.i.d.

Perennial allergic rhinitis, vasomotor rhinitis

Adults and adolescents age 12 and older: 2 sprays (Astelin) per nostril b.i.d.

Allergic conjunctivitis

Adults and adolescents age 3 and older: 1 drop (Optivar) in each eye b.i.d.

Contraindications

• Hypersensitivity to drug or its components (Astelin, Optivar)

• None (Astepro)

Precautions

Use cautiously in:

• concurrent use of alcohol and CNS depressants (avoid Astepro use)

• pregnant or breastfeeding patients

• children (safety and efficacy not established for those younger than age 3 [Optivar]; age 5 [Astelin]; age 12 [Astepro]).

Administration

• Follow manufacturer's directions and prime Astelin nasal spray before use.

• Prime Astepro nasal spray before initial use and when it hasn't been used for 3 or more days.

• Be aware that patient shouldn't wear contact lenses when the eyes are red and that Optivar shouldn't be used to treat redness caused by contact lenses.

• Wait 10 minutes before allowing patient to put soft contact lenses back in after Optivar administration, because the preservative benzalkonium chloride may be absorbed.

Adverse reactions

CNS: dizziness (with Astelin); headache, fatigue, somnolence (with Astelin, Astepro)

EENT: transient eye burning or stinging (with Optivar); nasal burning, nasal discomfort, sneezing (with Astepro); pharyngitis, paroxysmal sneezing, rhinitis, epistaxis (with Astelin)

GI: nausea, dry mouth (with Astelin); nasal discomfort (with Astepro); epistaxis (with Astelin, Astepro)

Other: weight increase (with Astelin); bitter taste

Interactions

Drug-drug. Cimetidine: increased mean Cmax and area under the curve of orally administered azelastine

CNS depressants: additional decreased alertness and impairment of CNS performance (with Astelin, Astepro)

Drug-behaviors. Alcohol use: decreased alertness and impairment of CNS performance (with Astelin, Astepro)

Patient monitoring

• Monitor patient for bothersome adverse reactions.

Patient teaching

• Instruct patient on proper use of nasal spray and eyedrops.

• Advise patient to avoid other antihistamines, alcohol, and other CNS depressants such as sedatives while using nasal spray.

• Instruct patient to avoid spraying nasal spray into the eyes.

• Advise patient not to wear contact lenses if the eyes are red. Instruct the patient who wears soft contact lenses and whose eyes aren't red to wait at least 10 minutes after instilling eye-drops before inserting contact lenses.

• Caution patient to avoid driving and other hazardous activities until drug's effects on concentration and alertness are known.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and behaviors mentioned above.

azelastine

/azel·as·tine/ (ah-zel´as-tēn″) a topical antihistamine used as the hydrochloride salt in the treatment of seasonal allergic rhinitis and allergic conjunctivitis.

azelastine

an H1-selective antihistamine that also inhibits leukotriene and platelet activating factor (PAF) synthesis and release.
indications This drug is used to treat seasonal allergic rhinitis and seasonal allergic conjunctivitis.
contraindications Known hypersensitivity, acute asthma attacks, and lower respiratory tract disease prohibit this drug's use.
adverse effects Side effects include sedation (more common with increased doses), increased drowsiness, weight increase, and myalgia.

azelastine

An ANTIHISTAMINE drug used in the treatment of hay fever. Brand names are Optilast and Rhinolast.
References in periodicals archive ?
05% Supply level Dual action Opatanol Olopatadine At least (Alcon) Hydrochloride Additional 1mg/mL Supply level Optilast Azelastine At least (Meda) Hydrochloride Additional 0.
The scratching was inhibited by the H Ghistamine-receptor antagonist azelastine, but not by the peripherally acting H -antagonist terfenadine, at the oral dose of 30 mg/kg.
Second-generation drugs developed later, including loratadine (Claritin), fexofenadine (A llegra), cetirizine (Zyrtec), and azelastine (Astelin Nasal Spray), are less likely to cause these effects.
A combination of local intranasal glucocorticosteroids and topical antihistamine azelastine has been recommended.
In some areas the effects elicited were comparable to those of a number of pharmaceutical preparations used in treating asthma and allergic rhinitis including azelastine and dexamethasone.
Materials and methods: The release of soluble mediators from basophilic cells, mast cells and lung epithelial cells, which are essential for the initiation of early- and late-phase allergic reactions, was analyzed in relation to the synthetic anti-allergic drugs azelastine and dexamethasone.
The Food and Drug Administration requested more information on a new formulation of azelastine hydrochloride nasal spray, Meda said in a statement.
Among its advantages is less of a taste problem, compared with the last similar product approved in 1996, azelastine HCl (Astelin nasal spray, Meda Pharmaceuticals Inc.
Among its other advantages is less of a taste problem, compared with the last similar product approved in 1996, azelastine HCl (Astelin nasal spray, Meda Pharmaceuticals Inc.
The product, 'Higuard', is the first Rx-to-OTC switch product of azelastine hydrochloride, an anti-allergy compound originally approved for prescription use.