azelastine

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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 ?
Meda agreed last month to permit Apotex to begin making a generic version of Astelin prior to patent expiry in 2011 as part of a legal settlement.
Major shifts between our key currencies, price reductions on certain European markets, and generic competition for Astelin and Optivar in the US contributed to lower sales, SEK 11,571 million (13,178).
Currency effects and increased competition for the Astelin and Optivar products are the most important reasons for lower sales compared to last year.
Currency effects and generic competition for the Astelin and Optivar products in the US account for the main part of this decrease.
Mainly currency effects but also increased competition for Astelin and Optivar reduced sales by more than SEK 400 million, compared with the same period last year.
Astepro--further development of Astelin * The first combination of an NSAID and proton pump inhibitor--ketoprofen and omeprazole * Onsolis--a unique pain treatment product
Generic copies of Astelin threaten sales from 2010 91
Table 24: Sales forecasts for Astelin and Astepro in allergic rhinitis in the US and five major EU markets ($ 000s), 2009-2019 116
Market launch for Astepro in the US * The FDA approved Astepro - the new formulation of Astelin - in October 2008.
A Randomized, Double-Blind, Placebo-Controlled, Three-Way Cross-Over Study was conducted in 108 SAR patients to Compare the Relative Efficacy of Captisol-Enabled([R]) Budesonide + Azelastine Nasal Spray (Single Solution) and Rhinocort Aqua (Suspension) + Astelin Nasal Spray (Solution) against Placebo Nasal Spray Solution in the Treatment of Allergic Rhinitis in an Environmental Exposure Chamber (EEC).
Astepro Nasal Spray is an improvement over the marketed Astelin Nasal Spray and is better tolerated by patients using the new spray.