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.
Astelin Nasal Spray (azelastine hydrochloride nasal spray, 137 mcg; MedPointe Pharmaceuticals) The FDA approved a new dosing regimen for Astelin nasal spray, 137 mcg, for patients 12 years and older with seasonal allergic rhinitis.
AdvancePCS is working with 11 manufacturers to offer discounts on 21 different drugs, including the nasal antihistamine Astelin, two hormone replacement therapy products, several angiotensin-converting enzyme inhibitors, and 10 oral contraceptives.
It will also take a few more quarters before the comparison effect with Astelin, which received generic competition last year, has completely disappeared from the income statement.
The first-quarter sales were pulled down by negative currency effects of SEK286m, but also by increased competition for rhinitis drug Astelin and eye drops Optivar, which had a negative impact of SEK400m.
Azelastine HC1 metered spray, marketed as Astelin by Wallace Laboratories Inc.
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).
The clarity regarding (epilepsy drug candidate) Retigabine and the Astelin combination results in a modest short-term potential backed by the recent launches, a stable cash flow and higher margins," Swedbank said.
Currency effects and increased competition for the Astelin and Optivar products are the most important reasons for lower sales compared to last year.
However, Meda's biggest product, Astelin for treatment of allergic and non-allergic rhinitis, registered a decrease in sales, to SEK261m from SEK278m.
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.