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

An ANTIHISTAMINE drug used in the treatment of hay fever. Brand names are Optilast and Rhinolast.
References in periodicals archive ?
Astepro is a once-daily nasal spray for treatment of seasonal and perennial allergic rhinitis.
Astepro Nasal Spray is a prescription medicine for people 12 years of age and older and is approved to treat nasal symptoms caused by seasonal allergies or environmental irritants.
In October 2009, Meda started the launch of Astepro 0.15%, an azelastine-based nasal spray against allergic rhinitis, and of cancer pain drug Onsolisis (fentanyl buccal soluble film) in the US market.
The new Astepro nasal spray, based on azelastine, is the first nasal antihistamine with once-daily dosing to be approved for use in the USA, Meda said.
In the autumn of 2008, the FDA approved Astepro for the treatment of allergic and non-allergic rhinitis.
Azelastine Hydrochloride Nasal Apotex Astepro Nasal
has received Food and Drug Administration approval for Astepro (azelastine HCl) 0.15% nasal spray, intended for the treatment of the symptoms of seasonal and perennial allergic rhinitis (SAR and PAR).
Astepro is said to relieve rhinitis symptoms, including nasal congestion, without an added decongestant (such as pseudoephedrine) and is formulated with azelastine, a leading nasal antihistamine in the treatment of seasonal rhinitis in the United States.
"The approval of Astepro represents a milestone for Meda as we continue to expand and strengthen our allergy treatment franchise," comments Sharon Clarke, president and general manager of Meda Pharmaceuticals.
"We believe Astepro can simplify the physician's treatment decision for patients with seasonal and perennial allergic rhinitis and help patients who want rapid nasal symptom relief."
For allergy sufferers requiring a prescription, MEDA's new Astepro is designed to provide powerful efficacy, rapid relief and improved tolerability.