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.
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05% Supply level Dual action Opatanol Olopatadine At least (Alcon) Hydrochloride Additional 1mg/mL Supply level Optilast Azelastine At least (Meda) Hydrochloride Additional 0.
4; all from Sigma-Aldrich, Germany) and treated (10 min, 37[degrees]C) with Gencydo[R]or azelastine (Sigma-Aldrich, Taufldrchen, Germany) before stimulation (30 min, 37[degrees]C) with 20 ng/ml DNP-HSA (Sigma-Aldrich, Taufkirchen, Germany).
Effect of topical applications of budesonide and azelastine on nasal symptoms, eosinophil count and mediator release in atopic patients after nasal allergen challenge during the pollen season.
The product, 'Higuard', is the first Rx-to-OTC switch product of azelastine hydrochloride, an anti-allergy compound originally approved for prescription use.
Dymista is a novel nasal formulation of azelastine and fluticasone.
Dymista Nasal Spray is a prescription medicine used to treat symptoms of seasonal allergic rhinitis in people 6 years of age and older, who need treatment with both azelastine hydrochloride and fluticasone propionate.
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.
They can also access the dual acting drugs, ie, ketotifen and olopatadine, as well as selective antihistamines (eg, azelastine and emedastine), all of which can be used in a similar manner to a mast cell stabilizer with certain caveats.
Scoparone (purity 98%, HPLC), azelastine, anti-dinitrophenyl (DNP) IgE, DNP-human serum albumin (HSA) and HEPES were purchased from Sigma-Aldrich Chemical Co.
A 53-year-old woman presented with a history of sinusitis for more than 2 years despite treatment with multiple rounds of antibiotics, twice-daily sinus rinses, and treatment with azelastine nasal spray.
Two other second generation antihistamines, azelastine (approved in 1996) and ketotifen (approved in 1999) are approved for topical use only; azelastine in the nose and eyes, and ketotifen in the eyes only.