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an antihistamine used intranasally as the hydrochloride salt in treatment of hay fever and topically to the conjunctiva in treatment of allergic conjunctivitis.
Miller-Keane Encyclopedia and Dictionary of Medicine, Nursing, and Allied Health, Seventh Edition. © 2003 by Saunders, an imprint of Elsevier, Inc. All rights reserved.


Astelin, Astepro, Optivar

Pharmacologic class: Histamine 1 (H1)-receptor antagonist

Therapeutic class: Respiratory inhalant, ophthalmologic agent

Pregnancy risk category C


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.


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.


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

• None (Astepro)


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]).


• 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


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.

McGraw-Hill Nurse's Drug Handbook, 7th Ed. Copyright © 2013 by The McGraw-Hill Companies, Inc. All rights reserved


An ANTIHISTAMINE drug used in the treatment of hay fever. Brand names are Optilast and Rhinolast.
Collins Dictionary of Medicine © Robert M. Youngson 2004, 2005
References in periodicals archive ?
In August 2015, Breckenridge received approval for Azelastine HC1 Nasal Solution (Nasal Spray), a generic version of Astelin, marketed by Meda Pharmaceuticals.
Sales were pulled down by negative currency effects of SEK174m and by generic competition for the company's products Astelin and Optivar.
Sales dropped 12% year-on-year to SEK3.043bn in April-June 2010, mainly due to currency effects and increased competition for rhinitis drug Astelin and eye drops Optivar in the USA, Meda said.
Meda had expected to get approval before July for the drug, intended to replace Astelin, which made up 16 percent of first-quarter sales.
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.
The patients who had reactions were treated with one or a combination of the following: nebulized breathing treatment with albuterol, two sprays in each nostril of azelastine (Astelin), and diphenhydramine (Benadryl), either orally or intramuscularly.
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.
But they also cause a variety of annoying side effects, including sleepiness, delayed reaction times, attention problems and decreased memory.(1) Newer drugs, such as fexofenadine (Allegra), loratadine (Claritin) and cetirizine (Zyrtec), all taken in pill form, as well as the intranasal antihistamine azelastine (Astelin), and ketotifen, an antihistamine drop for your eyes, are less sedating and thus the treatment of choice.
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 (Astelin) is the only intranasal antihistamine currently approved in the United States.
Azelastine HC1 metered spray, marketed as Astelin by Wallace Laboratories Inc., is the first second-generation antihistamine approved for this indication.
"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.