azelastine†

General

Pronunciation:
a-zel-as-teen

Trade Name(s)

Astepro Allergy

Ther. Class.

allergy, cold and cough remedies

antihistamines

† See ophthalmic medications for ophthalmic use

Indications

Temporary relief of nasal congestion, runny nose, sneezing, and itchy nose due to hay fever or other upper respiratory allergies.

Action

Locally antagonizes the effects of histamine at H₁ -receptor sites; does not bind to or inactivate histamine.

Therapeutic Effect(s):

Decreased sneezing, nasal rhinitis, pruritus and postnasal drip.

Pharmacokinetics

Absorption: 40% absorbed after intranasal administration.

Distribution: Widely distributed to tissues.

Metabolism and Excretion: Most of absorbed azelastine is metabolized by the liver (converted to an active metabolite.

Half-life: 22–25 hr.

TIME/ACTION PROFILE (relief of symptoms)

ROUTE	ONSET	PEAK	DURATION
Intranasal	rapid	2–3 hr†	12 hr

†Plasma concentration.

Contraindication/Precautions

Contraindicated in:

Hypersensitivity.

Use Cautiously in:

OB: Safety not established in pregnancy;
Lactation: Safety not established in breastfeeding;
Pedi: Safety not established in children <6 yr.

Adverse Reactions/Side Effects

EENT: epistaxis, nasal burning, pharyngitis, sinusitis, sneezing

GI: bitter taste, dry mouth, nausea

Metabolic: ↑ weight

MS: myalgia

Neuro: drowsiness, dizziness, dysesthesia, fatigue, headache

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

Additive CNS depression with CNS depressants, including alcohol, sedative/hypnotics, and opioid analgesics.
Concurrent use of cimetidine ↑ blood levels.

Drug-Natural Products:

Concomitant use of kava, valerian, skullcap, chamomile, or hops can ↑ CNS depression.

Route/Dosage

Intranasal (Adults and Children ≥12 yr): 2 sprays/nostril once daily or 1–2 sprays/nostril twice daily.

Intranasal (Children 6–11 yr): 1 spray/nostril twice daily.

Availability (generic available)

Nasal spray: 205.5 mcg/spray (60–200 sprays/bottle) ^OTC

In Combination with: fluticasone (Dymista); see combination drugs.

Assessment

Assess allergy symptoms (rhinitis, sneezing, conjunctivitis, hives) before and periodically during therapy.
Assess lung sounds and character of bronchial secretions. Maintain fluid intake of 1500–2000 mL/day to decrease viscosity of secretions.

Lab Test Considerations:

May cause false-negative allergy skin testing. Discontinue antihistamines at least 72 hr before testing.

Implementation

Intranasal Before initial use, remove the safety clip on the bottle and prime the delivery system with 6 sprays or until a fine mist appears. When ≥3 days have elapsed since last use, reprime the unit with 2 sprays or until a fine mist appears.

Patient/Family Teaching

Instruct patient in the proper technique for administration of azelastine. Keep head tilted downward toward toes during instillation of intranasal spray to decrease bitter taste.
May cause drowsiness. Caution patient to avoid driving or other activities requiring alertness until effects of the medication are known.
Advise patient to avoid taking alcohol or other CNS depressants concurrently with this drug.
Advise patient that good oral hygiene, frequent rinsing of the mouth, and sugarless gum or candy may help relieve dry mouth. Patient should notify dentist if dry mouth persists >2 wk.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Instruct patient to contact health care professional if symptoms persist.

Evaluation/Desired Outcomes