azelastine

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.

Adv. Reactions/Side Effects ⬆ ⬇

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

GI: bitter taste, dry mouth, nausea

Metab: ↑weight

MS: myalgia

Neuro: drowsiness, dizziness, dysesthesia, fatigue, headache

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.

Availability ⬆ ⬇

(Generic available)

Nasal spray: 205.5 mcg/spray (60–200 sprays/bottle) ^OTC
In combination with: fluticasone (Dymista); see Appendix [not included in this PDA edition].

Route/Dosage ⬆ ⬇

(Adults and Children ≥12 yr): 2 sprays/nostril once daily or 1–2 sprays/nostril twice daily.
(Children 6–11 yr): 1 spray/nostril twice daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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

Therapeutic effects:

Decreased sneezing, nasal rhinitis, pruritus and postnasal drip.

Classifications ⬆ ⬇

Therapeutic Classification: allergy, cold and cough remedies, antihistamines

Pharmacokinetics ⬆ ⬇

Absorption: 40% absorbed after intranasal administration.

Distribution: Widely distributed to tissues.

Metabolism/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.

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.

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Indications ⬇

Contraind./Precautions ⬆ ⬇