azelastine (Rx)

>10%

Bitter taste (8-19.7%)

Headache (8-14.8%)

Somnolence (1-11.5%)

Cold symptoms/rhinitis (2-17%)

Cough (11%)

1-10%

Nasal burning (4.1%)

Sneezing (3.1%)

Dry mouth (2.8%)

Nausea (2.8%)

Conjunctivitis (2-5%)

Asthma (5%)

Fatigue (2.3%)

Rhinitis (2.3%)

Pharyngitis (4%)

Dizziness (2%)

Weight increase (2%)

Myalgia (<2%)

<1%

Amenorrhea

Breast pain

Constipation

Contact dermatitis

Eczema

Flushing

Glossitis

Hyperkinesia

Hypertension

Tachycardia

Vertigo

Vomiting

Postmarketing Reports

Anaphylactoid reaction

Application site irritation

Atrial fibrillation

Chest pain

Confusion

Dyspnea

Facial edema

Involuntary muscle contractions

Nasal sores

Palpitations

Paresthesia

Parosmia

Pruritus

Rash

Disturbance or loss of sense of smell and/or taste

Tolerance

Urinary retention

Vision abnormal

Xerophthalmia

Contraindications

Documented hypersensitivity

Cautions

May cause CNS depression/drowsiness; use caution when performing tasks requiring mental alertness eg, operating heavy machinery

Avoid administering concurrent CNS depressants that may add to somnolence

Caution in premature newborns and neonates

Pregnancy

Limited data from postmarketing experience over decades of use in pregnant women have not identified any drug associated risks of miscarriage, birth defects, or other adverse maternal or fetal outcomes

Animal data

• In animal reproduction studies, there was no evidence of fetal harm at oral doses approximately 5 times the clinical daily dose; oral administration to pregnant mice, rats, and rabbits, during the period of organogenesis, produced developmental toxicity that included structural abnormalities, decreased embryo-fetal survival, and decreased fetal body weights at doses 270 times and higher than maximum recommended human daily intranasal dose of 1.096 mg; relevance of these findings in animals to pregnant women considered questionable based upon high animal to human dose multiple

Lactation

There are no data on presence in human milk, effects on breastfed infant, or on milk production; breastfed infants should be monitored for signs of milk rejection during use by lactating women; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

H1-receptor antagonist; inhibits release of histamine and other mediators involved in allergic response; may reduce hyperactivity of airways if used intranasally

Absorption

Bioavailability: 40%

Onset: 1-3 hr

Duration: 12 hr

Peak serum time: 2-4 hr

Distribution

Protein bound: 88%

Vd: 14.5 L/kg

Metabolism

Metabolized by hepatic P450

Metabolites: Desmethylazelastine

Elimination

Half-life: 22 hr

Clearance: 0.5 L/hr/kg

Excretion: Feces (75%)