olopatadine intranasal (Rx)

>10%

Bitter taste (12.8%; 1% pediatric)

Respiratory epistaxis (3-25%)

1-10%

Headache (4.4%)

Depression (2%)

Fatigue (1%)

Somnolence (1%)

Weight gain (1%)

Epistaxis (3.2%; 5.7% pediatric)

Upper respiratory tract infection (2.6% pediatric)

Pharyngolaryngeal pain (2.2%)

Postnasal drip (1.5%)

Cough (1.4%)

Urinary tract infection (1.2%)

Upper respiratory tract infection in children (3%)

<1%

CPK elevation

Dry mouth

Anosmia

Hyposmia

Nasopharyngitis

Throat irritation

Influenza

Contraindications

Hypersensitivity

Cautions

May cause epistaxis, nasal ulceration, or nasal septal perforation

Avoid with nasal disease other than allergic rhinitis

May impair mental/physical abilities required for hazardous tasks (eg, driving, operating machinery)

Avoid concurrent use of alcohol or other CNS depressants (possible additive sedation)

Pregnancy Category: C

Lactation: Unknown whether distributed in breast milk, caution advised

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

Antihistamine (H1 antagonist); inhibits release of histamine from mast cells.

Pharmacokinetics

Half-Life: 8-12 hr

Onset of action: 30 min (seasonal allergy)

Absorption: Systemic 57%

Bioavailability 57%

Peak Plasma Time: 0.25-2 hr

Peak Plasma Concentration: 23.3 ng/mL

Protein Bound: 55% (predominantly albumin)

Metabolites: N-desmethyl olopatadine; olopatadine N-oxide

Metabolism: Liver; not extensive

Excretion: Urine (60-70% unchanged); feces (17%)

Intranasal Administration

Prime nasal spray before initial use and when not in use for >7 days