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

Published data from postmarketing experience with antihistamines, have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

However, there are no published human data specific to this drug

Animal data

• In animal reproductive studies, oral administration of olopatadine hydrochloride to pregnant rats and rabbits caused a decrease in number of live fetuses at maternal doses approximately 110 and 1460 times the maximum recommended human daily intranasal dose (MRHDID) on a mg/m2 basis, respectively

Lactation

• There are no data on presence of drug in human milk, effects on breastfed infant, or on milk production; although orally administered drug is present in rat milk, there is no information about nasally administered drug
• It is not known whether topical nasal administration could result in sufficient systemic absorption to produce detectable quantities in human breast milk
• The developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breast fed 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

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