bepotastine (Rx)

>10%

Mild taste disturbance (25%)

1-10%

Ocular irritation (2-5%)

Headache (2-5%)

Nasopharyngitis (2-5%)

Postmarketing Reports

Hypersensitivity reactions, including itching, body rash, and swelling lips, tongue and/or throat

Contraindications

Hypersensitivity

Cautions

Remove contact lenses prior to instillation; benzalkonium chloride may be absorbed by soft contact lenses

To minimize contaminating dropper tip and solution, advise the patient not to touch the eyelids

Store at room temp; protect from light & excessive heat

Keep bottle tightly closed when not in use

Do not wear contact lenses if eye is red

Pregnancy

There are no available human data for use during pregnancy to inform any drug-associated risks; oral administration of bepotastine besilate to pregnant rats or rabbits during organogenesis or during pre/postnatal period did not produce adverse embryofetal or offspring effects at clinically relevant systemic exposures; maternal toxicity was observed in rabbits at lowest dose administered, 20 mg/kg/day (215 times the maximum recommended human ophthalmic dose, RHOD, on a mg/m² basis)

Lactation

There are no data on human milk, effects on breastfed infant or milk production; 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

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

Topical H1 receptor antagonist; inhibits histamine release from mast cells

Pharmacokinetics

Cmax: 5.1-7.3 ng/mL

Absorption: Minimal systemic absorption

Protein bound: 55%

Peak serum time: 1-2 hr

Metabolism: Minimally metabolized by CYP450 isozymes

Excretion: Urine (75-90% excreted unchanged)