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Bepotastine

Pronunciation

(be poe TAS teen)

Index Terms

  • Bepotastine Besilate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic, as besilate:

Bepreve: 1.5% (5 mL, 10 mL) [contains benzalkonium chloride]

Brand Names: U.S.

  • Bepreve

Pharmacologic Category

  • Histamine H1 Antagonist
  • Histamine H1 Antagonist, Second Generation
  • Mast Cell Stabilizer

Pharmacology

Direct H1-receptor antagonist and inhibits release of histamine from mast cells

Absorption

Minimal systemic absorption

Metabolism

Minimal via CYP enzymes

Excretion

Urine (~75% to 90% unchanged)

Onset of Action

Within 3 minutes (Macejko, 2010)

Time to Peak

Serum: 1-2 hours

Duration of Action

Up to 16 hours (Williams, 2011)

Protein Binding

~55%

Use: Labeled Indications

Treatment of itching associated with allergic conjunctivitis

Contraindications

Hypersensitivity to bepotastine or any component of the formulation

Dosing: Adult

Allergic conjunctivitis: Ophthalmic: Instill 1 drop into the affected eye(s) twice daily

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Allergic conjunctivitis: Ophthalmic: Children ≥2 years: Refer to adult dosing.

Administration

For topical ophthalmic use only. Contact lenses should be removed prior to application, may be inserted after 10 minutes. Do not insert contacts if eyes are red. Avoid contaminating the applicator tip.

Storage

Store at room temperature of 15°C to 25°C (59°F to 77°F).

Drug Interactions

There are no known significant interactions.

Adverse Reactions

>10%: Gastrointestinal: Dysgeusia (25%)

1% to 10%:

Central nervous system: Headache (2% to 5%)

Ophthalmic: Eye irritation (2% to 5%)

Respiratory: Nasopharyngitis (2% to 5%)

<1% (Limited to important or life-threatening): Hypersensitivity reaction, pharyngeal edema, pruritus, skin rash, swelling of lips, swollen tongue

Warnings/Precautions

Special populations:

• Contact lens wearers: Contains benzalkonium chloride which may be absorbed by soft contact lenses; remove lens prior to administration and wait 10 minutes before reinserting.

Other warnings/precautions:

• Appropriate use: For topical ophthalmic use only. Not for the treatment of contact lens irritation; do not wear contact lenses if eye is red.

Pregnancy Risk Factor

C

Pregnancy Considerations

Teratogenic effects were not observed in most animal reproduction studies following oral administration; however, a decrease in fetal weight and a decrease in live births were observed in some studies. In humans, plasma concentrations are below the limit of quantification (<2 ng/mL) 24 hours after ophthalmic administration.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience bad taste, headache, rhinitis, or pharyngitis. Have patient report immediately to prescriber vision changes, eye pain, or severe eye irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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