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Bepotastine (ophthalmic): Drug information

Bepotastine (ophthalmic): Drug information
(For additional information see "Bepotastine (ophthalmic): Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Bepreve
Brand Names: Canada
  • Bepreve
Pharmacologic Category
  • Histamine H1 Antagonist;
  • Histamine H1 Antagonist, Second Generation;
  • Mast Cell Stabilizer
Dosing: Adult
Allergic conjunctivitis

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

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosing: Pediatric
Allergic conjunctivitis

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

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>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%, postmarketing, and/or case reports: Hypersensitivity reaction, pharyngeal edema, pruritus, skin rash, swelling of lips, swollen tongue

Contraindications

Hypersensitivity to bepotastine or any component of the formulation

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.

Dosage Forms: US

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]

Generic: 1.5% (5 mL, 10 mL)

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Bepotastine Besilate Ophthalmic)

1.5% (per mL): $52.13

Solution (Bepreve Ophthalmic)

1.5% (per mL): $69.06

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

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

Solution, Ophthalmic, as besilate:

Bepreve: 1.5% (1 mL, 5 mL, 10 mL) [contains benzalkonium chloride]

Administration: Adult

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.

Administration: Pediatric

Ophthalmic: 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.

Use: Labeled Indications

Allergic conjunctivitis: Treatment of itching associated with allergic conjunctivitis

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Plasma concentrations are below the limits of detection 24 hours after ophthalmic use. If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988).

Breastfeeding Considerations

It is not known if bepotastine is present in breast milk following ophthalmic use; however, plasma concentrations are below the limits of detection 24 hours after instillation. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Mechanism of Action

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

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Within 3 minutes (Macejko 2010)

Duration: Up to 16 hours (Williams 2011)

Absorption: Minimal systemic absorption

Protein binding: ~55%

Metabolism: Minimal via CYP enzymes

Time to peak, serum: 1 to 2 hours

Excretion: Urine (~75% to 90% unchanged)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Probenil | Traler | Traler LC;
  • (BD) Bangladesh: Bepogen | Bepost | Bepotas | Betasil | Betastin | Eyetin | Ocustin;
  • (CO) Colombia: Dolcettina | Traler;
  • (EC) Ecuador: Elar b;
  • (EG) Egypt: Cornefresh | Orchabepost;
  • (IN) India: Allerbep | Analar gold | Beipos | Bepochek | Bepocin | Bepodrops | Bepofree | Beporest | Beposurge | Bepotime | Botas | Dabfit | Optistat | Zyclear;
  • (KR) Korea, Republic of: Talion | Twolion;
  • (MX) Mexico: Betalast;
  • (PY) Paraguay: Traler
  1. Bepreve (bepotastine) [prescribing information]. Tampa, FL: Bausch & Lomb Inc; August 2022.
  2. Bepreve (bepotastine) [product monograph]. Laval, Quebec, Canada: Valeant Canada; July 2016.
  3. Macejko TT, Bergmann MT, Williams JI, et al, "Multicenter Clinical Evaluation of Bepotastine Besilate Ophthalmic Solutions 1.0% and 1.5% to Treat Allergic Conjunctivitis," Am J Ophthalmol, 2010, 150(1):122-127.e5. [PubMed 20488431]
  4. Samples JR, Meyer SM. Use of ophthalmic medications in pregnant and nursing women. Am J Ophthalmol. 1988;106(5):616-623. [PubMed 2903673]
  5. Williams JI, Kennedy KS, Gow JA, et al, "Prolonged Effectiveness of Bepotastine Besilate Ophthalmic Solution for the Treatment of Ocular Symptoms of Allergic Conjunctivitis," J Ocul Pharmacol Ther, 2011, 27(4):385-93. [PubMed 21649522]
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