Bepotastine Besilate

Class: Antiallergic Agents
Chemical Name: 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]-,benzene sulfonate (1:1); (2) (+)-4-{4-[(S)-(4-Chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl}butanoic acid monobenzenesulfonate.
Molecular Formula: C₂₁H₂₅ClN₂O₃.C₆H₆O₃S.547.10
CAS Number: 190786-44-8
Brands: Bepreve

Introduction

Histamine H ₁-receptor antagonist with mass-cell stabilizing activity.^{1 2 3 5}

Uses for Bepotastine Besilate

Allergic Conjunctivitis

Symptomatic treatment of ocular itching associated with allergic conjunctivitis.^{1 3 7 8 9 10}

Bepotastine Besilate Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution.^{1 2 3 5 6}

Remove soft contact lenses prior to administration of each dose (since benzalkonium chloride may be absorbed by the lenses); may reinsert lenses after 10 minutes following administration if eyes are not red.^{1 5}

Avoid contamination of the solution container.^{1 5}

Dosage

Available as bepotastine besilate; dosage expressed in terms of the salt.¹

Pediatric Patients

Allergic Conjunctivitis

Ophthalmic

Children ≥2 years of age: 1 drop of a 1.5% solution in the affected eye(s) twice daily.¹

Adults

Allergic Conjunctivitis

Ophthalmic

1 drop of a 1.5% solution in the affected eye(s) twice daily.^{1 5}

Cautions for Bepotastine Besilate

Contraindications

• 
  

  Manufacturer states none known.¹

  
  

Warnings/Precautions

Administration

For topical ophthalmic use only.¹

Proper Handling to Avoid Contamination

To avoid contamination of the dropper tip and solution, do not to touch the eyelids or surrounding areas with the dropper tip.¹

Close container tightly when not in use.¹

Contact Lenses

Remove contact lenses prior to administration of each dose, since benzalkonium chloride preservative may be absorbed by soft contact lenses; lenses may be reinserted after 10 minutes following administration if eyes are not red; patient should not wear contact lenses if eyes are red.^{1 5} Not indicated for contact lens-related ocular irritation.^{1 5}

Specific Populations

Pregnancy

Category C.^{1 5}

Lactation

Distributed into milk in rats following oral administration.¹

Not known whether bepotastine besilate distributes into human milk following topical application to the eye.¹ Use caution.¹

Pediatric Use

Safety and efficacy not established in pediatric patients <2 years of age.¹ Efficacy in pediatric patients <10 years of age was extrapolated from clinical trials conducted in pediatric patients >10 years of age and adults.¹

Geriatric Use

No overall differences in efficacy or safety observed between geriatric and younger patients.¹

Common Adverse Effects

Mild taste following instillation,^{1 3 6} ocular irritation, headache, nasopharyngitis.^{1 2 3 10}

Interactions for Bepotastine Besilate

Minimally metabolized by CYP isoenzymes.¹

Drugs Metabolized by Hepatic Microsomal Enzymes

Low potential for drug interactions via inhibition of CYP isoenzymes 3A4, 2C9, and 2C19.¹

Effect on metabolism of substrates of CYP isoenzymes 1A2, 2C8, and 2D6 not established.¹

Bepotastine Besilate Pharmacokinetics

Absorption

Bioavailability

Peak plasma concentrations achieved approximately 1–2 hours after instillation.¹

Distribution

Plasma Protein Binding

Approximately 55%.¹

Elimination

Metabolism

Minimally metabolized by CYP isoenzymes.¹

Elimination Route

Excreted principally in urine as unchanged drug (75–90%).¹

Stability

Storage

Ophthalmic

Solution

15–25°C.¹

ActionsActions

• 
  

  Inhibits the release of histamine and other mediators (e.g., leukotrienes, platelet activating factor [PAF]) involved in allergic reactions.^{1 2 3 5}

  
  


• 
  

  Exhibits mast-cell stabilizing activity.^{1 2 3 5}

  
  


• 
  

  Inhibits eosinophil migration to and activation at inflammatory sites.²

  
  

Advice to Patients

• 
  

  Importance of learning and adhering to proper administration techniques to avoid contamination of the solution.^{1 5}

  
  


• 
  

  Importance of removing contact lenses prior to administration of each ophthalmic dose, since benzalkonium chloride preservative may be absorbed by soft lenses; may reinsert contact lenses after 10 minutes following administration if eyes are not red; importance of not wearing contact lenses if eyes are red.^{1 5}

  
  


• 
  

  Not indicated for contact lens-related ocular irritation.^{1 5}

  
  


• 
  

  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹

  
  


• 
  

  Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.¹

  
  


• 
  

  Importance of informing patients of other important precautionary information.

  
  


• 
  

  (See Cautions.)¹

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Bepotastine Besilate

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Ophthalmic	Solution	1.5%	Bepreve	Ista

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Bepreve 1.5% Solution (ISTA PHARMACEUTICALS): 10/$189.98 or 30/$529.97

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions October 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Ista Pharmaceuticals. Bepreve(bepotastine besilate) ophthalmic solution prescribing information. Irvine, CA; 2009 Aug. (

2. Abelson MB, Torkildsen GL, Williams JI et al. Time to onset and duration of action of the antihistamine bepotastine besilate ophthalmic solution 1.0% and 1.5% in allergic conjunctivitis: a phase III, single-center, prospective, randomized, double-masked, placebo controlled, conjunctival allergen challenge assessment in adults and children. Clin Ther. 2009; 31:1908-21. [PubMed 19843481]

3. Anon. Bepotastine (Bepreve)—An ophthalmic H₁ antihistamine. Med Lett. 2010; 52:8-12.

4. Protzko EE, Gomes PJ, Williams JI et al. The ocular comfort and safety of the novel anti-Histamine bepotastine besilate ophthalmic solution 1.5% in a healthy pediatric population. J Allergy Clin Immunol. 2009; (Suppl 2): S50.

5. Hussar DA, Abbas CA. New drugs: asenapine, iloperidone, and bepotastine besilate. J Am Pharm Assoc. 2010; 50:107-10.

6. Gow JA, Protzko EE, Gomes PJ et al. Safety of the antihistamine bepotastine besilate ophthalmic solution in a healthy pediatric population from 3 to 9 years of age. Poster presented at: 35th Symposium on Cataract, IOL, and Refractive Surgery of the American Society of Cataract and Refractive Surgery. San Francisco, CA: 2009 April 4-8. Abstract 559458.

7. Meier EJ, Macejko TT, Bergmann MT et al. Bepotastine besilate ophthalmic solution 1.0% provides rapid relief of rhinorrhea, total non-ocular symptoms, tearing, and ciliary and episcleral hyperemia following dosing in a multi-site clinical model of allergic conjunctivitis. J Allergy Clin Immunol. 2009; 123 (Suppl): S57.

8. Torkildsen GL, Gomes PJ, Williams JI et al. Bepotastine besilate ophthalmic solution 1.5% reduces ocular itching in a clinical model of allergic conjunctivitis. J Allergy Clin Immunol. 2009; 123 (Suppl): S57.

9. Macejko TT, Meier EJ, Bergmann MT et al. Bepotastine besilate ophthalmic solution 1.5% for up to 8 hours following dosing reduces total non-ocular symptoms, rhinorrhea, and tearing in a multi-site clinical model of allergic conjunctivitis. J Allergy Clin Immunol. 2009; 123 (Suppl):S57.

10. Bergmann MT, Gomes PJ, Williams JI et al. Bepotastine besilate ophthalmic solution 1.5% reduces ocular itching in a multisite clinical model of allergic conjunctivitis. Poster presented at the 35th Symposium on Cataract, IOL, and Refractive Surgery of the American Society of Cataract and Refractive Surgery. San Francisco, CA: 2009 April 4-8. Abstract 559520.

11. ISTA Pharmaceuticals, Irvine, CA: Personal communication.

12. Wadhwa SD. Medical review(s) for bepotastine besilate ophthalmic solution 1.5% (Bepreve), application number 22-228. Rockville, MD: US Food and Drug Administration; 2009 Apr 27. From FDA website ().

More Bepotastine Besilate resources

• Bepotastine Besilate Side Effects (in more detail)
• Bepotastine Besilate Dosage
• Bepotastine Besilate Use in Pregnancy & Breastfeeding
• Bepotastine Besilate Support Group
• 10 Reviews for Bepotastine Besilate - Add your own review/rating

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