Drug information of Bepotastine


Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. 

It works by blocking the action and preventing the release of histamine, a substance in the body that causes allergic symptoms.

Bepotastine ophthalmic is used to treat itching of the eyes caused by allergic conjunctivitis.

Mechanism of effect

Because of a type 1 hypersensitivity reaction cascade that is triggered by antigen exposure, allergic conjunctivitis occurs. Allergen exposure is followed by conjunctival mast cell degranulation and histamine released as a result of the formation of complementary IgE cross-links on the conjunctiva. Due to the release of histamine, symptoms such as itching can be observed. Bepotastine works to relieve itchy eyes by three primary mechanisms of action. It is a non-sedating, selective antagonist of the histamine 1 (H1) receptor, a mast cell stabilizer, and it suppresses the migration of eosinophils into inflamed tissues to prevent tissue damage and worsening of allergic inflammation of the conjunctiva.


Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. It belongs to the second-generation piperidine chemical class. It is a mast cell stabilizer and suppresses the migration of eosinophils into inflamed tissues. Furthermore, bepotastine does not interact with serotonin, muscarinic, benzodiazepine, and beta-adrenergic receptor that would otherwise result in adverse reactions such as dry mouth or sonmolence.


  • Absorption:
    Minimal systemic absorption
  • Bioavailability:

oral: high
topical: minimal

·         Protein binding : ~55%

·         Metabolism:Minimal metabolism via CYP enzymes

  • Half-Life:

Elimination half life = 2.5 hours

  • Excretion:Renal (75–90%)

Drug indications

itchy eyes

For the symptomatic treatment of itchy eyes (caused by IgE-induced mast cell degranulation) due to allergic conjunctivitis


  • Usual Adult Dose for Allergic Conjunctivitis

Instill 1 drop into the affected eye(s) twice a day

  • Usual Pediatric Dose for Allergic Conjunctivitis

2 years or older:

Instill 1 drop into the affected eye(s) twice a day

Drug contraindications

Hypersensitivity to this drug


There are no known significant interactions.


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

Points of recommendation

Before using bepotastine eye drops,

  • tell your doctor and pharmacist if you are allergic to bepotastine, any other medications, or any of the ingredients in bepotastine eye drops. Ask your pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have or have ever had any medical condition.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while using bepotastine eye drops, call your doctor.
  • tell your doctor if you wear contact lenses. You should not wear contact lenses if your eyes are red and you should not use bepotastine eye drops to treat irritation that you think may be caused by contact lenses. Bepotastine eye drops contain benzalkonium chloride, which can be absorbed by soft contact lenses. You should also not apply bepotastine eye drops while you are wearing contact lenses. Remove your contact lenses before you use bepotastine eye drops and do not replace them for at least 10 minutes afterward.
  • Place the missed dose in your eye(s) as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not use a double dose to make up for a missed one.
  • When you use bepotastine eye drops, be careful not to let the tip of the bottle touch your eye, fingers, or any surface. If the tip does touch another surface, bacteria may get into the eye drops. Using eye drops that are contaminated with bacteria may cause serious damage to the eye or loss of vision. If you think your eye drops have become contaminated, call your doctor or pharmacist.

Pregnancy level


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