Bepotastine

Bepotastine Uses, Dosage, Side Effects, Food Interaction and all others data.

Bepotastine Besilate 1.5% is a sterile drops for ophthalmic use. Bepotastine is direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.

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.Onset of action = 0.25 hours;Duration of action = 12-24 hours;

Trade Name Bepotastine
Availability Prescription only
Generic Bepotastine
Bepotastine Other Names bepotastina, Bepotastine
Related Drugs prednisone, cetirizine ophthalmic, dexamethasone ophthalmic, prednisolone ophthalmic, azelastine ophthalmic, doxylamine
Weight 1.5%
Type Ophthalmic solution
Formula C21H25ClN2O3
Weight Average: 388.888
Monoisotopic: 388.155370383
Protein binding

55.4% mean plasma protein binding with 10 mg oral dose. Extent of protein binding is independent of plasma drug concentration.

Groups Approved
Therapeutic Class Ophthalmic Anti-allergic preparations
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Bepotastine
Bepotastine

Uses

Betastin is used for the treatment of itching associated with signs and symptoms of allergic conjunctivitis.

Bepotastine is also used to associated treatment for these conditions: Pruritus

How Bepotastine works

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.

Dosage

Bepotastine dosage

Instill one drop of Betastin eye drops into the affected eye(s) twice a day.

Pediatric Use: Safety and effectiveness in children below the age of 2 years have not been established.

Side Effects

The most common reported side effect occurring in approximately 25% of subjects was a mild taste following instillation. Other side effects occurring in 2-5% of subjects were eye irritation, headache, and nasopharyngitis.

Precaution

• To minimize the risk of contamination, do not touch dropper tip to any surface.

• It should not be used to treat contact lens-related irritation.

• Patients should be advised not to wear contact lens when using this drop.

Interaction

No drug interactions observed but patients who are sensitive to this product molecule should be used with caution.

Food Interaction

  • Take with or without food. Orally formulated bepotastine bioavailability is not significantly impacted by food.

Elimination Route

Tmax, after single dose, opthalmic = 1.2 hours; Cmax, 1.5%, opthalmic dose = 7.3 ±1.9 ng/mL; After 24 hours post-installation, levels of bepotastine are below quantifiable limit of 2 ng/mL. Minimal systemic absorption with opthalmic dosage form.

Half Life

Elimination half life = 2.5 hours

Elimination Route

When a oral dose of 2.5 - 40 mg bepotastine is given, 75%-90% of the dose was excreted unchanged in the urine by 24 hours.

Pregnancy & Breastfeeding use

Pregnancy: Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

Lactation: It is not known if Bepotastine besilate is excreted in human milk. Caution should be exercised when it is administered to a nursing woman.

Contraindication

Contraindicated in patients with a history of hypersensitivity reactions to Bepotastine Besilate or any of the other ingredients of this product.

Acute Overdose

If you use more Bepotastine Besilate eye drops than you should, rinse your eye with warm water. Do not put in any more drops until it is time for your next regular dose. Pharmaceutical Precautions.

Interaction with other Medicine

No information provided.

Storage Condition

• Store in a cool, dry place & protected from light

• Keep out of reach of children

• Do not use more than 4 weeks after opening.

Innovators Monograph

You find simplified version here Bepotastine

*** Taking medicines without doctor's advice can cause long-term problems.
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