Bepotastina
Bepotastina Uses, Dosage, Side Effects, Food Interaction and all others data.
Bepotastina Besilate 1.5% is a sterile drops for ophthalmic use. Bepotastina is direct H1-receptor antagonist and an inhibitor of the release of histamine from mast cells.
Bepotastina 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 | Bepotastina |
Availability | Prescription only |
Generic | Bepotastine |
Bepotastine Other Names | bepotastina, Bepotastine |
Related Drugs | prednisone, cetirizine ophthalmic, dexamethasone ophthalmic, prednisolone ophthalmic, azelastine ophthalmic, doxylamine |
Type | |
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 | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Betastin is used for the treatment of itching associated with signs and symptoms of allergic conjunctivitis.
Bepotastina is also used to associated treatment for these conditions: Pruritus
How Bepotastina 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. Bepotastina 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
Bepotastina 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 Bepotastina 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 Bepotastina Besilate or any of the other ingredients of this product.
Acute Overdose
If you use more Bepotastina 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.
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