Bepiastine

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = 4-[[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidin-1-yl]methyl]benzoic acid | image = Bepotastine.svg | width = 200 | tradename = Talion, Bepreve | Drugs.com = | MedlinePlus = a611020 | pregnancy_AU = B3 | pregnancy_US = C | legal_AU = S4 | legal_US = Rx-only | routes_of_administration = Oral, Ophthalmic | bioavailability = 75% | protein_bound = 55% | metabolism = Minimal | elimination_half-life = 1-2 hours | excretion = Renal | CAS_number = 125602-71-3 | ATC_prefix = R06 | ATC_suffix = AX27 | PubChem = 60852 | DrugBank = DB04890 | ChemSpiderID = 54832 | UNII = 0P6C6ZOP5U | KEGG = D03013 | ChEBI = 31245 | ChEMBL = 1201200 | C=21 | H=24 | Cl=1 | N=1 | O=3 | smiles = Clc1ccc(cc1)C(O)(c2ncccc2)C3CCN(CC3)Cc4ccc(cc4)C(=O)O }}

Bepotastine is a second-generation antihistamine that is used primarily in the treatment of allergic rhinitis and urticaria. It is marketed under the brand names Talion and Bepreve, among others. Bepotastine is available in both oral and ophthalmic formulations.

Pharmacology

Bepotastine acts as a selective antagonist of the histamine H1 receptor, which is responsible for mediating the effects of histamine in allergic reactions. By blocking this receptor, bepotastine reduces the symptoms associated with allergic responses, such as itching, swelling, and redness.

Mechanism of Action

Bepotastine works by inhibiting the binding of histamine to the H1 receptor, thereby preventing the cascade of events that lead to allergic symptoms. It also stabilizes mast cells, preventing the release of inflammatory mediators.

Pharmacokinetics

Bepotastine is rapidly absorbed following oral administration, with a bioavailability of approximately 75%. It is minimally metabolized and is primarily excreted unchanged in the urine. The elimination half-life of bepotastine is approximately 1 to 2 hours.

Clinical Use

Bepotastine is indicated for the treatment of symptoms associated with allergic rhinitis, such as sneezing, nasal congestion, and itchy eyes. It is also used to treat chronic urticaria, providing relief from itching and hives.

Dosage and Administration

The typical oral dosage for adults is 10 mg twice daily. For ophthalmic use, one drop of the 1.5% solution is instilled into the affected eye(s) twice daily.

Side Effects

Common side effects of bepotastine include drowsiness, dry mouth, and headache. Ophthalmic use may cause mild eye irritation or discomfort.

Contraindications

Bepotastine is contraindicated in patients with a known hypersensitivity to the drug or any of its components.

Also see

• Antihistamine
• Allergic rhinitis
• Urticaria
• Histamine H1 receptor