Bepotastine

DB04890

small molecule approved

Deskripsi

Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. Bepotastine was approved in Japan for use in the treatment of allergic rhinitis and uriticaria/puritus in July 2000 and January 2002, respectively, and is marketed by Tanabe Seiyaku Co., Ltd. under the brand name Talion. It is available in oral and opthalmic dosage forms in Japan. The opthalmic solution is FDA approved since Sept 8, 2009 and is under the brand name Bepreve.

Struktur Molekul 2D

Berat 388.888
Wujud liquid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Elimination half life = 2.5 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

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.

Metabolisme

Minimal metabolism via CYP enzymes

Rute Eliminasi

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.

Interaksi Makanan

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

Interaksi Obat

751 Data
Benzylpenicilloyl polylysine Bepotastine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Bepotastine.
Amphetamine Amphetamine may decrease the sedative activities of Bepotastine.
Phentermine Phentermine may decrease the sedative activities of Bepotastine.
Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Bepotastine.
Benzphetamine Benzphetamine may decrease the sedative activities of Bepotastine.
Diethylpropion Diethylpropion may decrease the sedative activities of Bepotastine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Bepotastine.
Mephentermine Mephentermine may decrease the sedative activities of Bepotastine.
MMDA MMDA may decrease the sedative activities of Bepotastine.
Midomafetamine Midomafetamine may decrease the sedative activities of Bepotastine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Bepotastine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Bepotastine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Bepotastine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Bepotastine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Bepotastine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Bepotastine.
Metamfetamine Metamfetamine may decrease the sedative activities of Bepotastine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Bepotastine.
Ritobegron Ritobegron may decrease the sedative activities of Bepotastine.
Mephedrone Mephedrone may decrease the sedative activities of Bepotastine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Bepotastine.
Gepefrine Gepefrine may decrease the sedative activities of Bepotastine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Bepotastine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Bepotastine.
Pitolisant The therapeutic efficacy of Pitolisant can be decreased when used in combination with Bepotastine.
Cyclosporine Cyclosporine may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Bepotastine which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Bepotastine which could result in a higher serum level.

Target Protein

Histamine H1 receptor HRH1

Referensi & Sumber

Synthesis reference: Tae Hee Ha, Chang Hee Park, Won Jeoung Kim, Soohwa Cho, Han Kyong Kim, Kwee Hyun Suh, "PROCESS FOR PREPARING BEPOTASTINE AND INTERMEDIATES USED THEREIN." U.S. Patent US20100168433, issued July 01, 2010.
Artikel (PubMed)
  • PMID: 16455807
    Ohashi R, Kamikozawa Y, Sugiura M, Fukuda H, Yabuuchi H, Tamai I: Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate. Drug Metab Dispos. 2006 May;34(5):793-9. Epub 2006 Feb 2.
  • PMID: 16914135
    Andoh T, Kuraishi Y: Suppression by bepotastine besilate of substance P-induced itch-associated responses through the inhibition of the leukotriene B4 action in mice. Eur J Pharmacol. 2006 Oct 10;547(1-3):59-64. Epub 2006 Jul 25.
  • PMID: 22035879
    Simons FE, Simons KJ: Histamine and H1-antihistamines: celebrating a century of progress. J Allergy Clin Immunol. 2011 Dec;128(6):1139-1150.e4. doi: 10.1016/j.jaci.2011.09.005. Epub 2011 Oct 27.
  • PMID: 21386912
    Wingard JB, Mah FS: Critical appraisal of bepotastine in the treatment of ocular itching associated with allergic conjunctivitis. Clin Ophthalmol. 2011;5:201-7. doi: 10.2147/OPTH.S8665. Epub 2011 Feb 15.

Contoh Produk & Brand

Produk: 12 • International brands: 1
Produk
  • Bepotastine Besilate
    Solution / drops • 15 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bepotastine Besilate
    Solution / drops • 15 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bepotastine Besilate
    Solution • 15 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bepotastine Besilate
    Solution • 15 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bepotastine Besilate
    Solution / drops • 15 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bepotastine Besilate
    Solution / drops • 15 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bepotastine Besilate Ophthalmic Solution 1.5%
    Solution / drops • 15 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bepotastine Besilate Ophthalmic Solution 1.5%
    Solution / drops • 15 mg/1mL • Ophthalmic • US • Generic • Approved
Menampilkan 8 dari 12 produk.
International Brands
  • Talion

Sekuens Gen/Protein (FASTA)

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