Epinastine

DB00751

small molecule approved investigational

Deskripsi

Epinastine is used for the prevention of itching associated with allergic conjunctivitis. It has a multi-action effect that inhibits the allergic response in 3 ways: 1. stabilizes mast cells by preventing mast cell degranulation to control the allergic response, 2. prevents histamine binding to both the H1- and H2-receptors to stop itching and provide lasting protection, and 3. prevents the release of proinflammatory chemical mediators from the blood vessel to halt progression of the allergic response.

Struktur Molekul 2D

Berat 249.3104
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 12 hours
Volume Distribusi -
Klirens (Clearance) * 56 L/hr [patients with allergic conjunctivitis receiving one drop of ELESTAT® ophthalmic solution in each eye twice daily for seven days]

Absorpsi

The absolute bioavailability of epinastine is about 40%.

Metabolisme

Mainly excreted unchanged, less than 10% metabolized.

Rute Eliminasi

Epinastine is mainly excreted unchanged. The renal elimination is mainly via active tubular secretion.

Interaksi Obat

1235 Data
Buprenorphine Epinastine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Epinastine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Epinastine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Epinastine.
Hydrocodone Epinastine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Epinastine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Epinastine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Epinastine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Epinastine.
Mirtazapine Epinastine may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Epinastine.
Orphenadrine Epinastine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Epinastine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Epinastine.
Pramipexole Epinastine may increase the sedative activities of Pramipexole.
Ropinirole Epinastine may increase the sedative activities of Ropinirole.
Rotigotine Epinastine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Epinastine.
Sodium oxybate Epinastine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Epinastine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Epinastine.
Thalidomide Epinastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Epinastine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Benzylpenicilloyl polylysine Epinastine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Epinastine.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Epinastine.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Epinastine.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Epinastine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Epinastine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Epinastine.
Atazanavir Epinastine can cause a decrease in the absorption of Atazanavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bosutinib Epinastine can cause a decrease in the absorption of Bosutinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefditoren Epinastine can cause a decrease in the absorption of Cefditoren resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefpodoxime Epinastine can cause a decrease in the absorption of Cefpodoxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cefuroxime Epinastine can cause a decrease in the absorption of Cefuroxime resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dabrafenib The serum concentration of Epinastine can be decreased when it is combined with Dabrafenib.
Dasatinib Epinastine can cause a decrease in the absorption of Dasatinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Delavirdine Epinastine can cause a decrease in the absorption of Delavirdine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexmethylphenidate The therapeutic efficacy of Dexmethylphenidate can be decreased when used in combination with Epinastine.
Erlotinib Epinastine can cause a decrease in the absorption of Erlotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Fosamprenavir Epinastine can cause a decrease in the absorption of Fosamprenavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Gefitinib Epinastine can cause a decrease in the absorption of Gefitinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Indinavir Epinastine can cause a decrease in the absorption of Indinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Itraconazole Epinastine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ledipasvir Epinastine can cause a decrease in the absorption of Ledipasvir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methylphenidate The therapeutic efficacy of Methylphenidate can be decreased when used in combination with Epinastine.
Nelfinavir Epinastine can cause a decrease in the absorption of Nelfinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nilotinib Epinastine can cause a decrease in the absorption of Nilotinib resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pazopanib The therapeutic efficacy of Pazopanib can be decreased when used in combination with Epinastine.
Rilpivirine Epinastine can cause a decrease in the absorption of Rilpivirine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Risedronic acid Epinastine can cause an increase in the absorption of Risedronic acid resulting in an increased serum concentration and potentially a worsening of adverse effects.
Saquinavir Epinastine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Dicoumarol The risk or severity of adverse effects can be increased when Epinastine is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Epinastine is combined with Phenindione.
Warfarin The risk or severity of adverse effects can be increased when Epinastine is combined with Warfarin.
Phenprocoumon The risk or severity of adverse effects can be increased when Epinastine is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Epinastine is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Epinastine is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Epinastine is combined with Coumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Epinastine is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Epinastine is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Epinastine is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Epinastine is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Epinastine is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Epinastine is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Epinastine is combined with (S)-Warfarin.
Mirabegron The serum concentration of Epinastine can be increased when it is combined with Mirabegron.
Mesalazine The therapeutic efficacy of Mesalazine can be decreased when used in combination with Epinastine.
Ethanol Epinastine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Epinastine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Epinastine.
Sertraline The risk or severity of adverse effects can be increased when Epinastine is combined with Sertraline.
Desvenlafaxine The serum concentration of Epinastine can be increased when it is combined with Desvenlafaxine.
Citalopram The risk or severity of QTc prolongation can be increased when Epinastine is combined with Citalopram.
Sibutramine The risk or severity of adverse effects can be increased when Epinastine is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Epinastine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Epinastine is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Epinastine is combined with Milnacipran.
Seproxetine The risk or severity of adverse effects can be increased when Epinastine is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Epinastine is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Epinastine is combined with Alaproclate.
Lisdexamfetamine The serum concentration of dextroamphetamine, an active metabolite of Lisdexamfetamine, can be increased when used in combination with Epinastine.
Amphetamine Amphetamine may decrease the sedative activities of Epinastine.
Phentermine Phentermine may decrease the sedative activities of Epinastine.
Benzphetamine Benzphetamine may decrease the sedative activities of Epinastine.
Diethylpropion Diethylpropion may decrease the sedative activities of Epinastine.
Mephentermine Mephentermine may decrease the sedative activities of Epinastine.
MMDA MMDA may decrease the sedative activities of Epinastine.
Midomafetamine Midomafetamine may decrease the sedative activities of Epinastine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Epinastine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Epinastine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Epinastine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Epinastine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Epinastine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Epinastine.
Metamfetamine Metamfetamine may decrease the sedative activities of Epinastine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Epinastine.
Ritobegron Ritobegron may decrease the sedative activities of Epinastine.
Mephedrone Mephedrone may decrease the sedative activities of Epinastine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Epinastine.

Target Protein

Histamine H1 receptor HRH1
Histamine H2 receptor HRH2
Alpha-1A adrenergic receptor ADRA1A
Alpha-2A adrenergic receptor ADRA2A
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 7 HTR7

Referensi & Sumber

Synthesis reference: Akiharu Isowaki, Tomoko Nakajima, Akira Ohtori, "Percutaneously Absorptive Ophthalmic Preparation Comprising Epinastine." U.S. Patent US20090143359, issued June 04, 2009.
Artikel (PubMed)
  • PMID: 1972625
    Walther G, Daniel H, Bechtel WD, Brandt K: New tetracyclic guanidine derivatives with H1-antihistaminic properties. Chemistry of epinastine. Arzneimittelforschung. 1990 Apr;40(4):440-6.
  • PMID: 1982280
    Schilling JC, Adamus WS, Kuthan H: Antihistaminic activity and side effect profile of epinastine and terfenadine in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1990 Dec;28(12):493-7.

Contoh Produk & Brand

Produk: 10 • International brands: 26
Produk
  • Elestat
    Solution / drops • 0.5 mg/1mL • Ophthalmic • US • Approved
  • Epinastine
    Solution / drops • 0.5 mg/1mL • Ophthalmic • US • Generic • Approved
  • Epinastine HCl
    Solution • 0.5 mg/1mL • Ophthalmic • US • Generic • Approved
  • Epinastine HCl
    Solution • 0.5 mg/1mL • Ophthalmic • US • Generic • Approved
  • Epinastine Hydrochloride
    Solution / drops • 0.5 mg/1mL • Ophthalmic • US • Generic • Approved
  • Epinastine Hydrochloride
    Solution • 0.5 mg/1mL • Ophthalmic • US • Generic • Approved
  • Epinastine Hydrochloride
    Solution • 0.5 mg/1mL • Ophthalmic • US • Generic • Approved
  • Epinastine Hydrochloride
    Solution / drops • 0.5 mg/1mL • Ophthalmic • US • Generic • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Alegain — Kyorin Rimedio
  • Alenapion — Choseido Pharmaceutical
  • Alesion — Boehringer Ingelheim
  • Alesiotec — Nihon Yakuhin Kogyo
  • Alket — Poen
  • Allernothin — Morishita Jintan
  • Allerstin — Dong Koo
  • Alpeed — Daito
  • Aplatin — Taiyo Pharmaceutical
  • Aresten — Il Sung

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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