Peringatan Keamanan

The most common adverse effects experienced during clinical trials were abdominal pain, dizziness, headache, and somnolence FDA Label. Bilastine is associated with Q/T prolongation. The no observed adverse effect level of bilastine is 1200 mg/kg/day in rats and 125 mg/kg/day in dogs A19750.

Bilastine

DB11591

small molecule approved investigational

Deskripsi

Bilastine is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.

Struktur Molekul 2D

Berat 463.622
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean half life of elimination is 14.5h [FDA Label].
Volume Distribusi -
Klirens (Clearance) Bilastine has a total clearance is 9.20 L/h and a renal clearance of 8.7 L/h [FDA Label].

Absorpsi

Bilastine has a Tmax of 1.13 h FDA Label. The absolute bioavailability is 61%. No accumulation observed with daily dosing of 20-100 mg after 14 days. Cmax decreased by 25 % and 33% when taken with a low fat and high fat meal compared to fasted state. Administration with grapefruit juice decreased Cmax by 30%.

Metabolisme

Bilastine does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans FDA Label.

Rute Eliminasi

Bilastine is mainly excreted in the feces (66.5%) with some excreted in the urine (28.3%) FDA Label. Nearly all is excreted as the parent compound.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Avoid other fruit juice as well for optimal absorption.
  • 2. Take on an empty stomach. Take at least two hours before or one hour after eating.

Interaksi Obat

402 Data
Benzylpenicilloyl polylysine Bilastine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Bilastine.
Amphetamine Amphetamine may decrease the sedative activities of Bilastine.
Phentermine Phentermine may decrease the sedative activities of Bilastine.
Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Bilastine.
Benzphetamine Benzphetamine may decrease the sedative activities of Bilastine.
Diethylpropion Diethylpropion may decrease the sedative activities of Bilastine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Bilastine.
Mephentermine Mephentermine may decrease the sedative activities of Bilastine.
MMDA MMDA may decrease the sedative activities of Bilastine.
Midomafetamine Midomafetamine may decrease the sedative activities of Bilastine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Bilastine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Bilastine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Bilastine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Bilastine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Bilastine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Bilastine.
Metamfetamine Metamfetamine may decrease the sedative activities of Bilastine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Bilastine.
Ritobegron Ritobegron may decrease the sedative activities of Bilastine.
Mephedrone Mephedrone may decrease the sedative activities of Bilastine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Bilastine.
Gepefrine Gepefrine may decrease the sedative activities of Bilastine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Bilastine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Bilastine.
Leuprolide The risk or severity of QTc prolongation can be increased when Bilastine is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Goserelin.
Erythromycin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Erythromycin.
Azithromycin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Azithromycin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Moxifloxacin.
Ranolazine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Ranolazine.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Bilastine is combined with Sulfisoxazole.
Amitriptyline The risk or severity of QTc prolongation can be increased when Bilastine is combined with Amitriptyline.
Methadone The risk or severity of QTc prolongation can be increased when Bilastine is combined with Methadone.
Diltiazem The risk or severity of QTc prolongation can be increased when Bilastine is combined with Diltiazem.
Clozapine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Clozapine.
Sulpiride The risk or severity of QTc prolongation can be increased when Bilastine is combined with Sulpiride.
Nimodipine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Nimodipine.
Promazine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Prochlorperazine.
Droperidol The risk or severity of QTc prolongation can be increased when Bilastine is combined with Droperidol.
Imipramine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Imipramine.
Chlorpromazine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Chlorpromazine.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Bilastine.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Ciprofloxacin.
Fluorouracil The risk or severity of QTc prolongation can be increased when Bilastine is combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Bilastine is combined with Perflutren.
Cinnarizine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Cinnarizine.
Atropine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Atropine.
Chloroquine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Chloroquine.
Efavirenz The risk or severity of QTc prolongation can be increased when Bilastine is combined with Efavirenz.
Adenosine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Adenosine.
Pentamidine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Bilastine is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Bilastine is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Bilastine is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Cinoxacin.
Loperamide The risk or severity of QTc prolongation can be increased when Bilastine is combined with Loperamide.
Granisetron The risk or severity of QTc prolongation can be increased when Bilastine is combined with Granisetron.
Ondansetron The risk or severity of QTc prolongation can be increased when Bilastine is combined with Ondansetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Bilastine is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Desloratadine.
Telithromycin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Telithromycin.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Bilastine is combined with Dimenhydrinate.
Primaquine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Primaquine.
Papaverine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Papaverine.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Chlorpheniramine.
Nifedipine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Nifedipine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Ofloxacin.
Propafenone The risk or severity of QTc prolongation can be increased when Bilastine is combined with Propafenone.
Flecainide The risk or severity of QTc prolongation can be increased when Bilastine is combined with Flecainide.
Clarithromycin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Clarithromycin.
Levacetylmethadol The risk or severity of QTc prolongation can be increased when Bilastine is combined with Levacetylmethadol.
Saquinavir The risk or severity of QTc prolongation can be increased when Bilastine is combined with Saquinavir.
Clomipramine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Clomipramine.
Mibefradil The risk or severity of QTc prolongation can be increased when Bilastine is combined with Mibefradil.
Probucol The risk or severity of QTc prolongation can be increased when Bilastine is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Terlipressin.
Prenylamine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Prenylamine.
Fluspirilene The risk or severity of QTc prolongation can be increased when Bilastine is combined with Fluspirilene.
Lofexidine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Lofexidine.
Azimilide The risk or severity of QTc prolongation can be increased when Bilastine is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Bilastine is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Bilastine is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Bilastine is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Telavancin.
Pazopanib The risk or severity of QTc prolongation can be increased when Bilastine is combined with Pazopanib.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Bilastine is combined with Nemonoxacin.
Panobinostat The risk or severity of QTc prolongation can be increased when Bilastine is combined with Panobinostat.
Nilvadipine The risk or severity of QTc prolongation can be increased when Bilastine is combined with Nilvadipine.
Antazoline The risk or severity of QTc prolongation can be increased when Bilastine is combined with Antazoline.

Target Protein

Histamine H1 receptor HRH1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27110120
    Wang XY, Lim-Jurado M, Prepageran N, Tantilipikorn P, Wang de Y: Treatment of allergic rhinitis and urticaria: a review of the newest antihistamine drug bilastine. Ther Clin Risk Manag. 2016 Apr 13;12:585-97. doi: 10.2147/TCRM.S105189. eCollection 2016.
  • PMID: 22616813
    Lucero ML, Arteche JK, Sommer EW, Casadesus A: Preclinical toxicity profile of oral bilastine. Drug Chem Toxicol. 2012 Jun;35 Suppl 1:25-33. doi: 10.3109/01480545.2012.682652.

Contoh Produk & Brand

Produk: 12 • International brands: 1
Produk
  • Apo-bilastine Oral Solution
    Solution • 2.5 mg / mL • Oral • Canada • Generic • Approved
  • Apo-bilastine Orodispersible Tablets
    Tablet, orally disintegrating • 10 mg • Oral • Canada • Generic • Approved
  • Apo-bilastine Tablets
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Auro-bilastine
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Blexten
    Tablet • 20 mg • Oral • Canada • Approved
  • Blexten
    Solution • 2.5 mg / mL • Oral • Canada • Approved
  • Blexten
    Tablet, orally disintegrating • 10 mg • Oral • Canada • Approved
  • Gln-bilastine
    Tablet • 20 mg • Oral • Canada • Approved
Menampilkan 8 dari 12 produk.
International Brands
  • Bilaxten — Faes Farma

Sekuens Gen/Protein (FASTA)

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