Rupatadine

DB11614

small molecule approved

Deskripsi

Rupatadine is a dual histamine H1 receptor and platelet activating factor receptor antagonist that is used for symptomatic relief in seasonal and perennial rhinitis as well as chronic spontaneous urticaria. It was approved for marketing in Canada under the tradename Rupall and comes in tablet formulation for adult use and liquid formulation for pediatric use.

Struktur Molekul 2D

Berat 415.97
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of elimination is 15.9 h in children 2-5 years old, 12.3 h in children 6-11 years old, 5.9 h in adults, and 8.7 h in geriatric patients [FDA Label].
Volume Distribusi The apparent volume of distribution is 9799 L [FDA Label].
Klirens (Clearance) Systemic clearance is 1556.2 L/h in young adults and 798.2 L/h in geriatric patients [FDA Label].

Absorpsi

Rupatidine is rapidly absorbed with a Tmax of 1 h FDA Label. Administration with a high fat meal increases exposure by 23% and increases Tmax to 2 h.

Metabolisme

Rupatadine is metabolized by oxidation mediated primarily by CYP3A4 FDA Label. CYP2C9, CYP2C19, and CYP2D6 are also involved to a lesser extent. The metabolites desloratidine and hydroxylated forms of desloratidine retain some activity as H1 receptor antagonists.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of rupatadine.
  • 2. Take with or without food.

Interaksi Obat

852 Data
Benzylpenicilloyl polylysine Rupatadine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Rupatadine.
Mirabegron The serum concentration of Rupatadine can be increased when it is combined with Mirabegron.
Amphetamine Amphetamine may decrease the sedative activities of Rupatadine.
Phentermine Phentermine may decrease the sedative activities of Rupatadine.
Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Rupatadine.
Benzphetamine Benzphetamine may decrease the sedative activities of Rupatadine.
Diethylpropion Diethylpropion may decrease the sedative activities of Rupatadine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Rupatadine.
Mephentermine Mephentermine may decrease the sedative activities of Rupatadine.
MMDA MMDA may decrease the sedative activities of Rupatadine.
Midomafetamine Midomafetamine may decrease the sedative activities of Rupatadine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Rupatadine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Rupatadine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Rupatadine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Rupatadine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Rupatadine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Rupatadine.
Metamfetamine Metamfetamine may decrease the sedative activities of Rupatadine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Rupatadine.
Ritobegron Ritobegron may decrease the sedative activities of Rupatadine.
Mephedrone Mephedrone may decrease the sedative activities of Rupatadine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Rupatadine.
Gepefrine Gepefrine may decrease the sedative activities of Rupatadine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Rupatadine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Rupatadine.
Leuprolide The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Goserelin.
Erythromycin The serum concentration of Rupatadine can be increased when it is combined with Erythromycin.
Azithromycin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Azithromycin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Moxifloxacin.
Sulfisoxazole The metabolism of Rupatadine can be decreased when combined with Sulfisoxazole.
Diltiazem The metabolism of Rupatadine can be decreased when combined with Diltiazem.
Sulpiride The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Sulpiride.
Nimodipine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Nimodipine.
Promazine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Prochlorperazine.
Droperidol The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Droperidol.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Rupatadine.
Ciprofloxacin The metabolism of Rupatadine can be decreased when combined with Ciprofloxacin.
Fluorouracil The metabolism of Rupatadine can be decreased when combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Perflutren.
Cinnarizine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Cinnarizine.
Atropine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Atropine.
Adenosine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Adenosine.
Pentamidine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Cinoxacin.
Granisetron The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Granisetron.
Ondansetron The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Ondansetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Desloratadine.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Dimenhydrinate.
Papaverine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Papaverine.
Chlorpheniramine The metabolism of Rupatadine can be decreased when combined with Chlorpheniramine.
Nifedipine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Nifedipine.
Levofloxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Levofloxacin.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Ofloxacin.
Probucol The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Terlipressin.
Prenylamine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Prenylamine.
Fluspirilene The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Fluspirilene.
Lofexidine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Lofexidine.
Azimilide The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Telavancin.
Pazopanib The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Pazopanib.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Nemonoxacin.
Nilvadipine The metabolism of Rupatadine can be decreased when combined with Nilvadipine.
Antazoline The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Antazoline.
Crizotinib The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Crizotinib.
Bedaquiline The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Fendiline.
Eperisone The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Eperisone.
Butriptyline The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Butriptyline.
Lenvatinib The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Lenvatinib.
Melperone The metabolism of Rupatadine can be decreased when combined with Melperone.
Benidipine The metabolism of Rupatadine can be decreased when combined with Benidipine.
Dexchlorpheniramine maleate The metabolism of Rupatadine can be decreased when combined with Dexchlorpheniramine maleate.
Amifampridine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Amifampridine.
Mocetinostat The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Mocetinostat.
Entinostat The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Entinostat.
Gilteritinib The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Gilteritinib.
CUDC-101 The risk or severity of QTc prolongation can be increased when Rupatadine is combined with CUDC-101.
Simendan The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Simendan.
Ricolinostat The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Ricolinostat.
Mizolastine The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Mizolastine.
Abexinostat The risk or severity of QTc prolongation can be increased when Rupatadine is combined with Abexinostat.

Target Protein

Platelet-activating factor receptor PTAFR
Histamine H1 receptor HRH1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 8996188
    Merlos M, Giral M, Balsa D, Ferrando R, Queralt M, Puigdemont A, Garcia-Rafanell J, Forn J: Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21.
  • PMID: 15457928
    Alfaro V: Role of histamine and platelet-activating factor in allergic rhinitis. J Physiol Biochem. 2004 Jun;60(2):101-11.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Rupall
    Tablet • 10 mg • Oral • Canada • Approved
  • Rupall
    Solution • 1 mg / mL • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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