Peringatan Keamanan

Overdosage can potentially result in severe central anticholinergic effects.

Darifenacin

DB00496

small molecule approved investigational

Deskripsi

Darifenacin (Enablex®, Novartis) is a medication used to treat urinary incontinence.

Darifenacin blocks M3 muscarinic acetylcholine receptors, which mediate bladder muscle contractions. This block reduces the urgency to urinate and so it should not be used in people with urinary retention.

It is unknown if M3 receptor selectivity is clinically advantageous in overactive bladder syndrome treatments.

Struktur Molekul 2D

Berat 426.55
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of darifenacin following chronic dosing is approximately 13-19 hours.
Volume Distribusi * 163 L
Klirens (Clearance) * 40 L/h [extensive metabolizers] * 32 L/h [poor metabolizers]

Absorpsi

The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.

Metabolisme

Hepatic. Primarily mediated by the cytochrome P450 enzymes CYP2D6 and CYP3A4.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

859 Data
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Darifenacin.
Eliglustat The metabolism of Darifenacin can be decreased when combined with Eliglustat.
Aclidinium The risk or severity of adverse effects can be increased when Darifenacin is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Darifenacin.
Mirabegron The risk or severity of urinary retention can be increased when Darifenacin is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Darifenacin is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Darifenacin.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Darifenacin.
Tiotropium The risk or severity of adverse effects can be increased when Darifenacin is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Darifenacin is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Darifenacin is combined with Umeclidinium.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Darifenacin.
Glycopyrronium The risk or severity of adverse effects can be increased when Darifenacin is combined with Glycopyrronium.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Darifenacin is combined with Botulinum toxin type A.
Glucagon Darifenacin may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Darifenacin may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Darifenacin is combined with Botulinum toxin type B.
Eluxadoline The risk or severity of constipation can be increased when Darifenacin is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Darifenacin is combined with Ramosetron.
Naltrexone The risk or severity of adverse effects can be increased when Darifenacin is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Darifenacin is combined with Bezitramide.
Butorphanol The risk or severity of adverse effects can be increased when Darifenacin is combined with Butorphanol.
Pentazocine The risk or severity of adverse effects can be increased when Darifenacin is combined with Pentazocine.
Nalbuphine The risk or severity of adverse effects can be increased when Darifenacin is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Darifenacin is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Darifenacin is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Darifenacin is combined with Diphenoxylate.
Dezocine The risk or severity of adverse effects can be increased when Darifenacin is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Darifenacin is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Darifenacin is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Darifenacin is combined with Diamorphine.
Etorphine The risk or severity of adverse effects can be increased when Darifenacin is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Darifenacin is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Darifenacin is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Darifenacin is combined with Carfentanil.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Darifenacin is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Darifenacin is combined with Dihydromorphine.
DPDPE The risk or severity of adverse effects can be increased when Darifenacin is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Darifenacin is combined with Lofentanil.
Normethadone The risk or severity of adverse effects can be increased when Darifenacin is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Darifenacin is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Darifenacin is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Darifenacin is combined with Nicomorphine.
Meptazinol The risk or severity of adverse effects can be increased when Darifenacin is combined with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Darifenacin is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Darifenacin is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Darifenacin is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Darifenacin is combined with Carfentanil, C-11.
Benzhydrocodone The risk or severity of adverse effects can be increased when Darifenacin is combined with Benzhydrocodone.
Hydromorphone The risk or severity of adverse effects can be increased when Darifenacin is combined with Hydromorphone.
Morphine The risk or severity of adverse effects can be increased when Darifenacin is combined with Morphine.
Sufentanil The risk or severity of adverse effects can be increased when Darifenacin is combined with Sufentanil.
Alfentanil The risk or severity of adverse effects can be increased when Darifenacin is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Darifenacin is combined with Fentanyl.
Levacetylmethadol The risk or severity of adverse effects can be increased when Darifenacin is combined with Levacetylmethadol.
Ketobemidone The risk or severity of adverse effects can be increased when Darifenacin is combined with Ketobemidone.
Meperidine The risk or severity of adverse effects can be increased when Darifenacin is combined with Meperidine.
Tapentadol The risk or severity of urinary retention and constipation can be increased when Darifenacin is combined with Tapentadol.
Naloxegol The risk or severity of adverse effects can be increased when Darifenacin is combined with Naloxegol.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Darifenacin.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Darifenacin.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Darifenacin.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Darifenacin.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Darifenacin.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Darifenacin.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Darifenacin.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Darifenacin.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Darifenacin.
Tridihexethyl The risk or severity of adverse effects can be increased when Darifenacin is combined with Tridihexethyl.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Darifenacin is combined with Anisotropine methylbromide.
Atropine The risk or severity of adverse effects can be increased when Darifenacin is combined with Atropine.
Mecamylamine The risk or severity of adverse effects can be increased when Darifenacin is combined with Mecamylamine.
Pirenzepine The risk or severity of adverse effects can be increased when Darifenacin is combined with Pirenzepine.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Darifenacin is combined with Homatropine methylbromide.
Benzquinamide The risk or severity of adverse effects can be increased when Darifenacin is combined with Benzquinamide.
Propantheline The risk or severity of adverse effects can be increased when Darifenacin is combined with Propantheline.
Dicyclomine The risk or severity of adverse effects can be increased when Darifenacin is combined with Dicyclomine.
Tropicamide The risk or severity of adverse effects can be increased when Darifenacin is combined with Tropicamide.
Amantadine The risk or severity of adverse effects can be increased when Darifenacin is combined with Amantadine.
Methantheline The risk or severity of adverse effects can be increased when Darifenacin is combined with Methantheline.
Cycrimine The risk or severity of adverse effects can be increased when Darifenacin is combined with Cycrimine.
Cyclopentolate The risk or severity of adverse effects can be increased when Darifenacin is combined with Cyclopentolate.
Pentolinium The risk or severity of adverse effects can be increased when Darifenacin is combined with Pentolinium.
Trimethaphan The risk or severity of adverse effects can be increased when Darifenacin is combined with Trimethaphan.
Flavoxate The risk or severity of adverse effects can be increased when Darifenacin is combined with Flavoxate.
Diphenidol The risk or severity of adverse effects can be increased when Darifenacin is combined with Diphenidol.
Fenoterol The risk or severity of adverse effects can be increased when Darifenacin is combined with Fenoterol.
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione The risk or severity of adverse effects can be increased when Darifenacin is combined with Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione.
Isopropamide The risk or severity of adverse effects can be increased when Darifenacin is combined with Isopropamide.
Mepenzolate The risk or severity of adverse effects can be increased when Darifenacin is combined with Mepenzolate.
Hexocyclium The risk or severity of adverse effects can be increased when Darifenacin is combined with Hexocyclium.
Dimetindene The risk or severity of adverse effects can be increased when Darifenacin is combined with Dimetindene.
Dexetimide The risk or severity of adverse effects can be increased when Darifenacin is combined with Dexetimide.
Chlorphenoxamine The risk or severity of adverse effects can be increased when Darifenacin is combined with Chlorphenoxamine.
Butylscopolamine The risk or severity of adverse effects can be increased when Darifenacin is combined with Butylscopolamine.
Homatropine The risk or severity of adverse effects can be increased when Darifenacin is combined with Homatropine.
Thonzylamine The risk or severity of adverse effects can be increased when Darifenacin is combined with Thonzylamine.
Methscopolamine The risk or severity of adverse effects can be increased when Darifenacin is combined with Methscopolamine.
Oxitropium The risk or severity of adverse effects can be increased when Darifenacin is combined with Oxitropium.
Batefenterol The risk or severity of adverse effects can be increased when Darifenacin is combined with Batefenterol.

Target Protein

Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M4 CHRM4
Muscarinic acetylcholine receptor M5 CHRM5

Referensi & Sumber

Synthesis reference: Valeriano Merli, Augusto Canavesi, Paola Daverio, "Processes for preparing darifenacin hydrobromide." U.S. Patent US20070197631, issued August 23, 2007.

Contoh Produk & Brand

Produk: 73 • International brands: 2
Produk
  • Apo-darifenacin
    Tablet, extended release • 15 mg • Oral • Canada • Generic • Approved
  • Apo-darifenacin
    Tablet, extended release • 7.5 mg • Oral • Canada • Generic • Approved
  • Darifenacin
    Tablet, extended release • 7.5 mg/1 • Oral • US • Approved
  • Darifenacin
    Tablet, extended release • 15 mg/1 • Oral • US • Approved
  • Darifenacin
    Tablet, extended release • 7.5 mg/1 • Oral • US • Generic • Approved
  • Darifenacin
    Tablet, extended release • 15 mg/1 • Oral • US • Generic • Approved
  • Darifenacin
    Tablet, film coated, extended release • 7.5 mg/1 • Oral • US • Generic • Approved
  • Darifenacin
    Tablet, film coated, extended release • 15 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 73 produk.
International Brands
  • Emselex — Novartis
  • Xelena — Dr. Reddy's

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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