Peringatan Keamanan

Rat, Oral, LD50: ~ 681 mg/kg
Mouse, Oral, LD50: ~ 316 mg/kg
Rat, Intravenous, NOAEL: 10 mg/kg
Mouse, Intravenous, NOAEL: 10 mg/kg

Fesoterodine

DB06702

small molecule approved

Deskripsi

Fesoterodine is an antimuscarinic prodrug for the treatment of overactive bladder syndrome.

Struktur Molekul 2D

Berat 411.5769
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 7-8 hours for the active metabolite 5-hydroxymethyl tolterodine
Volume Distribusi IV, 5-HMT: 169 L
Klirens (Clearance) 5-HMT, healthy subjects: 14.4 L/h 5-HMT is also secreted into the nephron.

Absorpsi

Tmax (5-HMT): 5 hours post-adminitration of fesoterodine. AUC (0,?)= 49.5 ng·h/ ml Bioavailability, 5-HMT = 52%

Metabolisme

Metabolized by ubiquitous, nonspecific esterases to transform fesoterodine into 5-HMT Extensive metabolism via CYP2D6 and CYP3A4 into inactive metabolites

Rute Eliminasi

Renal: 70% of fesoterodine was recovered in urine as 5-HMT; 35% carboxy metabolite; 18% carboxy-N-desisopropylmetabolite, and 1% N-desisopropyl metabolite Fecal: 7% Hepatic: fesoterodine elimination via CYP2D6 and CYP3A4

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1422 Data
Aclidinium The risk or severity of adverse effects can be increased when Fesoterodine is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Fesoterodine.
Mirabegron The risk or severity of urinary retention can be increased when Fesoterodine is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Fesoterodine is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Fesoterodine.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Fesoterodine.
Tiotropium The risk or severity of adverse effects can be increased when Fesoterodine is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Fesoterodine is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Fesoterodine is combined with Umeclidinium.
Glycopyrronium The risk or severity of adverse effects can be increased when Fesoterodine is combined with Glycopyrronium.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Fesoterodine is combined with Botulinum toxin type A.
Glucagon Fesoterodine may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Fesoterodine may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Fesoterodine is combined with Botulinum toxin type B.
Eluxadoline The risk or severity of constipation can be increased when Fesoterodine is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Fesoterodine is combined with Ramosetron.
Naltrexone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Fesoterodine is combined with Bezitramide.
Tramadol The risk or severity of adverse effects can be increased when Fesoterodine is combined with Tramadol.
Hydromorphone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Oxycodone.
Butorphanol The risk or severity of adverse effects can be increased when Fesoterodine is combined with Butorphanol.
Sufentanil The risk or severity of adverse effects can be increased when Fesoterodine is combined with Sufentanil.
Nalbuphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Fesoterodine is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Fesoterodine is combined with Remifentanil.
Hydrocodone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Hydrocodone.
Diphenoxylate The risk or severity of adverse effects can be increased when Fesoterodine is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Fesoterodine is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Diamorphine.
Ethylmorphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Fesoterodine is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Fesoterodine is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Fesoterodine is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Dihydromorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Fesoterodine is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Fesoterodine is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Fesoterodine is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Fesoterodine is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Nicomorphine.
Meptazinol The risk or severity of adverse effects can be increased when Fesoterodine is combined with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Fesoterodine is combined with Carfentanil, C-11.
Methadone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Methadone.
Pentazocine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Pentazocine.
Buprenorphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Buprenorphine.
Morphine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Morphine.
Codeine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Codeine.
Meperidine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Meperidine.
Alfentanil The risk or severity of adverse effects can be increased when Fesoterodine is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Fesoterodine is combined with Fentanyl.
Tapentadol The risk or severity of urinary retention and constipation can be increased when Fesoterodine is combined with Tapentadol.
Benzhydrocodone The risk or severity of adverse effects can be increased when Fesoterodine is combined with Benzhydrocodone.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Fesoterodine is combined with Dextropropoxyphene.
Levacetylmethadol The risk or severity of adverse effects can be increased when Fesoterodine is combined with Levacetylmethadol.
Naloxegol The risk or severity of adverse effects can be increased when Fesoterodine is combined with Naloxegol.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Fesoterodine.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Fesoterodine.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Fesoterodine.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Fesoterodine.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Fesoterodine.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Fesoterodine.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Fesoterodine.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Fesoterodine.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Fesoterodine.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Fesoterodine.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Fesoterodine.
Atropine The risk or severity of adverse effects can be increased when Atropine is combined with Fesoterodine.
Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Fesoterodine.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Homatropine methylbromide is combined with Fesoterodine.
Tropicamide The risk or severity of adverse effects can be increased when Tropicamide is combined with Fesoterodine.
Methantheline The risk or severity of adverse effects can be increased when Methantheline is combined with Fesoterodine.
Cycrimine The risk or severity of adverse effects can be increased when Cycrimine is combined with Fesoterodine.
Cyclopentolate The risk or severity of adverse effects can be increased when Cyclopentolate is combined with Fesoterodine.
Pentolinium The risk or severity of adverse effects can be increased when Pentolinium is combined with Fesoterodine.
Trimethaphan The risk or severity of adverse effects can be increased when Trimethaphan is combined with Fesoterodine.
Diphenidol The risk or severity of adverse effects can be increased when Diphenidol is combined with Fesoterodine.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Fesoterodine.
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 Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione is combined with Fesoterodine.
Isopropamide The risk or severity of adverse effects can be increased when Isopropamide is combined with Fesoterodine.
Mepenzolate The risk or severity of adverse effects can be increased when Mepenzolate is combined with Fesoterodine.
Hexocyclium The risk or severity of adverse effects can be increased when Fesoterodine is combined with Hexocyclium.
Dimetindene The risk or severity of adverse effects can be increased when Fesoterodine is combined with Dimetindene.
Dexetimide The risk or severity of adverse effects can be increased when Fesoterodine is combined with Dexetimide.
Chlorphenoxamine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Chlorphenoxamine.
Butylscopolamine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Butylscopolamine.
Homatropine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Homatropine.
Thonzylamine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Thonzylamine.
Methscopolamine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Methscopolamine.

Target Protein

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

Referensi & Sumber

Synthesis reference: Claus Meese, "CHIRAL INTERMEDIATE, PROCESS FOR PRODUCING THE SAME AND ITS USE IN THE MANUFACTURE OF TOLTERODINE, FESOTERODINE, OR THE ACTIVE METABOLITE THEREOF." U.S. Patent US20090192224, issued July 30, 2009.
Artikel (PubMed)
  • PMID: 21545485
    Malhotra B, Dickins M, Alvey C, Jumadilova Z, Li X, Duczynski G, Gandelman K: Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Br J Clin Pharmacol. 2011 Aug;72(2):263-9. doi: 10.1111/j.1365-2125.2011.04007.x.
  • PMID: 19835561
    Malhotra B, Gandelman K, Sachse R, Wood N, Michel MC: The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. Curr Med Chem. 2009;16(33):4481-9.

Contoh Produk & Brand

Produk: 65 • International brands: 0
Produk
  • Ach-fesoterodine
    Tablet, extended release • 4 mg • Oral • Canada • Generic • Approved
  • Ach-fesoterodine
    Tablet, extended release • 8 mg • Oral • Canada • Generic • Approved
  • Apo-fesoterodine
    Tablet, extended release • 4 mg • Oral • Canada • Generic • Approved
  • Apo-fesoterodine
    Tablet, extended release • 8 mg • Oral • Canada • Generic • Approved
  • Fesoterodine Fumarate
    Tablet, film coated, extended release • 4 mg/1 • Oral • US • Generic • Approved
  • Fesoterodine Fumarate
    Tablet, film coated, extended release • 8 mg/1 • Oral • US • Generic • Approved
  • Fesoterodine Fumarate
    Tablet, film coated, extended release • 4 mg/1 • Oral • US • Generic • Approved
  • Fesoterodine Fumarate
    Tablet, film coated, extended release • 8 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 65 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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