Peringatan Keamanan

Clinically significant adverse reactions to imidafenacin are acute glaucoma (0.06%), urinary retention (0.03%), and heptic dysfunction (0.02%) FDA Label. The most common adverse effects observed with imidafenacin are thirst (37.7%), constipation (13.6%).

Imidafenacin

DB09262

small molecule investigational

Deskripsi

Imidafenacin is an antispasmodic agent with anticholinergic effects. It antagonizes muscarinic receptors in the bladder to reduce the frequency of urination in the treatment of overactive bladder. It is marketed in Japan under the tradenames Staybla by Ono Pharmaceutical and Uritos by Kyojin Pharmaceutical.

Struktur Molekul 2D

Berat 319.408
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 3 h [A19796].
Volume Distribusi The estimated volume of distribution is 43.9 L [A19796].
Klirens (Clearance) The estimated clearance is 21.2 L/h [A19796].

Absorpsi

The absolute oral bioavailability is 57.8% A19796. Tmax is 1-3 h after administration.

Metabolisme

Thought to be metabolized v by CYP3A4 and UGT1A4 A19796. No active metabolites have been observed.

Rute Eliminasi

10% is excreted in the urine as the parent compound A19796. Most is eliminated by metabolism thought to be mediated by CYP3A4 and UGT1A4.

Interaksi Obat

1227 Data
Aclidinium The risk or severity of adverse effects can be increased when Imidafenacin is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Imidafenacin.
Mirabegron The risk or severity of urinary retention can be increased when Imidafenacin is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Imidafenacin is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Imidafenacin.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Imidafenacin.
Tiotropium The risk or severity of adverse effects can be increased when Imidafenacin is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Imidafenacin is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Imidafenacin is combined with Umeclidinium.
Glycopyrronium The risk or severity of adverse effects can be increased when Imidafenacin is combined with Glycopyrronium.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Imidafenacin is combined with Botulinum toxin type A.
Glucagon Imidafenacin may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Imidafenacin may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Imidafenacin is combined with Botulinum toxin type B.
Eluxadoline The risk or severity of constipation can be increased when Imidafenacin is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Imidafenacin is combined with Ramosetron.
Naltrexone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Imidafenacin is combined with Bezitramide.
Tramadol The risk or severity of adverse effects can be increased when Imidafenacin is combined with Tramadol.
Morphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Morphine.
Hydromorphone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Oxycodone.
Butorphanol The risk or severity of adverse effects can be increased when Imidafenacin is combined with Butorphanol.
Pentazocine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Pentazocine.
Sufentanil The risk or severity of adverse effects can be increased when Imidafenacin is combined with Sufentanil.
Nalbuphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Imidafenacin is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Imidafenacin is combined with Remifentanil.
Buprenorphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Buprenorphine.
Hydrocodone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Hydrocodone.
Diphenoxylate The risk or severity of adverse effects can be increased when Imidafenacin is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Imidafenacin is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Diamorphine.
Ethylmorphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Imidafenacin is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Imidafenacin is combined with Carfentanil.
Dihydrocodeine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Dihydrocodeine.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Imidafenacin is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Dihydromorphine.
Tapentadol The risk or severity of urinary retention and constipation can be increased when Imidafenacin is combined with Tapentadol.
Ketobemidone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Ketobemidone.
DPDPE The risk or severity of adverse effects can be increased when Imidafenacin is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Imidafenacin is combined with Lofentanil.
Opium The risk or severity of adverse effects can be increased when Imidafenacin is combined with Opium.
Normethadone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Imidafenacin is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Nicomorphine.
Meptazinol The risk or severity of adverse effects can be increased when Imidafenacin is combined with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Imidafenacin is combined with Carfentanil, C-11.
Methadone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Methadone.
Codeine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Codeine.
Benzhydrocodone The risk or severity of adverse effects can be increased when Imidafenacin is combined with Benzhydrocodone.
Meperidine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Meperidine.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Imidafenacin is combined with Dextropropoxyphene.
Alfentanil The risk or severity of adverse effects can be increased when Imidafenacin is combined with Alfentanil.
Fentanyl The risk or severity of adverse effects can be increased when Imidafenacin is combined with Fentanyl.
Levacetylmethadol The risk or severity of adverse effects can be increased when Imidafenacin is combined with Levacetylmethadol.
Naloxegol The risk or severity of adverse effects can be increased when Imidafenacin is combined with Naloxegol.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Imidafenacin.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Imidafenacin.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Imidafenacin.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Imidafenacin.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Imidafenacin.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Imidafenacin.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Imidafenacin.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Imidafenacin.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Imidafenacin.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Imidafenacin.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Imidafenacin.
Atropine The risk or severity of adverse effects can be increased when Atropine is combined with Imidafenacin.
Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Imidafenacin.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Homatropine methylbromide is combined with Imidafenacin.
Benzquinamide The risk or severity of adverse effects can be increased when Benzquinamide is combined with Imidafenacin.
Tropicamide The risk or severity of adverse effects can be increased when Tropicamide is combined with Imidafenacin.
Methantheline The risk or severity of adverse effects can be increased when Methantheline is combined with Imidafenacin.
Cycrimine The risk or severity of adverse effects can be increased when Cycrimine is combined with Imidafenacin.
Cyclopentolate The risk or severity of adverse effects can be increased when Cyclopentolate is combined with Imidafenacin.
Pentolinium The risk or severity of adverse effects can be increased when Pentolinium is combined with Imidafenacin.
Trimethaphan The risk or severity of adverse effects can be increased when Trimethaphan is combined with Imidafenacin.
Diphenidol The risk or severity of adverse effects can be increased when Diphenidol is combined with Imidafenacin.
Fenoterol The risk or severity of adverse effects can be increased when Fenoterol is combined with Imidafenacin.
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 Imidafenacin.
Isopropamide The risk or severity of adverse effects can be increased when Isopropamide is combined with Imidafenacin.
Mepenzolate The risk or severity of adverse effects can be increased when Mepenzolate is combined with Imidafenacin.
Hexocyclium The risk or severity of adverse effects can be increased when Hexocyclium is combined with Imidafenacin.
Dimetindene The risk or severity of adverse effects can be increased when Dimetindene is combined with Imidafenacin.
Dexetimide The risk or severity of adverse effects can be increased when Dexetimide is combined with Imidafenacin.
Chlorphenoxamine The risk or severity of adverse effects can be increased when Chlorphenoxamine is combined with Imidafenacin.
Butylscopolamine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Butylscopolamine.
Homatropine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Homatropine.
Thonzylamine The risk or severity of adverse effects can be increased when Imidafenacin is combined with Thonzylamine.

Target Protein

Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17396619
    Kobayashi F, Yageta Y, Segawa M, Matsuzawa S: Effects of imidafenacin (KRP-197/ONO-8025), a new anti-cholinergic agent, on muscarinic acetylcholine receptors. High affinities for M3 and M1 receptor subtypes and selectivity for urinary bladder over salivary gland. Arzneimittelforschung. 2007;57(2):92-100.
  • PMID: 10428387
    Miyachi H, Kiyota H, Uchiki H, Segawa M: Synthesis and antimuscarinic activity of a series of 4-(1-Imidazolyl)-2,2-diphenylbutyramides: discovery of potent and subtype-selective antimuscarinic agents. Bioorg Med Chem. 1999 Jun;7(6):1151-61.
  • PMID: 27430986
    Kuraoka S, Ito Y, Wakuda H, Shinozuka K, Onoue S, Yamada S: Characterization of muscarinic receptor binding by the novel radioligand, (3)Himidafenacin, in the bladder and other tissues of rats. J Pharmacol Sci. 2016 Jul;131(3):184-9. doi: 10.1016/j.jphs.2016.06.002. Epub 2016 Jun 23.
  • PMID: 12452898
    Chess-Williams R: Muscarinic receptors of the urinary bladder: detrusor, urothelial and prejunctional. Auton Autacoid Pharmacol. 2002 Jun;22(3):133-45.
  • PMID: 19122340
    Ohno T, Nakade S, Nakayama K, Kitagawa J, Miyabe H, Konomi T, Miyata Y: Population pharmacokinetic analysis of a novel muscarinic receptor antagonist, imidafenacin, in healthy volunteers and overactive bladder patients. Drug Metab Pharmacokinet. 2008;23(6):456-63.

Contoh Produk & Brand

Produk: 0 • International brands: 2
International Brands
  • Staybla — Ono Pharmaceutical
  • Uritos — Kyorin Pharmaceutical

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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