Peringatan Keamanan

The acute oral LD50 in rats is 460 mg/kg.L8645

Overdose information

An overdose with oxybutynin may manifest clinically as CNS overactivity, fever, palpitations, cardiac arrhythmias, urinary retention, respiratory failure, paralysis, in addition to coma.T689,L8648 Provide supportive care immediately. Activated charcoal in addition to a cathartic agent should be administered. There have been 2 reports of an overdose with a 100 mg dose of oxybutynin. One case was a 13-year-old boy and another was a 34-year-old woman. Alcohol was also ingested simultaneously in both cases. The patients received supportive treatment and fully recovered.T689

Oxybutynin

DB01062

small molecule approved investigational

Deskripsi

Overactive bladder (OAB) is a common condition negatively impacting the lives of millions of patients worldwide. Due to its urinary symptoms that include nocturia, urgency, and frequency, this condition causes social embarrassment and a poor quality of life.A185996,A185999

Oxybutynin, also marketed as Ditropan XL, is an anticholinergic medication used for the relief of overactive bladder symptoms that has been optimized for high levels of safety and efficacy since initial FDA approval in 1975.A183782,L8648 This drug relieves undesirable urinary symptoms, increasing the quality of life for patients affected by OAB. It is often used as first-line therapy for OAB.A185990

Struktur Molekul 2D

Berat 357.4864
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma elimination half-life is about 2 hours. In the elderly, the elimination half-life is prolonged up to 5 hours.[A183782,A185990]
Volume Distribusi Oxybutynin has a wide volume of distribution of 193 L.[L8648] In rats, oxybutynin penetrates the central nervous system.[A186050]
Klirens (Clearance) -

Absorpsi

Oxybutynin should be swallowed whole with the help of liquids.L8648 A pharmacokinetic study revealed that oxybutynin was rapidly absorbed, and peak concentrations were reached within about 1 hour of administration, measured at 8.2 ngml-1 and AUC was 16 ngml-1.A185987 The biovailability of oxybutynin is about 6%, and the plasma concentration of the active metabolite, desethyloxybutynin is 5 to 12 times greater than that of oxybutynin.A183782 Bioavailability is increased in the elderly.A185990 Food has been shown to increase the exposure to controlled-release oxybutynin.A186035

Metabolisme

Oxybutynin is heavily metabolized by the CYP3A4 enzyme systemA185990 in both the liver and the wall of the intestine. It undergoes first-pass metabolism, and its resulting primary active metabolite, N-desethyloxybutynin circulates. It is active at the muscarinic receptors in both the bladder and the salivary gland.A183782 Hepatic biotransformation also produces its major inactive metabolite, phenylcyclohexylglycolic acid.A185990

Rute Eliminasi

Oxybutynin is heavily cleared by the liver.A185987 Under 0.1% of an administered dose is found as unchanged drug in the urine. Less than 0.1% of a single dose of oxybutynin is excreted as desethyloxybutynin.A185987,L8648

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food.

Interaksi Obat

1087 Data
Eliglustat The metabolism of Eliglustat can be decreased when combined with Oxybutynin.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Oxybutynin.
Aclidinium The risk or severity of adverse effects can be increased when Oxybutynin is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Oxybutynin.
Mirabegron The risk or severity of urinary retention can be increased when Oxybutynin is combined with Mirabegron.
Potassium chloride The risk or severity of gastrointestinal ulceration can be increased when Oxybutynin is combined with Potassium chloride.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Oxybutynin.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Oxybutynin.
Tiotropium The risk or severity of adverse effects can be increased when Oxybutynin is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Oxybutynin is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Oxybutynin is combined with Umeclidinium.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Oxybutynin.
Colchicine The metabolism of Colchicine can be decreased when combined with Oxybutynin.
Fentanyl The risk or severity of adverse effects can be increased when Oxybutynin is combined with Fentanyl.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Oxybutynin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Oxybutynin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Oxybutynin.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Oxybutynin.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Oxybutynin.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Oxybutynin.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Oxybutynin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Oxybutynin.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Oxybutynin.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Oxybutynin.
Glycopyrronium The risk or severity of adverse effects can be increased when Oxybutynin is combined with Glycopyrronium.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Oxybutynin.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Oxybutynin.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Oxybutynin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Oxybutynin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Oxybutynin.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Oxybutynin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Oxybutynin.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Oxybutynin.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Oxybutynin.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Oxybutynin is combined with Botulinum toxin type A.
Glucagon Oxybutynin may increase the gastrointestinal motility reducing activities of Glucagon.
Sulpiride Oxybutynin may increase the anticholinergic activities of Sulpiride.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Oxybutynin is combined with Botulinum toxin type B.
Eluxadoline The risk or severity of constipation can be increased when Oxybutynin is combined with Eluxadoline.
Ramosetron The risk or severity of constipation can be increased when Oxybutynin is combined with Ramosetron.
Naltrexone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Naltrexone.
Bezitramide The risk or severity of adverse effects can be increased when Oxybutynin is combined with Bezitramide.
Butorphanol The risk or severity of adverse effects can be increased when Oxybutynin is combined with Butorphanol.
Pentazocine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Pentazocine.
Nalbuphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Oxybutynin is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Oxybutynin is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Oxybutynin is combined with Diphenoxylate.
Dezocine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Oxybutynin is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Diamorphine.
Etorphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Oxybutynin is combined with Dextromoramide.
Desomorphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Desomorphine.
Carfentanil The risk or severity of adverse effects can be increased when Oxybutynin is combined with Carfentanil.
Alphacetylmethadol The risk or severity of adverse effects can be increased when Oxybutynin is combined with Alphacetylmethadol.
Dihydromorphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Dihydromorphine.
Tapentadol The risk or severity of urinary retention and constipation can be increased when Oxybutynin is combined with Tapentadol.
DPDPE The risk or severity of adverse effects can be increased when Oxybutynin is combined with DPDPE.
Lofentanil The risk or severity of adverse effects can be increased when Oxybutynin is combined with Lofentanil.
Normethadone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Normethadone.
Piritramide The risk or severity of adverse effects can be increased when Oxybutynin is combined with Piritramide.
Alphaprodine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Alphaprodine.
Nicomorphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Nicomorphine.
Meptazinol The risk or severity of adverse effects can be increased when Oxybutynin is combined with Meptazinol.
Phenoperidine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Phenoperidine.
Phenazocine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Phenazocine.
Tilidine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Tilidine.
Carfentanil, C-11 The risk or severity of adverse effects can be increased when Oxybutynin is combined with Carfentanil, C-11.
Morphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Morphine.
Methadone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Methadone.
Buprenorphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Buprenorphine.
Ketobemidone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Ketobemidone.
Meperidine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Meperidine.
Alfentanil The risk or severity of adverse effects can be increased when Oxybutynin is combined with Alfentanil.
Levacetylmethadol The risk or severity of adverse effects can be increased when Oxybutynin is combined with Levacetylmethadol.
Benzhydrocodone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Benzhydrocodone.
Hydromorphone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Oxycodone.
Codeine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Codeine.
Dextropropoxyphene The risk or severity of adverse effects can be increased when Oxybutynin is combined with Dextropropoxyphene.
Oxymorphone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Oxymorphone.
Ethylmorphine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Ethylmorphine.
Dihydrocodeine The risk or severity of adverse effects can be increased when Oxybutynin is combined with Dihydrocodeine.
Opium The risk or severity of adverse effects can be increased when Oxybutynin is combined with Opium.
Sufentanil The risk or severity of adverse effects can be increased when Oxybutynin is combined with Sufentanil.
Hydrocodone The risk or severity of adverse effects can be increased when Oxybutynin is combined with Hydrocodone.
Naloxegol The risk or severity of adverse effects can be increased when Oxybutynin is combined with Naloxegol.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Oxybutynin.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Oxybutynin.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Oxybutynin.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Oxybutynin.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Oxybutynin.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Oxybutynin.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Oxybutynin.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Oxybutynin.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Oxybutynin.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Oxybutynin.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Oxybutynin.

Target Protein

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

Referensi & Sumber

Synthesis reference: Masakatsu Shibasaki, "Method of producing oxybutynin and its derivatives." U.S. Patent US20040006243, issued January 08, 2004.
Artikel (PubMed)
  • PMID: 3234461
    Douchamps J, Derenne F, Stockis A, Gangji D, Juvent M, Herchuelz A: The pharmacokinetics of oxybutynin in man. Eur J Clin Pharmacol. 1988;35(5):515-20. doi: 10.1007/bf00558247.
  • PMID: 20428289
    Kennelly MJ: A comparative review of oxybutynin chloride formulations: pharmacokinetics and therapeutic efficacy in overactive bladder. Rev Urol. 2010 Winter;12(1):12-9.
  • PMID: 7620236
    Yarker YE, Goa KL, Fitton A: Oxybutynin. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in detrusor instability. Drugs Aging. 1995 Mar;6(3):243-62. doi: 10.2165/00002512-199506030-00007.
  • PMID: 27556018
    Willis-Gray MG, Dieter AA, Geller EJ: Evaluation and management of overactive bladder: strategies for optimizing care. Res Rep Urol. 2016 Jul 27;8:113-22. doi: 10.2147/RRU.S93636. eCollection 2016.
  • PMID: 30248206
    Plata M, Bravo-Balado A, Robledo D, Trujillo CG, Caicedo JI, Catano JG, Arenas J, Rondon M, Londono D: Prevalence of lower urinary tract symptoms and overactive bladder in men and women over 18 years old: The Colombian overactive bladder and lower urinary tract symptoms (COBaLT) study. Neurourol Urodyn. 2019 Jan;38(1):200-207. doi: 10.1002/nau.23828. Epub 2018 Sep 24.
  • PMID: 28608746
    Aprile S, Canavesi R, Matucci R, Bellucci C, Del Grosso E, Grosa G: New insights in the metabolism of oxybutynin: evidence of N-oxidation of propargylamine moiety and rearrangement to enaminoketone. Xenobiotica. 2018 May;48(5):478-487. doi: 10.1080/00498254.2017.1342288. Epub 2017 Jul 6.
  • PMID: 14606931
    Guay DR: Clinical pharmacokinetics of drugs used to treat urge incontinence. Clin Pharmacokinet. 2003;42(14):1243-85. doi: 10.2165/00003088-200342140-00004.
  • PMID: 11939551
    Shibukawa A, Ishizawa N, Kimura T, Sakamoto Y, Ogita K, Matsuo Y, Kuroda Y, Matayatsu C, Nakagawa T, Wainer IW: Plasma protein binding study of oxybutynin by high-performance frontal analysis. J Chromatogr B Analyt Technol Biomed Life Sci. 2002 Feb 25;768(1):177-88.
Menampilkan 8 dari 11 artikel.
Textbook
  • Jennifer Dwyer; Chad A. LaGrange (2019). Oxybutinin. StatPearls Publishing.

Contoh Produk & Brand

Produk: 313 • International brands: 2
Produk
  • Albert Oxybutynin
    Tablet • 5 mg • Oral • Canada • Approved
  • Apo-oxybutynin
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Apo-oxybutynin
    Syrup • 1 mg / mL • Oral • Canada • Generic • Approved
  • Ava-oxybutynin
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Ditropan
    Tablet • 5 mg/1 • Oral • US • Approved
  • Ditropan
    Syrup • 5 mg/5mL • Oral • US • Approved
  • Ditropan Syrup 1mg/ml
    Syrup • 1 mg / mL • Oral • Canada • Approved
  • Ditropan Tablets 5mg
    Tablet • 5 mg • Oral • Canada • Approved
Menampilkan 8 dari 313 produk.
International Brands
  • Lenditro
  • Lyrinel XL

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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