Peringatan Keamanan

Patients presenting with an overdose typically present with flushing, hyperthermia, tachycardia, ileus, urinary retention, loss of ocular accommodation, light sensitivity, mydriasis, nausea, vomiting, dizziness, light headedness, and obstipation.L4755,L33105 Patients should be treated with symptomatic and supportive therapy, which may include the use of catheters for urinary retention, cardiovascular support, airway maintenance, ventilation, or neostigmine.L4755

The oral LD50 in mice is 570 mg/kg, and in rats is 709 mg/kg.L33100 The intraperitoneal LD50 in mice is 90 mg/kg, and in rats is 196 mg/kg.L33100

Glycopyrronium

DB00986

small molecule approved investigational vet_approved

Deskripsi

Glycopyrronium, also known as NVA237 or glycopyrrolate, is a racemic mixture of two enantiomers.L33110 They are both quaternary ammonium compounds and long acting muscarinic antagonists.L33110 It is one of the most commonly prescribed anticholinergic medications.A233535,A233540 Early research into glycopyrronium use was for its indication as an adjunct therapy in the treatment of peptic ulcers.A233570,L33090 Later research, taking advantage of the systemic distribution of muscarinic receptors through the body, found that glycopyrronium could also be used for reducing sweat gland,L4755 oral,L33140 airway, and gastric secretions;L33120 as well as reducing cardiac inhibitory reflexes;L33120 and reducing bronchoconstriction in COPD.L33105 Glycopyrronium is commonly prescribed as a first line treatment for a wide variety indications and is considered to have a wider therapeutic window than tiotropium.A233565

Glycopyrronium was originally granted FDA approval on 11 August 1961.L33090

Struktur Molekul 2D

Berat 318.4305
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 after inhalation is approximately 33-53 hours.[L33110] The mean half life of a 6 µg/kg intravenous dose is 0.83 ± 0.27 hours.[L33120] The mean half life of oral glycopyrronium is 3.0 hours.[L33140]
Volume Distribusi The mean volume of distribution in patients aged 1-14 years old is 1.3-1.8 L/kg, with a range of 0.7-3.9 L/kg.[L4755] The volume of distribution in adults aged 60-75 years is 0.42 ± 0.22 L/kg.[L4755]
Klirens (Clearance) A 6 µg/kg intravenous dose has a clearance of 0.54 ± 0.14 L/kg/h.[L33120] An oral solution has a clearance of 5.28-38.95 L/h/kg in healthy adults and 8.07-25.65 L/h/kg in patients with cerebral palsy.[L33140]

Absorpsi

In adults, a 66 mg topical dose of glycopyrronium reaches a Cmax of 0.08 ± 0.04 ng/mL, with a Tmax of 1 hour, and an AUC0-24 of 0.88 ± 0.57 h\*ng/mL.L4755 Inhaled glycopyrronium is approximately 40% bioavailable.L33110 A 25 µg inhaled solution reaches a Cmax of 34.5 pg/mL, with a Tmax of <20 minutes, and an AUC0-inf of 255 h\*pg/mL.L33105 An 8 µg/kg intramuscular dose reaches a Cmax of 3.47 ± 1.48 µg/L, with a Tmax of 27.48 ± 6.12 minutes, and an AUC of 6.64 ± 2.33 h\*g/L.L33120 Oral glycopyrronium has highly variable pharmacokinetics, reaching a mean Cmax of 0.318 ng/mL, a Tmax of 3.1 hours, and an AUC0-24 of 1.74 h\*ng/mL.L33140

Metabolisme

Glycopyrronium is hydrolyzed to the inactive M9 metabolite.L33110,L33115 Metabolism was mainly mediated by CYP2D6, with minor contributions from CYP1A2, CYP2B6, CYP2C9, CYP2C18, CYP2C19, and CYP3A4.L33110,L33115

Rute Eliminasi

85% of an intravenous dose was recovered in the urine, with <5% recovered in the bile.L4755 >80% of the recovered dose is the unchanged parent drug.L4755 The remainder is recovered as the inactive M9 metabolite.L33110,L33115

Interaksi Makanan

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

Interaksi Obat

518 Data
Aclidinium The risk or severity of adverse effects can be increased when Glycopyrronium is combined with Aclidinium.
Mianserin Mianserin may increase the anticholinergic activities of Glycopyrronium.
Mirabegron The risk or severity of urinary retention can be increased when Glycopyrronium is combined with Mirabegron.
Pramlintide The risk or severity of reduced gastrointestinal motility can be increased when Pramlintide is combined with Glycopyrronium.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Glycopyrronium.
Tiotropium The risk or severity of adverse effects can be increased when Glycopyrronium is combined with Tiotropium.
Topiramate The risk or severity of hyperthermia and oligohydrosis can be increased when Glycopyrronium is combined with Topiramate.
Umeclidinium The risk or severity of adverse effects can be increased when Glycopyrronium is combined with Umeclidinium.
Metformin The serum concentration of Metformin can be increased when it is combined with Glycopyrronium.
Atenolol The bioavailability of Atenolol can be increased when combined with Glycopyrronium.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Glycopyrronium.
Metildigoxin The serum concentration of Metildigoxin can be increased when it is combined with Glycopyrronium.
Acetyldigoxin The serum concentration of Acetyldigoxin can be increased when it is combined with Glycopyrronium.
Tramadol The risk or severity of adverse effects can be increased when Tramadol is combined with Glycopyrronium.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Glycopyrronium.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Glycopyrronium.
Benzatropine The risk or severity of adverse effects can be increased when Benzatropine is combined with Glycopyrronium.
Ziprasidone The risk or severity of adverse effects can be increased when Ziprasidone is combined with Glycopyrronium.
Disopyramide The risk or severity of adverse effects can be increased when Disopyramide is combined with Glycopyrronium.
Amitriptyline The risk or severity of adverse effects can be increased when Amitriptyline is combined with Glycopyrronium.
Ipratropium The risk or severity of adverse effects can be increased when Ipratropium is combined with Glycopyrronium.
Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Glycopyrronium.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Glycopyrronium.
Terfenadine The risk or severity of adverse effects can be increased when Terfenadine is combined with Glycopyrronium.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Glycopyrronium.
Clozapine The risk or severity of adverse effects can be increased when Clozapine is combined with Glycopyrronium.
Doxylamine The risk or severity of adverse effects can be increased when Doxylamine is combined with Glycopyrronium.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Glycopyrronium.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Glycopyrronium.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Glycopyrronium.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Glycopyrronium.
Promazine The risk or severity of adverse effects can be increased when Promazine is combined with Glycopyrronium.
Hyoscyamine The risk or severity of adverse effects can be increased when Hyoscyamine is combined with Glycopyrronium.
Cyproheptadine The risk or severity of adverse effects can be increased when Cyproheptadine is combined with Glycopyrronium.
Imipramine The risk or severity of adverse effects can be increased when Imipramine is combined with Glycopyrronium.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Glycopyrronium.
Chlorpromazine The risk or severity of adverse effects can be increased when Chlorpromazine is combined with Glycopyrronium.
Gallamine triethiodide The risk or severity of adverse effects can be increased when Gallamine triethiodide is combined with Glycopyrronium.
Darifenacin The risk or severity of adverse effects can be increased when Darifenacin is combined with Glycopyrronium.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Glycopyrronium.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Glycopyrronium.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Glycopyrronium.
Nortriptyline The risk or severity of adverse effects can be increased when Nortriptyline is combined with Glycopyrronium.
Amoxapine The risk or severity of adverse effects can be increased when Amoxapine is combined with Glycopyrronium.
Lamotrigine The risk or severity of Tachycardia can be increased when Lamotrigine is combined with Glycopyrronium.
Atropine The risk or severity of adverse effects can be increased when Atropine is combined with Glycopyrronium.
Nicardipine The risk or severity of adverse effects can be increased when Nicardipine is combined with Glycopyrronium.
Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Glycopyrronium.
Paroxetine The risk or severity of adverse effects can be increased when Paroxetine is combined with Glycopyrronium.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Homatropine methylbromide is combined with Glycopyrronium.
Rocuronium The risk or severity of adverse effects can be increased when Rocuronium is combined with Glycopyrronium.
Scopolamine The risk or severity of adverse effects can be increased when Scopolamine is combined with Glycopyrronium.
Benzquinamide The risk or severity of adverse effects can be increased when Benzquinamide is combined with Glycopyrronium.
Clidinium The risk or severity of adverse effects can be increased when Clidinium is combined with Glycopyrronium.
Propiomazine The risk or severity of adverse effects can be increased when Propiomazine is combined with Glycopyrronium.
Propantheline The risk or severity of adverse effects can be increased when Propantheline is combined with Glycopyrronium.
Dicyclomine The risk or severity of adverse effects can be increased when Dicyclomine is combined with Glycopyrronium.
Biperiden The risk or severity of adverse effects can be increased when Biperiden is combined with Glycopyrronium.
Brompheniramine The risk or severity of adverse effects can be increased when Brompheniramine is combined with Glycopyrronium.
Flupentixol The risk or severity of adverse effects can be increased when Flupentixol is combined with Glycopyrronium.
Cocaine The risk or severity of adverse effects can be increased when Cocaine is combined with Glycopyrronium.
Quinidine The risk or severity of adverse effects can be increased when Quinidine is combined with Glycopyrronium.
Maprotiline The risk or severity of adverse effects can be increased when Maprotiline is combined with Glycopyrronium.
Methantheline The risk or severity of adverse effects can be increased when Methantheline is combined with Glycopyrronium.
Cycrimine The risk or severity of adverse effects can be increased when Cycrimine is combined with Glycopyrronium.
Tolterodine The risk or severity of adverse effects can be increased when Tolterodine is combined with Glycopyrronium.
Oxybutynin The risk or severity of adverse effects can be increased when Oxybutynin is combined with Glycopyrronium.
Promethazine The risk or severity of adverse effects can be increased when Promethazine is combined with Glycopyrronium.
Diphenhydramine The risk or severity of adverse effects can be increased when Diphenhydramine is combined with Glycopyrronium.
Doxacurium The risk or severity of adverse effects can be increased when Doxacurium is combined with Glycopyrronium.
Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Glycopyrronium.
Flavoxate The risk or severity of adverse effects can be increased when Flavoxate is combined with Glycopyrronium.
Desipramine The risk or severity of adverse effects can be increased when Desipramine is combined with Glycopyrronium.
Orphenadrine The risk or severity of adverse effects can be increased when Orphenadrine is combined with Glycopyrronium.
Escitalopram The risk or severity of adverse effects can be increased when Escitalopram is combined with Glycopyrronium.
Quetiapine The risk or severity of adverse effects can be increased when Quetiapine is combined with Glycopyrronium.
Mivacurium The risk or severity of adverse effects can be increased when Mivacurium is combined with Glycopyrronium.
Diphenidol The risk or severity of adverse effects can be increased when Diphenidol is combined with Glycopyrronium.
Aripiprazole The risk or severity of adverse effects can be increased when Aripiprazole is combined with Glycopyrronium.
Chlorprothixene The risk or severity of adverse effects can be increased when Chlorprothixene is combined with Glycopyrronium.
Metocurine The risk or severity of adverse effects can be increased when Metocurine is combined with Glycopyrronium.
Pancuronium The risk or severity of adverse effects can be increased when Pancuronium is combined with Glycopyrronium.
Pipecuronium The risk or severity of adverse effects can be increased when Pipecuronium is combined with Glycopyrronium.
Methotrimeprazine The risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Glycopyrronium.
Solifenacin The risk or severity of adverse effects can be increased when Solifenacin is combined with Glycopyrronium.
Isopropamide The risk or severity of adverse effects can be increased when Isopropamide is combined with Glycopyrronium.
Rapacuronium The risk or severity of adverse effects can be increased when Rapacuronium is combined with Glycopyrronium.
Mepenzolate The risk or severity of adverse effects can be increased when Mepenzolate is combined with Glycopyrronium.
Pizotifen The risk or severity of adverse effects can be increased when Pizotifen is combined with Glycopyrronium.
Fesoterodine The risk or severity of adverse effects can be increased when Fesoterodine is combined with Glycopyrronium.
Hexocyclium The risk or severity of adverse effects can be increased when Hexocyclium is combined with Glycopyrronium.
Dimetindene The risk or severity of adverse effects can be increased when Dimetindene is combined with Glycopyrronium.
Dexetimide The risk or severity of adverse effects can be increased when Dexetimide is combined with Glycopyrronium.
Benactyzine The risk or severity of adverse effects can be increased when Benactyzine is combined with Glycopyrronium.
Trimebutine The risk or severity of adverse effects can be increased when Trimebutine is combined with Glycopyrronium.
Dosulepin The risk or severity of adverse effects can be increased when Dosulepin is combined with Glycopyrronium.
Imidafenacin The risk or severity of adverse effects can be increased when Imidafenacin is combined with Glycopyrronium.
Butylscopolamine The risk or severity of adverse effects can be increased when Butylscopolamine is combined with Glycopyrronium.
Thonzylamine The risk or severity of adverse effects can be increased when Thonzylamine is combined with Glycopyrronium.
Methscopolamine The risk or severity of adverse effects can be increased when Methscopolamine is combined with Glycopyrronium.

Target Protein

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

Referensi & Sumber

Synthesis reference: Michael Woehrmann, Lara Terstegen, Stefan Biel, Thomas Raschke, Svenja-Kathrin Cerv, Werner Zilz, Sven Untiedt, Thomas Nuebel, Uwe Schoenrock, Heiner Max, Helga Biergiesser, Yvonne Eckhard, Heike Miertsch, Heike Foelster, Cornelia Meier-Zimmerer, Bernd Traupe, Inge Kruse, "GLYCOPYRROLATE IN COSMETIC PREPARATIONS." U.S. Patent US20090208437, issued August 20, 2009.
Artikel (PubMed)
  • PMID: 10385241
    Haddad EB, Patel H, Keeling JE, Yacoub MH, Barnes PJ, Belvisi MG: Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways. Br J Pharmacol. 1999 May;127(2):413-20.
  • PMID: 31495925
    Reid SM, Westbury C, Guzys AT, Reddihough DS: Anticholinergic medications for reducing drooling in children with developmental disability. Dev Med Child Neurol. 2020 Mar;62(3):346-353. doi: 10.1111/dmcn.14350. Epub 2019 Sep 8.
  • PMID: 30994316
    Kirchertz R, Hilbert T: A week of slow hearts: anaesthesia for eye surgery and shortage of glycopyrrolate. Minerva Anestesiol. 2019 Sep;85(9):1033-1034. doi: 10.23736/S0375-9393.19.13607-3. Epub 2019 Apr 16.
  • PMID: 31130562
    Yamamura Y, Nonaka M: Sialorrhea Successfully Treated by the Combined Use of Selective M1 and M3 Muscarinic Acetylcholine Receptor Antagonists. J Nippon Med Sch. 2019;86(2):117-121. doi: 10.1272/jnms.JNMS.2019_86-207.
  • PMID: 2068048
    Schiavone A, Brambilla A: Muscarinic M3 receptors mediate secretion from sweat glands in the rat. Pharmacol Res. 1991 Apr;23(3):233-9. doi: 10.1016/s1043-6618(05)80082-9.
  • PMID: 15691866
    Aihara T, Nakamura Y, Taketo MM, Matsui M, Okabe S: Cholinergically stimulated gastric acid secretion is mediated by M(3) and M(5) but not M(1) muscarinic acetylcholine receptors in mice. Am J Physiol Gastrointest Liver Physiol. 2005 Jun;288(6):G1199-207. doi: 10.1152/ajpgi.00514.2004. Epub 2005 Feb 3.
  • PMID: 29093194
    Saternos HC, Almarghalani DA, Gibson HM, Meqdad MA, Antypas RB, Lingireddy A, AbouAlaiwi WA: Distribution and function of the muscarinic receptor subtypes in the cardiovascular system. Physiol Genomics. 2018 Jan 1;50(1):1-9. doi: 10.1152/physiolgenomics.00062.2017. Epub 2017 Nov 1.
  • PMID: 22854200
    Sykes DA, Dowling MR, Leighton-Davies J, Kent TC, Fawcett L, Renard E, Trifilieff A, Charlton SJ: The Influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium. J Pharmacol Exp Ther. 2012 Nov;343(2):520-8. doi: 10.1124/jpet.112.194456. Epub 2012 Aug 1.
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Sekuens Gen/Protein (FASTA)

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