Peringatan Keamanan

Toxicity information regarding pyridostigmine is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as bradycardia, excessive bronchial secretions, and cholinergic crisis. Symptomatic and supportive measures are recommended.L32408, L32413

Pyridostigmine

DB00545

small molecule approved investigational

Deskripsi

Myasthenia gravis is an autoimmune disease involving dysfunction at the neuromuscular junction, most commonly due to autoantibodies directed against the acetylcholine receptor (AChR), which results in muscle tone loss, muscle weakness, and fatigue.A231004 Acetylcholinesterase inhibitors have been the symptomatic treatment of choice in myasthenia gravis since the 1930s with the early use of physostigmine and neostigmine. By inhibiting the breakdown of acetylcholine in the neuromuscular junction, they increase signalling and relieve symptoms.A231004, L32408, L32413 Pyridostigmine is the current drug of choice, with superior pharmacokinetics and reduced side effects compared to neostigmine.L32408, L32413 In addition to treating myasthenia gravis, pyridostigmine is used to reverse neuromuscular blocks, relieve symptoms in congenital myasthenic syndromes, and protect against certain nerve agents, notably during the Gulf War.A231009, A231014, L32413, L32418

Pyridostigmine was granted initial FDA approval on April 6, 1955, as an oral tablet. Possible dose forms have been expanded to include extended-release tablets, syrups, and injections, marketed under various brand and generic names.L32408, L32413

Struktur Molekul 2D

Berat 181.2117
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Pyridostigmine administered intravenously in healthy, myasthenic, and surgical patients has a range of elimination half-lives, between 0.38 and 1.86 hours.[A231019]
Volume Distribusi Pyridostigmine administered intravenously in healthy, myasthenic, and surgical patients has a range of distribution volumes, between 0.53 and 1.76 L/kg.[A231019]
Klirens (Clearance) Pyridostigmine administered intravenously in healthy, myasthenic, and surgical patients has a range of clearance values, between 0.29 and 1.0 L/h/kg.[A231019]

Absorpsi

Pyridostigmine administered orally is poorly absorbed in the GI tract, with an oral bioavailability of only 10-20%. However, this may in part be due to some metabolism by both the blood and liver.A231019, L32418 Approximately 1-2 hours following a single oral dose of 60 mg, the Cmax was determined to be 40-60 ?g/L.A231019 Pyridostigmine follows approximately linear kinetics, with a direct correlation between the dose and plasma AUC.A231019 Pyridostigmine taken orally with food results in a flatter peak to the plasma concentration vs. time curve. The peak plasma concentrations are reached ~90 minutes later than in fasted subjects but with no change in bioavailability or AUC.A231024

Metabolisme

Pyridostigmine is hydrolyzed by cholinesterases systemically, including in the blood, and by microsomal enzymes in the liver, though this remains poorly defined. The primary hydrolysis product is 3-hydroxy-N-methyl-pyridinium (HNM), which can be glucuronidated.A231019, L32418 One study suggested the existence of as many as eight metabolites in the urine of patients receiving radiolabeled pyridostigmine intravenously, including various glucuronidated, demethylated, and oxidized (quinone) metabolites.A231029, L32418 Another study confirmed that HNM is the main metabolite, and suggested additional possible metabolites such as a 3,4- or 3,6-dihydroxy-N-methyl-pyridinium or a methoxy- or acetoxy-N-methyl-pyridinium.A231034 The exact products formed, apart from HNM, require further validation.

Rute Eliminasi

Pyridostigmine is primarily renally eliminated.L32413 Roughly 90% of an intravenous dose is recovered in the urine within 24 hours, with unchanged pyridostigmine and its main metabolite HNM recovered in an approximately 4:1 ratio.A231019, A231034, L32418

Interaksi Makanan

1 Data
  • 1. Take with food. Food decreases irritation.

Interaksi Obat

294 Data
Methocarbamol The therapeutic efficacy of Pyridostigmine can be decreased when used in combination with Methocarbamol.
Dipyridamole The therapeutic efficacy of Pyridostigmine can be decreased when used in combination with Dipyridamole.
Ephedrine Pyridostigmine may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Pyridostigmine may increase the neuromuscular blocking activities of Bambuterol.
Sar9, Met (O2)11-Substance P Pyridostigmine may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Moxisylyte Pyridostigmine may increase the neuromuscular blocking activities of Moxisylyte.
Procaine Pyridostigmine may increase the neuromuscular blocking activities of Procaine.
Cocaine Pyridostigmine may increase the neuromuscular blocking activities of Cocaine.
Trimethaphan Pyridostigmine may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Pyridostigmine may increase the neuromuscular blocking activities of Doxacurium.
Chloroprocaine Pyridostigmine may increase the neuromuscular blocking activities of Chloroprocaine.
Tubocurarine Pyridostigmine may increase the neuromuscular blocking activities of Tubocurarine.
Aclidinium Pyridostigmine may increase the neuromuscular blocking activities of Aclidinium.
Clevidipine Pyridostigmine may increase the neuromuscular blocking activities of Clevidipine.
Mirabegron Pyridostigmine may increase the neuromuscular blocking activities of Mirabegron.
Propacetamol Pyridostigmine may increase the neuromuscular blocking activities of Propacetamol.
Butyrylthiocholine Pyridostigmine may increase the neuromuscular blocking activities of Butyrylthiocholine.
Oxybuprocaine Pyridostigmine may increase the neuromuscular blocking activities of Oxybuprocaine.
Benzonatate Pyridostigmine may increase the neuromuscular blocking activities of Benzonatate.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Pyridostigmine.
Tramadol The therapeutic efficacy of Tramadol can be decreased when used in combination with Pyridostigmine.
Trospium The therapeutic efficacy of Trospium can be decreased when used in combination with Pyridostigmine.
Oxyphenonium The therapeutic efficacy of Oxyphenonium can be decreased when used in combination with Pyridostigmine.
Butabarbital The therapeutic efficacy of Butabarbital can be decreased when used in combination with Pyridostigmine.
Butalbital The therapeutic efficacy of Butalbital can be decreased when used in combination with Pyridostigmine.
Benzatropine The therapeutic efficacy of Benzatropine can be decreased when used in combination with Pyridostigmine.
Ziprasidone The therapeutic efficacy of Ziprasidone can be decreased when used in combination with Pyridostigmine.
Disopyramide The therapeutic efficacy of Disopyramide can be decreased when used in combination with Pyridostigmine.
Talbutal The therapeutic efficacy of Talbutal can be decreased when used in combination with Pyridostigmine.
Pentobarbital The therapeutic efficacy of Pentobarbital can be decreased when used in combination with Pyridostigmine.
Ipratropium The therapeutic efficacy of Ipratropium can be decreased when used in combination with Pyridostigmine.
Methadone The therapeutic efficacy of Methadone can be decreased when used in combination with Pyridostigmine.
Olanzapine The therapeutic efficacy of Olanzapine can be decreased when used in combination with Pyridostigmine.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Pyridostigmine.
Buclizine The therapeutic efficacy of Buclizine can be decreased when used in combination with Pyridostigmine.
Clozapine The therapeutic efficacy of Clozapine can be decreased when used in combination with Pyridostigmine.
Doxylamine The therapeutic efficacy of Doxylamine can be decreased when used in combination with Pyridostigmine.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Pyridostigmine.
Oxyphencyclimine The therapeutic efficacy of Oxyphencyclimine can be decreased when used in combination with Pyridostigmine.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Pyridostigmine.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Pyridostigmine.
Secobarbital The therapeutic efficacy of Secobarbital can be decreased when used in combination with Pyridostigmine.
Promazine The therapeutic efficacy of Promazine can be decreased when used in combination with Pyridostigmine.
Hyoscyamine The therapeutic efficacy of Hyoscyamine can be decreased when used in combination with Pyridostigmine.
Cyproheptadine The therapeutic efficacy of Cyproheptadine can be decreased when used in combination with Pyridostigmine.
Methscopolamine bromide The therapeutic efficacy of Methscopolamine bromide can be decreased when used in combination with Pyridostigmine.
Metharbital The therapeutic efficacy of Metharbital can be decreased when used in combination with Pyridostigmine.
Fluoxetine The therapeutic efficacy of Fluoxetine can be decreased when used in combination with Pyridostigmine.
Chlorpromazine The therapeutic efficacy of Chlorpromazine can be decreased when used in combination with Pyridostigmine.
Tridihexethyl The therapeutic efficacy of Tridihexethyl can be decreased when used in combination with Pyridostigmine.
Triflupromazine The therapeutic efficacy of Triflupromazine can be decreased when used in combination with Pyridostigmine.
Dextromethorphan The therapeutic efficacy of Dextromethorphan can be decreased when used in combination with Pyridostigmine.
Anisotropine methylbromide The therapeutic efficacy of Anisotropine methylbromide can be decreased when used in combination with Pyridostigmine.
Amoxapine The therapeutic efficacy of Amoxapine can be decreased when used in combination with Pyridostigmine.
Atropine The therapeutic efficacy of Atropine can be decreased when used in combination with Pyridostigmine.
Thiopental The therapeutic efficacy of Thiopental can be decreased when used in combination with Pyridostigmine.
Nicardipine The therapeutic efficacy of Nicardipine can be decreased when used in combination with Pyridostigmine.
Mecamylamine The therapeutic efficacy of Mecamylamine can be decreased when used in combination with Pyridostigmine.
Pirenzepine The therapeutic efficacy of Pirenzepine can be decreased when used in combination with Pyridostigmine.
Paroxetine The therapeutic efficacy of Paroxetine can be decreased when used in combination with Pyridostigmine.
Homatropine methylbromide The therapeutic efficacy of Homatropine methylbromide can be decreased when used in combination with Pyridostigmine.
Scopolamine The therapeutic efficacy of Scopolamine can be decreased when used in combination with Pyridostigmine.
Isoflurane The therapeutic efficacy of Isoflurane can be decreased when used in combination with Pyridostigmine.
Benzquinamide The therapeutic efficacy of Benzquinamide can be decreased when used in combination with Pyridostigmine.
Clidinium The therapeutic efficacy of Clidinium can be decreased when used in combination with Pyridostigmine.
Propiomazine The therapeutic efficacy of Propiomazine can be decreased when used in combination with Pyridostigmine.
Propantheline The therapeutic efficacy of Propantheline can be decreased when used in combination with Pyridostigmine.
Primidone The therapeutic efficacy of Primidone can be decreased when used in combination with Pyridostigmine.
Dicyclomine The therapeutic efficacy of Dicyclomine can be decreased when used in combination with Pyridostigmine.
Biperiden The therapeutic efficacy of Biperiden can be decreased when used in combination with Pyridostigmine.
Brompheniramine The therapeutic efficacy of Brompheniramine can be decreased when used in combination with Pyridostigmine.
Methylphenobarbital The therapeutic efficacy of Methylphenobarbital can be decreased when used in combination with Pyridostigmine.
Amantadine The therapeutic efficacy of Amantadine can be decreased when used in combination with Pyridostigmine.
Maprotiline The therapeutic efficacy of Maprotiline can be decreased when used in combination with Pyridostigmine.
Methantheline The therapeutic efficacy of Methantheline can be decreased when used in combination with Pyridostigmine.
Hexafluronium The therapeutic efficacy of Hexafluronium can be decreased when used in combination with Pyridostigmine.
Cycrimine The therapeutic efficacy of Cycrimine can be decreased when used in combination with Pyridostigmine.
Desloratadine The therapeutic efficacy of Desloratadine can be decreased when used in combination with Pyridostigmine.
Glycopyrronium The therapeutic efficacy of Glycopyrronium can be decreased when used in combination with Pyridostigmine.
Tolterodine The therapeutic efficacy of Tolterodine can be decreased when used in combination with Pyridostigmine.
Oxybutynin The therapeutic efficacy of Oxybutynin can be decreased when used in combination with Pyridostigmine.
Promethazine The therapeutic efficacy of Promethazine can be decreased when used in combination with Pyridostigmine.
Diphenhydramine The therapeutic efficacy of Diphenhydramine can be decreased when used in combination with Pyridostigmine.
Pentolinium The therapeutic efficacy of Pentolinium can be decreased when used in combination with Pyridostigmine.
Flavoxate The therapeutic efficacy of Flavoxate can be decreased when used in combination with Pyridostigmine.
Desipramine The therapeutic efficacy of Desipramine can be decreased when used in combination with Pyridostigmine.
Orphenadrine The therapeutic efficacy of Orphenadrine can be decreased when used in combination with Pyridostigmine.
Phenobarbital The therapeutic efficacy of Phenobarbital can be decreased when used in combination with Pyridostigmine.
Escitalopram The therapeutic efficacy of Escitalopram can be decreased when used in combination with Pyridostigmine.
Diphenidol The therapeutic efficacy of Diphenidol can be decreased when used in combination with Pyridostigmine.
Chlorprothixene The therapeutic efficacy of Chlorprothixene can be decreased when used in combination with Pyridostigmine.
Fenoterol The therapeutic efficacy of Fenoterol can be decreased when used in combination with Pyridostigmine.
Amobarbital The therapeutic efficacy of Amobarbital can be decreased when used in combination with Pyridostigmine.
Aprobarbital The therapeutic efficacy of Aprobarbital can be decreased when used in combination with Pyridostigmine.
Butobarbital The therapeutic efficacy of Butobarbital can be decreased when used in combination with Pyridostigmine.
Heptabarbital The therapeutic efficacy of Heptabarbital can be decreased when used in combination with Pyridostigmine.
Hexobarbital The therapeutic efficacy of Hexobarbital can be decreased when used in combination with Pyridostigmine.
Methotrimeprazine The therapeutic efficacy of Methotrimeprazine can be decreased when used in combination with Pyridostigmine.
Tiotropium The therapeutic efficacy of Tiotropium can be decreased when used in combination with Pyridostigmine.
Barbital The therapeutic efficacy of Barbital can be decreased when used in combination with Pyridostigmine.

Target Protein

Coagulation factor X F10
Cholinesterase BCHE
Acetylcholinesterase ACHE

Referensi & Sumber

Synthesis reference: Gennaro, A.R., ed. (1990) Remington's Pharmaceutical Sciences, 18th ed., Easton, PA, Mack Publishing Co., p. 898.
Artikel (PubMed)
  • PMID: 12933939
    Singer W, Opfer-Gehrking TL, McPhee BR, Hilz MJ, Bharucha AE, Low PA: Acetylcholinesterase inhibition: a novel approach in the treatment of neurogenic orthostatic hypotension. J Neurol Neurosurg Psychiatry. 2003 Sep;74(9):1294-8.
  • PMID: 26376969
    Gilhus NE, Verschuuren JJ: Myasthenia gravis: subgroup classification and therapeutic strategies. Lancet Neurol. 2015 Oct;14(10):1023-36. doi: 10.1016/S1474-4422(15)00145-3.
  • PMID: 29874875
    Rodriguez Cruz PM, Palace J, Beeson D: The Neuromuscular Junction and Wide Heterogeneity of Congenital Myasthenic Syndromes. Int J Mol Sci. 2018 Jun 5;19(6). pii: ijms19061677. doi: 10.3390/ijms19061677.
  • PMID: 29381222
    Lee M, Beeson D, Palace J: Therapeutic strategies for congenital myasthenic syndromes. Ann N Y Acad Sci. 2018 Jan;1412(1):129-136. doi: 10.1111/nyas.13538.
  • PMID: 3524957
    Aquilonius SM, Hartvig P: Clinical pharmacokinetics of cholinesterase inhibitors. Clin Pharmacokinet. 1986 May-Jun;11(3):236-49. doi: 10.2165/00003088-198611030-00005.
  • PMID: 7439266
    Aquilonius SM, Eckernas SA, Hartvig P, Lindstrom B, Osterman PO: Pharmacokinetics and oral bioavailability of pyridostigmine in man. Eur J Clin Pharmacol. 1980 Nov;18(5):423-8. doi: 10.1007/BF00636797.
  • PMID: 5463535
    Kornfeld P, Samuels AJ, Wolf RL, Osserman KE: Metabolism of 14C-labeled pyridostigmine in myasthenia gravis. Evidence for multiple metabolites. Neurology. 1970 Jul;20(7):634-41. doi: 10.1212/wnl.20.7.634.
  • PMID: 4554662
    Somani SM, Roberts JB, Wilson A: Pyridostigmine metabolism in man. Clin Pharmacol Ther. 1972 May-Jun;13(3):393-9. doi: 10.1002/cpt1972133393.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 49 • International brands: 12
Produk
  • Jamp Pyridostigmine Bromide
    Tablet • 60 mg • Oral • Canada • Generic • Approved
  • Mestinon
    Solution • 60 mg/5mL • Oral • US • Approved
  • Mestinon
    Tablet • 60 mg/1 • Oral • US • Approved
  • Mestinon
    Tablet, extended release • 180 mg/1 • Oral • US • Approved
  • Mestinon
    Tablet • 60 mg • Oral • Canada • Approved
  • Mestinon-SR
    Tablet, extended release • 180 mg • Oral • Canada • Approved
  • Pryidostigmine Bromide
    Solution • 60 mg/5mL • Oral • US • Generic • Approved
  • Pryidostigmine Bromide
    Solution • 60 mg/5mL • Oral • US • Generic • Approved
Menampilkan 8 dari 49 produk.
International Brands
  • Amiasten — AC Farma
  • Amygra — Tabros
  • Antilon — Yuan Chou
  • Astinon — Samarth
  • Kalymin — Arzneimittelwerk Dresden
  • Kalymin forte — Temmler
  • Kalymin N — Temmler
  • Kalymin retard — Temmler
  • Meshanon60 — Hasan
  • Mestinon retard — Meda

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