Peringatan Keamanan

Symptoms of overdose are expected to be similar to those of cholinomimetics, which involve the central nervous system, the parasympathetic nervous system, and the neuromuscular junction.L51534 Effects of a cholinergic crisis include severe nausea, vomiting, gastrointestinal cramping, salivation, lacrimation, urination, defecation, sweating, bradycardia, hypotension, respiratory depression, collapse, and convulsions. Muscle weakness or fasciculations may also occur, with respiratory muscle weakness having the potential to bring fatal results. In one patient who consumed an oral daily dose of 32 mg developed bradycardia, QT prolongation, ventricular tachycardia and torsades de pointes accompanied by a brief loss of consciousness. In one patient with a history of hallucinations who consumed a daily dose of 24 mg galantamine, hallucinations requiring hospitalization occurred. A patient who ingested 160 mg of galantamine from an oral solution developed sweating, vomiting, bradycardia, and near-syncope one hour following consumption.L51534

As in any case of overdose, general supportive measures should be initiated. Tertiary anticholinergics such as intravenous atropine may be used to reverse the cholinergic effects of galantamine. The recommended initial dose of atropine intravenously administered for galantamine overdose ranges from 0.5 to 1.0 mg. It is not known whether galantamine can be removed by dialysis.L51534

Benzgalantamine

DB19353

small molecule approved

Deskripsi

Benzgalantamine is a prodrug of galantamine. Gastrointestinal adverse effects are the most frequently reported side effects in patients undergoing treatment with cholinesterase inhibitors, including galantamine, and are often a reason for treatment discontinuation.A264454 As a prodrug, benzagalantamine remains inert as it passes through the stomach, thereby avoiding many of the gastrointestinal effects associated with peripheral cholinesterase inhibition.L51564

Benzgalantamine was approved by the FDA in July 2024 for the treatment of mild-to-moderate dementia in Alzheimer's patients.L51534,L51564

Struktur Molekul 2D

Berat 391.467
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Benzgalantamine is rapidly converted to the active moiety galantamine following absorption in the intestines, with systemic benzgalantamine exposure representing <1% that of galantamine.L51534 See galantamine for detailed information regarding pharmacokinetic parameters.

Metabolisme

Following conversion to galantamine, CYP3A4 and CYP2D6 are the major enzymes responsible for galantamine's metabolism.L51534 CYP2D6 is involved in the formation of O-desmethyl-galantamine, whereas CYP3A4 mediates the formation of galantamine-N-oxide.L51534 Galantamine is also glucuronidated and excreted unchanged in urine.L51534

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. The co-administration of benzgalantamine with alcohol may result in dose dumping, although this risk has not been fully characterized in humans.
  • 2. Take with or without food. Administration with food does not alter pharmacokinetics to a clinically relevant extent.

Interaksi Obat

392 Data
Ceritinib Benzgalantamine may increase the bradycardic activities of Ceritinib.
Ivabradine Benzgalantamine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Benzgalantamine.
Dipyridamole The therapeutic efficacy of Benzgalantamine can be decreased when used in combination with Dipyridamole.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Benzgalantamine.
Procaine Benzgalantamine may increase the neuromuscular blocking activities of Procaine.
Benzonatate Benzgalantamine may increase the neuromuscular blocking activities of Benzonatate.
Oxybuprocaine Benzgalantamine may increase the neuromuscular blocking activities of Oxybuprocaine.
Cocaine Benzgalantamine may increase the neuromuscular blocking activities of Cocaine.
Trimethaphan Benzgalantamine may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Benzgalantamine may increase the neuromuscular blocking activities of Doxacurium.
Chloroprocaine Benzgalantamine may increase the neuromuscular blocking activities of Chloroprocaine.
Tubocurarine Benzgalantamine may increase the neuromuscular blocking activities of Tubocurarine.
Ephedrine Benzgalantamine may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Benzgalantamine may increase the neuromuscular blocking activities of Bambuterol.
Butyrylthiocholine Benzgalantamine may increase the neuromuscular blocking activities of Butyrylthiocholine.
Clevidipine Benzgalantamine may increase the neuromuscular blocking activities of Clevidipine.
Sar9, Met (O2)11-Substance P Benzgalantamine may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Isavuconazonium Benzgalantamine may increase the neuromuscular blocking activities of Isavuconazonium.
Mirabegron Benzgalantamine may increase the neuromuscular blocking activities of Mirabegron.
Aclidinium Benzgalantamine may increase the neuromuscular blocking activities of Aclidinium.
Moxisylyte Benzgalantamine may increase the neuromuscular blocking activities of Moxisylyte.
Propacetamol Benzgalantamine may increase the neuromuscular blocking activities of Propacetamol.
Tramadol The therapeutic efficacy of Tramadol can be decreased when used in combination with Benzgalantamine.
Trospium The therapeutic efficacy of Trospium can be decreased when used in combination with Benzgalantamine.
Oxyphenonium The therapeutic efficacy of Oxyphenonium can be decreased when used in combination with Benzgalantamine.
Butabarbital The therapeutic efficacy of Butabarbital can be decreased when used in combination with Benzgalantamine.
Butalbital The therapeutic efficacy of Butalbital can be decreased when used in combination with Benzgalantamine.
Benzatropine The therapeutic efficacy of Benzatropine can be decreased when used in combination with Benzgalantamine.
Ziprasidone The therapeutic efficacy of Ziprasidone can be decreased when used in combination with Benzgalantamine.
Disopyramide The therapeutic efficacy of Disopyramide can be decreased when used in combination with Benzgalantamine.
Talbutal The therapeutic efficacy of Talbutal can be decreased when used in combination with Benzgalantamine.
Pentobarbital The therapeutic efficacy of Pentobarbital can be decreased when used in combination with Benzgalantamine.
Amitriptyline The therapeutic efficacy of Amitriptyline can be decreased when used in combination with Benzgalantamine.
Ipratropium The therapeutic efficacy of Ipratropium can be decreased when used in combination with Benzgalantamine.
Methadone The therapeutic efficacy of Methadone can be decreased when used in combination with Benzgalantamine.
Olanzapine The therapeutic efficacy of Olanzapine can be decreased when used in combination with Benzgalantamine.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Benzgalantamine.
Terfenadine The therapeutic efficacy of Terfenadine can be decreased when used in combination with Benzgalantamine.
Buclizine The therapeutic efficacy of Buclizine can be decreased when used in combination with Benzgalantamine.
Clozapine The therapeutic efficacy of Clozapine can be decreased when used in combination with Benzgalantamine.
Doxylamine The therapeutic efficacy of Doxylamine can be decreased when used in combination with Benzgalantamine.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Benzgalantamine.
Oxyphencyclimine The therapeutic efficacy of Oxyphencyclimine can be decreased when used in combination with Benzgalantamine.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Benzgalantamine.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Benzgalantamine.
Metocurine iodide The therapeutic efficacy of Metocurine iodide can be decreased when used in combination with Benzgalantamine.
Secobarbital The therapeutic efficacy of Secobarbital can be decreased when used in combination with Benzgalantamine.
Promazine The therapeutic efficacy of Promazine can be decreased when used in combination with Benzgalantamine.
Hyoscyamine The therapeutic efficacy of Hyoscyamine can be decreased when used in combination with Benzgalantamine.
Cyproheptadine The therapeutic efficacy of Cyproheptadine can be decreased when used in combination with Benzgalantamine.
Imipramine The therapeutic efficacy of Imipramine can be decreased when used in combination with Benzgalantamine.
Methscopolamine bromide The therapeutic efficacy of Methscopolamine bromide can be decreased when used in combination with Benzgalantamine.
Metharbital The therapeutic efficacy of Metharbital can be decreased when used in combination with Benzgalantamine.
Fluoxetine The therapeutic efficacy of Fluoxetine can be decreased when used in combination with Benzgalantamine.
Chlorpromazine The therapeutic efficacy of Chlorpromazine can be decreased when used in combination with Benzgalantamine.
Gallamine triethiodide The therapeutic efficacy of Gallamine triethiodide can be decreased when used in combination with Benzgalantamine.
Darifenacin The therapeutic efficacy of Darifenacin can be decreased when used in combination with Benzgalantamine.
Tridihexethyl The therapeutic efficacy of Tridihexethyl can be decreased when used in combination with Benzgalantamine.
Triflupromazine The therapeutic efficacy of Triflupromazine can be decreased when used in combination with Benzgalantamine.
Dextromethorphan The therapeutic efficacy of Dextromethorphan can be decreased when used in combination with Benzgalantamine.
Anisotropine methylbromide The therapeutic efficacy of Anisotropine methylbromide can be decreased when used in combination with Benzgalantamine.
Nortriptyline The therapeutic efficacy of Nortriptyline can be decreased when used in combination with Benzgalantamine.
Amoxapine The therapeutic efficacy of Amoxapine can be decreased when used in combination with Benzgalantamine.
Cisatracurium The therapeutic efficacy of Cisatracurium can be decreased when used in combination with Benzgalantamine.
Atropine The therapeutic efficacy of Atropine can be decreased when used in combination with Benzgalantamine.
Thiopental The therapeutic efficacy of Thiopental can be decreased when used in combination with Benzgalantamine.
Nicardipine The therapeutic efficacy of Nicardipine can be decreased when used in combination with Benzgalantamine.
Mecamylamine The therapeutic efficacy of Mecamylamine can be decreased when used in combination with Benzgalantamine.
Pirenzepine The therapeutic efficacy of Pirenzepine can be decreased when used in combination with Benzgalantamine.
Paroxetine The therapeutic efficacy of Paroxetine can be decreased when used in combination with Benzgalantamine.
Azatadine The therapeutic efficacy of Azatadine can be decreased when used in combination with Benzgalantamine.
Homatropine methylbromide The therapeutic efficacy of Homatropine methylbromide can be decreased when used in combination with Benzgalantamine.
Rocuronium The therapeutic efficacy of Rocuronium can be decreased when used in combination with Benzgalantamine.
Atracurium besylate The therapeutic efficacy of Atracurium besylate can be decreased when used in combination with Benzgalantamine.
Meclizine The therapeutic efficacy of Meclizine can be decreased when used in combination with Benzgalantamine.
Scopolamine The therapeutic efficacy of Scopolamine can be decreased when used in combination with Benzgalantamine.
Isoflurane The therapeutic efficacy of Isoflurane can be decreased when used in combination with Benzgalantamine.
Benzquinamide The therapeutic efficacy of Benzquinamide can be decreased when used in combination with Benzgalantamine.
Clidinium The therapeutic efficacy of Clidinium can be decreased when used in combination with Benzgalantamine.
Propiomazine The therapeutic efficacy of Propiomazine can be decreased when used in combination with Benzgalantamine.
Propantheline The therapeutic efficacy of Propantheline can be decreased when used in combination with Benzgalantamine.
Primidone The therapeutic efficacy of Primidone can be decreased when used in combination with Benzgalantamine.
Dicyclomine The therapeutic efficacy of Dicyclomine can be decreased when used in combination with Benzgalantamine.
Biperiden The therapeutic efficacy of Biperiden can be decreased when used in combination with Benzgalantamine.
Brompheniramine The therapeutic efficacy of Brompheniramine can be decreased when used in combination with Benzgalantamine.
Methylphenobarbital The therapeutic efficacy of Methylphenobarbital can be decreased when used in combination with Benzgalantamine.
Quinidine The therapeutic efficacy of Quinidine can be decreased when used in combination with Benzgalantamine.
Amantadine The therapeutic efficacy of Amantadine can be decreased when used in combination with Benzgalantamine.
Maprotiline The therapeutic efficacy of Maprotiline can be decreased when used in combination with Benzgalantamine.
Methantheline The therapeutic efficacy of Methantheline can be decreased when used in combination with Benzgalantamine.
Hexafluronium The therapeutic efficacy of Hexafluronium can be decreased when used in combination with Benzgalantamine.
Cycrimine The therapeutic efficacy of Cycrimine can be decreased when used in combination with Benzgalantamine.
Desloratadine The therapeutic efficacy of Desloratadine can be decreased when used in combination with Benzgalantamine.
Glycopyrronium The therapeutic efficacy of Glycopyrronium can be decreased when used in combination with Benzgalantamine.
Tolterodine The therapeutic efficacy of Tolterodine can be decreased when used in combination with Benzgalantamine.
Oxybutynin The therapeutic efficacy of Oxybutynin can be decreased when used in combination with Benzgalantamine.
Promethazine The therapeutic efficacy of Promethazine can be decreased when used in combination with Benzgalantamine.
Diphenhydramine The therapeutic efficacy of Diphenhydramine can be decreased when used in combination with Benzgalantamine.
Pentolinium The therapeutic efficacy of Pentolinium can be decreased when used in combination with Benzgalantamine.

Target Protein

Acetylcholinesterase ACHE
Cholinesterase BCHE
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
Muscle nicotinic acetylcholine receptor

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29067291
    Baakman AC, 't Hart E, Kay DG, Stevens J, Klaassen ES, Maelicke A, Groeneveld GJ: First in human study with a prodrug of galantamine: Improved benefit-risk ratio? Alzheimers Dement (N Y). 2016 Jan 20;2(1):13-22. doi: 10.1016/j.trci.2015.12.003. eCollection 2016 Jan.
  • PMID: 33083515
    Bakker C, van der Aart J, Hart EP, Klaassen ES, Bergmann KR, van Esdonk MJ, Kay DG, Groeneveld GJ: Safety, pharmacokinetics, and pharmacodynamics of Gln-1062, a prodrug of galantamine. Alzheimers Dement (N Y). 2020 Oct 13;6(1):e12093. doi: 10.1002/trc2.12093. eCollection 2020.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Zunveyl
    Tablet, delayed release • 5 mg/1 • Oral • US • Approved
  • Zunveyl
    Tablet, delayed release • 10 mg/1 • Oral • US • Approved
  • Zunveyl
    Tablet, delayed release • 15 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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