Peringatan Keamanan

The oral LD50 of the active ingredient, galantamine hydrobromide, in rats is 75 mg/kg.L13709 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. 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.L13571

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.L13571

Galantamine

DB00674

small molecule approved

Deskripsi

Galantamine is a tertiary alkaloid and reversible, competitive inhibitor of the acetylcholinesterase (AChE) enzyme, which is a widely studied therapeutic target used in the treatment of Alzheimer's disease.A1018 First characterized in the early 1950s, galantamine is a tertiary alkaloid that was extracted from botanical sources, such as Galanthus nivalis.A201968 Galantamine was first studied in paralytic and neuropathic conditions, such as myopathies and postpolio paralytic conditions, and for reversal of neuromuscular blockade.A182993,A201968 Following the discovery of its AChE-inhibiting properties, the cognitive effects of galantamine were studied in a wide variety of psychiatric disorders such as mild cognitive impairment, cognitive impairment in schizophrenia and bipolar disorder, and autism; however, re-development of the drug for Alzheimer’s disease did not commence until the early 1990s due to difficulties in extraction and synthesis.A201968 Galantamine blocks the breakdown of acetylcholine in the synaptic cleft, thereby increasing acetylcholine neurotransmission. It also acts as an allosteric modulator of the nicotinic receptor, giving its dual mechanism of action clinical significance.A182993

The drug was approved by the FDA in 2001 for the treatment of mild to moderate dementia of the Alzheimer's type. As Alzheimer's disease is a progressive neurodegenerative disorder, galantamine is not known to alter the course of the underlying dementing process. Galantamine works to block the enzyme responsible for the breakdown of acetylcholine in the synaptic cleft, thereby enhancing cholinergic neuron function and signalling. Under this hypothesized mechanism of action, the therapeutic effects of galantamine may decrease as the disease progression advances and fewer cholinergic neurons remain functionally intact.L13571 It is therefore not considered to be a disease-modifying drug.A203558 Galantamine is marketed under the brand name Razadyne, and is available as oral immediate- and extended-release tablets and solution.L13571

Struktur Molekul 2D

Berat 287.3535
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Galantamine has a terminal half-life of about 7 hours.[L13571]
Volume Distribusi The mean volume of distribution is 175 L. About 52.7% of galantamine is distributed to blood cells, the blood to plasma concentration ratio of galantamine is 1.2.[L13571] Galantamine penetrates the blood–brain barrier.[A201968]
Klirens (Clearance) The renal clearance is 65 mL/min and the total plasma clearance is about 300 mL/min.[A182993]

Absorpsi

Over a dose range of 8-32 mg/day, galantamine exhibits a dose-linear pharmacokinetic profile. The oral bioavailability of galantamine ranges from 90-100%. Following oral administration, the Tmax is about 1 hour.L13571 Following 10 hours of administration, the mean galantamine plasma concentrations were 82–97 µg/L for the 24 mg/day dose and 114–126 µg/L for the 32 mg/day dose.A182993

Metabolisme

In vitro study findings suggest that about 75% of the drug is metabolized by CYP2D6 and CYP3A4. CYP2D6 promotes O-demethylation of the drug to form O-desmethyl-galantamine and the CYP3A4-mediated pathway forms the galantamine-N-oxide.A182993 Important metabolic pathways also include N-demethylation, epimerization, and sulfate conjugation.A203444 Other metabolites include norgalantamine, O-desmethyl-galantamine, O-desmethyl-norgalantamine, epigalantamine and galantaminone, which do not retain clinically significant pharmacology activities.A1022 Galantamine can also undergo glucuronidation: in one oral radiolabeled drug study in poor and extensive CYP2D6 metabolizers, about 14-24% of the total radioactivity was identified as galantamine glucuronide 8 hours post-dose. O-demethylation by CYP2D6 becomes prominent in patients with who are extensive metabolizers of CYP2D6, but unchanged galatamine (39-77%) and its glucuronide metabolite (14-24%) predominated in the plasma of both poor and extensive metabolizers of CYP2D6 in a radiolabelled drug study.L13571 The total plasma clearance, or nonrenal clearnace, accounts for 20–25% of drug elimination.A182993

Rute Eliminasi

Renal clearance accounts for about 20–25% of total plasma clearance of the drug in healthy individuals: the elimination of galantamine has been shown to be decreased in subjects with renal impairment.A1022 Following oral or intravenous administration, approximately 20% of the dose is excreted as unchanged in the urine within 24 h.A182993 In a radiolabelled drug study, about 95% and 5% of the total radioactivity was recovered in the urine and feces, respectively. Of the dose recovered in the urine, about 32% was in the unchanged parent compound, and 12% was in the glucuronide form.L13571

Interaksi Makanan

1 Data
  • 1. Take with food. Food delays the rate of absorption but not the extent.

Interaksi Obat

892 Data
Ceritinib Galantamine may increase the bradycardic activities of Ceritinib.
Ivabradine Galantamine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Galantamine.
Dipyridamole The therapeutic efficacy of Galantamine can be decreased when used in combination with Dipyridamole.
Ephedrine Galantamine may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Galantamine may increase the neuromuscular blocking activities of Bambuterol.
Sar9, Met (O2)11-Substance P Galantamine may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Procaine Galantamine may increase the neuromuscular blocking activities of Procaine.
Cocaine Galantamine may increase the neuromuscular blocking activities of Cocaine.
Trimethaphan Galantamine may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Galantamine may increase the neuromuscular blocking activities of Doxacurium.
Chloroprocaine Galantamine may increase the neuromuscular blocking activities of Chloroprocaine.
Tubocurarine Galantamine may increase the neuromuscular blocking activities of Tubocurarine.
Aclidinium Galantamine may increase the neuromuscular blocking activities of Aclidinium.
Clevidipine Galantamine may increase the neuromuscular blocking activities of Clevidipine.
Moxisylyte Galantamine may increase the neuromuscular blocking activities of Moxisylyte.
Butyrylthiocholine Galantamine may increase the neuromuscular blocking activities of Butyrylthiocholine.
Propacetamol Galantamine may increase the neuromuscular blocking activities of Propacetamol.
Oxybuprocaine Galantamine may increase the neuromuscular blocking activities of Oxybuprocaine.
Benzonatate Galantamine may increase the neuromuscular blocking activities of Benzonatate.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Galantamine.
Mirabegron The serum concentration of Galantamine can be increased when it is combined with Mirabegron.
Tramadol The therapeutic efficacy of Tramadol can be decreased when used in combination with Galantamine.
Trospium The therapeutic efficacy of Trospium can be decreased when used in combination with Galantamine.
Oxyphenonium The therapeutic efficacy of Oxyphenonium can be decreased when used in combination with Galantamine.
Butabarbital The therapeutic efficacy of Butabarbital can be decreased when used in combination with Galantamine.
Butalbital The therapeutic efficacy of Butalbital can be decreased when used in combination with Galantamine.
Talbutal The therapeutic efficacy of Talbutal can be decreased when used in combination with Galantamine.
Ipratropium The therapeutic efficacy of Ipratropium can be decreased when used in combination with Galantamine.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Galantamine.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Galantamine.
Oxyphencyclimine The therapeutic efficacy of Oxyphencyclimine can be decreased when used in combination with Galantamine.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Galantamine.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Galantamine.
Secobarbital The therapeutic efficacy of Secobarbital can be decreased when used in combination with Galantamine.
Methscopolamine bromide The therapeutic efficacy of Methscopolamine bromide can be decreased when used in combination with Galantamine.
Metharbital The therapeutic efficacy of Metharbital can be decreased when used in combination with Galantamine.
Tridihexethyl The therapeutic efficacy of Tridihexethyl can be decreased when used in combination with Galantamine.
Triflupromazine The therapeutic efficacy of Triflupromazine can be decreased when used in combination with Galantamine.
Dextromethorphan The therapeutic efficacy of Dextromethorphan can be decreased when used in combination with Galantamine.
Anisotropine methylbromide The therapeutic efficacy of Anisotropine methylbromide can be decreased when used in combination with Galantamine.
Thiopental The therapeutic efficacy of Thiopental can be decreased when used in combination with Galantamine.
Mecamylamine The therapeutic efficacy of Mecamylamine can be decreased when used in combination with Galantamine.
Pirenzepine The therapeutic efficacy of Pirenzepine can be decreased when used in combination with Galantamine.
Homatropine methylbromide The therapeutic efficacy of Homatropine methylbromide can be decreased when used in combination with Galantamine.
Scopolamine The therapeutic efficacy of Scopolamine can be decreased when used in combination with Galantamine.
Benzquinamide The therapeutic efficacy of Benzquinamide can be decreased when used in combination with Galantamine.
Clidinium The therapeutic efficacy of Clidinium can be decreased when used in combination with Galantamine.
Propiomazine The therapeutic efficacy of Propiomazine can be decreased when used in combination with Galantamine.
Propantheline The therapeutic efficacy of Propantheline can be decreased when used in combination with Galantamine.
Dicyclomine The therapeutic efficacy of Dicyclomine can be decreased when used in combination with Galantamine.
Methylphenobarbital The therapeutic efficacy of Methylphenobarbital can be decreased when used in combination with Galantamine.
Methantheline The therapeutic efficacy of Methantheline can be decreased when used in combination with Galantamine.
Hexafluronium The therapeutic efficacy of Hexafluronium can be decreased when used in combination with Galantamine.
Cycrimine The therapeutic efficacy of Cycrimine can be decreased when used in combination with Galantamine.
Glycopyrronium The therapeutic efficacy of Glycopyrronium can be decreased when used in combination with Galantamine.
Pentolinium The therapeutic efficacy of Pentolinium can be decreased when used in combination with Galantamine.
Flavoxate The therapeutic efficacy of Flavoxate can be decreased when used in combination with Galantamine.
Diphenidol The therapeutic efficacy of Diphenidol can be decreased when used in combination with Galantamine.
Fenoterol The therapeutic efficacy of Fenoterol can be decreased when used in combination with Galantamine.
Amobarbital The therapeutic efficacy of Amobarbital can be decreased when used in combination with Galantamine.
Aprobarbital The therapeutic efficacy of Aprobarbital can be decreased when used in combination with Galantamine.
Butobarbital The therapeutic efficacy of Butobarbital can be decreased when used in combination with Galantamine.
Heptabarbital The therapeutic efficacy of Heptabarbital can be decreased when used in combination with Galantamine.
Hexobarbital The therapeutic efficacy of Hexobarbital can be decreased when used in combination with Galantamine.
Tiotropium The therapeutic efficacy of Tiotropium can be decreased when used in combination with Galantamine.
Barbital The therapeutic efficacy of Barbital can be decreased when used in combination with Galantamine.
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione The therapeutic efficacy of Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione can be decreased when used in combination with Galantamine.
Isopropamide The therapeutic efficacy of Isopropamide can be decreased when used in combination with Galantamine.
Mepenzolate The therapeutic efficacy of Mepenzolate can be decreased when used in combination with Galantamine.
Gantacurium The therapeutic efficacy of Gantacurium can be decreased when used in combination with Galantamine.
Pizotifen The therapeutic efficacy of Pizotifen can be decreased when used in combination with Galantamine.
Fesoterodine The therapeutic efficacy of Fesoterodine can be decreased when used in combination with Galantamine.
Hexocyclium The therapeutic efficacy of Hexocyclium can be decreased when used in combination with Galantamine.
Dimetindene The therapeutic efficacy of Dimetindene can be decreased when used in combination with Galantamine.
Agmatine The therapeutic efficacy of Agmatine can be decreased when used in combination with Galantamine.
Hexamethonium The therapeutic efficacy of Hexamethonium can be decreased when used in combination with Galantamine.
Dexetimide The therapeutic efficacy of Dexetimide can be decreased when used in combination with Galantamine.
Benactyzine The therapeutic efficacy of Benactyzine can be decreased when used in combination with Galantamine.
Umeclidinium The therapeutic efficacy of Umeclidinium can be decreased when used in combination with Galantamine.
Imidafenacin The therapeutic efficacy of Imidafenacin can be decreased when used in combination with Galantamine.
Butylscopolamine The therapeutic efficacy of Butylscopolamine can be decreased when used in combination with Galantamine.
Thonzylamine The therapeutic efficacy of Thonzylamine can be decreased when used in combination with Galantamine.
Methscopolamine The therapeutic efficacy of Methscopolamine can be decreased when used in combination with Galantamine.
Revefenacin The therapeutic efficacy of Revefenacin can be decreased when used in combination with Galantamine.
Oxitropium The therapeutic efficacy of Oxitropium can be decreased when used in combination with Galantamine.
Propiverine The therapeutic efficacy of Propiverine can be decreased when used in combination with Galantamine.
Batefenterol The therapeutic efficacy of Batefenterol can be decreased when used in combination with Galantamine.
Mebeverine The therapeutic efficacy of Mebeverine can be decreased when used in combination with Galantamine.
Tropatepine The therapeutic efficacy of Tropatepine can be decreased when used in combination with Galantamine.
Prifinium The therapeutic efficacy of Prifinium can be decreased when used in combination with Galantamine.
Piperidolate The therapeutic efficacy of Piperidolate can be decreased when used in combination with Galantamine.
Benzilone The therapeutic efficacy of Benzilone can be decreased when used in combination with Galantamine.
Difemerine The therapeutic efficacy of Difemerine can be decreased when used in combination with Galantamine.
Phenglutarimide The therapeutic efficacy of Phenglutarimide can be decreased when used in combination with Galantamine.
Mazaticol The therapeutic efficacy of Mazaticol can be decreased when used in combination with Galantamine.
Etybenzatropine The therapeutic efficacy of Etybenzatropine can be decreased when used in combination with Galantamine.
Emepronium The therapeutic efficacy of Emepronium can be decreased when used in combination with Galantamine.
Poldine The therapeutic efficacy of Poldine can be decreased when used in combination with Galantamine.
Bevonium The therapeutic efficacy of Bevonium can be decreased when used in combination with Galantamine.

Target Protein

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

Referensi & Sumber

Synthesis reference: Vijaya Bolugoddu, Sanjay Shukla, Mukunda Jambula, Rajeshwar Sagyam, Ramchandra Pingili, Ananda Thirunavakarasu, "Preparation of (-)-galantamine hydrobromide." U.S. Patent US20060009640, issued January 12, 2006.
Artikel (PubMed)
  • PMID: 11129124
    Scott LJ, Goa KL: Galantamine: a review of its use in Alzheimer's disease. Drugs. 2000 Nov;60(5):1095-122.
  • PMID: 10606746
    Greenblatt HM, Kryger G, Lewis T, Silman I, Sussman JL: Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution. FEBS Lett. 1999 Dec 17;463(3):321-6.
  • PMID: 12177686
    Lilienfeld S: Galantamine--a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer's disease. CNS Drug Rev. 2002 Summer;8(2):159-76.
  • PMID: 12137632
    Olin J, Schneider L: Galantamine for Alzheimer's disease. Cochrane Database Syst Rev. 2002;(3):CD001747.
  • PMID: 28031923
    Mucke HA: The case of galantamine: repurposing and late blooming of a cholinergic drug. Future Sci OA. 2015 Sep 3;1(4):FSO73. doi: 10.4155/fso.15.73. eCollection 2015 Nov.
  • PMID: 11950787
    Mannens GS, Snel CA, Hendrickx J, Verhaeghe T, Le Jeune L, Bode W, van Beijsterveldt L, Lavrijsen K, Leempoels J, Van Osselaer N, Van Peer A, Meuldermans W: The metabolism and excretion of galantamine in rats, dogs, and humans. Drug Metab Dispos. 2002 May;30(5):553-63. doi: 10.1124/dmd.30.5.553.
  • PMID: 14674789
    Farlow MR: Clinical pharmacokinetics of galantamine. Clin Pharmacokinet. 2003;42(15):1383-92. doi: 10.2165/00003088-200342150-00005.
  • PMID: 26813123
    Ferreira-Vieira TH, Guimaraes IM, Silva FR, Ribeiro FM: Alzheimer's disease: Targeting the Cholinergic System. Curr Neuropharmacol. 2016;14(1):101-15. doi: 10.2174/1570159x13666150716165726.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 149 • International brands: 3
Produk
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International Brands
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