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Degenerative Diseases of the Nervous System
Published in Philip B. Gorelick, Fernando D. Testai, Graeme J. Hankey, Joanna M. Wardlaw, Hankey's Clinical Neurology, 2020
James A. Mastrianni, Elizabeth A. Harris
Galantamine reversibly and competitively inhibits acetylcholinesterase and enhances the response of nicotinic receptors to acetylcholine.12 Galantamine is available in 4 mg and 8 mg, with a liquid preparation (4 mg/mL), which is useful for titration. The dose can be titrated from 4 mg twice daily to 8 mg twice daily over 4 weeks according to tolerance and benefit, but patients with hepatic impairment should be started with 4 mg daily. Galantamine is contraindicated in patients with severe renal impairment, but no dose adjustment is required for mild to moderate renal impairment (creatinine clearance rate > 9 mL/min). Most adverse effects occur in the first 4 weeks, including nausea, vomiting, diarrhea, anorexia, and agitation. A long-acting form of galantamine is also available and can be given once a day.
Phytotherapeutic Potential For the Treatment of Alzheimer’s Disease
Published in Atanu Bhattacharjee, Akula Ramakrishna, Magisetty Obulesu, Phytomedicine and Alzheimer’s Disease, 2020
Muhammad Akram, Atanu Bhattacharjee, Naveed Munir, Naheed Akhter, Fozia Anjum, Abida Parveen, Samreen Gul Khan, Muhammad Daniyal, Muhammad Riaz, Fahad Said Khan, Rumaisa Ansari, Umme Laila
Galantamine is an alkaloid derived originally from Galanthus nivalis, known commonly as snowdrops (Perry 1999), and is used as a cholinesterase inhibitor. It not only inhibits cholinesterase activity but also alters the nicotinic acetylcholine receptors. The drug is metabolized by cytochrome P450 (CYP-450) enzymes and has a half-life of 5 to 6 h (Abbasi 2006). Clinical trials have not shown any hepatic toxicity of galantamine (Raskind 2000). Four trials, performed on patients with mild AD, have shown that galantamine is effective at improving cognition and memory at a specific dose of 24 mg/d for a duration of up to six months. These trials proved that the patients with mild AD can get relief from their symptoms using galantamine at the specific doses described (Akhondzadeh 2002; Raskind 2000).
Pharmacological Management of Alzheimer’s Disease
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Rakesh Kumar, Rajan Kumar, Abhinav Anand, Neha Sharma, Navneet Khurana
Galantamine is used in cognitive decline in mild to the moderate AD. Galantamine acts on nicotinic receptors as an allosteric modulator. It is possibly increasing cholinergic transmission by presynaptic nicotinic stimulation (Birks, 2012). At the 8 and 16 mg dose twice daily, the efficacy of galantamine was demonstrated with some side effects at the decreased dose in at least four randomized trials for 3–6 months. As per Cochrane review, it was concluded that galantamine showed positive effects for 3–6 months study with no additional changes at the overdose of 16 mg per day (Birks, 2012; Andrea et al., 2013).
Aconiti lateralis Radix Praeparata inhibits Alzheimer’s disease by regulating the complex regulation network with the core of GRIN1 and MAPK1
Published in Pharmaceutical Biology, 2021
Yutao Wang, Huixiang Zhang, Jing Wang, Ming Yu, Qianqian Zhang, Shan Yan, Dingyun You, Lanlan Shi, Lihuan Zhang, Limei Wang, Hongxiang Wu, Xue Cao
For another, GRIN1 and MAPK1 have been closely related to neurodegeneration, synaptic plasticity, cell survival and AD in previous researches (Coyle et al. 2016; Preciados et al. 2016; Sun and Nan 2017; Lu and Malemud 2019). GRIN1 protein is a critical subunit of NMDA (Kaniakova et al. 2012), which is the target of memantine (Robinson and Keating 2006), and plays a key role in memory and learning by regulating the plasticity of synapses (Mori et al. 2011; Wang et al. 2011). GluN1 receptors and GRIN1 gene expression levels and location are significantly different in AD samples compared to controls (Leuba et al. 2014; Mohamed et al. 2015; Agca et al. 2020). The MAPK1 gene is believed as one age-dependent transcriptional changing gene that involves in the abnormal hyperphosphorylation of the tau-protein, causing aggregated neurofibrillary tangles (Kálmán et al. 2009). Moreover, galantamine could treat Alzheimer’s disease by attenuating the activation of MAPK1 (Noda et al. 2010). Taken these results together, we hypothesise that the complex regulation network with the core of GRIN1 and MAPK1 may play a key role in the process of Fuzi anti-AD.
Pharmacogenomics of drugs used to treat brain disorders
Published in Expert Review of Precision Medicine and Drug Development, 2020
The effects of galantamine are potentially influenced by APOE, APP, ACHE, BCHE, CHRNA4, CHRNA7 and CHRNB2 variants. This drug is a major substrate of CYP2D6, CYP3A4, ABCB1 and UGT1A1, and an inhibitor of ACHE and BCHE [92, 101–104]. Major metabolic pathways are glucuronidation, O-demethylation, N-demethylation, N-oxidation, and epimerization [105]. Galantamine is extensively metabolized by the enzymes CYP2D6 and CYP3A and is a substrate of ABCB1. CYP2D6 are major determinants of galantamine pharmacokinetics, with CYP2D6-PMs presenting 45% and 61% higher dose-adjusted galantamine plasma concentrations than heterozygous and homozygous CYP2D6-EMs [92, 106]; however, these pharmacokinetic changes might not substantially affect pharmacodynamics [107]. The co-administration of galantamine with CYP2D6 and CYP3A4 strong inhibitors increases its bioavailability [108, 109]. Interaction with foods and nutritional components may alter galantamine bioavailability and therapeutic effects [110].
Determination of galantamine in human plasma by LC-MS/MS using carbamazepine as an internal standard: Method validation and application to a pharmacokinetic study of galantamine hydrobromide prolonged-release capsules in healthy Thai volunteers
Published in Cogent Medicine, 2020
Darunee Hongwiset, Songwut Yotsawimonwat, Chokchai Wongsinsup, Saowarunee Sangsrijan, Chuleegone Sornsuvit
Galantamine, a cholinergic agent, is one of the approved drugs for the treatment of mild to moderate Alzheimer’s disease (AD). With a dual mechanism of action, reversible competitive inhibitor of acetylcholinesterase and allosteric modulator of nicotinic receptor, galantamine is an effective drug which was widely used. Various formulations of galantamine are available in forms of oral solutions, tablets and capsules. Since the use of galantamine is increased, new formulations and/or generic formulations are required. Pharmacokinetic and bioequivalence studies are also essential as a tool in drug development. These studied required a sensitive and robust bioanalytical method. In this study, a rapid HPLC-MS/MS method for quantification of galantamine in human plasma with simple solvent-solvent extraction was developed, validated and applied in the pharmacokinetic study of 8 mg galantamine hydrobromide release capsules in healthy Thai volunteers.