Cholinesterase inhibitors galantamine

The courts, however, are not bound by the decision of the Patent Office to issue the patent. In considering whether the application had utility, the Federal Circuit approvingly quoted the district court s determination that the application "did not provide analysis or insight connecting the [summaries of the six references]. .. to galantamine s potential to treat Alzheimer s disease [4]." In conjunction with this analysis, witness testimony given at trial was also considered. For example, the sole inventor testified that "when I submitted this patent, I certainly wasn t sure, and a lot of other people weren t sure, that cholinesterase inhibitors [such as galantamine] would ever work [to treat Alzheimer s disease] [5]." (Emphasis added). 

Galantamine is a cholinesterase inhibitor that also has activity as a nicotinic receptor agonist. 

Galantamine Cholinesterase inhibitor APOE Prospective Unrelated Cognition Controversial results depending on authors and study model... 

Galantamine (Reminyl). Galantamine is the newest of the cholinesterase inhibitors approved in the United States. It is started at 4 mg twice a day and can be increased to 8 mg twice daily after 4 weeks of treatment. The maximum dose of galantamine is 12 mg twice a day. The side effects of galantamine include nausea, diarrhea, loss of appetite, and weight loss. 

Galantamine is used for the treatment of mild to moderate Alzheimer s disease. However in 2005 the U.S. Food and Drug Administration sent out a warning indicating that the product should not be used in patients with mild cognitive impairment (MCI) because of increased mortality observed in trials for MCI with galantamine. Galantamine is a competitive and reversible cholinesterase inhibitor. 

Galantamine, like other cholinesterase inhibitors, is currently approved by the FDA only for the treatment of mild to moderate... 

Galantamine is metabolized primarily by CYP 2D6 and 3A4, and levels may be altered by inducers or inhibitors of these enzymes. Galantamine has not been shown to inhibit major cytochrome P450 enzymes. However, the pharmacodynamic interactions associated with other cholinesterase inhibitors may occur. 

Cholinesterase inhibitors donepezil hydrochloride galantamine hydrobromide rivastigmine tartrate... 

Galantamine (Razadyne) [Cholinesterase Inhibitor] Uses Alzheimer Dz Action Acetylcholinesterase inhibitor Dose 4 mg PO bid, T to 8 mg bid after 4 wk may T to 12 mg bid in 4 wk Caution [B, ] T Effect w/ suc-cinylcholine, amiodarone, dildazem, verapamil, NSAIDs, digoxin X- effect w/ anticholinergics, T risk of death vs placebo Contra Severe renal/hepadc impair Disp Tabs, soln SE GI disturbances, wt loss, sleep disturbances, dizziness, HA Interactions T Effects W/ amitriptyline, cimeddine, erythromycin, fluoxetine, fluvoxamine, ketoconazole, paroxetine, quinidine EMS Use succinylcholine w/ caudon, may need a reduced dose monitor ECG for induced conduction abnormalities OD May cause cholinergic Sxs (SLUDGE), muscle weakness, resp depression, and Szs atropine may be used as antidote... 

Donepezil, rivastigmine, and galantamine are newer cholinesterase inhibitors with adequate penetration into the CNS and a spectrum of action more limited to indirect cholinomimetic effects than tacrine s. The cholinesterase inhibitors should be used with caution in patients receiving other drugs that inhibit cytochrome P450 enzymes (eg, ketoconazole, quinidine see Chapter 4 Drug Biotransformation). 

Treatment of choice - a centrally acting cholinesterase inhibitor (e.g. donepezil, galantamine, rivastigmine)... 

If treatment A/ith antidepressants fails to improve apathy and depressed mood in the elderly, it is possible that this represents early Alzheimer disease and a cholinesterase inhibitor like galantamine may be helpful... 

Cholinesterase inhibitors like galantamine depend upon the presence of infacf fargefs for acefylcholine for maximum effecfiveness and fhus may be most effective in the early stages of Alzheimer disease... 

Some Alzheimer patients who fail fo respond fo another cholinesterase inhibitor may respond when switched to galantamine... 

Some Alzheimer patients who fail to respond to galantamine may respond to another cholinesterase inhibitor... 

Coyle J, Kershaw P. Galantamine, a cholinesterase inhibitor that allosterically modulates nicotinic receptors effects on the course of Alzheimer s disease. Biol Psychiatry 2001 49 289-99. 

Abstract Alzheimer s disease is an illness that affects not only the pahents themselves but also those around them. Traditionally, cholinesterase inhibitors have been the first-line medications used in treating Alzheimer s disease. There are currently fom approved cholinesterase inhibitors tacrine, donepezil, rivastigmine, and galantamine. Each of these medications has a unique pharmacokinetic profile and mechanism of action. Researchers in the past 5-10 years have accumulated much data on the use of cholinesterase inhibitors. The use of cholinesterase inhibitors may preserve activities of daily living, slow progression of memory loss, and improve behavioral and cognitive symptoms associated with Alzheimer s and other related dementias. There is also some evidence to suggest that the efficacy in some cases may last more than a few years. In addition, there is some evidence that the use of cholinesterase inhibitors may be associated with reduction of caretaker stress. The use of cholinesterase inhibitor, however, does not drastically improve... 

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