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Donepezil side effects

Donepezil should be initiated at a 5-mg/day dose in the morning and titrated to 10 mg/day after 4 to 6 weeks if it is well tolerated. Table 63-6 summarizes cholinesterase inhibitor dosing recommendations. The most common donepezil side effects are nausea, vomiting. [Pg.1165]

Tacrine is particularly damaging to the liver and can result in hepatotoxicity. Because tacrine is more likely to cause adverse reactions and drug interactions, it must be administered more frequently (4 times a day) and is rarely used in current therapy. Donepezil has fewer and milder side effects than tacrine It is considered the agent of first choice However, some patients may achieve a better response with one drug than another. Additional adverse reactions are listed in the Summary Drug Table Cholinesterase Inhibitors. [Pg.305]

The initial enthusiasm for tacrine and velnacrine, which are the anticholinesterases most studied clinically, has been tempered by the fact that not all patients respond. Most show the peripheral parasympathomimetic effects of cholinesterase inhibition, e.g. dyspepsia and diarrhoea, as well as nausea and vomiting, and about half of the patients develop hepatotoxicity with elevated levels of plasma alanine transaminase. While some peripheral effects can be attenuated with antimuscarinics that do not enter the brain, these add further side-effects and the drop-out rate from such trials is high (<75%) in most long-term studies. Donepezil appears to show less hepatotoxicity but its long-term value remains to be determined. [Pg.387]

Donepezil is a piperidine cholinesterase inhibitor, which reversibly and non-competitively inhibits centrally active acetylcholinesterase 34 This specificity is claimed to result in fewer peripheral side effects as compared to the other ChE inhibitors. [Pg.518]

Adverse reactions with donepezil include nausea, vomiting, and diarrhea. These are typical cholinergic side effects to expect with all of the cholinesterase inhibitors. Table 32-6 compares the major side effects for all of the approved agents for Alzheimer s disease.34-38... [Pg.518]

Only a small number of drug interactions have been reported with donepezil. In vitro studies show a low rate of binding of donepezil to cytochrome P-450 (CYP)3A4 or 2D6. Whether or not donepezil has the potential for enzyme induction is not known. No interactions with theophylline, cimeti-dine, warfarin, digoxin, or ketoconazole have been documented. In vitro studies show that inhibitors of CYP3A4 and 2D6 have the potential to inhibit the metabolism of donepezil. The clinical relevance of this is unknown. However, monitoring for possible increased peripheral side effects is advised... [Pg.518]

CYP3A4 and 2D6 are the major enzymes involved in the metabolism of galantamine. Pharmacokinetic studies with inhibitors of this system have resulted in increased galantamine concentrations or reductions in clearance. Similarly to donepezil, if inhibitors are given concurrently with galantamine, monitoring for increased cholinergic side effects should be done. Studies with inducers of these enzymes have not been completed.37... [Pg.520]

Like other cholinesterase inhibitors, donepezil carries the risk of cholinergic side effects. In fact, if the dose of a cholinesterase inhibitor is increased too rapidly, it may even worsen behavior. The principal side effects of donepezil include upset stomach, diarrhea, headache, and dizziness. It is usually started at 5 mg taken once daily in the evening. After 1 month, the dose of donepezil can be increased to lOmg/day. [Pg.300]

Donepezil HC1, a piperidine, is a highly selective inhibitor of the enzyme AChE [3,4] that is chemically unique from other AChE inhibitors [5, 6]. In vitro and preclinical studies have demonstrated that donepezil is approximately 1200 times more selective for AChE in the brain than for butyrylcholinesterase (BuChE) in the periphery [3, 4, 7]. Phase II and III studies conducted in the United States have shown that donepezil (5 or 10 mg once daily) produces statistically significant improvements in cognition and global function in patients with AD [8-10]. Its clinical efficacy and minimal side-effect profile are thought to be related to its specific inhibition of AChE in the areas of the brain affected by the cholinergic deficit that typifies this disease [3, 4, 7],... [Pg.120]

Donepezil is primarily a reversible inhibitor of acetylcholinesterase with a long elimination half-life. It lacks the hepatotoxicity of tacrine but frequently causes nausea, vomiting and diarrhoea. These side effects, together with occasional bradycardia, sycope and changes in the sleep architecture, are directly associated with a central and peripheral enhancement of cholinergic function. At the present time, donepezil is the most widely prescribed anticholinesterase in the United States and Europe. [Pg.363]

Cholinesterase inhibitors, such as donepezil, are the first line of drug treatment as they can decrease the rate of cognitive decline in some patients. But there are side effects with these agents that are related to excessive cholinergic stimulation, for example abdominal cramps, bronchoconstriction, salivation and so on. [Pg.125]

Magnuson TM, Keller BK, Burke WJ. Extrapyramidal side effects in a patient treated with risperidone plus donepezil. Am J Psychiatry 1998 155(10) 1458-9. [Pg.639]

ZT-1 induced a dose-dependent elevation of ACh in the cortex of conscious rats. Compared with donepezil, ZT-1 was found to be 20-fold more potent at increasing cortical ACh levels it showed a longer duration of action and fewer side effects. [Pg.170]

The most prominent side effects of donepezil are gastrointestinal effects, which are usually mild and transient... [Pg.136]

Donepezil was the second cholinesterase inhibitor approved in the US [6]. It is currently the only acetylchohnesterase approved by the FDA for the treatment of severe Alzheimer s disease. Donepezil is a reversible, noncompetitive chohnesterase inhibitor. It has a high binding specificity for brain acetylcholinesterase, with httle to no affinity for butylchohnesterase. Compared with the other cholinesterase inhibitors in this class, donepezil may be better tolerated, with less gastrointestinal side effects. The long half-life of this medication allows once a day dosing (See Table 3). [Pg.30]


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See also in sourсe #XX -- [ Pg.207 ]




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