ライフサイエンスコーパス: donepezil

1 course of the acetylcholinesterase inhibitor donepezil.

2 attenuation by the AChE-selective inhibitor donepezil.

3 events or deaths, or between 5 mg and 10 mg donepezil.

4 d rats, which was significantly increased by donepezil.

5 the reversible acetylcholinesterase blocker donepezil.

6 mals and the acetylcholinesterase inhibitor, donepezil (1 mg/kg), protected against the acute cogniti

7 months of age for 6 months of treatment) of donepezil (1, 2, 4 mg/kg, in drinking water) on tissue a

8 that include their prescribed dosage ranges, donepezil (1-1000 nM) and galantamine (50-1000 nM) incre

9 d start memantine 20 mg per day, or continue donepezil 10 mg per day and start memantine 20 mg per da

10 of 12-19), and had been stably treated with donepezil 10 mg per day for 3 or more months.

11 Scotland and randomly allocated to continue donepezil 10 mg per day without memantine, discontinue d

12 Patients were randomly assigned to receive donepezil 5 mg or placebo orally every morning for 7 day

13 AD patients before and after treatment with donepezil (5 and 10 mg/day) for at least 5 weeks and com

14 disease received 24 weeks of treatment with donepezil (5 mg/day for the first 28 days and 10 mg/day

15 period in which they were randomly allocated donepezil (5 mg/day) or placebo.

16 eted this period were rerandomised to either donepezil (5 or 10 mg/day) or placebo, with double-blind

17 After stabilization on donepezil (5.7 +/- 1.7 weeks at 10 mg) patients showed i

18 5) for rivastigmine to -2.17 for 10 mg daily donepezil (95% CI -2.98 to -1.35).

19 Consistently, systemic treatment with donepezil, a centrally active acetylcholinesterase inhib

20 Donepezil, a cholinesterase inhibitor, restored performa

21 Prior studies have suggested that donepezil, a neurotransmitter modulator, may improve cog

22 5-(11)C-methoxy-donepezil, a noncompetitive acetylcholinesterase ligand,

23 II study was conducted to determine whether donepezil, a US Food and Drug Administration-approved re

24 combination of donepezil and memantine over donepezil alone.

25 Donepezil also reduced response amplitude in visual cort

26 The dose of 4 mg/kg of donepezil also significantly increased synaptic density

27 Donepezil, an acetylcholinesterase inhibitor, is an appr

28 and (2) a pharmacological intervention using donepezil, an acetylcholinesterase inhibitor.

29 E, alone and in complexes with drug ligands; donepezil, an Alzheimer's disease drug, binds differentl

30 articipants (10% [95% CI, 0%-21%]) receiving donepezil and 9 of 27 participants (33% [95% CI, 16%-51%

31 Donepezil and antidepressant therapy temporarily improve

32 ophoric features of cholinesterase inhibitor donepezil and diarylthiazole as potential multitarget-di

33 levels and Ki values for AChE inhibition for donepezil and galantamine in rat, mouse, and rabbit afte

34 are acetylcholinesterase inhibitors, such as donepezil and galantamine.

35 pport slightly different modes of action for donepezil and galantamine.

36 ine from the brain is in general faster that donepezil and is faster in rabbits compared to rats and

37 randomised, double-blind, placebo-controlled Donepezil and Memantine in Moderate to Severe Alzheimer'

38 o significant benefits of the combination of donepezil and memantine over donepezil alone.

39 al cognition (n = 73) showed no benefit with donepezil and no increase in recurrence of major depress

40 The efficacy of donepezil and of memantine did not differ significantly

41 sity improved significantly on day 8 in both donepezil and placebo groups.

42 no significant differences were seen between donepezil and placebo in behavioural and psychological s

43 eta-analysis indicated beneficial effects of donepezil and rivastigmine for cognitive and psychiatric

44 nue donepezil without memantine, discontinue donepezil and start memantine 20 mg per day, or continue

45 l without memantine, 76 (26%) to discontinue donepezil and start memantine, and 73 (25%) to continue

46 onepezil, discontinue donepezil, discontinue donepezil and start memantine, or continue donepezil and

47 nd start memantine, and 73 (25%) to continue donepezil and start memantine.

48 e donepezil and start memantine, or continue donepezil and start memantine.

49 tarted memantine, and 43 [59%] who continued donepezil and started memantine).

50 without memantine, 41 [54%] who discontinued donepezil and started memantine, and 43 [59%] who contin

51 ffects of continuation or discontinuation of donepezil and starting of memantine on subsequent nursin

52 ignificant difference between the effects of donepezil and those of placebo on the basis of the chang

53 The combination of 5al, donepezil, and memantine (triple combination) produces s

54 The cholinesterase inhibitors rivastigmine, donepezil, and metrifonate, which are devoid of nicotini

55 In cognitively intact patients, donepezil appears to have no clear benefit for preventin

56 rent AD therapeutics memantine (Namenda) and donepezil (Aricept), using similar doses for each, revea

57 Administration of the 4 mg/kg dose of donepezil, as compared to vehicle and lower doses of don

58 Patients assigned to continue donepezil, as compared with those assigned to discontinu

59 r's disease, we report herein a new class of donepezil-based "bio-oxidizable" prodrugs 1 designed to

60 imination task, once while ingesting 5 mg of donepezil before every training session and once while p

61 Autoradiography showed high (11)C-donepezil binding (dissociation constant, 6-39 nM) in pi

62 We also demonstrated high (11)C-donepezil binding in bacterial abscesses.

63 We detected significantly decreased (11)C-donepezil binding in the small intestine (-35%; P = 0.00

64 Decreases in (11)C-donepezil binding may, therefore, represent a marker of

65 g affinities and levels of nonspecific (11)C-donepezil binding to porcine tissues.

66 After donepezil, cerebral cortical inhibition in AD brain aver

67 To evaluate the effectiveness of donepezil compared with placebo in cancer patients with

68 No significant benefits were seen with donepezil compared with placebo in institutionalisation

69 .09 [95% CI 1.29-3.39]) than in the combined donepezil continuation groups, and no difference during

70 Alzheimer's disease (who had been prescribed donepezil continuously for at least 3 months at a dose o

71 receive 2000 IU of vitamin E daily, 10 mg of donepezil daily, or placebo for three years.

72 Cholinergic enhancement with donepezil decreased the spatial spread of excitatory fMR

73 ylcholinesterase inhibitors rivastigmine and donepezil did not potentiate nAChR-mediated responses, w

74 Treatment with donepezil did not significantly improve the overall comp

75 more nursing home placements in the combined donepezil discontinuation groups during the first year (

76 unction]) to continue donepezil, discontinue donepezil, discontinue donepezil and start memantine, or

77 ting better cognitive function]) to continue donepezil, discontinue donepezil, discontinue donepezil

78 Clinical trials of this donepezil dose schedule are not testing the effect of ne

79 hibition, 3-15 times higher galantamine than donepezil doses are needed.

80 All patients were offered open-label donepezil during the second week.

81 -dwelling patients who had been treated with donepezil for at least 3 months and who had moderate or

82 sent study, we explored the utility of (11)C-donepezil for imaging acetylcholinesterase densities in

83 d dexterity (P < .001), with the benefits of donepezil greater for those who were more cognitively im

84 dence interval, 0.74 to 1.41; P=0.91) or the donepezil group (hazard ratio, 0.80; 95 percent confiden

85 ly assigned to treatment, 47 patients in the donepezil group and 56 in the placebo group were assessa

86 e risk of entering institutional care in the donepezil group compared with placebo was 0.97 (95% CI 0

87 that as compared with the placebo group, the donepezil group had a reduced likelihood of progression

88 e placebo group and 22 of 113 (19.5%) in the donepezil group had a reduction of 30% or greater in the

89 The donepezil group was more likely than the placebo group t

90 nificant differences between the placebo and donepezil groups in scores for the Neuropsychiatric Inve

91 improvement in speech comprehension, whereas donepezil had a negative effect.

92 Only 5 mg daily donepezil had an effect on the Clinicians' Global Impres

93 compared with those assigned to discontinue donepezil, had a score on the SMMSE that was higher by a

94 We examined the effects of donepezil hydrochloride (Aricept) on cognition and brain

95 eports state that widely prescribed doses of donepezil hydrochloride provide nearly complete inhibiti

96 up to 3 nM), outperforming the standard drug donepezil (IC50 = 11 nM), most of the corresponding 1,4-

97 reatment in patients with AD, the effects of donepezil, if any, on the AD process are not known.

98 nhancement with the cholinesterase inhibitor donepezil improved target detection, and modeling sugges

99 , placebo-controlled study on the effects of donepezil in 27 older adults with mild memory deficits.

100 Withdrawal of donepezil in patients with moderate-to-severe Alzheimer'

101 from in vitro biochemical tests suggest that donepezil is 40- to 500-fold more potent than galantamin

102 Donepezil is a high-affinity ligand for acetylcholineste

103 Donepezil is not cost effective, with benefits below min

104 These results suggest that a higher dose of donepezil may have a measurable impact on tissue level o

105 These preliminary results suggest that donepezil may have a potentially protective effect in Al

106 erate to severe AD receiving stable doses of donepezil, memantine resulted in significantly better ou

107 or greater in the CMAI score (the value for donepezil minus that for placebo, -0.9 percentage point;

108 ted mean difference in change [the value for donepezil minus that for placebo], -0.06; 95% confidence

109 effect of the acetylcholinesterase inhibitor donepezil on magnetic resonance markers of neurodegenera

110 nce (95% CI -1.74 to -0.16) with 10 mg daily donepezil on the Alzheimer's Disease Functional Assessme

111 se (5 mg for 6 weeks, 10 mg for 18 weeks) of donepezil or placebo.

112 while subjects were on a 10mg daily dose of donepezil or placebo.

113 intenance antidepressant pharmacotherapy and donepezil or to maintenance antidepressant pharmacothera

114 BADLS points better (0.5-1.6; p<0.0001) with donepezil over the first 2 years.

115 social treatment program to receive 10 mg of donepezil per day (128 patients) or placebo (131 patient

116 We propose that (11)C-donepezil PET imaging may be able to quantify the parasy

117 (11)C-donepezil PET is suitable for imaging acetylcholinestera

118 for modeling uptake kinetics in future (11)C-donepezil PET studies.

119 Using 5-[(11)C]-methoxy-donepezil positron emission tomography, we studied 12 pa

120 We aimed to determine whether donepezil produces worthwhile improvements in disability

121 le scores were improved after treatment with donepezil, relative to placebo, at weeks 6, 12, 18, and

122 of brain AChE inhibition for galantamine and donepezil, respectively, are 7.1 and 2.3 microg/g in rat

123 he brain-to-plasma ratio for galantamine and donepezil, respectively, ranges from 1.2 to 1.5 in the r

124 No correlations were found between the (11)C-donepezil signal and disease duration, severity of const

125 l, as compared to vehicle and lower doses of donepezil, significantly reduced brain tissue soluble Ab

126 rs was not lower among patients treated with donepezil than among those given placebo.

127 Although donepezil therapy was associated with a lower rate of pr

128 iodistribution and kinetic analyses of (11)C-donepezil time-activity curves were assessed with dynami

129 nded, placebo-controlled, phase III trial of donepezil to confirm these favorable results.

130 n subjects with the cholinesterase inhibitor donepezil (trade name: Aricept) and measured the effects

131 At endpoint, the donepezil-treated patients had significantly smaller mea

132 ate concentration tended to be higher in the donepezil-treated patients than in the patients who rece

133 ), a selective 5-HT6 receptor antagonist, in donepezil-treated patients with moderate Alzheimer's dis

134 Idalopirdine improved cognitive function in donepezil-treated patients with moderate Alzheimer's dis

135 ave demonstrated the symptomatic efficacy of donepezil treatment in patients with AD, the effects of

136 Decisions to stop or continue donepezil treatment should be informed by potential risk

137 Donepezil treatment significantly enhanced the response

138 Three donepezil, two galantamine, one rivastigmine, and two me

139 In contrast, tacrine and donepezil, typical AChE inhibitors, could not prevent sy

140 l abscesses was PET-scanned to explore (11)C-donepezil uptake in infections.

141 A linear correlation was seen between (11)C-donepezil volumes of distribution and standardized uptak

142 rrence rates of major depression of 44% with donepezil vs 12% with placebo (likelihood ratio = 4.91;

143 potentiate nAChR-mediated responses, whereas donepezil was a reasonably potent inhibitor of nicotine-

144 The cholinesterase inhibitor donepezil was administered to normal healthy human subje

145 lzheimer's disease, continued treatment with donepezil was associated with cognitive benefits that ex

146 poprotein E epsilon4 alleles, the benefit of donepezil was evident throughout the three-year follow-u

147 Peripheral metabolization of (11)C-donepezil was low (>90% unchanged ligand at 60 min).

148 Finally, the analgesic effect of donepezil was markedly reduced by a microinjection of th

149 In addition, perceptual learning with donepezil was more selective to the trained direction of

150 In this 12-week trial, donepezil was not more effective than placebo in treatin

151 Donepezil was not significantly superior to placebo in t

152 emission tomography tracer 5-[(11)C]-methoxy-donepezil was recently validated for imaging acetylcholi

153 Donepezil was tested in a double-blind, placebo-controll

154 Rivastigmine, but not donepezil, was associated with greater risk of adverse e

155 ); however, significant differences favoring donepezil were observed for memory (recognition, P = .02

156 No major adverse effects of donepezil were observed, but it had an unpredicted negat

157 an acetylcholinesterase inhibitor treatment (donepezil) when compared to a placebo control group.

158 without memantine, 42 [58%] who discontinued donepezil without memantine, 41 [54%] who discontinued d

159 l groups (36 [49%] in patients who continued donepezil without memantine, 42 [58%] who discontinued d

160 patients were randomly assigned to continue donepezil without memantine, 73 (25%) to discontinue don

161 l without memantine, 73 (25%) to discontinue donepezil without memantine, 76 (26%) to discontinue don

162 10 mg per day without memantine, discontinue donepezil without memantine, discontinue donepezil and s

163 etermine whether long-term administration of donepezil would slow amyloid plaque deposition or confer