ライフサイエンスコーパス: varenicline

1 efloquine) and nicotine addiction (cytisine, varenicline).

2 ntions (408 placebo, 418 nicotine patch, 420 varenicline).

3 alpha4beta2-nAChR-selective partial agonist varenicline.

4 ement therapy, 28% had bupropion, and 1% had varenicline.

5 ate cortex were not mitigated by nicotine or varenicline.

6 de-effect profile in comparison with that of varenicline.

7 l study to assess the efficacy and safety of varenicline.

8 with limited efficacy by the partial agonist varenicline.

9 malized 9 weeks after discontinuation of the varenicline.

10 s or partial nAChR agonists like cytisine or varenicline.

11 Intervention Varenicline.

12 es of several bioactive molecules, including varenicline.

13 atment (NRT; reference group), bupropion, or varenicline.

14 n the potency of nicotine but not (+)-EPI or varenicline.

15 impairments were mitigated with nicotine and varenicline.

16 the sensitivity of receptors to choline and varenicline.

17 Systemic varenicline (0, 0.5 or 2.5 mg/kg; intraperitoneal) block

18 Varenicline (0.004-0.04 mg/kg/h) was administered intrav

19 Varenicline (0.01, 0.1, 1.0 mg/kg) had no effect on cont

20 Conversely, low doses of varenicline (0.0125-0.05 mg/kg, i.p.) that had little ef

21 While varenicline (0.1-0.3 mg/kg, i.p.) reduced 2% and 20% alc

22 was attenuated by bilateral microinfusion of varenicline (0.3 mul/side) into the nucleus accumbens (N

23 ional receptor occupancy by a single dose of varenicline (0.5 mg) and the corresponding varenicline d

24 , participants received either a low dose of varenicline (0.5 mg) or matching placebo pill (double-bl

25 pancy in human brain of a single low dose of varenicline (0.5 mg), and to explore the relationship be

26 ifferences for abstinence were, for patch vs varenicline, -0.76% (95% CI, -7.4% to 5.9%); for patch v

27 ne patch; 21 mg per day with taper) trial of varenicline (1 mg twice a day) and bupropion (150 mg twi

28 Participants received varenicline (1 mg twice daily) or placebo, along with sm

29 ognitive behavioral therapy and double-blind varenicline (1 mg, 2 per day) or placebo from weeks 12 t

30 A moderate dose of varenicline (1) significantly reduced the P50 sensory ga

31 cribe a novel series of compounds from which varenicline (1, 6,7,8,9-tetrahydro-6,10-methano-6H-pyraz

32 Varenicline, 1 mg twice daily, or placebo for 12 weeks,

33 ilar between groups (serious adverse events: varenicline 11.9%, placebo 11.3%; major adverse cardiova

34 tion phase; 26 discontinued participation (7 varenicline, 19 placebo) and were considered to have rel

35 at 52 weeks (nicotine patch, 20.8% [50/241]; varenicline, 19.1% [81/424]; and C-NRT, 20.2% [85/421]).

36 at 26 weeks (nicotine patch, 22.8% [55/241]; varenicline, 23.6% [100/424]; and C-NRT, 26.8% [113/421]

37 verse events by treatment group were nausea (varenicline, 25% [511 of 2016 participants]), insomnia (

38 Varenicline (27.6%) and combination NRT (31.5%) (eg, pat

39 The most frequent adverse event was nausea (varenicline, 27.0%; placebo, 10.4%).

40 tment were nausea (98 participants receiving varenicline [28.1%]) and insomnia (72 receiving bupropio

41 11.3%; major adverse cardiovascular events: varenicline 4.0%, placebo 4.6%).

42 roduction of pharmacotherapies like Chantix (varenicline), a selective alpha4beta2 nicotinic partial

43 Varenicline, a new nicotinic ligand based on the structu

44 smoking cessation clinical trials, comparing varenicline, a nicotinic acetylcholine receptor (nAChR)

45 Recently, the smoking cessation therapeutic varenicline, a nicotinic acetylcholine receptor (nAChR)

46 Varenicline, a novel alpha4beta2 nAChR partial agonist,

47 Varenicline, a partial agonist at the alpha4beta2 nAChRs

48 Varenicline, a partial agonist at the alpha4beta2 nicoti

49 Varenicline, a partial agonist for a4ss2 nicotinic acety

50 Varenicline, a partial alpha4beta2 nicotinic acetylcholi

51 Varenicline, a pharmacotherapy for tobacco addiction, re

52 e patch (active patch plus placebo pill), or varenicline (active pill plus placebo patch), plus behav

53 Varenicline acts as a nicotinic receptor partial agonist

54 Furthermore, chronic varenicline administration decreased ethanol consumption

55 combination with NRT was more effective than varenicline alone at achieving tobacco abstinence at 12

56 e and bupropion proved more efficacious than varenicline alone for male smokers and for smokers with

57 of varenicline and bupropion, compared with varenicline alone, increased prolonged abstinence but no

58 ation of the patch; or rescue treatment with varenicline alone.

59 l significance (14.4% vs 7.8%; P = .03); the varenicline-alone group experienced more abnormal dreams

60 Conversely, 5-iodo-A-85380, sazetidine-A, varenicline, alpha-conotoxin MII, and bPiDDB (N,N-dodeca

61 Varenicline also seems to be a weak partial agonist at a

62 Varenicline, an approved smoking cessation medication, s

63 Varenicline, an effective smoking cessation medication,

64 As a result of adverse events, 9.6% of varenicline and 4.3% of placebo participants discontinue

65 Here we demonstrate that varenicline and alcohol exposure, either alone or in com

66 patch treatment, combination treatment with varenicline and bupropion proved more efficacious than v

67 Twelve weeks of varenicline and bupropion SR or varenicline and placebo.

68 neuropsychiatric safety risk and efficacy of varenicline and bupropion with nicotine patch and placeb

69 reports of behavior changes associated with varenicline and bupropion, and these drugs' benefits out

70 Our meta-analysis suggests varenicline and bupropion, as well as individual and tel

71 Among cigarette smokers, combined use of varenicline and bupropion, compared with varenicline alo

72 macogenetic investigation of the efficacy of varenicline and bupropion, we examined whether genes imp

73 safety of the smoking cessation medications varenicline and bupropion.

74 pril 2012, 203 received 12-weeks' open-label varenicline and cognitive behavioral therapy and 87 met

75 treatment, maintenance pharmacotherapy with varenicline and cognitive behavioral therapy improved pr

76 inic acetylcholine receptor (nAChR) agonists varenicline and cytisine are widely used as smoking cess

77 In conclusion, these studies indicate that varenicline and cytisine diminish the dysphoric-like sta

78 Varenicline and cytisine, but not 3-pyr-Cyt, diminished

79 We examined the impact of varenicline and nicotine (both alone and in combination)

80 mygdala-insula circuit was down-regulated by varenicline and nicotine in abstinent smokers.

81 moking abstinence, we examined the impact of varenicline and nicotine, two modestly efficacious pharm

82 The varenicline and placebo groups did not differ significan

83 68.4% versus 66.5% of the varenicline and placebo groups, respectively, completed

84 onsmokers underwent approximately 17 days of varenicline and placebo pill administration and were sca

85 cipants underwent ~17 days of order-balanced varenicline and placebo pill administration and were sca

86 lve weeks of varenicline and bupropion SR or varenicline and placebo.

87 al effects of the nicotinic partial agonists varenicline and sazetidine-A during withdrawal from chro

88 ies demonstrate a functional dissociation of varenicline and sazetidine-A on hippocampal network acti

89 Treating normal metabolisers with varenicline and slow metabolisers with nicotine patch co

90 acy and safety of combination treatment with varenicline and sustained-release bupropion for smokers

91 e relationship between receptor occupancy by varenicline and tobacco withdrawal symptoms ((*)denoting

92 h groups underwent MRI twice while receiving varenicline and twice while receiving a placebo pill, we

93 ral different binding modes for epibatidine, varenicline, and 5a-g.

94 sed for smoking cessation therapy (nicotine, varenicline, and cytisine) and by sazetidine.

95 eported to date, including the marketed drug varenicline, and therefore may fully satisfy the crucial

96 nicotine replacement therapy, bupropion, and varenicline) are effective in patients with COPD.

97 -specific infusions of sazetidine-A, but not varenicline, are efficacious in reducing nicotine withdr

98 inic acetylcholine receptor (nAChR), such as varenicline, are therapeutically used in smoking cessati

99 We conclude that varenicline as a smoking cessation agent differs from ni

100 actions may be involved in the mechanism of varenicline as a smoking cessation aid.

101 we have examined the functional activity of varenicline at a variety of rat neuronal nicotinic recep

102 We assessed whether varenicline, begun in-hospital, is efficacious for smoki

103 nt treatment; 6557 for bupropion; 51,450 for varenicline) between Jan 1, 2007, and June 30, 2012.

104 Twelve weeks of varenicline, bupropion SR, or placebo plus intensive smo

105 nding of the larger agonists epibatidine and varenicline, but dispensable for binding of the smaller,

106 icotine, and the smoking cessation compounds varenicline (Chantix) and cytisine (Tabex), have been ev

107 moking cessation, we examined the actions of varenicline (Chantix) during long-term nicotine exposure

108 ding to alpha7 by the smoking cessation drug varenicline (Chantix; Pfizer, Groton, CT), an alpha4beta

109 ed randomized controlled trials (N=8,027) of varenicline conducted by Pfizer, using complete intent-t

110 For varenicline, continuous abstinence (weeks 9-12) was asso

111 These studies investigated the effects of varenicline, cytisine, and the cytisine-derivative 3-(py

112 However, varenicline did not significantly decrease self-administ

113 Administration of varenicline diminished smoking cue-elicited ventral stri

114 Varenicline displays high alpha4beta2 nAChR affinity and

115 f varenicline (0.5 mg) and the corresponding varenicline dissociation constant (K(V)), along with the

116 that unlike binding to its target receptor, varenicline does not form a cation-pi interaction with T

117 Varenicline does not seem to be associated with an incre

118 Varenicline dose-dependently reduced responding maintain

119 eys, whereas (+)-EPI and the partial agonist varenicline engendered, respectively, complete and parti

120 In a community sample, varenicline exerts a robust and favorable effect on smok

121 Varenicline facilitates smoking cessation in clinical st

122 and make a quit attempt at 3 months, use of varenicline for 24 weeks compared with placebo significa

123 cent clinical trials support the efficacy of varenicline for managing global nicotine withdrawal symp

124 logic resembles the previous development of varenicline for smoking cessation.

125 ine), predicts response to nicotine patch or varenicline for smoking cessation.

126 -prevalence abstinence rates were 60% in the varenicline group (24 of 40) vs 19% (9 of 47) in the pla

127 The varenicline group (n = 760) had significantly higher con

128 rious adverse events occurred in 3.7% of the varenicline group and 2.2% of the placebo group (P = .07

129 revalence abstinence rates were 47.3% in the varenicline group and 32.5% in the placebo group (P=0.01

130 The varenicline group did not differ from placebo in terms o

131 The varenicline group had significantly higher continuous ab

132 However, compared with placebo, the varenicline group scored higher on working and declarati

133 m weeks 12 through 76, 30% (12 of 40) in the varenicline group vs 11% (5 of 47) in the placebo group

134 up during weeks 21 through 24 (37.8% for the varenicline group vs 12.5% for the placebo group; RD, 25

135 hrough 64, 45% (18 of 40) among those in the varenicline group vs 15% (7 of 47) in the placebo group

136 s the placebo group (n = 750) (32.1% for the varenicline group vs 6.9% for the placebo group; risk di

137 3.7]) and weeks 21 through 52 (27.0% for the varenicline group vs 9.9% for the placebo group; RD, 17.

138 s 9 through 24, 29.7% of participants in the varenicline group were continuously abstinent compared w

139 eks 9 through 52, 23% of participants in the varenicline group were continuously abstinent compared w

140 t (weeks 9-12), 43.9% of participants in the varenicline group were continuously abstinent from smoki

141 verse events by 10.5% of participants in the varenicline group, 12.6% in the bupropion SR group, and

142 evere neuropsychiatric adverse events in the varenicline group, 22 (2.2%) of 989 in the bupropion gro

143 ted in 67 (6.5%) of 1026 participants in the varenicline group, 68 (6.7%) of 1017 in the bupropion gr

144 Two varenicline-group participants died during the nontreatm

145 A moderate dose of varenicline had no significant effect on spatial working

146 At 24 weeks, patients randomized to varenicline had significantly higher rates of smoking ab

147 Mecamylamine and varenicline had similar potencies to block nicotine and

148 Moderate-dose treatment with varenicline has a unique treatment profile on core schiz

149 nAChR partial agonist and like cytisine and varenicline has antidepressant-like effects in animal mo

150 Varenicline has been approved in the United States for s

151 Varenicline has been shown to be a partial agonist of al

152 Varenicline has lower potency and higher efficacy at alp

153 to determine the effects of sazetidine-A and varenicline in animals chronically treated with saline,

154 Varenicline in combination with NRT was more effective t

155 nt the co-crystal structures of cytisine and varenicline in complex with Aplysia californica acetylch

156 The selectivity of varenicline in decreasing ethanol consumption combined w

157 We have investigated the role of varenicline in the modulation of ethanol consumption and

158 nicotine replacement therapy, bupropion, and varenicline in the South Indian state of Kerala to under

159 We show that acute administration of varenicline, in doses reported to reduce nicotine reward

160 Varenicline increased smoking cessation in smokers with

161 In the randomized controlled trials, varenicline increased the risk of nausea (odds ratio=3.6

162 Varenicline-induced activation of lateral orbitofrontal

163 ining the alpha4 subunit (alpha4* nAChRs) in varenicline-induced reduction of alcohol consumption, we

164 Varenicline, initiated in-hospital following ACS, is eff

165 Infusion of varenicline into the posterior, but not the anterior VTA

166 Varenicline is a clinically available, partial agonist a

167 Thus, whereas varenicline is a partial agonist at some heteromeric neu

168 It is remarkable that varenicline is a potent, full agonist at alpha7 receptor

169 We also find that varenicline is a potent, partial agonist at alpha4beta2

170 Varenicline is an effective and increasingly prescribed

171 Varenicline is an effective pharmacotherapy to aid smoki

172 Varenicline is an efficacious, safe, and well-tolerated

173 This analysis revealed no evidence that varenicline is associated with adverse neuropsychiatric

174 this study was to investigate whether use of varenicline is associated with such events.

175 Varenicline is effective for smoking cessation in smoker

176 However, varenicline is not a hydrogen-bond acceptor to the backb

177 Varenicline is the most efficacious pharmacotherapy curr

178 wn that acute administration of nicotine and varenicline lowered ICSS thresholds.

179 deficits in an animal model and suggest that varenicline may be effective at treating nicotine withdr

180 In contrast, varenicline may have cognitive-enhancing effects.

181 and mild side effects in humans suggest that varenicline may prove to be a treatment for alcohol depe

182 abstinence compared with 43.2% and 48.6% in varenicline monotherapy (odds ratio [OR], 1.49; 95% CI,

183 abstinence compared with 24.5% and 29.2% in varenicline monotherapy (OR, 1.39; 95% CI, 0.93-2.07; P

184 abstinence compared with 27.6% and 31.9% in varenicline monotherapy (OR, 1.52; 95% CI, 1.04-2.22; P

185 t an opportunity for physicians to prescribe varenicline more broadly, even for patients with comorbi

186 h the patch alone and 16.5% with a switch to varenicline (odds ratio=2.80, 95% CI=1.11-7.06).

187 Varenicline offers a treatment option for smokers whose

188 The present study evaluated the effects of varenicline on contextual fear conditioning and its effe

189 stinent to explicitly examine the effects of varenicline on cue reactivity independent of withdrawal.

190 moking cessation, we assessed the effects of varenicline on emotional processing (a biomarker of depr

191 To investigate the influence of varenicline on mood and behavior independent of smoking

192 ng status and administration of nicotine and varenicline on probabilistic reversal learning choice be

193 oups: (1) nicotine patch only (n = 241); (2) varenicline only (including 1 prequit week; n = 424); an

194 ropsychiatric adverse events attributable to varenicline or bupropion relative to nicotine patch or p

195 Capitella teleta, Ct-AChBP, in complex with varenicline or lobeline, which are both partial agonists

196 hiatric adverse events in patients receiving varenicline or nicotine replacement therapy (N=35,800) a

197 hospitalized with an ACS were randomized to varenicline or placebo for 12 weeks.

198 ouble-blind design, in which we administered varenicline or placebo to healthy subjects over 7 days (

199 of open-label treatment with nicotine patch, varenicline, or C-NRT produced no significant difference

200 reness regarding potential hepatotoxicity of varenicline, particularly among patients with pre-existi

201 nt (K(V)), along with the effect of low-dose varenicline, pill placebo, and smoking-to-satiety on wit

202 The varenicline-placebo and bupropion-placebo RDs were 1.59

203 The varenicline-placebo and bupropion-placebo risk differenc

204 ere randomly assigned to receive 12 weeks of varenicline plus bupropion or varenicline plus placebo.

205 gher abstinence rate than those who received varenicline plus placebo (39.8% compared with 25.9%; odd

206 ve 12 weeks of varenicline plus bupropion or varenicline plus placebo.

207 Switching to varenicline produced less robust effects, but point abst

208 All medications were well tolerated, but varenicline produced more frequent adverse events than d

209 ment therapy RCTs, 28 bupropion RCTs, and 18 varenicline RCTs, we found no increase in the risk of al

210 Varenicline reduced craving and withdrawal and, for thos

211 In contrast, varenicline reduced gain magnitude processing, but did s

212 Varenicline reduced nicotine upregulation of alpha4beta2

213 These data show for the first time that varenicline reduces relapse triggered by contexts that p

214 pha4* nAChRs is necessary and sufficient for varenicline reduction of alcohol consumption.

215 dministration issued a black box warning for varenicline regarding neuropsychiatric events.

216 e evidence supports the superior efficacy of varenicline relative to both placebo and bupropion, indi

217 Our network meta-analysis revealed that varenicline (relative risk [RR]: 2.64; 95% confidence in

218 Our findings demonstrate that low-dose varenicline results in saturation of alpha4beta2(*) nACh

219 e data demonstrate, for the first time, that varenicline reverses nicotine withdrawal-induced deficit

220 95% confidence interval [CI], 0.54-1.73) or varenicline (RR, 1.30; 95% CI, 0.79-2.23).

221 .21-0.85) and no clear evidence of harm with varenicline (RR, 1.34; 95% CI, 0.66-2.66) or nicotine re

222 bupropion (RR, 1.62 [CI, 1.49 to 1.76]), and varenicline (RR, 2.27 [CI, 2.02 to 2.55]) were also effe

223 These results suggest that varenicline's downregulation of anticipatory reward proc

224 These effects likely contribute to varenicline's efficacy as a pharmacotherapy for smoking

225 e in vivo binding properties are well known, varenicline's neurobiological mechanisms of action are s

226 Varenicline's reciprocal actions in the reward-activated

227 Varenicline's short-term and long-term efficacy exceeded

228 We conclude that varenicline selectively attenuates the reinforcing effec

229 Neither bupropion nor varenicline showed an increased risk of any cardiovascul

230 Smoking to satiety, but not low-dose varenicline, significantly reduced withdrawal symptoms.

231 s (genes included nAChR subunits, additional varenicline-specific genes, and genes involved in nicoti

232 Given the actions of varenicline tartrate and bupropion hydrochloride sustain

233 ies such as nicotine replacement therapy and varenicline tartrate may aid cessation treatment.

234 tinic actions, we investigated the effect of varenicline tartrate, a relatively specific alpha4beta2

235 iatric disorders was significantly lower for varenicline than for nicotine replacement therapy (2.28%

236 he continuous abstinence rate was higher for varenicline than placebo during weeks 9 through 12 (47.0

237 ntary face of the receptor's binding site by varenicline, the endogenous agonist acetylcholine, and t

238 Within 5 days of starting the varenicline, the patient developed new onset of nausea,

239 ases of drug-induced liver injury related to varenicline therapy, highlighting the need for clinician

240 Varenicline titrated to 1 mg twice daily (n = 344) or bu

241 Twenty-four weeks of varenicline titrated to 1 mg twice daily or placebo with

242 1:1:1 ratio to receive brief counseling and varenicline titrated to 1 mg twice per day (n = 352), bu

243 patient had received a new prescription for varenicline to aid with smoking cessation approximately

244 ning nicotine replacement therapy (NRT) with varenicline to improve abstinence is effective and safe.

245 Varenicline-treated participants achieved higher abstine

246 Varenicline-treated participants had higher CARs versus

247 on of (18)F-AZAN brain uptake in smokers and varenicline-treated subjects.

248 resent study examined the effects of chronic varenicline treatment on self-administration of IV nicot

249 Each varenicline treatment was followed by saline-control tre

250 cally exposed to ethanol for 2 months before varenicline treatment.

251 In conclusion, short-term varenicline use did not influence negative biases in emo

252 Varenicline use was also associated with a generalized s

253 in mood and behavior are directly related to varenicline use, or caused by smoking cessation itself o

254 ed greater overall side-effect severity with varenicline versus placebo (beta=-1.06, 95% CI -2.08 to

255 k continuous abstinence rates were 44.0% for varenicline vs 17.7% for placebo (odds ratio [OR], 3.85;

256 e continuous abstinence rates were 21.9% for varenicline vs 8.4% for placebo (OR, 3.09; 95% CI, 1.95-

257 Different loci are associated with varenicline vs bupropion response, suggesting that addit

258 NRT, -4.0% (95% CI, -10.8% to 2.8%); and for varenicline vs C-NRT, -3.3% (95% CI, -9.1% to 2.6%).

259 e 6-month postquit follow-up visit, only the varenicline vs placebo comparison remained significant.

260 mit on effective K(V) with respect to plasma varenicline was 0.49 nM.

261 Varenicline was associated with a significantly reduced

262 Varenicline was begun 1 week prior to TQD, continued for

263 The varenicline was discontinued on day 5 by the patient.

264 Varenicline was more effective than placebo, nicotine pa

265 At end of treatment, varenicline was more efficacious than nicotine patch in

266 The most common adverse event with varenicline was nausea, which occurred in 101 participan

267 rebound increase in ethanol intake when the varenicline was no longer administered.

268 Varenicline was safe and generally well tolerated, with

269 Varenicline was significantly more efficacious than plac

270 Varenicline was trapped as a weak base in acidic compart

271 No sex differences in efficacy for varenicline were observed.

272 ral effects of smoking status, nicotine, and varenicline were tested for on MRI contrasts that captur

273 nicotine replacement therapy, bupropion, and varenicline-were associated with an increased risk of ca

274 ine replacement therapy (NRT), bupropion, or varenicline when trying to quit double their odds of suc

275 ne replacement therapy [NRT], bupropion, and varenicline), which is most effective in helping people

276 ed trial compared the efficacy and safety of varenicline with placebo for smoking cessation in 714 sm

277 cordings to pinpoint crucial interactions of varenicline with residues on the complementary face of t

278 of alpha4beta2(*) nAChRs by a single dose of varenicline, with a 90% lower confidence limit of 89% oc

279 The therapeutic potential of varenicline would escalate if it also diminished conditi

280 We hypothesize that varenicline would have a third mechanism to blunt respon