ライフサイエンスコーパス: varenicline

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

2 (nicotine replacement therapy, bupropion, or varenicline).

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

4 the sensitivity of receptors to choline and varenicline.

5 tro without affecting other known targets of varenicline.

6 alpha4beta2-nAChR-selective partial agonist varenicline.

7 d by low doses of the smoking cessation drug varenicline.

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

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

10 with limited efficacy by the partial agonist varenicline.

11 malized 9 weeks after discontinuation of the varenicline.

12 s or partial nAChR agonists like cytisine or varenicline.

13 Intervention Varenicline.

14 impairments were mitigated with nicotine and varenicline.

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

16 ate cortex were not mitigated by nicotine or varenicline.

17 es of several bioactive molecules, including varenicline.

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

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

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

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

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

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

24 ubthreshold doses of NS9283 (2.5 mg/kg) plus varenicline (0.1 mg/kg) synergistically reduced ethanol

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

44 11.3%; major adverse cardiovascular events: varenicline 4.0%, placebo 4.6%).

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

46 Varenicline, a new nicotinic ligand based on the structu

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

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

49 Varenicline, a novel alpha4beta2 nAChR partial agonist,

50 Varenicline, a partial agonist at the alpha4beta2 nAChRs

51 Varenicline, a partial agonist for a4ss2 nicotinic acety

52 The smoking cessation agent varenicline, a partial agonist of alpha4beta2 nAChRs, re

53 Varenicline, a partial alpha4beta2 nicotinic acetylcholi

54 Varenicline, a pharmacotherapy for tobacco addiction, re

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

56 Varenicline acts as a nicotinic receptor partial agonist

57 Furthermore, chronic varenicline administration decreased ethanol consumption

58 ine patch with varenicline rather than using varenicline alone and using varenicline rather than elec

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

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

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

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

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

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

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

66 Varenicline, an approved smoking cessation medication, s

67 Varenicline, an effective smoking cessation medication,

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

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

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

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

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

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

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

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

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

77 safety of the smoking cessation medications varenicline and bupropion.

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

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

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

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

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

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

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

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

86 The varenicline and placebo groups did not differ significan

87 68.4% versus 66.5% of the varenicline and placebo groups, respectively, completed

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

115 However, varenicline did not significantly decrease self-administ

116 Administration of varenicline diminished smoking cue-elicited ventral stri

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

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

119 Varenicline does not seem to be associated with an incre

120 Varenicline dose-dependently reduced responding maintain

121 ion with varenicline, may allow use of lower varenicline doses to decrease varenicline side effects.

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

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

124 Varenicline facilitates smoking cessation in clinical st

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

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

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

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

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

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

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

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

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

134 The varenicline group had significantly higher continuous ab

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

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

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

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

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

140 3.7]) and weeks 21 through 52 (27.0% for the varenicline group vs 9.9% for the placebo group; RD, 17.

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

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

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

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

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

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

147 Two varenicline-group participants died during the nontreatm

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

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

150 Mecamylamine and varenicline had similar potencies to block nicotine and

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

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

153 Varenicline has been approved in the United States for s

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

155 Varenicline has lower potency and higher efficacy at alp

156 a comorbid psychiatric condition, initiating varenicline in adults even if they are unready to quit,

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

158 Varenicline in combination with NRT was more effective t

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

160 The selectivity of varenicline in decreasing ethanol consumption combined w

161 ial agonist and alpha7 receptor full agonist varenicline in rats that self-administered nicotine but

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

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

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

165 Varenicline increased smoking cessation in smokers with

166 There was little evidence showing that varenicline increased the likelihood of mental health re

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

168 Varenicline-induced activation of lateral orbitofrontal

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

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

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

172 Varenicline is a clinically available, partial agonist a

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

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

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

176 Varenicline is an effective and increasingly prescribed

177 Varenicline is an effective pharmacotherapy to aid smoki

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

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

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

181 Varenicline is effective for smoking cessation in smoker

182 Varenicline is less likely to be prescribed to people wi

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

184 Varenicline is the most efficacious pharmacotherapy curr

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

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

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

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

189 n, and when administered in combination with varenicline, may allow use of lower varenicline doses to

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

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

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

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

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

195 Varenicline offers a treatment option for smokers whose

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

211 The varenicline-placebo and bupropion-placebo risk differenc

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

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

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

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

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

217 ing varenicline rather than bupropion, using varenicline rather than a nicotine patch in adults with

218 Strong recommendations include using varenicline rather than a nicotine patch, using varenicl

219 enicline rather than a nicotine patch, using varenicline rather than bupropion, using varenicline rat

220 ather than using varenicline alone and using varenicline rather than electronic cigarettes.Conclusion

221 ions include combining a nicotine patch with varenicline rather than using varenicline alone and usin

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

223 Varenicline reduced craving and withdrawal and, for thos

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

225 Varenicline reduced nicotine upregulation of alpha4beta2

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

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

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

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

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

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

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

233 95% confidence interval [CI], 0.54-1.73) or varenicline (RR, 1.30; 95% CI, 0.79-2.23).

234 .21-0.85) and no clear evidence of harm with varenicline (RR, 1.34; 95% CI, 0.66-2.66) or nicotine re

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

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

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

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

239 Varenicline's reciprocal actions in the reward-activated

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

241 We conclude that varenicline selectively attenuates the reinforcing effec

242 enerable drug-like scaffolds, Loratadine and Varenicline, show the likely generality of the method fo

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

244 w use of lower varenicline doses to decrease varenicline side effects.

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

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

247 Given the actions of varenicline tartrate and bupropion hydrochloride sustain

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

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

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

251 fidence interval: 42%, 54%) to be prescribed varenicline than NRT, compared to smokers without neurod

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

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

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

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

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

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

258 1:1:1 ratio to receive brief counseling and varenicline titrated to 1 mg twice per day (n = 352), bu

259 NS9283 increased the potency of varenicline to activate and desensitize (alpha4)(3)(beta

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

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

262 Varenicline-treated participants achieved higher abstine

263 Varenicline-treated participants had higher CARs versus

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

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

266 Each varenicline treatment was followed by saline-control tre

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

268 ation (state; administration of nicotine and varenicline, two FDA-approved smoking cessation aids, du

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

270 Varenicline use was also associated with a generalized s

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

272 Exposure was prescription of varenicline versus NRT and the primary outcome was smoki

273 to determine the effectiveness and safety of varenicline versus NRT for smoking cessation in people w

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

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

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

277 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%).

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

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

280 Varenicline was associated with a significantly reduced

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

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

283 Varenicline was more effective than placebo, nicotine pa

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

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

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

287 Varenicline was safe and generally well tolerated, with

288 Varenicline was significantly more efficacious than plac

289 Varenicline was trapped as a weak base in acidic compart

290 with neurodevelopmental disorders prescribed varenicline were 38% more likely to quit smoking (95% co

291 No sex differences in efficacy for varenicline were observed.

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

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

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

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

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

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

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

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

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