エスゾピクロン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

  H361：生殖能または胎児への悪影響のおそれの疑い

• 注意書き

  P201：使用前に取扱説明書を入手すること。

  P202：全ての安全注意を読み理解するまで取り扱わないこ と。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P281：指定された個人用保護具を使用すること。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P308+P313：暴露または暴露の懸念がある場合：医師の診断/手当てを 受けること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P332+P313：皮膚刺激が生じた場合：医師の診断/手当てを受けるこ と。

  P362：汚染された衣類を脱ぎ、再使用す場合には洗濯をすること。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

エスゾピクロン 価格

エスゾピクロン 化学特性,用途語,生産方法

• 効能

  催眠鎮静薬

• 商品名

  ルネスタ (エーザイ)

• 説明

  Eszopiclone is a non-benzodiazepine hypnotic agent indicated for the treatment of insomnia to induce sleep and for sleep maintenance. It has similar pharmacokinetic and pharmacodynamic parameters as the previously marketed non-benzodiazepine hypnotics zolpidem and zaleplon. However, unlike its predecessors, eszopiclone is not restricted to short-term treatment of insomnia. Clinical studies of up to 6 months of use show that patients do not develop tolerance to its effect. Eszopiclone is the (S)-enantiomer of zopiclone, which has been marketed as the racemic mixture in Europe for almost 20 years. These agents belong to the cyclopyrrolone class of drugs that act as agonists at the type A GABA receptor. Eszopiclone has approximately 50-fold higher binding affinity than its antipode (R)-zopiclone for GABA-A receptor (IC₅₀=21 and 1130 nM, respectively). In addition, the two enantiomers exhibit significant differences in their pharmacokinetic parameters and in vivo efficacy. In healthy volunteers, eszopiclone has 2-fold higher C_max and 2-fold greater elimination half-life than the (R)-enantiomer.The two most frequent adverse events associated with eszopiclone treatment are unpleasant taste and headache. Other less frequent side effects include somnolence, dry mouth, and nausea.

• 化学的特性

  White To Pale Yellow

• 使用

  Eszopiclone is the active stereoizomer of Zopiclone and belongs to the class of drug known as cyclopyrrones. It is a nonbenzodiazepine hypnotic agent used as a treatment for insomnia. This is a controlled substance (depressant) in the US but not in Canada.

• 定義

  ChEBI: The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-te m use.

• 作用機序

  The cyclopyrrole zopiclone is described as a “superagonist” at BZRs with the subunit composition α1β2γ2 and α1β2γ3, because it potentiates the GABA-gated current more than the benzodiazepine (flunitrazepam) reference agonist. Racemic zopiclone has been available in Europe since 199,2 and the higher affinity S-enantiomer (eszopiclone) was marketed in the United States in 2005, primarily to treat insomnia, because of its rapid onset and moderate duration (half-life, ~6 hours) of hypnotic-sedative effect. Less than 10% of orally administered eszopiclone is excreted unchanged, because it undergoes extensive CYP3A4- and CYP2E1-catalyzed oxidation and demethylation to metabolites excreted primarily in urine. "

• 薬物動態学

  Zoplicone was originally marketed as a racemic mixture; however, because the sedative activity is primarily associated with the S-isomer, only the S-isomer is currently marketed in the United States (as esozoplicone) (36). It is soluble in dilute mineral acids. Unlike zolpidem and zaleplon, eszoplicone is not as specific for the α1 subunit of GABAA, but it binds broadly, like the benzodiazepines (Table 19.2). Its pharmacological and pharmacodynamic activities, however, are more closely related to those of the nonbenzodiazepines. It is rapidly absorbed, with an oral bioavailability of approximately 80%, reaching peak concentrations in 1 h and having a relatively long elimination half-life of approximately 6 hours (Table 19.2). Eszopliclone is primarily metabolized to (S)-zoplicone N-oxide and (S)-N-desmethylzoplicone by the CYP3A4. (S)-Ndesmethylzopiclone binds to GABA receptors with substantially lower potency than eszopiclone, and (S)-zopiclone-N-oxide shows no significant binding to this receptor. It does not accumulate with once-daily administration, and it exhibits linear (dose-proportional) pharmacokinetics over the range of 1 to 6 mg. Eszopiclone is weakly bound to plasma protein (52–60%), suggesting that eszopiclone distribution should not be affected by drug–drug interactions caused by protein binding. Up to 75% of an oral dose of racemic zopiclone is excreted in the urine, primarily as metabolites. A similar excretion profile would be expected for eszopiclone. Less than 10% of the orally administered eszopiclone dose is excreted in the urine as unchanged drug. After a high-fat meal, peak plasma concentrations can be delayed by approximately 1 hour without affecting its half-life.

• 代謝

  The effects of eszoplicone on sleep onset may be reduced if it is taken either with or immediately after a high-fat/heavy meal. In elderly subjects, the elimination half-life was prolonged to approximately 5 to 9 hours. Therefore, in elderly patients, the starting dose should be decreased to 1 mg, and the dose should not exceed 2 mg. No dose adjustment is necessary in patients with renal impairment, because less than 10% of the orally administered eszopiclone dose is excreted in the urine as parent drug. Although no pharmacokinetic or pharmacodynamic or drug interactions have been reported for eszopiclone, potent inhibitors of CYP3A4 could increase plasma levels of eszopiclone. Eszopiclone does not alter the clearance of drugs metabolized by common CYP450 enzymes. Potential pharmacodynamic interactions (additive pharmacological effects) with CNS depressants such as alcohol, anticonvulsants, antihistamines, antidepressants, or other psychotropic drugs could occur. Dosage adjustment may be necessary when eszopiclone is administered with CNS depressants; concomitant use with alcohol should be avoided.
  The primary advantage of eszoplicone is that it has been shown to be effective in chronic insomnia (long-term treatment) in measures of sleep latency, total sleep time, and wake time after sleep onset without development of tolerance. Eszoplicone would appear to be most effectively used for patients who tend to awaken during the night rather than patients for whom the primary problem is initiating sleep.

エスゾピクロン 生産企業

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