클로미프라민

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H302：삼키면 유해함

  H336：졸음 또는 현기증을 일으킬 수 있음

  H370：장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킴(노출되어도 특정 표적장기 독성을 일으키지 않는다는 결정적인 노출경로가 있다면 노출경로를 기재)

  H410：장기적 영향에 의해 수생생물에 매우 유독함

• 예방조치문구

  P260：분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P270：이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.

  P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

  P273：환경으로 배출하지 마시오.

  P301+P312：삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P304+P340：흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.

  P307+P311：노출된 경우,독성 물질 센터 또는 의사에게 전화하기

  P312：불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P321：(…) 처치를 하시오.

  P330：입을 씻어내시오.

  P391：누출물을 모으시오.

  P403+P233：용기는 환기가 잘 되는 곳에 단단히 밀폐하여 저장하시오.

  P405：밀봉하여 저장하시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

클로미프라민 화학적 특성, 용도, 생산

• 용도

  Antidepressan.

• 정의

  ChEBI: A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressan s, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias.

• Mechanism of action

  Clomipramine is different from the other TCAs, exhibiting preferential selectivity for inhibiting the reuptake of 5-HT at the presynaptic neuronal membrane. Its antidepressant mechanism of action as an inhibitor of the 5-HT transporter is reduced in vivo, however, because of the formation of its active metabolite, N-desmethylclomipramine, which inhibits the reuptake of NE. As a result of its common structure with the other TCAs, clomipramine shares the pharmacological and adverse-effect profile of the other TCAs.
  The efficacy of clomipramine relative to the other TCAs in the treatment of obsessive-compulsive disorder may be related to its potency in blocking 5-HT reuptake at the presynaptic neuronal membrane, suggesting a dysregulation of 5-HT for the pathogenesis of obsessive-compulsive disorder. Clomipramine appears to decrease the turnover of 5-HT in the CNS, probably because of a decrease in the release and/or synthesis of 5-HT.
  Although in vitro studies suggest that clomipramine is approximately four times more potent than fluoxetine as a 5-HT reuptake inhibitor, in vivo studies suggest the opposite. This difference has been attributed to the relatively long elimination half-lives for fluoxetine and its principal serotonergic metabolite norfluoxetine. In addition, metabolism of clomipramine to its N-desmethyl secondary amine metabolite decreases the potency and selectivity of 5-HT -reuptake inhibition of clomipramine, but not fluoxetine.

• Clinical Use

  Clomipramine is considered to be the most powerful antidepressant ever made. This dihydrodibenzazepine TCA, with actions on both the NE and 5-HT transporters, was the last of the major TCAs to come to market. Initially, the U.S. FDA regarded it as another “me-too” drug, and accordingly, they did not license it. Subsequently, however, it was licensed for the treatment of obsessive-compulsive disorders. Clomipramine differs from imipramine only by the addition of a 3-chloro group.

• 부작용

  Male patients taking clomipramine should be informed of sexual dysfunction as a side effect associated with antidepressants having significant serotonergic activity. Sexual dysfunction in men appears as ejaculatory incompetence, ejaculatory retardation, decreased libido, or inability to obtain or maintain an erection. Sexual dysfunction is dose-related and may be treated by simply lowering the drug dose.

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