A typical tricyclic antidepressant. It relieves the depressive state of patients with endogenous depression, but it also reduces thinking ability and concentration, and has an anti-anxiety effect. Its mechanism of action is said to be to prolong the activity of transmitters by inhibiting the reuptake of catecholamines and indolamines released from neurons in the hypothalamus, limbic system, and reticular formation in the central nervous system, and it is thought that it also has an anticholinergic effect. It also has antihistamine and antiserotonin effects. The side chain is demethylated in the body, becoming desmethylimipramine and an active metabolite belonging to tricyclic antidepressants. Side effects include drowsiness, blurred vision, dry mouth, constipation, increased intraocular pressure, orthostatic hypotension, extrapyramidal symptoms, and jaundice. Concomitant use with MAO (monoamine oxidase) inhibitors is contraindicated because it can cause symptoms such as generalized convulsions, fever, and tremors. Source: Encyclopaedia Britannica Concise Encyclopedia About Encyclopaedia Britannica Concise Encyclopedia Information |
代表的な三環系抗うつ剤。内因性うつ病患者の抑うつ状態を取除くが,思考力や集中力の低下,抗不安作用も認められる。作用機序は中枢の視床下部,辺縁系,網様体での神経細胞から遊離した伝達物質のカテコールアミン,インドールアミンなどの再取込みの抑制による伝達物質の活性を持続延長させることにあるといわれ,一部,抗コリン作用の関与も考えられている。抗ヒスタミン,抗セロトニン作用も認められている。体内で側鎖の脱メチル化が起り,デスメチルイミプラミンと三環系抗うつ剤に属する活性代謝物となる。副作用には,ねむけ,かすみ目,口渇,便秘,眼圧亢進,起立性低血圧,錐体外路症状,黄疸などがある。 MAO (モノアミン酸化酵素) 阻害薬との併用は,全身けいれん,発熱,振戦などの症状を起すので禁忌である。
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