主條目:Antidepressant、Reuptake inhibitor再回收抑制劑RI
藥化[]
- 為三個環,三級胺或是二級胺。
- 三級胺可以抑制norepinephrine 和 serotonin ,分別造成CNS stimulation和mood elevation
- 二級胺為SNRI:CNS stimulation效果較好。
- mood elevation 的 onset is slow, 需要兩週甚至更久。
- 對一般人(normal individuals)不會造成CNS stimulation或mood elevation的效果。
代謝[]
機轉和副作用[]
mood elevation[]
- Tricyclic antidepressants (TCAs) 抑制 norepinephrine 和 serotonin 的再回收,
CNS stimulation[]
但是其中有部份因為對NET的抑制作用強所以歸類為SNRI(二級胺),SNRI中的amoxepine和maprotiline又屬於第二代抗憂鬱藥
side effect[]
- TCAs also block serotonergic, α-adrenergic, histaminic, and muscarinic receptors. Actions at these receptors are probably responsible for many of the untoward effects of the TCAs.
- SNRI的副作用和他相同
治療學[]
憂鬱症[]
panic disorders[]
bed-wetting(尿床/夜尿,不是夜拍。) in children (older than six years)[]
chronic pain (‘neuropathic’ pain) in which the cause of the pain is unclear.[]
- TCAs, particularly amitriptyline
例子[]
- tertiary amines
- the prototypic drug:imipramine
- amitriptyline
- clomipramine
- doxepin
- trimipramine
- secondary amines: selective NE reuptake inhibitor
副作用[]
- 源自於α-adrenergic receptors的阻斷: orthostatic hypotension and reflex tachycardia.
- 源自於acetylcholine receptors的阻斷:blurred vision, xerostomia (dry mouth), urinary retention, constipation, and glaucoma的惡化(aggravation) and epilepsy.
- Weight gain體重增加和Sexual dysfunction性功能障礙.
毒性[]
- 有心血管毒性,會引起心律不整和其他嚴重的心血管問題(the inducement of cardiac arrhythmias and other serious cardiovascular problems).,所以被小心使用。
藥物連用的效果[]
- 長期治療憂鬱不會失去效果(loss of effectiveness.)
- Physical and psychological dependence(依賴)有被報告,所以必須慢慢地停藥(necessitating slow withdrawal)。
Precautions[]
- TCAs有窄的治療指數(a narrow therapeutic index),諸如5~6倍的單日imipramine最高劑量(five-to six-fold the maximal daily dose)就會致死(lethal)(a.)。
- TCAs用在manic-depressive patients(雙極性病患、躁鬱症(一下子躁症;一下子憂鬱症的病患))要小心,因為可能會引發躁症發作(may unmask manic behavior)。