抑郁症及其药物治疗李乐华要点.ppt

* With fluvoxamine, activity at sigma receptors might explain its notable efficacy in delusional depression. To date there does not seem to be a conclusive explanation, in terms of it’s pharmacologic profile, for the higher levels of nausea and sedation seen in clinical practice. What positive or negative effects could modulation of sigma neurotransmission add to an SSRI? The “sigma enigma” - it is possible that this could give greater antipsychotic actions to a drug, greater anxiolytic actions to a drug, but it could also increase GI motility. The agents for which sigma properties may be relevant include especially fluvoxamine, but perhaps also sertraline. * One class of antidepressants that combines the actions of both selective reuptake inhibitors and the selective norepinephrine uptake inhibitors is the class of dual serotonin and noradrenergic reuptake inhibitors (SNRIs). Venlafaxine is the only dual-action SNRI currently marketed. Depending on the dose, it has different degrees of inhibition of 5HT reuptake (most potent and therefore present at low doses), NE reuptake (moderate potency) at higher doses, and DA reuptake (least potent and therefore present only at the highest doses. However, there are no significant actions on other receptors. Venlafaxine is now available in an extended-release formulation (venlafaxine XR), which not only allows once daily administration but significantly reduces side effects, especially nausea. The increased tolerability of the extended release formulation is important, especially considering that higher doses of this agent is required to exploit both the 5HT and NE non-selective. * Mirtazapine belongs to the noradrenergic and specific serotonergic antidepressant class of antidepressants called (NaSSA). It’s primary therapeutic action is alpha 2 antagonism. When presynaptic alpha 2 heteroreceptors are blocked, 5HT is released, but it is directed to the 5HT1A receptor, because 5HT actions at 5HT2A, 5HT2C and 5HT3 receptors ar