商品名：Mirataz (transdermal), Remeron (human)
The antidepressant activity of mirtazapine appears to be mediated by antagonism at central pre-synaptic alpha2-receptors, which normally act as a negative feedback mechanism that inhibits further norepinephrine (NE) release. By blocking these receptors, mirtazapine overcomes the negative feedback loop and results in a net increase in NE. This mechanism may also contribute to the appetite stimulating effects of the medication since NE acts at other a-receptors to increase appetite. Additionally, mirtazapine antagonizes several serotonin (5HT) receptor subtypes. The drug is a potent inhibitor of the 5HT2 and 5HT3 receptors and of histamine (H1) receptors. Antagonism at the 5HT3 receptors accounts for the anti-nausea and antiemetic effects of the drug, and its action at H1receptors produces prominent sedative effects. It is a moderate peripheral alpha1 adrenergic antagonist, a property that may explain the occasional orthostatic hypotension associated with its use; it is a moderate antagonist of muscarinic receptors, which may explain the relatively low incidence of anticholinergic effects.
Misoprostol may be useful as primary or adjunctive therapy in treating or preventing gastric ulceration, especially when caused or aggravated by non-steroidal antiinflammatory drugs (NSAIDs). Misoprostol is most useful to prevent GI ulceration or GI adverse effects (anorexia, vomiting) associated with NSAID therapy. While it can be used for treating gastric ulcers, other drugs are probably just as effective and less expensive. It does not appear to be very effective in reducing gastric ulceration secondary to high dose corticosteroid therapy Misoprostol may be efficacious in reducing or reversing cyclosporine-induced nephrotoxicity. More data is needed to confirm this effect. One study demonstrated that misoprostol can reduce the clinical signs associated with atopy somewhat in dogs. Misoprostol’s effects on uterine contractibility and cervical softening/opening make it effective as an adjunctive treatment in pregnancy termination.
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