From Dirty Drugs to Hyperselectivity and Part Way Back Again
✍ Scribed by M. Briley
- Publisher
- John Wiley and Sons
- Year
- 1997
- Tongue
- English
- Weight
- 99 KB
- Volume
- 12
- Category
- Article
- ISSN
- 0885-6222
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✦ Synopsis
Tricyclic antidepressants (TCAs) are eective in the treatment of depression, but their usefulness is limited by adverse eects resulting from binding to muscarinic, histaminergic and other receptors. Selective serotonin reuptake inhibitors (SSRIs) have a more favourable tolerability pro®le, but their selectivity for serotonin reuptake appears to be associated with some decrease in ecacy, particularly in severe depression. Milnacipran is a new serotonin and noradrenaline reuptake inhibitor that has been developed for the treatment of depression. It inhibits monoamine reuptake both in vitro and in vivo, but does not bind to neurotransmitter receptors. Furthermore, milnacipran has no eect on auto-or heteroreceptors, and no adaptive changes in receptor function occur during longterm treatment. Milnacipran has been shown to be eective in behavioural tests of noradrenergic or serotonergic activity, and in animal models of depression; no sedative, stimulant or anticholinergic eects have been observed. It has a favourable pharmacokinetic pro®le, as it does not accumulate during repeated administration, does not form active metabolites, and is unlikely to interact signi®cantly with other drugs. Milnacipran, therefore, may oer therapeutic advantages, potentially combining the ecacy of TCAs with the good tolerability pro®le of SSRIs.