學名: Mianserin Tablet  (N.V.Organon)
商品名稱: Tolvon

生産商: N.V.Organon



1)  Mianserin is a tetracyclic antidepressant which differs chemically and pharmacologically from tricyclic antidepressants. Mianserin combines presynaptic alpha-adrenergic receptor blocking activity with anti- histaminic and sedative properties, but has little or no central anticholinergic activity, and minimal effect upon central serotoningeric mechanisms (Brogden et al, 1978). Unlike tricyclic antidepressants, which block the uptake of norepinephrine and reduce its turnover, mianserin does not effect norepinephrine uptake and increases it turnover (Brogden et al, 1978; Goodlet et al, 1977).
2)  EEG studies have indicated that mianserin has an EEG profile similar to that of amitriptyline (Fink et al, 1977; Fell et al, 1973; Itil et al, 1972). The unique quality of mianserin which differs greatly from tricyclic antidepressants, is that the drug is less likely to cause cardiotoxicity, anticholinergic effects (and possibly seizures), than tricyclic antidepressants. Overdosage of mianserin does not produce the severe complications observed with tricyclic antidepressants (convulsions, cardiac arrhythmias, respiratory depression, severe hypotension) (Crome et al, 1978; Crome & Newman, 1977).
3)  The effect of mianserin on plasma levels of beta-endorphin immunoreactivity was studied in 8 depressed patients (Drago et al, 1982). Seven patients showed a decreased plasma level of beta-endorphin immunoreactivity and also showed improvement in symptoms assessed by a modified comprehensive psychopathological rating scale. The one patient who did not improve also had decreased beta-endorphin immunoreactivity plasma levels. The role of beta-endorphin in depression is unknown; however, this evidence indicates a possible link. Further research is needed to fully understand the relationship.
4)  The anticholinergic and cardiovascular effects of mianserin in healthy subjects and subjects with cardiovascular disease have been reviewed (Kopera, 1983). Mianserin was devoid of anticholinergic and cardiovascular effects. Mianserin's effect on REM sleep was evaluated in 6 healthy males (Maeda et al, 1991). While REM sleep was suppressed during treatment, no rebound increase in REM sleep was observed after withdrawal of the drug. This data does not support the theory that antidepressant effect is associated with a rise in REM pressure.
5)  Both mianserin and its enantiomers are pharmacologically active (Pinder & van Delft, 1983). A relationship has been found between plasma levels of the S(+) mianserin and improved scores on the Montgomery-Asberg Depression Rating Scale (Mihara et al, 1997). This suggests that the S(+) enantiomer may be responsible for the therapeutic effect. The side effect profile (sedation), may also be attributable to the enantiomers. Mianserin metabolites are also active; therefore response should consider mianserin and desmethylmianserin plasma concentrations. However, it has been suggested that the antidepressant effects of mianserin are due primarily to the parent compound rather than the metabolites (Hand et al, 1991). The dextroenantiomer does have a higher affinity for the 5-HT2 receptor.
6)  Recently, differences were documented in enantiomer activity (Wood et al, 1993). In a rat model, it was found that (-) mianserin had a greater selectivity for the 5-HT3 reception, whereas, (+) mianserin showed greater selectivity for the 5-HT1C and 5-HT2 receptors.


HMG-COA reductase inhibitors (simvastatin,lovastatin) &SSRIs or nefazodone
· SSRIs(fluoxetine)或nefazodone會抑制simvastatin及lovastatin經由CYP3A4代謝
Venlafaxine & antihypertension agents
·高劑量venlafaxine會使血壓升高(dose dependent)
Trazodone & amiodarone
Mianserine & sedative compounds
Nefazodone & CYP3A4 substrates
·Nefazodone會抑制經由CYP3A4代謝之藥物,例如:alprazolam, triazolam, astemizole, cisapride
Mirtazapine &BZDs
Bupropion & lower seizure threshold agents
Bupropion & dopamine agonists
·與Dopamine agonists產生藥物藥效學交互作用


Bradyarrhythmia、Cardiotoxicity、Orthostatic hypotension、Ventricular arrhythmia、Erythema multiforme、Maculopapular eruption、Hyperglycemia、Hypophosphatemia、Isolated prolactin deficiency、Weight gain、Dysphagia、Excessive salivation、Glossitis、Agranulocytosis、Leukopenia、Arthritis、Restless legs syndrome、Delirium、Dyskinesia、Hyperactive behavior、Somnolence、Ototoxicity、Tinnitus、Decreased sexual function is described with the administration of mianserin (Kowalski et al, 1985a).
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