Determination of Mianserin and Metabolites in Plasma by Liquid Chromatography with Electrochemical Detection

Suckow, Raymond F.; Cooper, Thomas B.; Quitkin, Frederic M.; Stewart, Jonathan W.

doi:10.1002/jps.2600710812

Cited by 29 publications

(3 citation statements)

References 10 publications

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“…On the same day as the clinical ratings, blood samples were obtained about 12 h (between 11 and 13 h) after a bedtime dose. Plasma concentrations of mianserin and desmethylmianserin were measured in duplicate by the HPLC method of Suckow et al (1982). In individual cases a plasma concentration at steady state (CJ; an average of 3 weeks' measurements was calculated for mianserin, desmethylmianserin, and mianserin plus desmethylmianserin.…”

Section: Methodsmentioning

confidence: 99%

“…Desmethylmianserin is the major metabolite of mianserin in plasma (Suckow et al, 1982;Kondo et al, 1989). As reviewed by Pinder and van Delft (1 983) desmethylmianserin retains pharmacological properties indicative of antidepressant activity; it is slightly less potent than the parent compound as a noradrenaline uptake inhibitor and an antagonist at presynaptic adrenoceptors, but is more active as a serotonin uptake inhibitor.…”

Section: Introductionmentioning

confidence: 99%

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Is there a therapeutic window for plasma concentration of mianserin plus desmethylmianserin?

Otani

Kaneko

Sasa

et al. 1991

Human Psychopharmacology

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The relationship between clinical effects and plasma concentrations of mianserin and desmethylmianserin was studied in 29 cases of major depression during 3 weeks of mianserin treatment. The daily dose of mianserin was 30 mg in 27 cases and 20 mg in two cases. There was a significant U-shaped relationship between the final Montgomery Asberg Depression Rating Scale (MADRS) score and the steady-state plasma concentration of mianserin (p < 0.05) or desmethylmianserin (p < 0.05). A much stronger relationship was observed for mianserin plus desmethylmianserin @<0.001). A theoretical therapeutic window (where a final MADRS score was expected to be 10 or less) was 71-128 nmol/l for mianserin, 34-61 nmol/l for desmethylmianserin, and 101-183 nmol/l for mianserin plus desmethylmianserin. The proportion of responders was significantly higher inside than outside the window for mianserin plus desmethylmianserin (p =0,0033), but not for mianserin (p =0.063) or for desmethylmianserin (p =0.077). The occurrence of subjective side-effects was not dependent on the plasma concentrations of these compounds. The present study suggests that desmethylmianserin contributes substantially to the overall antidepressant effects of mianserin treatment, and that the therapeutic response is most dependent on the combined plasma concentration of mianserin and desmethylmianserin, with an optimal therapeutic response occurring in the intermediate range.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Is there a therapeutic window for plasma concentration of mianserin plus desmethylmianserin?

Otani

Kaneko

Sasa

et al. 1991

Human Psychopharmacology

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“…So far, there is no information on the simultaneous chromatographic separation of 4-arylpiperazines such as ziprasidone and aripiprazole and their oxidative impurities. In addition, spectrophotometric and HPLC methods have been developed and applied for the determination of benzothiazepine analogs such as olanzapine, mianserin, and quetiapine [21][22][23][24][25]. Recent advances in the fundamental understanding and practical relevance of the dual hydrophilic/reversed-phase regime indicate the successful application of mixed-mode chromatographic conditions in the investigation of serotonin receptor ligands and their related compounds [26][27][28].…”

Section: Introductionmentioning

confidence: 99%

Development of HPLC method for rapid profiling of serotonin receptor ligands and their oxidative degradants

Obradović

Savić

Joksimović

et al. 2023

Preprint

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The serotonin receptor ligands and their related compounds are used for the treatment of central nervous system (CNS)-related disorders. The retention profile of six serotonin receptor ligands such as aripiprazole, ziprasidone, risperidone, olanzapine, mianserin, and quetiapine was investigated on two stationary phases that differ in polarities (C8 alkyl and pentafluorophenylpropyl (PFP)). The design of experiments (DoE) methodology was used to define the retention mechanism and to produce acceptable separation results. The chromatographic conditions that provide the best selectivity characteristics are considered for the separation of structurally related oxidative impurities. The selected conditions (C8 stationary phase, 40% acetonitrile, 20mM ammonium acetate, 25 ℃) showed better sensitivity and improved selectivity in the separation of aripiprazole, ziprasidone, and their oxidative degradants compared to the already developed high-performance liquid chromatography methods. The selected method was validated for the determination of aripiprazole in pharmaceutical forms and was found to be selective, sensitive, precise, accurate, and robust. It can be used as a basis for rapid chromatographic profiling of serotonin receptor ligands and their related impurities.

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Mianserin suppositories in the treatment of post-operative delirium

Nakamura

Uchimura

Yamada

et al. 1997

Hum. Psychopharmacol. Clin. Exp.

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Mianserin suppositories (10–90 mg) were administered at bedtime to 16 patients with post‐operative delirium (mean age 69·5 years). By the Delirium Rating Scale (DRS: Trzepacz et al., 1988), the average score decreased from 21·2 prior to administration to 14·5 on the first day of treatment and to 7·1 on the seventh day. Improvement was observed in all cases (marked in 85 per cent and slight in 15 per cent). The plasma concentration of mianserin was 65 ng/ml on day 1, 93 ng/ml on day 3 and 65 ng/ml on day 5, having reached therapeutic levels within 24 h of beginning treatment. Decreases in the free‐3‐methoxy‐4‐hydroxyphenyl(ethylene)glycol (MHPG) concentrations in plasma were observed after drug administration, but free‐homovanillic acid (HVA) concentrations in plasma showed no significant change with the drug treatment. We consider mianserin suppositories to be an effective treatment for post‐operative delirium. © 1997 John Wiley & Sons, Ltd.

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Determination of Mianserin and Metabolites in Plasma by Liquid Chromatography with Electrochemical Detection

Cited by 29 publications

References 10 publications

Is there a therapeutic window for plasma concentration of mianserin plus desmethylmianserin?

Is there a therapeutic window for plasma concentration of mianserin plus desmethylmianserin?

Development of HPLC method for rapid profiling of serotonin receptor ligands and their oxidative degradants

Mianserin suppositories in the treatment of post-operative delirium

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