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Serum levels of maprotiline and its adverse effects on depressed patients
1Department of Neuropsychiatry, Faculty of Medicine, Toyama Medical and Pharmaceutical University, Japan.
Abstract:
The relationships between the side effects of maprotiline (MPT) and the serum concentration of MPT and desmethylmaprotiline (DMPT) were investigated with 27 blood samplings in 15 depressed inpatients. There were significant correlations between the side effects and serum levels of MPT and DMPT. Mild side effects frequently occurred at levels of more than 130 ng/ml of MPT and 70 ng/ml of DMPT. At more than 220 ng/ml of the MPT levels and 110 ng/ml of DMPT levels, severe side effects occurred. Nearly sigmoidal serum level/side effect response curves occurred with both compounds.
Insights
Maprotiline (MPT) and desmethylmaprotiline (DMPT) serum levels correlate significantly with side effects in depressed patients. Mild side effects appeared above 130 ng/ml MPT and 70 ng/ml DMPT, severe effects above 220 ng/ml MPT and 110 ng/ml DMPT.
Area of Science:
- Pharmacology
- Clinical Psychology
- Neuroscience
Background:
- Maprotiline is a tetracyclic antidepressant.
- Understanding the relationship between drug concentration and side effects is crucial for therapeutic drug monitoring.
Purpose of the Study:
- To investigate the correlation between maprotiline (MPT) and desmethylmaprotiline (DMPT) serum concentrations and their associated side effects.
- To establish therapeutic ranges for MPT and DMPT serum levels concerning side effect occurrence.
Main Methods:
- Blood samples were collected from 15 depressed inpatients undergoing maprotiline treatment.
- 27 blood samplings were analyzed for MPT and DMPT serum concentrations.
- Side effects were systematically recorded and correlated with measured serum levels.
Main Results:
- Significant correlations were found between MPT/DMPT serum levels and the incidence/severity of side effects.
- Mild side effects were common at MPT levels >130 ng/ml and DMPT levels >70 ng/ml.
- Severe side effects occurred at MPT levels >220 ng/ml and DMPT levels >110 ng/ml.
- Sigmoidal serum level/side effect response curves were observed for both MPT and DMPT.
Conclusions:
- Therapeutic drug monitoring of maprotiline and desmethylmaprotiline is recommended to minimize side effects.
- Establishing specific serum concentration thresholds can guide dose adjustments for improved patient safety and treatment efficacy.