No abstract

Antidepressants have different receptor binding profiles, which are related to therapeutic action and adverse drug reactions. We constructed a model to classify antidepressants on the basis of their binding properties of most common transporter-and receptor sites. Receptor binding was quantified by calculating receptor occupancy for the 5-HT (serotonin) reuptake transporter, norepinephrinic reuptake transporter, 5-HT 2C -receptor, M 3 -receptor, H 1 -receptor and 1 -receptor. To identify groups of antidepressants that show similar patterns of receptor occupancy for different receptors, hierarchical cluster analysis (HCA) and principle component analysis (PCA) were used. In addition, to visualize (a)symmetry between binding profiles of antidepressants, radar plots were constructed. On the basis of both analyses, four clusters of antidepressants which exert similar pharmacological properties were identified. Potentially, this model could be a helpful tool in medical practice and may be used as a prediction model for adverse effects of drugs entering the market.

No abstract

4 original studies were selected on strategies to influence CYP metabolism. 2 studies on influencing CYP2D6 metabolism, 2 studies on influencing CYP1A2 metabolism. In all studies an effect of this influence was present.Ample clinical evidence is present, but shows promising results. Pharmacokinetic knowledge can and should be used in clinical settings to optimize pharmacotherapy for vulnerable patients. Also the access to expensive medication can be increased by reduction of high dosage schemes.