Title: How much citalopram is equivalent to 50 ng/ml sertraline? Standardization of serum concentrations of six different SSRIs by measuring serotonin transporter occupancy
Abstract: The serotonin transporter (5-HTT) is the primary target for selective serotonin reuptake inhibitors (SSRI). SSRI are an effective treatment for most mood and anxiety disorders, implying a role for the transporter in the pathophysiology of these diseases. Given the widespread use of SSRI, it is important to understand how plasma concentrations of SSRI relate to 5-HTT occupancy, as there is a weak correlation between oral dose and plasma concentration making it difficult to determine the minimal oral dose necessary to obtain complete blockade of 5-HTT. Positron emission tomography (PET) and Single Photon Emission Computed Tomography (SPECT) imaging studies describe a non-linear relationship reaching a plateau, between SSRI serum concentration and proportion of blockade. Medline and PubMed were searched to identify all PET or SPECT studies examining the serotonin transporter occupancy of SSRI and therapeutic drug monitoring (TDM). 23 articles met inclusion criteria, with information that enables the calculation of the following equation Eact = Emax*cpl/(EC50 + cpl). Whereas Eac is the actual occupation, Emax the maximal occupation, CPL the serum concentration of the chosen SSRI and EC50 the concentration at which 50% of the serotonin transporter is blocked. This equation enables the comparison of the different SSRI. A better comparability of different SSRIs can lead to an alleviated interpretation of clinical studies.
Publication Year: 2011
Publication Date: 2011-09-01
Language: en
Type: article
Indexed In: ['crossref']
Access and Citation
AI Researcher Chatbot
Get quick answers to your questions about the article from our AI researcher chatbot