Chapter category: Neuropharmacology
Clinical Pharmacokinetics of SSRIs
Selective Serotonin Reuptake Inhibitors (SSRIs): Past Present and Future
Edited by: S. Clare StanfordISBN: 1-57059-649-2
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Chapter authors:
Pierre Baumann, Chin B Eap and Pierre Voirol
Citalopram,1 fluoxetine,2,3 fluvoxamine,4 paroxetine5 and sertraline6 are the five anti- depressants which are known as selective serotonin reuptake inhibitors (SSRIs) (Fig. 2.1). Their clinical efficacy, good tolerance and safety have been demonstrated in many studies7,8 and some of them may also be prescribed successfully for the treatment of obsessive compulsive disorder, bulimia or panic attacks. Despite their common pharmacological properties, the SSRIs differ in their metabolism by cytochrome P450 and in their interaction profile with other drugs which are also substrates of this enzyme system. Sensitive and selective (including stereoselective) methods, using high performance liquid chromatography or gas chromatography, have been introduced for their quantitative analysis in blood samples.9 These have enabled studies of their pharmacokinetics as well as investigations of the relationship between plasma concentration and clinical efficacy. This review summarizes our present knowledge of the metabolism, pharmacokinetics and pharmacogenetics of this group of antidepressants.
Additional chapters from this book:
SSRIs: Where Now, Where Next?
David J. Heal and Sharon C. Cheetham
It is interesting to note that in the title of their review on fluoxetine (`Prozac',Lilly), Wong, Bymaster and Engleman1 describe this drug as "the first selective serotonin...
The Mechanism of Action of SSRIs:A New Hypothesis
Lori L. Davis, Kimberly A. Yonkers, Madhukar Trivedi, Gerald L.Kramer and Frederick Petty
The introduction of the selective serotonin reuptake inhibitors (SSRIs) into medical treatment in the 1980s revolutionized psychiatric practice and fueled the interest in the role of seroto...
SSRI-Induced Changes in Catecholaminergic Transmission
S. Clare Stanford
The selective serotonin reuptake inhibitors (SSRIs) are a chemically diverse group of compounds which share the characteristic of potently inhibiting neuronal reuptake of serotonin (5-hydroxyt...
SSRI-Induced Functional Changes in Serotonergic Neurons
Ildefonso Hervás, Andreu Raurich, Luz Romero, Roser Cortés and Francesc Artigas
The term `SSRIs' encompasses several chemical agents that have in common their ability to inhibit selectively the function of the serotonin (5-hydroxytryptamine, 5-HT) transporter. This is loc...
Mechanism of Action of Different Classes of Antidepressants: Evidence from 5-HT Challenge Studies
Ian M. Anderson and Christopher Mortimore
The discovery in the 1950s that imipramine and iproniazid had antidepressant properties was soon followed by the recognition that they acted on monoamine systems. This laid the foundation f...
SSRIs and Suicide
John A. Henry and Carol A. Rivas
The selective serotonin reuptake inhibitors (SSRIs) have increased in popularity and extent of use since their introduction. At the same time, our knowledge concerning the relationship between...
SSRIs and Sexual Function
Peter A. Sargent and Guy M. Goodwin
Human sexual dysfunction is described in ICD-101 under broad categories, reflecting the pragmatic division of the normal sexual response, into phases of desire, arousal, orgasm and ...
SSRIs, Drug Withdrawal and Abuse: Problem or Treatment?
C. Heather Ashton and Allan H. Young
Selective serotonin reuptake inhibitors (SSRIs) have considerable advantages over earlier antidepressants, such as most tricyclic antidepressants (TCAs) and monoamine oxidase inhibitors (MA...
SSRIs and Patient Groups with Specific Treatment Problems
John Hughes, Brian Lunn and John O'Brien
Selective serotonin reuptake inhibitors (SSRIs), whilst initially launched solely as anti- depressants, have been used increasingly as treatments for other disorders and in patients who are vu...
SSRIs in Depression: Distinctive Actions?
Julie Newman and Andrew A. Nierenberg
The introduction of the selective serotonin reuptake inhibitors (SSRIs) has radically changed the treatment of depression worldwide. The five currently marketed SSRIs, fluoxetine, sertraline, ...
Clinical Pharmacokinetics of SSRIs
Pierre Baumann, Chin B Eap and Pierre Voirol
Citalopram,1 fluoxetine,2,3 fluvoxamine,4 paroxetine5 and sertraline6 are the five anti- depressants which are known as selective seroton...
The Discovery of The SSRIs: A Milestone In Neuropsychopharmacology and Rational Drug Design
Arvid Carlsson
Besides being a major therapeutic advance, the selective serotonin reuptake inhibitors (SSRIs) have become important tools in basic and clinical brain research. They were the first drugs to...

