Evaluation of the pharmacokinetics, safety and clinical efficacy of sertraline used to treat social anxiety

  title={Evaluation of the pharmacokinetics, safety and clinical efficacy of sertraline used to treat social anxiety},
  author={Roberto Mandrioli and Laura Mercolini and Maria Augusta Raggi},
  journal={Expert Opinion on Drug Metabolism \& Toxicology},
  pages={1495 - 1505}
Introduction: Social anxiety disorder (SAD) is an emerging, often invalidating, syndrome with deep personal, social and psychological implications. While multiple treatment strategies exist, presently none of them can be considered superior to all others. Areas covered: The aim of this review is to provide the latest information on sertraline (SRT), one of the most important selective serotonin reuptake inhibitors (SSRIs) currently used for the pharmacological therapy of SAD. A literature… 
Discontinued anxiolytic drugs (2009 – 2014)
This review presents candidate drugs that were investigated for the treatment of anxiety-spectrum disorders and then discontinued between the 2009 and 2014 period, finding that repurposed drugs may provide some benefit in the future.
Molecular Basis of the Leishmanicidal Activity of the Antidepressant Sertraline as a Drug Repurposing Candidate
Sertraline killed Leishmania through a multitarget mechanism of action, tackling essential metabolic pathways of the parasite, and is a valuable candidate for visceral leishmaniasis treatment under a drug repurposing strategy.
Psychotropic drugs and liver disease: A critical review of pharmacokinetics and liver toxicity
The authors carefully review the pharmacokinetic disturbances induced by end-stage liver disease and the potential of psychopharmacological agents for liver toxicity.
The antidepressant sertraline provides a novel host directed therapy module for augmenting TB therapy
A novel host directed adjunct therapy regimen for TB with a clinically approved anti-depressant is advocated to achieve quicker and greater control of infection.
In Vitro Activity of Sertraline, an Antidepressant, Against Antibiotic-Susceptible and Antibiotic-Resistant Helicobacter pylori Strains
Results indicate that sertraline, an antidepressant substance, may be a promising anti-H.
High dose sertraline monotherapy fails to protect rhesus macaques from lethal challenge with Ebola virus Makona
It is demonstrated that high dose sertraline monotherapy provided no benefit for the prevention of Ebola virus disease in rhesus macaques with regards to reduction of viral load, morbidity, or survival highlighting the challenges of translating results between in vitro and in vivo models.
Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway.
  • Si Chen, J. Xuan, Lei Guo
  • Biology
    Toxicological sciences : an official journal of the Society of Toxicology
  • 2014
The findings suggest that sertraline induced apoptosis in HepG2 cells at least partially via activation of the TNF-MAP4K4-JNK cascade signaling pathway.
Sertraline induces endoplasmic reticulum stress in hepatic cells.
Glycosylated Sertraline-Loaded Liposomes for Brain Targeting: QbD Study of Formulation Variabilities and Brain Transport
Screening the formulation and process variables affecting the performance of sertraline-loaded pegylated and glycosylated liposomes for further scale-up processes revealed remarkable interaction between Ser-HCl and the charging agent to determine drug entrapment and leakage.
Utilization of Liver Microsomes to Estimate Hepatic Intrinsic Clearance of Monoamine Oxidase Substrate Drugs in Humans
Values of MAO substrate drugs can be quantitatively estimated with HLMs and could be used for semi-quantitative prediction of CLint,vivo values, and numerous proteins localized on inner and outer membranes of mitochondria were detected in both HL Ms and HLMt.


An evidence-based review of the clinical use of sertraline in mood and anxiety disorders.
Sertraline is as effective as other antidepressants over a wide range of indications but may offer tolerability benefits as well as efficacy in patients with psychiatric and/or medical comorbidities and certain subtypes of depression.
Clinical outcome and tolerability of sertraline in major depression A study with plasma levels
  • M. Mauri, V. Laini, G. Panza
  • Psychology, Medicine
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 2002
Multidimensional effects of sertraline in social anxiety disorder
Among common physiological symptoms in this population, blushing and palpitations appear more treatment responsive than trembling and sweating to acute treatment with sertraline, as well as across the spectrum of fear, avoidance, and physiological arousal in generalized SAD (GSAD).
Selective serotonin reuptake inhibitors (SSRIs): therapeutic drug monitoring and pharmacological interactions.
The main pharmacodynamic and pharmacokinetic properties of the six commercially available SSRIs are described, focusing on side and toxic effects, chemical-clinical correlations, interactions with other drugs, the role of therapeutic drug monitoring (TDM) and related bioanalytical methodologies.
Pharmacokinetic drug interaction potential of selective serotonin reuptake inhibitors
  • R. Lane
  • Medicine, Biology
    International clinical psychopharmacology
  • 1996
Knowing the substrates and inhibitors of CYP isoenzymes may help clinicians to anticipate and avoid pharmacokinetic drug interactions and may better define rational prescribing practices.
Efficacy of sertraline in severe generalized social anxiety disorder: results of a double-blind, placebo-controlled study.
The results of the current study confirm the efficacy and tolerability of sertraline in the treatment of severe social anxiety disorder.
The selective serotonin reuptake inhibitor sertraline: its profile and use in psychiatric disorders.
Sertraline's efficacy for both mood and anxiety disorders, relatively weak effect on the cytochrome P450 system, and tolerability profile and safety in overdose are factors that contribute to make it a first-line agent for treatment in both primary and tertiary care settings.
Sertraline in the treatment of anxiety disorders
A comparison of sertraline with other pharmacotherapeutic options shows it to be at least equivalent to other medications for anxiety disorders.
Sertraline: A Review of its Therapeutic Use in Post-Traumatic Stress Disorder
Sertraline has demonstrated efficacy in the treatment of PTSD, particularly in female patients and in non-combat-induced PTSD, and is generally well tolerated, and appears to have a lower potential for drug interactions than other SSRIs, although direct comparisons are lacking.
Clinical Pharmacokinetics of Sertraline
Sertraline is a naphthalenamine derivative with the predominant pharmacological action of inhibiting presynaptic reuptake of serotonin from the synaptic cleft that is well tolerated in therapeutic dosages and relatively safe in overdosage.