Clinical effects of pharmacological variations in selective serotonin reuptake inhibitors: an overview

  title={Clinical effects of pharmacological variations in selective serotonin reuptake inhibitors: an overview},
  author={Jos{\'e} Luis Carrasco and C Sandner},
  journal={International Journal of Clinical Practice},
  • J. CarrascoC. Sandner
  • Published 1 December 2005
  • Psychology, Biology
  • International Journal of Clinical Practice
Although the selective serotonin reuptake inhibitor (SSRI) class of antidepressants shares a common primary pharmacology, namely the inhibition of serotonin reuptake, their secondary pharmacology is remarkably heterogeneous. Inhibition of serotonin reuptake and the consequent increase in serotonin availability are responsible for the relief of depressive symptoms and for some of the adverse effects of this class of drugs. Transsynaptic effects such as modulation of signalling cascades, gene… 

The genetics of selective serotonin reuptake inhibitors.

Tolerability of Selective Serotonin Reuptake Inhibitors

It is recommended in the elderly that SSRIs should be titrated slowly to recommended therapeutic doses and used cautiously with other agents known to have the potential for drug interactions, although the overall evidence is weak.

Resistance to selective serotonin reuptake inhibitors: role of serotonergic mechanisms

Boosting 5-HT neurotransmission might be a useful strategy to restore the antidepressant effect in treatment-resistant depressed patients and remark on the inter-strain comparison of mice with a spontaneous tryptophan hydroxylase-2 mutation as a useful tool for understanding the mechanism underlying the response to SSRIs and testing new potential therapeutic strategies.

Selective Serotonin Reuptake Inhibitors and Associated Bleeding Risks: A Narrative and Clinical Review.

The bleeding risk associated with this class of medication merits further study, as three studies have found that SSRIs are not associated with increased bleeding and/or increased perioperative risk, while others have demonstrated that SSRs are associated with an increased risk inperioperative use.

Receptor targets for antidepressant therapy in bipolar disorder: an overview.

Roles of σ1 receptors in the mechanisms of action of CNS drugs

Positron emission tomography with the σ1 specific ligand carbon-11-labelled 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine ([11C]SA4503) indicated that fluvoxamine and donepezil can bind to ρ1 receptors in the healthy human brain in a dose-dependent manner.

Chirality of Modern Antidepressants: An Overview

The current review deals with chiral antidepressant drugs; presenting examples of stereoselectivity in the pharmacological actions of certain antidepressants and their metabolites and emphasizing the differences between pharmacological action of the racemates and pure enantiomers.

Review: Pharmacogenetic aspects of the effect of cytochrome P450 polymorphisms on serotonergic drug metabolism, response, interactions, and adverse effects

This review examines the genetically variable CYP450-mediated metabolism of a number of serotonin-active drugs that are often implicated in cases of serotonin toxicity, to assess the impact of pharmacogenetics on drug metabolism, response, interactions and adverse effects.

Pharmacological interaction with the sigma1 (σ1)-receptor in the acute behavioral effects of antidepressants.

The behavioral effects induced by mixed σ(1)-receptor/SSRI antidepressants, like fluvoxamine or sertraline, may involve a non-selective action at both targets, and the CFS appears to more reliably uncover a �o(1) pharmacological component in antidepressant screening.

Transgenic elimination of high-affinity antidepressant and cocaine sensitivity in the presynaptic serotonin transporter

Transgenic mice in which high-affinity recognition of multiple antidepressants and cocaine is eliminated are developed and it is established directly that SERT is the sole protein responsible for selective 5-HT reuptake inhibitor-mediated alterations in 5-hydroxytryptamine clearance, in5-HT1A autoreceptor modulation of raphe neuron firing, and in behaviors used to predict the utility of antidepressants.



Selective serotonin reuptake inhibitors in affective disorders — I. Basic pharmacology

There are important clinical differences among the SSRIs in their pharmacokinetic characteristics including differences in their half-lives, linear versus non-linear pharmacokinetics, effect of age on their clearance and their potential to inhibit drug metabolising cytochrome P450 (CYP) isoenzymes.

Sertraline: a new antidepressant.

Sertraline exhibits acute antidepressant effects in the dose range 50 to 200 mg/day; in the same dose range it prevents recurrence of depression and its side-effect profile is similar to that of drugs of the same class (dry mouth, nausea, and diarrhea being the most prominent).

Neuropharmacology of Paradoxic Weight Gain with Selective Serotonin Reuptake Inhibitors

A neuropharmacologic rationale for the apparent paradoxic effects of SSRIs on appetite appears to rest on the interaction of 5HT with multiple mechanisms, with the extent of weight gain observed being dependent on subtle, yet important pharmacologic differences within the group.

Comparison of the Effects of Antidepressants and Their Metabolites on Reuptake of Biogenic Amines and on Receptor Binding

The present survey compares the effects of antidepressants and their principal metabolites on reuptake of biogenic amines and on receptor binding to suggest that both dopaminergic and noradrenergic components play a role and that the hydroxybupropion metabolite contributes significantly to the antidepressant activity.

Adverse effects associated with selective serotonin reuptake inhibitors and tricyclic antidepressants: a meta-analysis.

SSRIs and TCAs are both associated with adverse effects, although the key effects differ between the drug classes, and there were no statistically significant differences between drug classes in terms of drop-outs due to adverse effects.

Neurotransmitter receptor and transporter binding profile of antidepressants and their metabolites.

Novel findings, not widely described previously, suggest that many of the individual drugs studied in these experiments possess some structural characteristic that determines affinity for several G protein-coupled, but not muscarinic, receptors.

Citalopram. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depressive illness.

Preliminary data suggest that citalopram may be particularly useful in patients who cannot tolerate the anticholinergic or cardiovascular side effects of tricyclic antidepressants and in those for whom sedation is not indicated.

Side effects of long-term treatment with fluoxetine.

This work reports for the first time on two cases of late-onset adverse effects occurring 6 and 10 years after chronic-fluoxetine treatment in which patients experienced symptoms of restlessness, tension, agitation, and sleep disturbances, suggesting the existence of a late-ONSet side-effect profile, which appears similar to acute side- effect symptomatology.