The opposite effects of fluvoxamine and sertraline in the treatment of psychotic major depression: a case report

Kishimoto, Akira; Todani, Ayako; Miura, Junko; Kitagaki, Tetsuno; Hashimoto, Kenji

doi:10.1186/1744-859x-9-23

Cited by 15 publications

(12 citation statements)

References 24 publications

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“…The efficacy results of this study are consistent with other studies using the same drug in populations from Europe and other regions [19] [26]- [28]. The observed 75% reduction in the HAMD-17 score with fluvoxamine treatment is similar to the clinically significant change of 71% recorded in another study [29].…”

Section: Discussionsupporting

confidence: 91%

Fluvoxamine in Treatment of Depression in Russian Patients: An Open-Label, Uncontrolled and Non-Randomized Multicenter Observational Study

Smulevich¹,

Ilyina²

2015

OJPsych

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Background: Fluvoxamine, a selective serotonin reuptake inhibitor is widely used in the treatment of depression, one of the most common disorders prevalent in Russia. However, studies demonstrating its efficacy and safety in routine settings in Russia are scarce. Methods: This prospective, uncontrolled, open-label study was conducted at 11 centers in Russia. Total 293 patients (aged ≥ 18 years), meeting DSM-IV criteria for depression and scoring ≥ 17 on 17-item Hamilton Rating Scale of Depression (HAMD-17) received fluvoxamine 50-300 mg for 6 weeks. Primary efficacy measures included change from baseline in the HAMD-17 and Clinical Global Impression (CGI) scores. Secondary efficacy measure was evaluation of sleep quality changes on HAMD-17 subscale. Safety was assessed by monitoring of adverse drug reactions (ADRs). Results: Mean age of patients was 42.7 years and the majority of them were women (72%). At the end of treatment (day 42), clinically significant reduction was observed in mean HAMD-17, CGI-severity of illness and HAMD-17 sleep sub-score from 23.1, 4.5 and 3.9 at baseline to day 42; change from baseline (∆) was: ∆-17.3 [95% CI: −18.0; −16.7]), ∆-2.1 and ∆-3.4 [95% CI: −3.53; −3.20]), respectively. At day 42, 20.8% patients reported as normal (not at all ill) on the CGI-severity scale and 85% patients reported as "much improved" or "very much improved" on the CGI-change in severity and quality of life scores. Nausea (12.6%) and somnolence (5.1%) were the most frequently reported ADRs. No deaths or serious ADRs were reported but eight patients discontinued treatment due to ADRs. Conclusion: Treatment with fluvoxamine under routine settings showed marked improvement in Russian patients with depression as measured by HAMD-17 and CGI ratings and was thus efficacious as well as safe and well-tolerated.

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Section: Discussionsupporting

confidence: 91%

Fluvoxamine in Treatment of Depression in Russian Patients: An Open-Label, Uncontrolled and Non-Randomized Multicenter Observational Study

Smulevich¹,

Ilyina²

2015

OJPsych

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“…Fluvoxamine abolished delusions, while sertraline was devoid of effect on this symptom. The authors attributed the efficacy of fluvoxamine on delusions to its σ 1 -agonist activity (56). Since the clinical dose of fluvoxamine was two times higher than the sertraline dose, whereas the fluvoxamine affinity for σ 1 -site is also two times higher, it may therefore be suggested that sertraline did not interact with the σ 1 -sites at its clinically active dose, contrarily to fluvoxamine, explaining its lack of effect on delusions.…”

Section: Discussionmentioning

confidence: 99%

“…These observations are coherent with the reports of Bergeron et al (31) and Rogoz and Skuza (54). Interestingly, several recent reports (35,55,56) demonstrated, on neurite sprouting in PC12 cells and from human clinical studies, that fluvoxamine's action involve a σ 1 -agonist effect in its pharmacological activity, while sertraline was devoid of effect or showed opposite effects. The effects observed with sertraline could in fact appear coherent with an "inverse agonist" activity at σ 1 -sites.…”

Section: Discussionmentioning

confidence: 99%

“…Taking into account the particular consequences on neuronal networks, particularly monoaminergic pathways, and the drug bioavailability and pharmacological selectivity profile, it is not surprising that it could behave as an agonist on one response and behave as an inverse agonist on another. Finally, in the human study (56), a difference of efficacy between fluvoxamine and sertraline on the appearance of delusions in a patient with psychotic depression was reported. Fluvoxamine abolished delusions, while sertraline was devoid of effect on this symptom.…”

Section: Discussionmentioning

confidence: 99%

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Pharmacological Interaction With the Sigma1 (σ1)-Receptor in the Acute Behavioral Effects of Antidepressants

et al. 2011

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Abstract. Selective agonists of the sigma-1 (σ 1 ) ligand-operated chaperone protein, like igmesine or PRE-084, are antidepressants in preclinical depression models. σ 1 -Protein activation may contribute to the antidepressant efficacy of drugs known to act as selective serotonin-reuptake inhibitors (SSRI) or noradrenaline reuptake inhibitors through direct or indirect involvement of the σ 1 -receptor in the drug effect. We here compared antidepressant effects in two behavioral procedures, the forced swimming test (FST) and conditioned fear stress (CFS). The involvement of the σ 1 -receptor was examined using a co-treatment with the σ 1 -antagonist BD1047 or using σ 1 -knockout (KO) mice. Igmesine but not PRE-084 decreased FST immobility. The SSRI fluoxetine and sertraline, but not fluvoxamine, and the tricyclic antidepressants imipramine, desipramine, and amitriptyline were also effective. Only the effect of igmesine was blocked by BD1047 or in σ 1 -KO mice. Igmesine, PRE-084, fluvoxamine, and sertraline decreased the CFS immobility in a BD1047-and σ 1 -KO-sensitive manner. Among tricyclics, only amitriptyline was effective and its effect was unaffected by BD1047 or in σ 1 -KO mice. The behavioral effects induced by mixed σ 1 -receptor/ SSRI antidepressants, like fluvoxamine or sertraline, may therefore involve a non-selective action at both targets. Moreover, the CFS appears to more reliably uncover a σ 1 pharmacological component in antidepressant screening.

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“…These observations suggest that the interaction between brain 5‐HT 1A and σ 1 receptors is involved in the amelioration of the depressive‐like state observed in picrotoxin‐treated mice. The effectiveness of SSRIs with an affinity for the σ 1 receptor has also been shown in a number of clinical studies (Carrasco and Sandner, ; Kishimoto et al, ). Taken together with the recent finding that fluvoxamine increases prefrontal dopamine release in picrotoxin‐treated mice and that the effect is mediated by co‐activation of the 5‐HT 1A and σ 1 receptors (Ago et al, ), it is likely that the increased prefrontal dopamine release results in an anti‐anhedonic effect.…”

Section: Discussionmentioning

confidence: 79%

Anti-anhedonic effect of selective serotonin reuptake inhibitors with affinity for sigma-1 receptors in picrotoxin-treated mice

Hasebe

Ago

Watabe

et al. 2017

British Journal of Pharmacology

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Male mice were treated with picrotoxin to decrease GABA A receptor function. Their anhedonic behaviour was measured using the female encounter test. The expression of c-Fos was determined immunohistochemically. KEY RESULTSPicrotoxin caused an anxiogenic effect on three behavioural tests, but it did not affect the immobility time in the forced swim test. Picrotoxin decreased female preference in the female encounter test and attenuated the female encounter-induced increase in c-Fos expression in the nucleus accumbens. Picrotoxin-induced anhedonia was ameliorated by fluvoxamine and S-(+)-fluoxetine, selective serotonin reuptake inhibitors with high affinity for the σ 1 receptor. The effect of fluvoxamine was blocked by a 5-HT 1A or a σ 1 receptor antagonist, and co-administration of the σ 1 receptor agonist (+)-SKF-10047 and the 5-HT 1A receptor agonist osemozotan mimicked the effect of fluvoxamine. By contrast, desipramine, duloxetine and paroxetine, which have little affinity for the σ 1 receptor, did not affect picrotoxin-induced anhedonia. The effect of fluvoxamine was blocked by a dopamine D 2/3 receptor antagonist. Methylphenidate, an activator of the prefrontal dopamine system, ameliorated picrotoxin-induced anhedonia. CONCLUSION AND IMPLICATIONSPicrotoxin-treated mice show anhedonic behaviour that is ameliorated by simultaneous activation of 5-HT 1A and σ 1 receptors. These findings suggest that the increased prefrontal dopamine release is associated with the anti-anhedonic effect observed in picrotoxin-treated mice.Abbreviations SSRI, selective serotonin reuptake inhibitor

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The opposite effects of fluvoxamine and sertraline in the treatment of psychotic major depression: a case report

Cited by 15 publications

References 24 publications

Fluvoxamine in Treatment of Depression in Russian Patients: An Open-Label, Uncontrolled and Non-Randomized Multicenter Observational Study

Fluvoxamine in Treatment of Depression in Russian Patients: An Open-Label, Uncontrolled and Non-Randomized Multicenter Observational Study

Pharmacological Interaction With the Sigma1 (σ1)-Receptor in the Acute Behavioral Effects of Antidepressants

Anti-anhedonic effect of selective serotonin reuptake inhibitors with affinity for sigma-1 receptors in picrotoxin-treated mice

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