Failure of Tibolone to Potentiate the Pharmacological Effect of Fluoxetine in Postmenopausal Major Depression

Berlanga, Carlos; Mendieta, Danelia; Alva, Guadalupe; Lara, María del Carmen

doi:10.1089/154099903321154121

Cited by 14 publications

(3 citation statements)

References 21 publications

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“…For the study, 31 postmenopausal patients with a MDD were divided into two groups of treatment: group 1 received fluoxetine plus TIB (16 patients), and group 2 received fluoxetine plus placebo (15 patients) for eight weeks. In the end, both treatments were well tolerated, but treatment with TIB plus fluoxetine did not produce a more robust antidepressant response than fluoxetine alone [ 35 ].…”

Section: Resultsmentioning

confidence: 99%

Effects of Tibolone on the Central Nervous System: Clinical and Experimental Approaches

Pinto‐Almazán

Segura-Uribe

Farfán‐García

et al. 2017

BioMed Research International

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Hormone replacement therapy (HRT) increases the risk of endometrial and breast cancer. A strategy to reduce this incidence is the use of tibolone (TIB). The aim of this paper was to address the effects of TIB on the central nervous system (CNS). For the present review, MEDLINE (via PubMed), LILACS (via BIREME), Ovid Global Health, SCOPUS, Scielo, and PsycINFO (ProQuest Research Library) electronic databases were searched for the results of controlled clinical trials on peri- and postmenopausal women published from 1990 to September 2016. Also, this paper reviews experimental studies performed to analyze neuroprotective effects, cognitive deficits, neuroplasticity, oxidative stress, and stroke using TIB. Although there are few studies on the effect of this hormone in the CNS, it has been reported that TIB decreases lipid peroxidation levels and improves memory and learning. TIB has important neuroprotective effects that could prevent the risk of neurodegenerative diseases in postmenopausal women as well as the benefits of HRT in counteracting hot flashes, improving mood, and libido. Some reports have found that TIB delays cognitive impairment in various models of neuronal damage. It also modifies brain plasticity since it acts as an endocrine modulator regulating neurotransmitters, Tau phosphorylation, and decreasing neuronal death. Finally, its antioxidant effects have also been reported in different animal models.

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Section: Resultsmentioning

confidence: 99%

Effects of Tibolone on the Central Nervous System: Clinical and Experimental Approaches

Pinto‐Almazán

Segura-Uribe

Farfán‐García

et al. 2017

BioMed Research International

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“…However, tibolone did not enhance the antidepressant effect of the SSRI fluoxetine in a group of postmenopausal patients with major depressive episodes (Berlanga et al 2003). …”

Section: Pharmacology Of Tibolonementioning

confidence: 99%

Beneficial effect of tibolone on mood, cognition, well-being, and sexuality in menopausal women

Genazzani

Pluchino²,

Bernardi³

et al. 2006

Neuropsychiatric Disease and Treatment

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Tibolone is a synthetic molecule used extensively for the management of menopausal symptoms, with the proposed additional advantage of enhanced mood and libido. Tibolone, after oral administration, is rapidly converted into 3 major metabolites: 3α-hydroxytibolone and 3β-hydroxytibolone, which have estrogenic effects, and the Δ 4 -isomer, which has progestogenic and androgenic effects. The tissue-selective effects of tibolone are the result of metabolism, of enzyme regulation, and of receptor activation which vary in different tissues. Tibolone seems to be effective on estrogen-withdrawal symptoms such as hot fl ushes, sweating, insomnia, headache, and vaginal dryness, with results generally comparable to the effects exerted by estrogen-based treatments, and the additional property of a progestogenic activity on the endometrium. As well as relieving vasomotor symptoms, tibolone has positive effects on sexual well-being and mood, and improves dyspareunia and libido. These effects may depend on both estrogenic and androgenic actions exerted at the genital level and in the central nervous system, and on a reduction of sex-hormone-binding globulin and an increase of free testosterone, without affecting Δ-5 androgens levels. Based on the evidence available, tibolone is a valuable treatment option to relieve menopausal complaints, especially in women suffering persistent fatigue, blunted motivation, and loss of sexual desire despite an adequate estrogen replacement.

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“…Pointing out that estrogen by itself probably does not produce antidepressant efects, the reduction that exerts on the potential binding of 5-HTT is enough to increase synaptic 5-HT concentration, a synergistic efect on serotonergic system of both estrogen and luoxetine, which contributes to the establishment of the antidepressant efect. Paradoxically, the combination with tibolone, a synthetic steroid, does not produce synergistic antidepressant efects with luoxetine [34]. The above suggests that substituents on steroid molecules could be a determinant in the potential interrelation in therapeutic eicacy between steroids and the serotonergic system.…”

Section: Serotonergic Changes Associated To Antidepressants and Hormomentioning

confidence: 99%

Depression and Serotonergic Changes during the Climacteric and Postmenopausal Stages: Hormonal Influences

García-Ríos¹,

Mora-Perez²,

Soria-Fregozo³

2017

A Multidisciplinary Look at Menopause

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Depression is a psychiatric disorder that afects a high percentage of women. Most of the depression disorders turn up during the premenopause and perimenopause stages when the hormonal oscillations make an impact in the brain function principally on the serotonergic system, which is related to neurobiology of depression. 5-HT1A and 5-HT2A receptors change on functionality and density in aferent areas related to emotional modulation and increased serotonin clearance, and the binding potential of serotonin transport has been related to the underlying mechanism of the depression during the climacteric or postmenopausal stage. Some indings have been proven on preclinical studies. These studies on animals have recognized how estrogen treatment activates intracellular signaling pathways as mitogen-activated protein (MAP)/extracellular signal-regulated kinase (ERK), tyrosine kinase brain-derived neurotrophic factor receptor (TrKB), insulin-like growth factor-1 receptor (IGF-1R), phosphatidylinositol 3-kinase (PI3)/serine/threonine-speciic protein kinase (Akt), and metabotropic glutamate receptor 1 (mGluR1) which interact with the serotonergic system to allow establishment of the estradiol efects on mood regulation. Thus, the interaction between the woman's reproductive status and the serotonin changes could be useful to create prevention strategies, early diagnosis, and medical treatment of climacteric and postmenopausal women with depression, in order to improve their quality of life.

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Failure of Tibolone to Potentiate the Pharmacological Effect of Fluoxetine in Postmenopausal Major Depression

Abstract: Combining tibolone and fluoxetine did not represent a more robust antidepressant response than fluoxetine alone in postmenopausal women with MDD.

Cited by 14 publications

References 21 publications

Effects of Tibolone on the Central Nervous System: Clinical and Experimental Approaches

Effects of Tibolone on the Central Nervous System: Clinical and Experimental Approaches

Beneficial effect of tibolone on mood, cognition, well-being, and sexuality in menopausal women

Depression and Serotonergic Changes during the Climacteric and Postmenopausal Stages: Hormonal Influences

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