Valproate is an anti-androgen and anti-progestin

@article{Death2005ValproateIA,
  title={Valproate is an anti-androgen and anti-progestin},
  author={Alison K. Death and Kristine C. Y. McGrath and David Handelsman},
  journal={Steroids},
  year={2005},
  volume={70},
  pages={946-953}
}
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30 Citations
Background Citations
8
Methods Citations
2
Results Citations
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30 Citations

Citation Type

Citation Type

Valproic acid and its derivatives enhanced estrogenic activity but not androgenic activity in a structure dependent manner.
The antiepileptic effect of sodium valproate during different phases of the estrous cycle in PTZ-induced seizures in rats
TLDR
The results of this study showed that VPA significantly improved antiepileptic parameters including ITMS, ITTS, SD, and MR, in which they were significantly more prominent during the luteal phase than the follicular phase.
Valproic acid activity in androgen-sensitive and -insensitive human prostate cancer cells.
TLDR
Findings suggest that VA might have clinical value in prostate cancer therapy in androgen-sensitive and -insensitive tumors, which is consistent with plasma concentrations reached under oral administration of therapeutical doses in patients treated for different diseases.
Inhibitory effect of valproic acid on ovarian androgen biosynthesis in rat theca-interstitial cells
TLDR
VPA exerts an inhibitory effect on hCG-stimulated androgen synthesis in rat T-I cells, suggesting that the mechanism of VPA’s inhibitoryEffect on androstenedione production occurs at a step after second messenger activation.
Antiepileptic Drugs Affect Neuronal Androgen Signaling via a Cytochrome P450-Dependent Pathway
TLDR
CYP3A2 and CYP3A11 are crucial mediators of AR expression and signaling after AED application and point to an important and novel function of P450 in regulation of steroid hormones and their receptors in endocrine tissues such as liver and brain.
The effect of VPA on bone: From clinical studies to cell cultures—The molecular mechanisms revisited
Epilepsy, sex hormones and antiepileptic drugs in female patients
TLDR
The aim of the present review is to critically evaluate the recently published data concerning the interactions between sex hormones, epilepsy and AEDs.
Subchronic effects of valproic acid on gene expression profiles for lipid metabolism in mouse liver.
Hormonal and reproductive disturbances in epileptic male patients: emerging issues.
Structure–activity relationships of synthetic progestins in a yeast-based in vitro androgen bioassay
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References

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Antiepileptic drugs inhibit cell growth in the human breast cancer cell line MCF7
Reproductive effects of valproate, carbamazepine, and oxcarbazepine in men with epilepsy
TLDR
VPA increases serum androgen concentrations in men with epilepsy, and the endocrine effects of CBZ and OXC were different, because CBZ appears to decrease the bioactivity of androgens, whereas OxC does not.
Higher androgens and weight gain with valproate compared with lamotrigine for epilepsy
Acute effects of anticonvulsant drugs on gonadotropin-stimulated and precursor-supported androgen production in the rat testis.
Valproate-Induced Hyperandrogenism During Pubertal Maturation in Girls with Epilepsy
TLDR
The observed increasing incidence ofhyperadrenalism along with pubertal development confirm a tendency to manifest hyperandrogenism in association with valproate as a function of sexual maturation.
Long-term valproate treatment induces changes in ovarian morphology and serum sex steroid hormone levels in female Wistar rats
TLDR
It is demonstrated that changes in gonadal structure and endocrine function also occur in intact animals indicating a drug-specific effect of valproate, and encourages further studies using animal models to elucidate possible mechanisms involved in the endocrine side-effects of antiepileptic drugs.
Effect of sodium valproate on luteinizing hormone secretion in pre- and postmenopausal women and its modulation by naloxone infusion.
TLDR
It is suggested that an acute increase in GABA-ergic tone may inhibit gonadotropin secretion in the estrogen-deprived state, or when endogenous opioid inhibition is blocked in postmenopausal women on estrogens, as well as during the luteal phase of the menstrual cycle.
Effects of chronic valproate treatment on reproductive endocrine hormones in female and male Wistar rats.
Early hormonal changes during valproate or carbamazepine treatment
TLDR
Hormonal changes occur after only 1 month’s use of VPA or CBZ, but the profile of hormonal changes appears to be different in women than in men.
Effects of antiepileptic drugs carbamazepine and sodium valproate on fertility of male rats.
TLDR
Mating performance, sex organs weights, semen quality, plasma concentrations of sexual hormones as well as histopathological findings were the criteria used to evaluate the reproductive efficiency of treated males.
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