Neuroendocrine responses to single oral doses of remoxipride and sulpiride in healthy female and male volunteers

Abstract

Six female and six male healthy volunteers received 100 mg remoxipride, 200 mg sulpiride and placebo as single oral doses in a double blind trial with a randomized crossover design. The main objective was to compare the effect of the two drugs on serum prolactin levels, but effects on other hormones were also investigated. Remoxipride and sulpiride increased the serum levels of prolactin to similar peak levels. This effect was larger in female than in male subjects. Sulpiride increased prolactin levels at much lower plasma concentrations than remoxipride, and sulpiride's effect on prolactin lasted for considerably longer than remoxipride's. No consistent effects on serum levels of LH, FSH, GH, oestradiol, progesterone, testosterone or cortisol could be detected after remoxipride and sulpiride compared to placebo. No drug-related effects on plasma homovanillic acid (HVA) were found.

Long-Term Effects of the Substituted Benzamide Derivative Amisulpride on Baseline and Stimulated Prolactin Levels

“…This increase in the prolactin concentrations was more pronounced in patients treated with amisulpride. This is consistent with the finding of a marked elevation of plasma prolactin levels by substituted benzamide antipsychotics as described in previous studies [11,12]. This result can be explained within the context of well-known neuroendocrinological regulatory mechanisms, including a blockade of the tonic dopaminergic inhibition of prolactin secretion within the tuberoinfundibular dopamine system [1,13,14].…”

Quetiapine reduces nocturnal urinary cortisol excretion in healthy subjects

“…The pronounced decrease in cortisol excretion after administration of low doses of quetiapine contrasts with findings of earlier studies investigating the effects of typical antipsychotics given to healthy subjects. The majority of these studies found unchanged cortisol levels after acute (Collu et al 1975;Jezova Repcekova et al 1979;Barbieri et al 1984;Laakmann et al 1984;Nurnberger et al 1984;von Bahr et al 1991;de Koning and de Vries 1995) or subchronic (Baptista et al 1997a(Baptista et al , 1997b administration of varying doses of different typical antipsychotics. One group found increased cortisol levels after low doses of haloperidol (Murburg et al 1986(Murburg et al , 1993, whereas in another study, haloperidol antagonized the cortisol increase due to heat stress (Hennig et al 1995).…”

Influence of the dosing interval on prolactin release after remoxipride.

“…infusions of 50 mg remoxipride and following single doses of 70, 100 and 140 mg remoxipride given as oral rapid administrations such as solution, immediate release capsules or intramuscular injection [7,13,20,37].…”

“…Controlled clinical trials have shown that remoxipride has a good antipsychotic effect, with a significantly lower frequency of extrapyramidal symptoms compared with haloperidol [4,5]. The effect of remoxipride on plasma prolactin elevation is short-lasting [6,7]. The trough plasma prolactin levels during steady-state treatment are generally not elevated, or only mildly to moderately elevated above the normal levels, during treatment with remoxipride, which differentiates remoxipride from classical neuroleptics [8][9][10][11].…”