Unsuccessful Suicide Attempt With Tiapride.

To the best of our knowledge, no case has been published in the literature that reports an overdose of tiapride, either alone or in combination with other drugs. We report a self-poisoning case in an 18-year-old girl, with approximately 10 times the usual daily dose (ie, 2.5 g). Although the blood concentration was 20/30-fold higher than usually observed after therapeutic drug intakes (17,300 mcg/L), the patient remained almost asymptomatic.

Tiapride impairs the aversive effect of electrical stimulation of the parabrachial complex in a conditioned place task.

The parabrachial complex has been related to various rewarding or aversive behavioral processes, including taste aversion learning and conditioned place aversion. This study examined the effect of tiapride, an antagonist of D2/D3 dopaminergic receptors, on place aversion induced by electrical stimulation of the external lateral parabrachial (LPBe) nucleus. Results obtained show that brain-stimulated animals avoid the area of the maze associated with electrical stimulation but show no such behavioral rejection when they receive an injection of 30 mg/kg tiapride. Furthermore, tiapride did not appear to affect the horizontal motor activity (crossing) of the animals. These results are discussed in the context of the different natural and artificial modalities used to induce aversive behavior and their relationship with dopamine systems.

[Assessment of a Tiapride solution for its administration through continuous intravenous perfusion]. / Estudio de estabilidad de tiaprida en disolución para administración en perfusión intravenosa continua.

OBJECTIVES: Tiapride is a substituted benzamide classified as an atypical neuroleptic. To our knowledge, there are no published data on its stability prepared as a continuous intravenous infusion. The current study analysed its stability in two different infusion solutions and concentrations over 48 hours. METHOD: Triplicate samples of tiapride were prepared in 0.9% sodium chloride and in 5% dextrose solutions at final concentrations of 1 and 2 mg/ml. Samples were collected in glass bottles without photoprotection and at room temperature (25 ± 2 °C). Sampling times at 0, 1, 3, 6, 12, 24 and 48 hours included a visual inspection for colour changes and appearance of precipitation as well as pH determination. Tiapride was quantified at selected times by mass spectrometry using high-performance liquid chromatography. Concentration values in the samples corresponding to 0 hours were given a reference value of 100%. Concentrations in subsequent samples greater than 90% were considered stable. RESULTS: No colour change or precipitation was observed during the study period. pH values ranged between 0.1 and 0.4 units. At 48 hours, the concentration of remaining tiapride in sodium chloride 1 mg/ml and 2 mg/ml was 93.8% and 91.6%, respectively. That in 5% dextrose 1 mg/ml and 2 mg/ml was 96.8% and 94.1%, respectively. CONCLUSION: Dilutions of tiapride in 0.9% sodium chloride and in 5% dextrose solution, at concentrations of 1 mg/ml and 2 mg/ml, in glass bottles and at room temperature were stable both physically and chemically during 48 hours.

Usefulness of administration of non-organophosphate cholinesterase inhibitors before acute exposure to organophosphates: assessment using paraoxon.

Reversible acetylcholinesterase (AChE) inhibitors can protect against the lethal effects of irreversible organophosphorus AChE inhibitors (OPCs), when administered before OPC exposure. We have assessed in vivo the mortality-reducing efficacy of a group of known AChE inhibitors, when given in equitoxic dosage before exposure to the OPC paraoxon. Protection was quantified in rats by determining the relative risk (RR) of death. Best in vivo protection from paraoxon-induced mortality was observed after prophylactic administration of physostigmine (RR = 0.30) or the oxime K-27 (RR = 0.34); both treatments were significantly superior to the pre-treatment with all other tested compounds, including the established substance pyridostigmine. Tacrine (RR = 0.67), ranitidine (RR = 0.72), pyridostigmine (RR = 0.76), tiapride (RR = 0.80) and 7-MEOTA (RR = 0.86) also significantly reduced the relative risk of paraoxon-induced death, but to a lesser degree. Methylene blue, amiloride and metoclopramide had an unfavorable effect (RR ≥ 1), significantly increasing mortality. When CNS penetration by prophylactic is undesirable K-27 is a promising alternative to pyridostigmine.

Efectos de la coadministración de gammahidroxibutirato (GHB) / Effects of coadministration of gammahydroxybutyrate (GHB) and L-741, 741, a selective D4 dopamine receptor antagonist, on agonistic behaviour in male mice

En estudios previos se ha descrito una potenciación del efecto antiagresivo tras la coadministración de gammahidroxibutirato (GHB) y tiapride, indicando la existencia de una interacción entre los receptores de GHB y dopaminérgicos D2. El objetivo de este trabajo fue examinar la posible existencia de una interacción entre los sistemas GHBérgico y dopaminérgico D4. Para ello se analizó el efecto de la administración aislada y conjunta de GHB (80 mg/kg) y L-741,741 (0.75-3 mg/kg), un antagonista selectivo de los receptores D4, sobre la conducta agonística en ratones machos, utilizando un modelo de agresión inducida por aislamiento. Treinta minutos después de la administración de los fármacos, se llevaron a cabo interacciones agonísticas de diez minutos de duración entre un animal aislado y un oponente anósmico en un área neutral, grabadas en vídeo para su posterior análisis etológico/conductual. No se encontraron diferencias significativas entre los grupos experimentales y el grupo control en ninguna de las categorías conductuales analizadas. Estos resultados sugieren que el GHB no interactúa con los receptores dopaminérgicos D4 (AU)

In previous studies, it has been described a potentiation of the antiaggressive effect after coadministration of gammahydroxybutyrate (GHB) and tiapride, indicating the exisence of an interaction between GHB and D2 dopamine receptors. The aim of this study was to examine the possible existence of an interaction between GHBergic and dopaminergic D4 systems. For this purpose, the effect of administration of gammahydroxybutyrate (GHB) and L-741,741 (0.75-3 mg/kg), a selective D4 dopamine antagonist, either alone or in combination, on agonistic behavior elicited by isolation was analized in male mice. Individually housed mice were exposed to anosmic «standard opponents» in a neutral area 30 minutes after the drugs administration, and the encounters were videotaped and evaluated using an ethologically based analysis. No significant differences were found between experimental and control groups in any of the behavioural categories analyzed. These results suggest that GHB does not interact with central dopamine D4 transmission (AU)

Cambio en el hábito de prescripción de psicofármacos en la Unidad de Salud Mental Infantil Virgen del Rocío de Sevilla. Comparación entre los años 1993 y 1998 / Changes in the prescribing habits of psychotropics in the Children's Mental Health Unit Virgen del Rocío de Sevilla. Comparison between 1993 and 1998

El objetivo del trabajo, es comprobar el posible cambio en el hábito de prescripcción de psicofármacos en la Unidad de Salud Mental Infantil (USMI) Virgen del Rocío de Sevilla. Sabíamos que se podían estar dando algunos cambios y que se estaban prescribiendo nuevos psicofármacos, como los neurolépticos atípicos y antidepresivos inhibidores de la recaptación de serotonina (ISRS), pero desconocíamos en qué proporción y si había diferencias con otros medicamentos en cuanto la edad y sexo. Para averiguarlo se comparó una muestra de pacientes nuevos atendidos en 1993 y 1998. Los psicofármacos se agruparon en 6 grupos, antiepilépticos, antidepresivos, benzodacepinas, estimulantes, neurolépticos y "otros", se averiguó el porcentaje en que fueron utilizados en 1993 y 1998, relacionándolo con la edad y el sexo.Los resultados obtenidos nos corroboran los cambios de tendencia en la prescripción de algunos medicamentos, y que hay preferencia de distintas edades y sexo para la indicación de algunos grupos farmacológicos y en concreto de algunos psicofármacos en los niños (AU)