RESUMEN
The main objective of this study was to evaluate the antinociceptive activity of three ethylenediamine derivatives and three ß-aminoethanol lipidic derivatives structurally related to dihydrosphingosine. These derivatives were selected on the basis of previous results from in vitro and in vivo anti-inflammatory studies. For all of the assayed compounds, an intraperitoneal dose of 3 mg/kg caused pronounced pain inhibition as measured by the acetic acid-induced writhing model in mice. Compounds 3 and 6 demonstrated strong antinociceptive activity at doses as low as 1 mg/kg and proved to be considerably more potent than the common nonsteroidal anti-inflammatory drugs (NSAIDs), acetylsalicylic acid (ASA) and acetaminophen (ACE). We further analyzed these compounds using the capsaicin- and glutamate-induced pain tests. Compounds 3 and 6 also exhibited considerable antinociceptive effects under these conditions, but their inhibitory effects in the formalin test were less pronounced. The exact mechanism of action for these compounds has yet to be established. However, based the results from a hot-plate test, it can be stated that these new drugs do not interact with the opioid system.
Asunto(s)
Amino Alcoholes/uso terapéutico , Analgésicos/uso terapéutico , Etilenodiaminas/uso terapéutico , Dolor/tratamiento farmacológico , Esfingosina/análogos & derivados , Acetaminofén/farmacología , Acetaminofén/uso terapéutico , Ácido Acético , Amino Alcoholes/farmacología , Analgésicos/farmacología , Animales , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/uso terapéutico , Aspirina/farmacología , Aspirina/uso terapéutico , Capsaicina , Relación Dosis-Respuesta a Droga , Etilenodiaminas/farmacología , Calor , Ratones , Dolor/inducido químicamente , Dolor/fisiopatología , Dimensión del Dolor , Esfingosina/químicaRESUMEN
Of 433 schistosomiasis mansoni patients in St. Lucia who were treated with hycanthone (3 mg/kg of body weight), 190 were seen 2 years after treatment and 143 of these had attended all follow-up examinations at 6 weeks, 6 months, 1 year and 2 years. Viable eggs were not detected in 86% at 1 year nor in 76% at 2 years. The reinfection rate, as judged by a significant increase in egg excretion, was 15% and was related to the geographic area to which the patient returned. Extremely high total reduction in egg excretion (98%) was achieved through 1 year, and even with reinfections this fell only to 87% at 2 years. Liver and spleen enlargement was related to intensity of infection and responded to treatment in 92% and 83% of instances, respectively. Among patients with hepatosplenomegaly, those 15 years or older showed less clinical response than younger patients but were too few for statistical comparison.
Asunto(s)
Schistosoma mansoni , Esquistosomiasis/tratamiento farmacológico , Esquistosomicidas/uso terapéutico , Tioxantenos/uso terapéutico , Adolescente , Adulto , Niño , Etilenodiaminas/administración & dosificación , Etilenodiaminas/efectos adversos , Etilenodiaminas/uso terapéutico , Heces/parasitología , Estudios de Seguimiento , Hepatomegalia/inducido químicamente , Humanos , Metanol/administración & dosificación , Metanol/efectos adversos , Metanol/uso terapéutico , Recuento de Huevos de Parásitos , Esquistosomiasis/parasitología , Esquistosomicidas/administración & dosificación , Esquistosomicidas/efectos adversos , Esplenomegalia/inducido químicamente , Tioxantenos/administración & dosificación , Tioxantenos/efectos adversos , Indias OccidentalesRESUMEN
Of 433 schistosomiasis mansoni patients in St. Lucia who were treated with hycanthone ( 3mg/kg of body weight), 190 were seen 2 years after treatment and 143 of these had attended all follow-up examinations at 6 weeks, 6 months, 1 year, and 2 years. Viable eggs were not detected in 86 percent at 1 year nor in 76 percent at 2 years. The reinfection rate, as judged by a significant increase in egg excretion, was 15 percent and was related to the geographic area to which the patient returned. Extremely high total reduction in egg excreation (98 percent) was achieved through 1 year, and even with reinfections this fell only to 87 percent at 2 years. Liver and spleen enlargement was related to intensity of infection and responded to treatment in 92 percent and 83 percent of instances, respectively. Among patients with hepatosplenomegaly, those 15 years or older showed less clinical response than younger patients but were too few for statistical comparison. (AU)