RESUMEN
AIMS: Although antinociception produced by non-steroidal anti-inflammatory drugs (NSAIDs) is partly attributed to nerve conduction inhibition, this has not been thoroughly examined yet. The aim of the present study was to reveal quantitatively how various types of NSAIDs affect compound action potentials (CAPs), a measure of nerve conduction. MAIN METHODS: CAPs were recorded from the frog sciatic nerve by using the air-gap method. KEY FINDINGS: Soaking the sciatic nerve with acetic acid-based NSAIDs (diclofenac and aceclofenac) reduced the peak amplitude of CAP in a concentration-dependent manner; their IC50 values were 0.94 and 0.47â¯mM, respectively. Other acetic acid-based NSAIDs (indomethacin, acemetacin and etodolac) also inhibited CAPs [the extent of inhibition: some 40% (1â¯mM), 40% (0.5â¯mM) and 15% (1â¯mM), respectively], except for sulindac and felbinac at 1â¯mM that had no effects on CAP peak amplitudes. A similar inhibition was produced by fenamic acid-based NSAIDs [tolfenamic acid (IC50â¯=â¯0.29â¯mM), meclofenamic acid (0.19â¯mM), flufenamic acid (0.22â¯mM) and mefenamic acid] which are similar in chemical structure to diclofenac and aceclofenac; their derivatives (2,6-dichlorodiphenylamine and N-phenylanthranilic acid) also inhibited. On the other hand, salicylic acid-based (aspirin), propionic acid-based (ketoprofen, naproxen, ibuprofen, loxoprofen and flurbiprofen) and enolic acid-based (meloxicam and piroxicam) NSAIDs had no effects on CAP peak amplitudes. SIGNIFICANCE: At least a part of antinociception produced by NSAIDs used as a dermatological drug to alleviate pain may be attributed to their inhibitory effects on nerve conduction, which depend on the chemical structures of NSAIDs.
Asunto(s)
Potenciales de Acción/efectos de los fármacos , Antiinflamatorios no Esteroideos/clasificación , Antiinflamatorios no Esteroideos/farmacología , Fibras Nerviosas/efectos de los fármacos , Nervio Ciático/efectos de los fármacos , Potenciales de Acción/fisiología , Analgésicos/clasificación , Analgésicos/farmacología , Animales , Aspirina/clasificación , Aspirina/farmacología , Relación Dosis-Respuesta a Droga , Femenino , Indometacina/clasificación , Indometacina/farmacología , Masculino , Naproxeno/clasificación , Naproxeno/farmacología , Fibras Nerviosas/fisiología , Ranidae , Nervio Ciático/fisiologíaAsunto(s)
Aspirina/administración & dosificación , Mortalidad/tendencias , Inhibidores de Agregación Plaquetaria/administración & dosificación , Antagonistas del Receptor Purinérgico P2Y/administración & dosificación , Aspirina/clasificación , Ensayos Clínicos como Asunto/métodos , Esquema de Medicación , Quimioterapia Combinada , Humanos , Antagonistas del Receptor Purinérgico P2Y/clasificación , Ticlopidina/administración & dosificación , Factores de TiempoRESUMEN
De acuerdo con las investigaciones más recientes, los beneficios de la aspirina se extienden a un amplio rango de pacientes que han sobrevivido a un accidente cardiovascular. En cuanto a su uso en personas clínicamente sanas, es todavía cuestión de valoración clínica pero está en progreso un estudio en gran escala que busca aclarar este punto
Asunto(s)
Humanos , Aspirina/administración & dosificación , Aspirina/análisis , Aspirina/clasificación , Infarto del Miocardio/cirugía , Infarto del Miocardio/diagnóstico , Infarto del Miocardio/fisiopatología , Infarto del Miocardio/mortalidad , Infarto del Miocardio/prevención & controlRESUMEN
A double blind cross over randomized study was conducted in 7 normal healthy volunteers. Single dose (700 mg) of buffered aspirin or aspirin with calcium carbonate or aspirin with caffeine was administered orally, at least 3 days apart. Blood samples were drawn at different time intervals after administration of drug for estimation of salicylate levels. The values of different pharmacokinetic parameters (AUC0-infinity, Cmax and tmax) did not show any significant difference, suggesting that these three brands of aspirin are biologically equivalent.
