RESUMO
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.
Assuntos
Potenciais de Ação/efeitos dos fármacos , Anti-Inflamatórios não Esteroides/classificação , Anti-Inflamatórios não Esteroides/farmacologia , Fibras Nervosas/efeitos dos fármacos , Nervo Isquiático/efeitos dos fármacos , Potenciais de Ação/fisiologia , Analgésicos/classificação , Analgésicos/farmacologia , Animais , Aspirina/classificação , Aspirina/farmacologia , Relação Dose-Resposta a Droga , Feminino , Indometacina/classificação , Indometacina/farmacologia , Masculino , Naproxeno/classificação , Naproxeno/farmacologia , Fibras Nervosas/fisiologia , Ranidae , Nervo Isquiático/fisiologiaRESUMO
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.
Assuntos
Aspirina/farmacocinética , Adulto , Aspirina/classificação , Cafeína , Carbonato de Cálcio , Método Duplo-Cego , Feminino , Humanos , Masculino , Salicilatos/sangue , Ácido Salicílico , Equivalência TerapêuticaAssuntos
Aspirina/administração & dosagem , Mortalidade/tendências , Inibidores da Agregação Plaquetária/administração & dosagem , Antagonistas do Receptor Purinérgico P2Y/administração & dosagem , Aspirina/classificação , Ensaios Clínicos como Assunto/métodos , Esquema de Medicação , Quimioterapia Combinada , Humanos , Antagonistas do Receptor Purinérgico P2Y/classificação , Ticlopidina/administração & dosagem , Fatores de TempoAssuntos
Anti-Inflamatórios não Esteroides/classificação , Aspirina/classificação , Rotulagem de Medicamentos , Salicilatos/classificação , Anti-Inflamatórios não Esteroides/efeitos adversos , Aspirina/efeitos adversos , Gastroenteropatias/induzido quimicamente , Humanos , Salicilatos/efeitos adversos , Estados Unidos , United States Food and Drug AdministrationRESUMO
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