barbituricos
TRANSCRIPT
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BARBITURICOS
KAREM A. MARTINEZ F.RESIDENTE ANESTESIOLOGIA Y REANIMACION HSB UNIVERSIDAD EL BOSQUE
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HISTORIA
1983: Adolf Von baeyer, Sintetiza el Acido barbiturico
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1934: Waters and Lundy, Introducen el Tiopental en la practica clinica (Efecto rapido y duracion corta)
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Oxigeno en posicion No 2Molecula de azufre en posicion No
2-inicio de accion rapido -Tio
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Tautomerizacion Ceto-enol especies reactivas en forma alcoholica (formacion de sales)
Reconstitucion en agua o suero fisiologico
Sustitucion del Hidrogeno posicion 5 de grupo arilo-alquilo (Actividad hipnotica)
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SustituirPosiciones al grupo barbiturico
Grupos arilo-alquilo (5)
HipnoticoAumento cadenas laterales
Sedante
Fenilo (C5)
Actividad antiepileptica
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METABOLISMO
Excepcion del fenobarbital (60-90%)
Metabolitos inactivos, hidrosolubles, eliminacion por la orina
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Transformacion mediante:1. Oxidacion regiones arilo-alquilo-
fenilo (C5) 2. N-Desalquilacion3. Desulfuracion de los tiobarbituricos (C2)4. Destruccion del anillo acido barbiturico
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Los farmacos que inducen la oxidacion microsomica potencian su metabolismo
Rifampicina
carbamacepina
Fenitoina
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Existe una diferencia entre la desaparicion plasmatica y la semivida de eliminacion
4 horas metohexital- Aclaramiento hepatico 3 veces mas rapido tasa de extraccion 0.5
12 Tiopental tasa de extraccion de 0.15
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Depresion del sistema nervioso central Depresion cardiovascular-
vasodilatacion periferica Sedacion Hipnosis Amnesia anterograda Dependencia fisica y psicologica
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1. KATZUNG. B. FARMACOLOGIA BASICA Y CLINICA. 9NA EDICION. 2005. CAPITULO 22 PAG 353-366. MANUAL MODERNO
2. MILLER. R, ERICKSSON.L, FLEISHER. L, MILLER S ANESTHESIA.7MA EDICION. 2010. CAPITULO 16 PAG 485-500. ELSEVIER
3. SMITH. T, PINNOCK C, LIN. T. FUNDAMENTALS OF ANAESTHESIA. THIRD EDITION. 2009. SECTION 3, PAG 569-583. CAMBRIDGE MEDICINE
BIBLIOGRAFIA