BENZODIAZEPINAS
KAREM A. MARTINEZ F.R1 ANESTESIOLOGIA Y REANIMACION
HSB
Anillo heterociclico
2 atomos de N estan localizados
en 1-4
Desordenes de suegno, ansiedad,
estatus epileptico y tension muscular
Acciones terapeuticas
mediada
Receptor GABA tipo A
Aumentan actividad neurotransmisora
inhibitoria
Modulan actividad en la membrana
pots sinaptica
Entrada de cloruro
hiperpolarizacion
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
• Heteropentamero• Sitios de union para:- Barbituricos- Benzodiazepinas (Subunidad alpha y gamma 2)
- GABA
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
Propiedades farmacologicas dependeran de la subunidad (Histidina)• Alpha 1-2-3-5 combinada con• Betha 1-2-3 subunidades• Gamma 2 (Brain-modulacion a BZN)
Insensibles a BZN•Alpha 4-6•DeltaAumentan o modulan afinidad por el neutotransmisor fisiologico GABA
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
Cerebro y corteza
Miller s. anesthesia. 7thedition. Chapter 16.2011
• Los efectos tranquilizantes son asociados a bajas dosis
• Lorazepam 2-3 veces mas sedante que Midazolam• Midazolam 5-6 veces mas potente que Diazepam• Lorazepam 4 veces mas amnesico que Midazolam
- Cuidado en pacientes ancianos
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
• Sedacion• amnesias
• Accion ansiolitica• Miorelajacion• Hipnosis
• Manejo de convulsiones
• Sindrome de abstinencia
• Accion anticonvulsivanete
Alpha 1 Cerebro y
corteza
Alpha 2 Sistema limbicoAlpha 3
Sustancia activadora reticular
A 5 Hipocampo
BENZODIAZEPINAS
Combinacion de varios receptores
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
• Lorazepam, midazolam y diazepam, los mas utilizados en la practica clinica
• Difieren en inicio de accion, duracion y terminacion de efectos
- Afinidad a los receptores y sus subunidades (potencia)
- Liposolubilidad (redistribucion)
- Farmacocinetica (Absorcion, distribucion, eliminacion)
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
• 99% Diazepam Union a proteinas plasmaticas• 95% Midazolam• 85% Lorazepam
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
MIDAZOLAM
HEPATICO- HIDROXILACIONEnzimas microsomales
HIDROXIMIDAZOLAM 20-30%Es conjugado y eliminado renal
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
EFECTOS ADVERSOS
• Depresion respiratoria• Incremento con opioides• Depresion cardiovascular
- Reversion con antagonista benzodiazepinas FLUMAZENIL-1-2 minutos inicio de accion
- 45-90 minutos duracion de accion (0.2, 1.0 mg bolo o 3mg /H)
Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011
BIBLIOGRAFIA
1. Evers, A, Maze M, Anesthetic Pharmacology. Basic principles and clinical practice. 2nd Edition. Chapter 29 Pag 483-493. 2011