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