J-INCOG
FARMACOLOGÍA
, synthesized from arachidonic acid and released by the action of phos-
pholipase A2 from lipids in cell membranes.
Eicosanoids are present in low concentrations in most cells butJ-INCOG
are syn-
thesized and released “on demand” in response to stimuli, including IgE-
mediated
FARMACOL O G Í Areactions,
D E Linflammatory
A I N F L Amediators,
MACIÓ trauma,
N heat, and toxins.
Eicosanoids interact with specific receptors, which are G-proteins cou-
pled to second messenger effector systems.
Vía de Ácido Araquidonico
Membrane
phospholipids
Fosfolipasa A2 es estimulado por mediadores – Brid
inflamatorios, trauma, toxinas y temperatura alta. Phospholipase A2 Glucocorticoids Prost
in the
TXA2 contr
Arachidonic acid
- ↑ Agregación plaquetaria ductu
– caus
- ↑Tono vasular –
and p
NSAIDs Cyclooxygenases Lipoxygenase Zileuton
by CO
PGI1 - Epoprostenol – COX1 (indu
- opuesto a TXA2 COXib COX2
enzy
PGE1 - alprostadil –
- ↓Tono vasular, Endoperoxides Hydroperoxides
- Protege mucosa GI Glucocorticoids
Receptors blocked
PGE2 - dinoprostone Leukotrienes
by –lukasts
- ↓Tono vasular, ↑tono uterino Montelukast
Zafirlukast
PGF2a - carboprost
- ↓Tono vasular, ↑tono uterino PGI2
PGD2 PGE2
TXA2
- Tono bronquial PGF2
Misoprostol - abortivo
Figure VI-4-1. Drugs Acting on Eicosanoids
ANTI-INFLAMATORIOS NO ESTEROIDEOS - AINE’S
- Inhiben reversiblemente la ciclooxigenasa: COX1 & COX2
- Analgésico, antipirético (pirógenos endógenos IL1 & IL3), anti-inflamatorio, anti-plaquetarios
- Dolor leve-moderado: Excepto Ketorolaco.
- Categoría C durante el embarazo → Se prefiere Acetaminofén.
AINE’s REVERSIBLES:
- Ácido propiónico: Ibuprofeno, Ketoprofeno, Desketoprofeno, Naproxeno, Fenoprofeno.
- Ácido acético: Diclofenac, Indometacina, Ketorolaco, Sulindaco.
- Mefamatos: ácido mefenámico.
Efectos adversos: isquemia renal, nefritis intersticial, úlcera gástrica, anemia aplásica. Asma
16
FARMACOLOGÍA
, synthesized from arachidonic acid and released by the action of phos-
pholipase A2 from lipids in cell membranes.
Eicosanoids are present in low concentrations in most cells butJ-INCOG
are syn-
thesized and released “on demand” in response to stimuli, including IgE-
mediated
FARMACOL O G Í Areactions,
D E Linflammatory
A I N F L Amediators,
MACIÓ trauma,
N heat, and toxins.
Eicosanoids interact with specific receptors, which are G-proteins cou-
pled to second messenger effector systems.
Vía de Ácido Araquidonico
Membrane
phospholipids
Fosfolipasa A2 es estimulado por mediadores – Brid
inflamatorios, trauma, toxinas y temperatura alta. Phospholipase A2 Glucocorticoids Prost
in the
TXA2 contr
Arachidonic acid
- ↑ Agregación plaquetaria ductu
– caus
- ↑Tono vasular –
and p
NSAIDs Cyclooxygenases Lipoxygenase Zileuton
by CO
PGI1 - Epoprostenol – COX1 (indu
- opuesto a TXA2 COXib COX2
enzy
PGE1 - alprostadil –
- ↓Tono vasular, Endoperoxides Hydroperoxides
- Protege mucosa GI Glucocorticoids
Receptors blocked
PGE2 - dinoprostone Leukotrienes
by –lukasts
- ↓Tono vasular, ↑tono uterino Montelukast
Zafirlukast
PGF2a - carboprost
- ↓Tono vasular, ↑tono uterino PGI2
PGD2 PGE2
TXA2
- Tono bronquial PGF2
Misoprostol - abortivo
Figure VI-4-1. Drugs Acting on Eicosanoids
ANTI-INFLAMATORIOS NO ESTEROIDEOS - AINE’S
- Inhiben reversiblemente la ciclooxigenasa: COX1 & COX2
- Analgésico, antipirético (pirógenos endógenos IL1 & IL3), anti-inflamatorio, anti-plaquetarios
- Dolor leve-moderado: Excepto Ketorolaco.
- Categoría C durante el embarazo → Se prefiere Acetaminofén.
AINE’s REVERSIBLES:
- Ácido propiónico: Ibuprofeno, Ketoprofeno, Desketoprofeno, Naproxeno, Fenoprofeno.
- Ácido acético: Diclofenac, Indometacina, Ketorolaco, Sulindaco.
- Mefamatos: ácido mefenámico.
Efectos adversos: isquemia renal, nefritis intersticial, úlcera gástrica, anemia aplásica. Asma
16
