The acute inflammatory response Flashcards
What is the mediator response to local injury?
Preformed mediators-histamine.
Membrane lipids- eicosanoids, leukotriened, substance P, CGRP.
Proteinases activation- bradykinin, complement.
Protein synthesis- iNOS, COX2, cytokines
What substances have a vasodilatory effect on blood vessels?
Histamine Eicosanoids Neuropeptides Bradykinin NO
What substances increase vascular permeability?
Histamine
Eicosanoids
Bradykinin
Complement C3a, C5a
What agents increase plasma leakage via an action directly on the endothelium?
Histamine
Bradykinin
How do neutrophil activators increase plasma leakage?
Via a neutrophil dependent mechanism
H1 receptor is Gq Gs or Gi linked?
Gq linked
What does H1 receptor stimulate?
Phospholipase C
H2 receptor is Gq Gs or Gi linked?
Gs
What does H2 receptor stimulate?
Adenylyl cyclase
H3 receptor is Gq Gs or Gi linked?
Gi
What does H3 receptor inhibit?
AC
H4 receptor is Gq Gs or Gi linked?
Gi
What does H4 receptor do?
Inhibit AC
Activate PLC via By subunits
What does IgE cause?
Immediate hypersensitivity
What does H1 do?
Vasodilator via NO release from endothelium.
Increased permeability-oedema.
Activation of sensory nerve-pain and itch.
Central histamine release causes what?
Wakefulness
H1 receptor antagonist causes what?
Drowsiness
Name 3 H1 receptor antagonists
Chlorpheniramine
Astemizole
Loratadine
What is the primary factor involved in the control of gastric acid secretion?
Histamine
What cells are H2 released from?
Enterochomaffin-like cells
Where are H2 receptors found?
Parietal cells
Name 1 H2 receptor antagonist
Cimetidine
Cimetidine is a what inhibitor?
CYP450
Out of ranitidine, famitidine and cimetidine, which has the fewest drug interactions?
Famitidine
Where are H3 receptors found?
Presynaptic nuerons
What do H3 receptors do?
Negatively regulate synthesis and release of HA and other neurotransmitters
Blocking central H3 receptors will enhance what?
Histamine release
H3 receptors have high what?
Basal activity
What is ciproxifan?
An inverse H3 agonist
Where are H4 receptors highly expressed?
White blood cells