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This lectures for these objectives occurred on 8/27, 8/30, 8/31, and 9/1.

Study MaterialsEdit

Link to HandoutsEdit

  • Antihistamines

Link to PanoptoEdit

  • 8/27 - Antihistamines
  • 8/30 - Antihistamines
  • 8/31 - 2nd Gen Antihistamines & H2 Blockers
  • 9/1 - H2 blockers

ObjectivesEdit

Edited by Coastermonger 20:24, September 23, 2010 (UTC)

Describe how histamine is synthesized in vivo.Edit

Histamine is synthesized from Histidine via the enzyme Histidine Decarboxylase (HDC). The molecule is subsequently stored primarily in mast cells.

Histamine synthesis

Recognize the two tautomeric forms of histamine and describe the relevance of these forms.Edit

Histamine tautomers

Describe the different types of histamine receptors.Edit

There are 4 types of histamine receptors. All of them are G protein coupled, they differ in their secondary messengers and tissue distribution.

Receptor Name Locaion Action When Stimulated
H1
  • Smooth Muscle of Intestine
  • Bronchi
  • Blood Vessels
  • Vascular Endothelial Cells
  • contraction in the ileum
  • bronchoconstriction
  • increased capillary permeability (edema)
  • uticaria (hives) and subsequent of
H2 Gastric Parietal Cells in the stomach gastric acid secretion
H3

Mainly in the CNS

  • presynaptic receptors on histamine containing neurons
H4

Describe the mechanism of action of H1 antihistamines.Edit

Describe the structure activity relationship for H1 antihistamines and apply this knowledge to clinical decision making.Edit

Explain the adverse effect profiles of the two generations of H1 antihistamines and describe the differences physicochemically.Edit

Recognize the structures of chromone based mast cell stabilizers.Edit

Describe the mechanism of action of mast cell stabilizers and given a clinical scenario, assess whether a mast cell stabilizer would be appropriate therapy.Edit

Describe the rationale for the design of cimetidine.Edit

Recognize the structures of H2 antagonists.Edit

Describe the mechanism of action of proton pump inhibitors.Edit

Given a structure, predict whether or not the compound would have proton pump inhibition activity.Edit

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