Inflammation Flashcards
What type of G protein is linked to the H1 receptor?
Gaq
-> increases Ca
What type of G protein is linked to the H2 receptor?
Gas
-> increases cAMP
What type of G protein is linked to the H3 receptor?
Gai/o
-> inhibits cAMP
What type of G protein is linked to the H4 receptor?
Gai/o
-> increases Ca
What is swelling (increased vascular permeability) mediated by?
Anaphylatoxins C3a, C5a, LtB4, TNFalpha, VEGF, PGE2, bradykinin
What is pain mediated by?
substance P, calcitonin gene related peptide, bradykinin, prostaglandins
What is redness mediated by?
histamine, 5HT, platelet aggregating factor, Bradykinin, nitric oxide, PGI2, PGE2
Which drug treats motion sickness?
chlopheniramine
H1 antagonist, crosses BBB
What is ranitidine?
Treatment for healing duodenal ulcers by suppressing gastric secretion (H2 antagonist)
What are kinins?
Proteins that cause vasodilation and smooth muscle contraction. They increase venular permeability, cause pain and contract smooth muscle. Actions mediated mostly by β2 receptors.
Formed from plasma protein precursors called kininogens by the action of enzymes: plasma and tissue kallikreins. Destroyed by carboxypeptidase N and angiotensin converting enzyme.
What is the common mechanism of action of non-steroidal anti-inflammatory drugs (NSAIDs)?
Inhibition of cyclooxgenase.
COX-1 is constitutive enzyme, COX-2 is induced at site of inflammation.
COX-1 inhibition has GIT toxic effects, COX-2 has cardiovascular side effects.
What is tumor necrosis factor?
Cell signalling protein, a cytokine family which causes apoptosis.
Induces fever, activates granulocytes and macrophages, promotes bone reabsorption by osteoclasts, romotes fibroblast proliferation, activates endothelial cells.
