S95: Anti-Inflammatory Drugs
WITH VERIFIED SOLUTIONS
What is the intermediate formed by COX between arachidonic acid
and PGH2? - answer PGG2
What mechanism is responsible for muscle relaxation? - answer Gs
- adenylyl cyclase --> cyclic AMP --> Ca
What mechanism is responsible for muscle contraction? - answer
Gq - phospholipase C --> IP3 --> Ca
What mechanism inhibits Gs? - answer Gi - reduces adenylyl
cyclase, CAMP
Whats a prostanoid? - answer ecoisanoid produced by COX
pathway (prostaglandin, thromboxane, prostacyclin)
What are the systemic effects of PGD2? - answer regulates
wake/sleep cycle, causes vasodilation
What are the systemic effects of PGE2? - answer vasodilation
(including afferent renal arteries), reduce nociception threshold,
increase mucus production, decrease gastric acid secretion
What are the systemic effects of PGI2? - answer vasodilation,
decrease platelet aggregation, also reduces nociception threshold
What are the general effects of INHIBITING prostanoids on the
immune system? - answer decrease inflammation, increased pain
, threshold (since prostanoids enhance pain), decrease leukocyte
infiltration
What are the general effects of INHIBITING prostanoids on the renal
system? - answer decrease blood flow to kidneys (afferent),
increased retention of potassium (hyperkalemia) and water (leads
to hyponatremia)
What are the general effects of INHIBITING prostanoids on the
cardiovascular system? - answer depending on whether platelet
aggregation is increased or decreased - stroke or bruising risk, MI,
dysregulation of blood pressure
What are the general effects of INHIBITING prostanoids on the GI
system? - answer decreased mucus secretion and DECREASED
INHIBITION of gastric acid can lead to gastric/duodenal ulcers
How do glucocorticoids influence production of prostanoids? -
answer inhibit cPLA2 which decreases amount of arachidonic acid
produced and therefore amount of prostanoids produced
What are the main differences between COX1 and COX2? - answer
COX1 is constitutively active in most cells in body - produce all five
of the main prostanoids (PGD2, PGE2, PGI2, TXA2, PGF2α) for
housekeeping purposes
COX2 is inducible, mostly in immune cells - mainly catalyzes
production of PGI2, PGE2 (therefore an inhibitor will prevent
vasodilation, increase pain threshold, decrease stomach mucus and
increase gastric acid secretions)
antipyretic - answer fever reducer
What is the mechanism of aspirin? (ASA) - answer irreversibly
binds to both COX-1 and COX-2
WITH VERIFIED SOLUTIONS
What is the intermediate formed by COX between arachidonic acid
and PGH2? - answer PGG2
What mechanism is responsible for muscle relaxation? - answer Gs
- adenylyl cyclase --> cyclic AMP --> Ca
What mechanism is responsible for muscle contraction? - answer
Gq - phospholipase C --> IP3 --> Ca
What mechanism inhibits Gs? - answer Gi - reduces adenylyl
cyclase, CAMP
Whats a prostanoid? - answer ecoisanoid produced by COX
pathway (prostaglandin, thromboxane, prostacyclin)
What are the systemic effects of PGD2? - answer regulates
wake/sleep cycle, causes vasodilation
What are the systemic effects of PGE2? - answer vasodilation
(including afferent renal arteries), reduce nociception threshold,
increase mucus production, decrease gastric acid secretion
What are the systemic effects of PGI2? - answer vasodilation,
decrease platelet aggregation, also reduces nociception threshold
What are the general effects of INHIBITING prostanoids on the
immune system? - answer decrease inflammation, increased pain
, threshold (since prostanoids enhance pain), decrease leukocyte
infiltration
What are the general effects of INHIBITING prostanoids on the renal
system? - answer decrease blood flow to kidneys (afferent),
increased retention of potassium (hyperkalemia) and water (leads
to hyponatremia)
What are the general effects of INHIBITING prostanoids on the
cardiovascular system? - answer depending on whether platelet
aggregation is increased or decreased - stroke or bruising risk, MI,
dysregulation of blood pressure
What are the general effects of INHIBITING prostanoids on the GI
system? - answer decreased mucus secretion and DECREASED
INHIBITION of gastric acid can lead to gastric/duodenal ulcers
How do glucocorticoids influence production of prostanoids? -
answer inhibit cPLA2 which decreases amount of arachidonic acid
produced and therefore amount of prostanoids produced
What are the main differences between COX1 and COX2? - answer
COX1 is constitutively active in most cells in body - produce all five
of the main prostanoids (PGD2, PGE2, PGI2, TXA2, PGF2α) for
housekeeping purposes
COX2 is inducible, mostly in immune cells - mainly catalyzes
production of PGI2, PGE2 (therefore an inhibitor will prevent
vasodilation, increase pain threshold, decrease stomach mucus and
increase gastric acid secretions)
antipyretic - answer fever reducer
What is the mechanism of aspirin? (ASA) - answer irreversibly
binds to both COX-1 and COX-2
