Lec 19 Flashcards
what enzyme(s) are inhibited by NSAIDs?
COX1 and COX2
what is Arachidonic acid?
an eicosanoid which is the precursor to prostaglandins, leukotrienes, lipoxins, and epi-lipoxins
prostaglandins and leukotrienes are responsible for ____ of inflammation
initiation
lipoxins and 15-epi-lipoxins are responsible for ____ of inflammation
resolution
what enzyme(s) are inhibited by aspirin?
COX2
Arachidonic acid’s role in initiation is ___-inflammatory, whereas its role in resolution is ___-inflammatory
pro
anti
what three classes of enzymes produce eicosanoids?
cyclooxygenases, lipoxygenases, and cytochrome P450
epoxygenases
Arachidonic acid is one of the key precursor ____ _____ involved in the biosynthesis of _____ ______.
fatty acids
lipid mediators.
T/F Arachidonic acid is an essential fatty acid synthesized in mammals
False, it is an essential fatty acid that cannot be synthesized in mammals
Arachidonic acid is a major component of ______, so that it is important for the integrity of cellular membranes.
phospholipids
what does Arachidonic acid regulate which may be important in animal tissues?
apoptosis
T/F The stereochemistry of eicosanoids is not important for their biological function.
False, it is important
what enzyme is responsible for the release of
Arachidonic Acid from membrane lipids?
Phospholipase A2
what does TXA2 do?
vasoconstriction and platelet formation
what does PGD2 do?
erythema, edema, pain, and decrease platelet formation
what does PGE2 do?
erythema, edema, pain, and fever
what does PGF2 do?
vasoconstriction
what does PGI2 do?
vasodilation and decrease platelet formation
which of the prostaglandins does misoprostol act like?
what does it do?
PGE1
induces labor
which prostaglandin receptor does alprostadil bind to?
what does it treat?
PGE1
E.D.
which prostaglandin receptor does dinoprostone bind to?
what does it do?
PGE2
induces abortion
which prostaglandin receptor does carboprost bind to?
what does it do?
PGF2
reduces postpartum hemorrhage and induces abortion
which of the prostaglandins does latanoprost act like?
what does it do?
PGF2
causes vasoconstriction in eyes
which prostaglandin receptor does epoprostenol bind to?
what does it do?
PGI2
dec platelet aggregation
flufenisal and diflunisal:
what are they?
NSAIDs
what drug class are mesalamine, sulfasalazine, and olsalazine? what are they used for?
salicylate
inflammatory bowel disease
what is indomethacin used for?
anti-inflamm/antipyretic
what is sulindac?
what is its relationship to arachidonic acid?
an arylacetic acid
competes with arachidonic acid at active site of COX
ketorolac is more potent as an? with minor?
has a high affinity for?
analgesic, anti-inflamm
COX1
tolmetin has a high affinity for?
COX1
diclofenac and etodolac bind to COX1 or COX2?
COX2
ibuprofen, naproxen, fenoprofen, ketoprofen, and flurbiprofen are all ____ acid analogs
arylpropionic
mefenamic acid, flufenamic acid, and meclofenamic acid are all what type of acid?
they are stronger than what drug?
anthranilic acid
aspirin
acetaminophen may act on COX3 in the?
CNS
what does Zileuton do?
what does it treat?
inhibits 5-lipoxygenase that converts arachidonic acid
chronic asthma
zafirleukast is used for?
chronic asthma
Montelukast is used for?
chronic asthma and allergic rhinitis
