Gout & Eicosanoid Pharm Flashcards Preview

SBM IV CT/MS > Gout & Eicosanoid Pharm > Flashcards

Flashcards in Gout & Eicosanoid Pharm Deck (34):
1

tx options for acute attacks of gout

naproxen po
colchicine po
prednisone po (or IV or intrarticular)

2

tx options for long term uric acid lowering and gout management

allopurinol po
probenecid po
pegloticase iv

3

where does uric acid come from?

breakdown of dietary purine and purines from pt's DNA --> hypoxanthine --> xanthine --> uric acid

4

lifestyle changes for gout

alter diet (lower purines, drink more water)
reduce alcohol intake

5

colchicine

for both acute attacks and prevention of gout
MOA: not clear, reduces WBC response to uric acid crystals
ADRs: nausea, vomiting, diarrhea often dose limiting

6

allopurinol

MOA: xanthine oxidase inhibitor
for gout prevention
ADRs: rare bad things like hypersensitivity, vasculitis, agranulocytosis, hepatic necrosis, TENs/Steven Johnson, can precipitate and acute attack
interactions: dramatic increase in toxicity of azathioprine and 6-MP

7

probenecid

MOA: increases renal excretion of uric acid (competitively inhibits reabsorption of uric acid in PCT) + competitively inhibits active tubular secretion of Pen antibiotics
ADRs: avoid in pts w/ previous allergy or uric acid kidney stones, may precipitate acute gout attack

8

pegloticase

pegylated urate oxidase enzyme (produced by e coli) that catalyses uric acid --> allantoin (harmless metabolite cleared by kidney)
IV, expensive
ADR: antibodies develop in 92% of pts, making drug less effective; occasionally causes anaphylaxis, can precipitate acute attacks of gout

9

drugs that imitate prostacyclin (PGI2)

epoprostenol, iloprost

10

drugs that imitate PGE2

misoprostol, alprostadil, dinoprostone

11

drug that imitates PGF2a

latanoprost

12

MOA of montelukast and zafirlukast

leukotriene receptor antagonist

13

MOA of zileuton

lipoxygenase inhibitor

14

where do eicosanoids come from?

synthesized as needed (not stored)
derived from phospholipids in cell membranes - arachidonic acids
arachadonic acid --> eicosanoids via PLA2 - phospholipase A2 = rate-limiting step

15

where do prostaglandins and leukotrienes come from?

arachidonic acids --> prostaglandins via COX
arachidonic acid --> leukotriene via LIPOXYGENASES

16

how does prostaglandin signalling work?

GPCR --> variety of secondary messengers

17

major areas effected by prostaglandins

1. airway
2. GI
3. vascular
4. uterine
PGF2 always contracts
PGI2 relaxes vascular and uterine tissue
PGE2 usually contracts

18

what prostacyclins are protective of GI tract?

PGE2 and PGI2: increase mucosal blood glow, increase mucus secretion + inhibit gastric acid secretion

19

major mediators of asthma

leukotrienes: LTC4, LTD4

20

major mediator of pain and fever

PGE2

21

which prostaglandins mediate dysmenorhea?

PGE2 and PGF2

22

which prostaglandin regulates intraocular eye pressure?

PGF2

23

difference in MOA b/t glucocorticoids and NSAIDS

glucocorticoids inhibit levels/quantity of COX2, while NSAIDs inhibit enzyme activity

24

counterbalance of thromboxane and prostacyclin in vascular system

COX1 makes platelets and TXA2 --> vasoconstriction, platelet aggregation
COX1+2 make endothelial PGI2 --> vasodilation and anti- platelet aggregation
results in physiological balance of platelet function

25

basis of adverse cardiac events assoc w/ COX2 inhibitors

tips the platelet function balance --> COX1 only --> vasoconstriction and platelet aggregation w/out counterbalance

26

SRS-A

slow reacting substance of anaphylaxis: mix of leukotrienes, especially LTC4 and LTD4 --> contract respiratory muscle

27

aspirin hypersensitivity asthma

block COX1 and COX2 --> more arachadonic acid diverted to make leukotrienes --> asthma

28

misoprostol

for ulcer prevention during long-term NSAID therapy
stim mucus and bicarb secretion, inhibits gastric acid secretion; heals gastric ulcers as effectively as H2 blockers
adverse effects: diarrhea, abdominal discomfort
contraindicated in pregnancy

29

what type of drug can keep patent ductus open in infants w/ heart defects?

PGE2 and analogs

30

how to close ductus arteriosus open in otherwise healthy infant?

NSAIDs - ibuprofen, indomethacin

31

iloprost (ilomedin)

prostacyclin analog for pulmonary hypertension

32

alprostadil

prostaglandin, PGE1 analog
vasodilator for erectile dysfunction that does not respond to PDE-5 inhibitors
admin: topical, injection, urethral suppository

33

montelukast

leukotriene inhibitor for asthma (LTD4-receptor antagonist), oral

34

zileuton

inhibitor of 5-lipoxygenase for asthma prophylaxis and chronic tx
po