Gout & Eicosanoid Pharm Flashcards

1
Q

tx options for acute attacks of gout

A

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

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2
Q

tx options for long term uric acid lowering and gout management

A

allopurinol po
probenecid po
pegloticase iv

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3
Q

where does uric acid come from?

A

breakdown of dietary purine and purines from pt’s DNA –> hypoxanthine –> xanthine –> uric acid

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4
Q

lifestyle changes for gout

A
alter diet (lower purines, drink more water)
reduce alcohol intake
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5
Q

colchicine

A

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

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6
Q

allopurinol

A

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

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7
Q

probenecid

A

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

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8
Q

pegloticase

A

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

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9
Q

drugs that imitate prostacyclin (PGI2)

A

epoprostenol, iloprost

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10
Q

drugs that imitate PGE2

A

misoprostol, alprostadil, dinoprostone

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11
Q

drug that imitates PGF2a

A

latanoprost

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12
Q

MOA of montelukast and zafirlukast

A

leukotriene receptor antagonist

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13
Q

MOA of zileuton

A

lipoxygenase inhibitor

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14
Q

where do eicosanoids come from?

A

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

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15
Q

where do prostaglandins and leukotrienes come from?

A

arachidonic acids –> prostaglandins via COX

arachidonic acid –> leukotriene via LIPOXYGENASES

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16
Q

how does prostaglandin signalling work?

A

GPCR –> variety of secondary messengers

17
Q

major areas effected by prostaglandins

A
  1. airway
  2. GI
  3. vascular
  4. uterine
    PGF2 always contracts
    PGI2 relaxes vascular and uterine tissue
    PGE2 usually contracts
18
Q

what prostacyclins are protective of GI tract?

A

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

19
Q

major mediators of asthma

A

leukotrienes: LTC4, LTD4

20
Q

major mediator of pain and fever

21
Q

which prostaglandins mediate dysmenorhea?

A

PGE2 and PGF2

22
Q

which prostaglandin regulates intraocular eye pressure?

23
Q

difference in MOA b/t glucocorticoids and NSAIDS

A

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

24
Q

counterbalance of thromboxane and prostacyclin in vascular system

A

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