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Block 4 Pharm > Gout and Eicosinoids-CT-MS > Flashcards

Gout and Eicosinoids-CT-MS Flashcards

1
Q

What are points for intervention in patients with gout?

A

1) Heavy dietary ingestion: alter diet 2) Alcohol: reduce intake of alcohol 3) Excessive excretion in urine: decrease production 4) Excessive production but low amounts in urine: decrease production, or increase urinary excretion 5) Severe pain of acute gout: treat pain and inflammation

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2
Q

What is the treatment for an acute gout attack?

A

1) NSAID (1st line) => Drug of choice unless contraindicated - Usually naproxen or indomethacin - Avoid aspirin (why?) 2) Colchicine (2nd line) => If can’t take NSAID or steroid - Effective but often get unpleasant side effects 3) Steroid, oral (3rd line) => For patient unable to take NSAID or colchicine - Usually oral prednisone or prednisolone

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3
Q

To what drug class does naproxen belong to?

A

NSAID (non-selective), anti-inflammatory, analgesic, antipyretic

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4
Q

What is the mechanism of action of naproxen?

A

inhibit COX 1 and 2, reducing production of inflammatory prostaglandins. Helps to relieve severe pain from gout within hours to days

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5
Q

What adverse drug reactions are associated with naproxen?

A

Gastric upset, gastritis, ulceration, ARF; avoid in patients with “allergy” to aspirin; fluid retention and edema

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6
Q

What interactions are associated with naproxen?

A
  • reduce activity of antihypertensives - may increase risk of GI bleeding with warfarin
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7
Q

To what drug class does colchicine belong?

A

antigout drug for both acute attacks and for prevention

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8
Q

What adverse drug effects are associated with colchicine?

A

most commonly nausea, vomiting, diarrhea–these are usually dose-limiting

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9
Q

What drug-drug interactions are associated with colchicine?

A

erythromycin and other macrolides may increase risk of toxicity

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10
Q

To what drug class does allopurinol belong?

A

antigout drug, xanthine oxidase inhibitor

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11
Q

What is the mechanism of action of allopurinol?

A

Blocks the enzyme xanthine oxidase (with its own metabolite), leads to less uric acid produced, and more hypoxanthine and xanthine in both blood and urine; when begun - May need to give colchicine as well to prevent acute flare of gout

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12
Q

What ADRs are associated with allopurinol?

A

hypersensitivity vasculitis, agranulocytosis, hepatic necrosis, TEN/Stevens Johnson syndrome; can precipitate an acute attack of gout

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13
Q

What drug-drug reactions are associated with allopurinol?

A

Dramatic increase in toxicity of azathioprine and 6-MP

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14
Q

What drugs are used for chronic/management of gout?

A

-Allopurinol po -Probenecid po -Pegloticase iv

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15
Q

What is the mechanism of action of probenecid?

A

Competitively inhibits the active reabsorption of uric acid at the PCT,thereby increasing urinary excretion of uric acid (uricosuric effect); also competitively inhibits the active tubular secretion of Pen and other weak acid antibiotics, thereby leading to higher serum levels

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16
Q

What ADRs are associated with probenecid?

A
  • Contraindicated with previous allergy, or those with uric acid kidney stones - Risk of aplastic anemia, hepatic necrosis, allergy - Can precipitate an acute attack of gout!!
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17
Q

What drug-drug interactions are associated with probenecid?

A

May significantly slow the renal clearance of drugs such as Pen G, cephalosporins, MTX (methotrexate)

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18
Q

What is the drug class and indication for pegloticase?

A

A pegylated urate oxidase enzyme (recombinant mammalian enzyme, produced in E. coli) approved by FDA for IV treatment of chronic severe symptomatic gout in adults who have not responded to, or can’t tolerate, older and simpler treatments

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19
Q

What is the mechanism of action of pegloticase?

A

Uricase catalyzes oxidation of uric acid to allantoin, a metabolite that is inert, water soluble, and cleared by the kidney

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20
Q

What are the ADRs of pegloticase?

A
  • Antibodies develop in 92% of patients => makes drug less effective - Occasionally (4/85 patients) can cause anaphylaxis; can precipitate acute attacks of gout - Should receive an antihistamine and a corticosteroid prior to infusion; prophylaxis with an NSAID or colchicine recommended for 6 months
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21
Q

What are eicosinoids made of?

A
  • Phospholipids with arachidonic acid being the primary source
22
Q

What are the rate limiting steps in the production of eiocosinoids?

A

1) Release of Arachidonic Acid by Phospholipase A2 - release of arachidonic acid may be limited by mediators of inflammation 2) Metabolism of Arachidonic Acid by either -Cyclo-oxygenases = Prostaglandins -Lipoxygenases = Leukotrienes

23
Q

What types of receptors do prostaglandins activate?

A

Prostaglandins activate g-protein coupled receptors (relax and contract muscle) - Clinically important effects in brain, circulation, GI, blood, kidney and reproductive organs

24
Q

What are the effects of prostaglandins on airway smooth muscle?

A

-PGE2, PGI2 = relax respiratory smooth muscle -PGF2a, = contract

25
Q

What are the effects of prostaglandins on GI smooth muscle?

A

-PGE2, PGF2a =contract longitudinal muscle (colicky cramps) watery diarrhea, vomiting -PGE2 = relaxes circular muscle

26
Q

What are the effects of prostaglandins on vascular smooth muscle?

A

-TXA2, PGF2a = vasoconstrictor -PGI2, PGE2 = vasodilator

27
Q

What are the effects of prostaglandins on uterine smooth muscle?

A

-PGE2, PGF2a, TXA2 = contract -PGI2 = relax

28
Q

What are the effects of PGE2 on the GI?

A
  • Cytoprotective effect (inc mucosal blood flow, inc mucus secretion) -Inhibit gastric acid secretion
29
Q

What are the major mediators of asthma?

A
  • LTC4, LTD4 pathologic for asthma - Bronchoconstriction, increase mucus secretion, increased vascular permeability
30
Q

What prostaglandins are important for sensing painful stimuli and causing fever?

A

PGE2 => sensitize nerve endings to painful stimuli - PGE2 elevates hypothalamic set-point for temperature control in fever

31
Q

What amplifies the inflammatory/immune response to RA?

A
  • Eicosanoids amplify the inflammatory/immune response in R.A.
32
Q

Which prostaglandins cause dysmenorrhea?

A

PGE2 and PGF2

33
Q

What is the role of PGF2 in the eye?

A

PGF2 lower intraocular pressure

34
Q

Which hormones reduce the activity of PLA 2 and the synthesis of COX 2?

A

Corticosteriods reduce the activity of PLA2 and synthesis of COX2

35
Q

Which drug is a irreversible COX inhibitor?

A

Aspirin irreversibly inhibit COXs while all other NSAIDs are reversible inhibitors (anti-thrombotic agent)

36
Q

What are COX 2 inhibitors responsible for?

A

1) Vasodilation

2) Anti-platelet Aggregation
- reason why COX 2 inhibitors are associated with adverse cardiac events

37
Q

What is the second messenger for leukotrienes?

A

The second messenger for leukotrienes is IP3 with a subsequent increase in [Ca2+] in the cytosol.

38
Q

What is SRS-A?

A

SRS-A = slow-reacting substance of anaphylaxis
- Material originally identified by bioassay from tissues of animals in anaphylactic shock

39
Q

What leukotrienes make up SRS-A?

A

LTC4 and LTD4

40
Q

What is the role of leukotrienes in inflammation?

A
  • Directly involved in edema formation
  • Increased vascular permeability
  • Chemotactic for neutrophils and eosinophils
  • Contribute to tissue damage
  • Participate in RA
41
Q

What is the role of leukotrienes in asthma?

A

Leukotrienes are one of the main mediators of asthma
-LTC4 and LTD4 are more potent that histamine or the PGs in contracting respiratory smooth muscle

42
Q

How can aspirin hypersensitivity cause asthma?

A

Aspirin induced hypersensitivity asthma may be exacerbated by diverting arachidonic acid to leukotrienes

43
Q

What are eicosinoids?

A

Eicosinoids are derivatives of arachidonic acid

44
Q

What is Misoprostol and what prostaglandin is it an analog of?

A

Misoprostol (prodrug) inhibits gastric acid secretion to prevent ulcers caused by NSAIDS but causes abortions
- It is an analog of PGE1 and its receptor is EP1

45
Q

What is the action of Misoprostol ?

A
  • Stimulates mucus and bicarbonate secretion, Inhibits gastric acid secretion
  • Heals gastric ulcers as effectively as H2 antagonists
  • Not as effective on duodenal ulcers
46
Q

What are the adverse side effects of misoprostol?

A

-Diarrhea and occasional abdominal discomfort

47
Q

What are the cardiac effects of prostaglandins on infants with heart defects?

A

PGE2 and analogs are used to keep patent ductus open in infants with heart defects

48
Q

What are the cardiac effects of NSAIDs on healthy infants?

A

NSAIDs (Ibuprofen, indomethacin) are used to close ductus in otherwise healthy infant.

49
Q

What is iloprost?

A

Iloprost is a stable second generation analog of prostacyclin that is used for pulmonary hypertension

50
Q

What is the use of Alprostadil?

A

Alprostadil is a PGE1 analog that works as a vasodilatorto treat erectile dysfunction that does not respond to PDE-5 inhibitors (e.g. sildenafil)

51
Q

What are the side effects of alprostadil?

A
  • penile pain (29-49% of users)
  • urethral bleeding (5%)
  • hypotension within 1 hour of use (3%)

Block 4 Pharm (5 decks)

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