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MSS > Drugs for Gout > Flashcards

Drugs for Gout Flashcards

1
Q

What are some of the therapeutic goals for treating gout?

A
  1. Increase excretion of uric acid 2. Inhibit inflammatory cells 3. Inhibit uric acid biosynthesis 4. Provide symptomatic relief (NSAIDs or steroids – short-term)
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2
Q

Used within the first 24 hours

A

NSAIDs:

Indomethacin

Naproxen

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3
Q

What should NOT be used to treat gout?

A

Aspirin – inhibits uric acid secretion at low dose

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4
Q

Provides symptomatic relief in patients that can’t take NSAIDs

Short term use

Adverse effects with extended use

A

Steroids

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5
Q

No effect on uric acid excretion

Antimitotic: arrests cell division n G1 by interfering with microtubule and spindle formation

Binds to microtubles in inflammatory cells = neutrophils: inhibits neutrophil activation and migration

Lessens the symptoms of inflammation

A

Colchicine

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6
Q

How is colchicine metabolized?

A

Oral administration

Rapid absorption but variability

Large volume of distribution

Metabolized by CYP450

Substrate for P-glycoprotein (transmembrane protein that eliminates drugs)

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7
Q

What are some adverse effects of colchicine?

A

Narrow therapeutic-toxicity window

GI: nausea, vomiting, diarrhea, abdominal pain

Usually a latent period before symptoms

Effects rapid proliferating cells of GI

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8
Q

What are some contraindications of colchicine?

A

Hepatic/renal disease (decrease dose or less frequent dosing)

Elderly patients

Especially if also taking CYP3A4 or P-gp inhibitor

Reasion = increase concentration of colchicine

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9
Q

How is colchicine used therapeutically?

A

Acute gout attacks (within hours)

Prophylactically in patients with chronic gout

Tends not to be the drug of choice because of adverse effects

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10
Q

When is it appropriate to use prophylactical therapy for gout?

A

Frequent attacks

Disabling attacks

Urate nephrolithiasis (uric acid stones)

Urate nephropathy

Tophaceous gout: nodular masses of uric acid crystals (tophi) are deposited in different soft tissue areas of the body

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11
Q

What are some non-pharmacologial measures individuals with gout should take?

A

Abstain from alcohol

Weight loss

Discontinue medicine that impair uric acid excretion (aspirin, thiazide diuretics)

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12
Q

Inhibits terminal steps in uric acid biosynthesis

Blocks xanthine oxidase

Decreases plasma uric acid concentration, uric acid crystals dissolve

A

Allopurinol

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13
Q

How is allopurinol metabolized?

A

Prodrug

Structural analog of hypoxanthine

Converted to oxypurinol by aldehyde oxidoreductase

Plasma half-life prolonged:

allopurinol (1-2 hours)

oxypurinol (18-30 hours)

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14
Q

What are some adverse effects of allopurinol?

A

Hypersensitivity: increases if taken with ACE inhibitors, thiazide diuretics, amoxicillin

Acute gout attack: mobilizes tissue stores of uric acid, give the drug with colchicine or NSAID

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15
Q

What are the therapeutic uses of allopurinol?

A

Prevention of primary hyperurecemia of chronic gout

Severe forms of gouty nephropathy, tophaceous deposits, renal urate stones

Prophylactic treatment in secondary forms of hyperurecemia due to hematological disorders of anti-neoplastic therapy

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16
Q

Non-purine xanthine oxidase inhibitor

Forms a stable complex with both the reduced and oxidized form of xanthine oxidase and inhibits catalytic function in both states

A

Febuxostat

17
Q

Comparison of Allopurinol and Febuxostat.

A
  • Febuxostat is more potent than allopurinol
  • Febuxostat is more effective than allopurinol in the subset of patients with imparied renal function
  • Incidence of adverse events (dizziness, diarrhea, headache, nausea) similar with both drugs
  • Incidence of CV side effects (antiplatelet trialists collaboration events) was numerically higher with febuxostat than allopurinol
18
Q

Converts uric acid to allantoin (an inactive and water soluble metabolite of uric acid)

PEGylated recombinant form of urate oxidase enzyme (uricase – normally absent in humans)

A

Pegloticase

19
Q

What are the pharmacokinetics of Pegloticase?

A

Intravenous administration (every 2 weeks)

Long half-life

20
Q

What are some adverse effects of Pegloticase?

A

Infusion site reactions

Gout flare: provide prophylaxis for acute gout flares

Immune response: can form antibodies directed at PEG portion of molecule

21
Q

What is Pegloticase therapeutically used for?

A

Refractory chronic gout

22
Q

What are uricosuric agents?

Give an example.

A

Something that increases the rate of excretion of uric acid

Probenecid

23
Q

How does probenecid increase uric acid exretion?

A

Increases uric acid secretion by competing with the renal tubular acid transporter so that less urate is reabsorbed

24
Q

What are the pharmacokinetics of Probenecid?

A

Oral administration

Dose-dependent half-life

Plasma protein binding

25
Q

What are some adverse effects of probenecid?

A

Some GI side effects

Ineffective in patients wtih renal insufficiency

Contraindicated in patient with uric acid kidney stones

26
Q

What is Probenecid therapeutically used for?

A

Used for chronic gout but rarely in patients with any kidney disease or overproducers of uric acid…more likely to produce uric acid stones

27
Q

What are some drug interactions with Probenecid?

A

Interfere with renal excretion of drugs that undergo active tubular secretion, especially weak acids.

Inhibition of glucuronide conjugation of other drugs.

Methotrexate, Clofibrate, Palatrexate, Penicillin, Salicylates

28
Q

Other gout drug interactions

A

Plasma levels of drugs that are metabolized by xanthine oxidase increase – possibly to toxic levels when administered with allopurinol or febuxostat.

Life-threatening toxicities are associated with administration of concomitant therapy with P-glycoprotein or CYP3A4 inhibitors or colchicine

MSS (24 decks)

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