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FPP MSS > Joint Disease Drugs > Flashcards

Joint Disease Drugs Flashcards

1
Q

What is the mechanism of Colchicine?

A

Anitmitotic; it arrest cells in G1 by binding microtubules in inflammatory cells (PMNs) which inhibits neutrophil activation/migration and lessons the symptoms of inflammation.

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2
Q

What are the uses of Colchicine?

A

1) Acute gout attacks (within hours)

2) Prophylactically in patients with chronic gout

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3
Q

Why does Colchicine tend to NOT be a drug of choice for gout?

A

Because of adverse effects

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4
Q

What are the adverse effects of Colchicine?

A

SIGNIFICANT effects and narrow therapeutic window

GI side effects: N/V/D/abdominal pain (because it effects the rapidly proliferating cells of GI tract)

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5
Q

How is Colchicine a) administered b) absorbed c) metabolized?

A

a) Colchicine is orally administered
b) Colchicine has rapid absorption and is deposited in tissue stores/forms complexes with tubulin so it has a large volume of distribution
c) Colchicine is metabolized by CYP540 enzymes and is a substrate for P-glycoprotein

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6
Q

What is Colchicine contraindicated?

A

1) hepatic and renal disease (lower dose)
2) elderly
3) Patients taking CYP3A4 or P-gp inhibitors (because Colchicine concentration increases)

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7
Q

What is the mechanism of Allopurinol?

A

It inhibits the terminal steps in uric acid biosynthesis by blocking Xanthine Oxidase to decrease plasma uric acid concentration and dissolve uric acid crystals

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8
Q

What are the uses of Allopurinol?

A

1) Prevention of primary hyperurecemia of Chronic Gout

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

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9
Q

How is Allopurinol metabolized?

A

Allopurinol is the analog of hypoxanthine but it is metabolized to a more active compound Oxypurinol by aldehyde oxidoreductase.

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10
Q

What is the difference between Oxypurinol and Allopurinol?

A

Oxypurinol is more active and has a longer half life (20 hours compared to 2 hours)

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11
Q

What are the side effects of Allopurinol?

A

1) Hypersensitivity (serious but not always immediate, increases with ACE inhibitors, amoxicillin and thiazide diuretics)
2) Acute Gout (mobilizes tissue stores of uric acid when biosynthesis is turned off - need to give NSAIDs or Colchicine)

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12
Q

What is the mechanism of Febuxostat?

A

Non-purine Xanthine Oxidase inhibitor that forms a stable complex with the oxidized and reduced forms of the enzyme to inhibit catalytic function in both states

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13
Q

What are the differences between Febuxostat and Allopurinol?

A

1) Febuxostat is more potent
2) Febuxostat is more effective for patients with renal failure
3) Adverse side effects are similar except Febuxostat has higher incidence of CV side effects

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14
Q

What are the uses of Febuxostat?

A

Same uses as Allopurinol

1) Prevention of primary hyperurecemia of Chronic Gout
2) Severe forms of gouty nephropathy, tophaceous deposits, renal urate stones

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15
Q

What is the mechanism of Pegloticase?

A

PEGylated recombinant form of urate-oxidase enzyme that converts uric acid to Allantoin.

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16
Q

What is Allantoin?

A

An inactive and water soluble metabolite of uric acid

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17
Q

What is Pegloticase used for?

A

1) patients with HUGE uric load

2) Refractory chronic gout

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18
Q

How is Pegloticase administered?

A

IV administration every two weeks (long half life)

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19
Q

What are the side effects of Pegloticase?

A

1) Infusion site reaction
2) Gout flare
3) Immune response (most concerning - can get antibodies against PEG portion of molecule)

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20
Q

What is the mechanism of Probenecid?

A

Increases the rate of excretion of uric acid by competing with renal tubular acid transporter so less urate is reabsorbed

21
Q

What are the uses of Probenecid?

A

Chronic Gout

22
Q

When is Probenecid contraindicated?

A

1) Patients with kidney disease

2) Overproducers of uric acid (more likely to produce uric acid stones in kidney)

23
Q

How is Probenecid administered?

A

Oral administration

24
Q

What is the half life of Probenecid dependent on?

A

Dose dependent

25
Q

What are the side effects of Probenecid?

A

1) Some GI

2) Ineffective in patients with renal insufficiency

26
Q

What are two drugs that have interactions with Allopurinol?

A

Mercaptopurine metabolism is decreased and Azathioprine detoxification is decreased so there is increased toxicity (BM suppression)

27
Q

What drugs are used to treat gout?

A

Colchicine, Allopurinol, Febuxostat, Probenecid, Pegloticase

28
Q

What is the mechanism of Etanercept?

A

Recombinant fusion protein that inhibits ability of TNF alpha to bind to its receptor

29
Q

How is Etanercept a) administered b) elimination half life and c) onset of action?

A

a) Administered IV or SubQ
b) Elimination half life is more than 3 days
c) Onset of action is 1-2 weeks

30
Q

What is Etanercept used for?

A

1) Moderate to severe RA
2) Juvenile RA
3) Early stage RA

31
Q

What are the adverse effects of Etanercept?

A

1) Injection site reactions
2) Increased risk of infections**
3) Lymphomas in children/adolescent patients

32
Q

What is the mechanism of Adalimumab?

A

IgG human monoclonal antibody that binds soluble AND transmembrane forms of TNF alpha and prevents it binding its receptor

33
Q

How is Adalimumab administered?

A

SubQ every other week

34
Q

What are the uses of Adalimumab?

A

1) Active rheumatoid arthritis (used alone or in combo with Methotrexate and other DMARDs)
2) Active juvenile idiopathic arthritis (alone or in combo with Methotrexate)

35
Q

What are the adverse effects of Adalimumab?

A

1) Injection site reactions
2) Increased risk of infections
3) Lymphomas

36
Q

What is the mechanism of Tocilizumab?

A

Humanized antibody binds to soluble and membrane bound IL6 receptors to inhibit IL6 mediated signaling

37
Q

How is Tocilizumab administered?

A

IV administration every 4 weeks or SubQ every other week

38
Q

What are the uses of Tocilizumab?

A

1) Indicated for adult patient with moderate to severely active RA who have had inadequate response to one or more TNF antagonists

39
Q

What are the side effects of Tocilizumab?

A

1) Injection site reactions
2) Increased risk of infections
3) Alterations in lipid profile** (Increases in total cholesterol, triglycerides, LDL or HDL)

40
Q

What is the mechanism of Tofacitinib?

A

It is a Janus Kinase inhibitor that inhibits cytokine signaling cascade

41
Q

What are the uses of Tofacitinib?

A

1) Treatment of moderately to severely active RA in patients who have had inadequate response/intolerance to methotrexate
2) May be used as mono therapy or in combo with methotrexate

42
Q

What are the side effects of Tofacitinib?

A

1) Increased risk of infections

2) Increase in cholesterol

43
Q

How is Tofacitinib administered?

A

Orally

44
Q

How is Tofacitinib metabolized?

A

Metabolism is mediated by CYP3A4 with minor CYP2C19 contribution

45
Q

What drugs are used to treat Rheumatoid arthritis?

A

Etanercept, Adalimumab, Tocilizumab, Tofacitinib, Abatacept, Anakinra, Rituximab

46
Q

What is the mechanism of Anakinra?

A

It blocks IL-1 receptor signaling

47
Q

What is the mechanism of Abatacept?

A

It blocks T cell activation

48
Q

What is the mechanism of Rituximab?

A

Antibody directed against CD20 antigen on B cells

49
Q

What is the mechanism of Methotrexate?

A

It inhibits the proliferation and activity of T cells and B cells

FPP MSS (6 decks)

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