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Pharmacology > RA and Gout Drugs > Flashcards

RA and Gout Drugs Flashcards

1
Q

What drugs are used for symptomatic relief of RA?

A

Analgesics, NSAID, and glucocorticoids - used early in onset of disease while waiting for effects of DMARDs/BRMs

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2
Q

Is Hydroxychloroquine used to treat mild or severe RA?

A

Mild

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3
Q

How long to see effects of Hydroxychloroquine?

A

3-6 months

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4
Q

Can you combine Hydroxychloroquine with other drugs?

A

YES - Sulfasalazine and Methotrexate

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5
Q

Can Hydroxychloroquine be used during pregnancy?

A

YES - safe for pregnancy and lactation

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6
Q

What is a rare but serious side effect of Hydroxychloroquine?

A

Ocular toxicity - can result in permanent vision loss

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7
Q

How long to see effects of Sulfasalazine?

A

1-3 months

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8
Q

Can Sulfasalazine be used during pregnancy?

A

YES!

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9
Q

What are potential side effects of Sulfasalazine use?

A

Can lead to agranulocytosis (often within 2 weeks of starting; reversible) and hepatotoxicity

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10
Q

What is the drug of choice for treating moderate to severe RA?

A

Methotrexate

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11
Q

Wait…isn’t Methotrexate used in cancer?

A

YES! However, in RA it is used in a much lower dose (1000x lower) and works via a different mechanism

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12
Q

Major clinical benefit of Methotrexate

A

Decreased appearance of new bone erosions

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13
Q

What is a common side effect of Methotrexate?

A

Dose-related hepatotoxicity - abstain from alcohol when using

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14
Q

What are some rare side effects of Methotrexate?

A

Pulmonary toxicity, bone marrow suppression, increased risk of lymphoma - have to be clinically monitored while taking Methotrexate to ensure these don’t happen

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15
Q

How is Methotrexate excreted?

A

Renally - patients with renal impairment at greater risk of developing side effects

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16
Q

What are some Methotrexate contraindications?

A

Pregnancy - may lead to abortion

Not recommended for patients with liver disease or renal impairment

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17
Q

What is an alternative if patient cannot use Methotrexate?

A

Leflunomide

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18
Q

Leflunomide MOA

A

Inhibits dihydroorotate dehydrogenase - inhibits both T cell proliferation and production of autoantibodies by B cells

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19
Q

What are some adverse effects of Leflunomide?

A

Hypertension (especially with NSAID use), diarrhea, nausea, rash, HEPATOTOXICITY (more severe in patients taking methotrexate, make sure to monitor liver enzymes)

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20
Q

What are three TNF-alpha inhibitors?

A

Etanercept, Adalimumab, and Infliximab

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21
Q

TNF-alpha inhibitor MOA

A

Bind to soluble TNF-alpha and prevent it from interacting with its receptor and inducing a biological response

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22
Q

How are TNF-alpha inhibitors administered?

A

Subcutaneous injection or IV - administered weekly/biweekly

23
Q

Can TNF-alpha inhibitors be used as a monotherapy?

A

Yes, but may also be used with methotrexate

24
Q

What are adverse effects associated with TNF-alpha inhibitors?

A

Increased risk of opportunistic infections (fungal and bacterial), potential reactivation of latent TB and latent HBV
Do not give to anyone with an acute or chronic infection - decreases immune response and can be fatal

25
What are rare side effects of TNF-alpha inhibitors?
Exacerbation of pre-exisiting CHF, development of demyelinating disorders (MS), appearance of malignancies, especially lymphoma
26
Abatacept MOA
Inhibits T cell activation by blocking delivery of CD28 co-stimualatory signal necessary for T cell activation Can be used in patients not responsive to TNF-alpha inhibitors
27
What are adverse effects associated with Abatacept?
Increased risk of serious infection - screen for latent TB and HBV
28
Can Abatacept be used in conjunction with TNF-alpha inhibitors?
NO! Will lead to massive immunosuppression
29
Rituximab MOA
Binds to CD20 on B cells - IV infusion depletes B cells from the blood Effective for patients not responsive to TNF-alpha inhibitors
30
How long until you see effects of Rituximab?
3 months, however a single infusion may have effects for up to 2 years
31
What are adverse effects associated with Rituximab?
Increased infections, reactivation of latent viruses, PML due to reactivation of JC virus
32
Anakinra MOA
IL-1 receptor antagonist - completely inhibits pro-inflammatory effects of IL-1
33
What are adverse effects associated with Anakinra?
Increased risk of neutropenia, serious infections | Should not be given to patients with acute or chronic infections
34
Tocilizumab MOA
Chimeric antibody directed against IL-6 cytokine receptor | Used in patients non-responsive to TNF-alpha inhibitors or in combination with methotrexate
35
What are adverse effects associated with Tocilizumab?
Increased risk of bone marrow suppression, serious infection, hepatotoxicity, increased cholesterol, increased risk of malignancy
36
In whom is Tocilizumab contraindicated?
Patients with acute/chronic infections, pre-existing liver disease, low blood counts, or patients on immunosuppressive therapy
37
Tofacitinib MOA
Inhibits JAK tyrosine kinases involved in immune cell cytokine signaling
38
What adverse effects are associated with Tofacitinib?
Lymphopenia, neutropenia, anemia, increased risk of serious infection, lipid abnormalities, increased liver enzymes
39
What class of drugs is used to treat an acute gouty attack?
NSAIDs - these are also given prophylactically in combination with other anti-gout drugs
40
What should not be used to treat acute gouty attack?
Aspirin and salicylates - inhibit uric acid excretion at low doses and can actually induce gout
41
Is Colchicine used to treat chronic gout?
NO - used to treat acute gouty attack and used in combination with other gout drugs for prophylaxis
42
Colchicine MOA
Prevents tubulin polymerization into microtubules - decreases leukocyte migration and phagocytosis
43
Colchicine is effective within ____ hours of a gouty attack
24-48 hours
44
Are side effects of Colchicine common?
YES! Has a very narrow therapeutic window - 80% of patients experience nausea, vomiting, diarrhea
45
What type of gout patient is Probenecid used in?
Uric acid underexcreter - do NOT give to patients who overproduce uric acid as this can lead to kidney stones
46
Probenecid MOA
Blocks URAT1 transporter - decreases uric acid reabsorption and facilitates uric acid excretion
47
What are contraindications associated with Probenecid?
Patients who overproduce uric acid (can lead to kidney stones) and patients with kidney stones or underlying renal insufficiency
48
What patients are Allopurinol and Febuxostat useful for?
Patients with grossly elevated uric acid (have tophi), patients with recurrent kidney stones, and patients with renal impairment
49
Allopurinol and Febuxostat MOA
Inhibit xanthine oxidase
50
What are side effects associated with Allopurinol and Febuxostat?
Can induce acute gouty attack if not taken with NSAIDs. May also cause rash, leukopenia, thrombocytopenia
51
What is a serious side effect associated with Allopurinol use?
Allopurinol hypersensitivity syndrome - very life threatening! Patients have rash, fever, hepatitis, acute renal failure This is more common in patients taking excessively high doses of the drug w/ renal impairment and/or use of diuretics
52
What drug-drug interactions may occur with Allopurinol or Febuxostat?
Toxic levels of 6-mercaptopurine and azathioprine - these are normally metabolized by xanthine oxidase
53
What drug is used to treat drug-resistance chronic gout?
Pegloticase

Pharmacology (5 decks)

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