Antirheumatic Drugs Flashcards

1
Q

Analgesia for osetoarthritis includes:

A

APAP
NSAIDs
COX-2 inhibitors

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2
Q

IF inflammation is present in osteoarthritis what should be prescribed?

A

NSAIDs
COX-2 inhibitors
Intra-articular corticosteroids

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3
Q

What drug is not effective in RA?

A

APAP, no effect on inflammatory component

Non-acetylated salicylates also less effective than traditional NSAIDs

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4
Q

Why is ASA rarely used in RA?

A

AE of high doses needed to achieve anti-inflamm effects

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5
Q

Which drugs are used for symptomatic therapy of RA and which to prevent/slow disease progression?

A

Symptomatic- NSAIDs, corticosteroids(systemic, intra-articular)
Prevent/slow- DMARDs (disease modifying antirheumatic drugs)

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6
Q

How are corticosteroids used in RA?

A
  • Life threatening complications of RA, like vasculitis
  • Bridge time to onset of action of DMARDs
  • Pulse for acute flare ups
  • Intra-articular therapy for very acute inflammation
  • *Do not use longterm d/t SE
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7
Q

Long term AE of corticosteroids:

A
Hyperglycemia 
Catatracts 
Glaucoma 
Aspetic necrosis of weight bearing joints
Osteoporosis
Cushing's syndrome
Adrenal suppresion 
Sodium and water retention 
CNS side effects (high doses)
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8
Q

When dosing corticosteroids, the ______ does possible should be used.

A

Lowest

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9
Q

Patients will need to be tapered after being on corticosteroids for how long and why?

A

> 2wks

prevent withdrawal secondary to adrenal suppression

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10
Q

Coricosteroids include:

A
Cortisone
Hydrocortisone
Prednisone 
Prednisolone 
Methylprednisolone
Triamcinolone
Dexamethasone 
Betamethasone
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11
Q

Which corticosteroids should be avoided in patients with CHF and HTN and why?

A

(in order of most to lease mineralcorticoid activity)
Cortisone
Hydrocort
Prednisone
Prednisolone
These have higher mineralcorticoid activity and cause more sodium and water retention

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12
Q

When should DMARDs be started?

A

As soon as RA is diagnosed to prevent/slow progression of joint destruction and deformities

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13
Q

Conventional DMARDs include:

A
Hydroxychloroquine (Plaquenil, Quineprox)
Methotrexate
Azathioprine (Imuran, AZA)
Gold 
Penicillamine 
Sulfasalazine 
Leflunomide 
Minocycline 
Cyclophosphamide
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14
Q

Biologic DMARDs include:

A
Etanercept (Enbrel)
Infliximab (Remicade)
Adalimumab (Humira)
Certolizumab pegol (Cimzia)
Golimumab (Simponi)
Tocilizumab (Acetmra)
Rituximab (Rituxan)
Abatacept (Orencia)
Anakinra (Kineret)
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15
Q

How long does it typically take DMARDs to elicit a response?

A

3-6months

use NSAIDs or corticosteroid to manage s/s, NSAIDs often continued even once DMARDs begin to work

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16
Q

What should be monitored to assess efficacy of DMARDs?

A

ROM

ADLs

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17
Q

Which DMARDs, which used to be the standard of care, are seldom used d/t their high incidence of toxicity?

A

Gold (oral or IV) and Penicillamine

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18
Q

S/s of toxicity of Gold or Penicillamine?

A

Myelosuppresion, proteinuria, stomatitis rash, altered taste perception (penicillamine), visual changes (gold)

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19
Q

Azathioprine, a conventional DMARD, is also used for ______ ______.

A

Crohns Disease (rarely used for RA)

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20
Q

Azathioprine is a prodrug for what and what does it do?

A

Mercaptopurine

Immunosuppressant

21
Q

S/s of azathioprine toxicity are:

A

Mylosuppression, hepatotoxicity, rash, infection

reserved for aggressive disease or serious complications like vasculitis

22
Q

Hydroxychloroquine (PO), a conventional DMARD, is also used as an ______ ______ .

A

Anti-malarial drug

23
Q

Hydroxychloroquine is most commonly used for what type of RA and may take up to how long before a clinical effect is seen?

A

Used for mild RA

May take 6mos

24
Q

Toxicity of Hydroxychloroquine includes what s/s:

A

Usually well tolerated, some GI upset

Retinopathy is rare but ophthalmology exams are recommended q6-12mos

25
Sulfasalazine (PO) is used for what type of RA and what other diseases?
Mild RA | Crohns Disease and ulcerative colitis (more often used for these)
26
What is Sulfasalazine's MOA:
Cleaved by intestinal bac to sulfapyridine(active metabolite) and 5-ASA. It can bind to iron and decrease absorption, significant in patients taking abx d/t decreased gut flora conversion to active form may be reduced
27
AE of Sulfasalazine:
GI upset Rash Bodily fluid can turn yellow-orange
28
Leflunomide's (PO), a conventional DMARD, MOA:
Inhibitor of pyrimidine synthesis= altered lymphocyte activation and decreased inflamm response
29
Leflunomide's is contraindicated in what type of patients?
``` Pregnant women (may d/c in potential fathers) Category X/teratogenic ```
30
Toxicties of Leflunomide include:
Hepatotoxicity Reversible alopecia GI distress
31
In case of toxicity or patients wishing to stop Leflunomide what can be given to lower drug levels?
Cholestyramine | otherwise half life of active met= 2wks and could take months
32
Methotrexate, a conventional DMARD, is available:
PO, IM, SubQ
33
MOA of Methotrexate:
Folate antagonist= purine biosynthesis inhibition cytokine production inhibition, adenosine production stimulation =anti-inflammatory effect (patients need folic acid replacement)
34
Advantages of Methotrexate:
Well tolerated Cheapest DMARD Symptomatic relief in 1 month
35
Toxicities of Methotrexate include:
GI upset Megaloblastic anemia (treat with folic acid) Hepatoxicity
36
What are biologic DMARDs?
Genetically developed proteins
37
Advantage of biologic DMARDs:
No routine laboratory monitoring
38
Disadvantages of biologic DMARDs:
Risk of infections and malignancy Temporarily suspend treatment if inf. occurs TB skin test prior to use Very expensive IV, subQ with common injection site reactions
39
Etanercept, infliximab, adalimumab, certolizumab, pegol, golimumab are all biologic DMARDs that are also:
TNF-a Blockers | Downregulate or antagonize tumor necrosis factor-a = cytokine mediator of RA
40
Many of the TNF-a blockers are used in combination with:
Methotrexate or other DMARDs
41
What black box warning do TNF-a blockers carry with them?
Serious risk of infection (invasive fungal infections, reactivated of TB, etc) Lymphoma and other malignancies in children and adolescents
42
What is Rituximab's MOA:
Depletes B cells which have been shown to be responsible for inflammation in RA
43
When is Rituximab used?
When patients fail traditional DMARDs and anti-TNF agents
44
What are the black box warnings associated with Rituximab?
- Fatal infusion reactions (prevent with methylpred, APAP, and antihistamines - severe mucocutaneous reactions - PML (progressive multifocal leukoencephalopathy)
45
What is Abatacept, a biologic DMARD, MOA:
Inhibits T cell activation | used when patients fail traditional DMARDs and anti-TNF agents
46
What is Anakinra, a biologic DMARD, MOA:
Antagonizes IL-1 receptors (pro-inflam cytokine) (used when patients fail traditional DMARDs and anti-TNF agents; may be used in combo with traditional DMARDs but never combined wtih anti-TNF drugs d/t increased risk of infection
47
What is Tocilizumab, a biologic DMARD, MOA:
Inhibits IL-6 (inflam. cytokines) | Used when patients fail anti-TNF
48
What black box warning does Tocilizumab carry?
Serious risk of infections (fungal inf., reactivation of latent TB, opportunistic infections)
49
What type of supplements might a patient on sulfasalazine need to take?
Iron