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Flashcards in antiarthritics Deck (34):
1

Hydroxychloroquine Sulfate (Plaquenil)

Nonbiologic Disease Modifying Antirheumatic Drugs (DMARDs)

half-life: 6-7 days! long!

deposits in tissues (eyes)-->*irreversible ocular toxicity*
retinopathy

fetal uveal tissue (CI in preg.)

may use in combo with corticosteroids and salicylates

2

Methotrexate (Trexall, Rheumatrex)

non-bio DMARD
*see immune lecture
v. common, cheap

3

Sulfasalazine (Azulfidine)

non-bio DMARD

split in intestine-->5-ASA*(active) and SP (danger)
SP-->acetyl-SP: slow or fast metabolizers-->slow metabs @ risk for adverse events

affin. for CT, immunosuppr.

*reversible* neutropenia (vs. hydroxchloraquine)

4

Leflunomide (Arava®)

non-bio DMARD

inhibits dihydroorotate dehydrogenase (pyrimidine biosyn.)
*antiproliferative*,
anti-inflamm, tx for RA

6-12 hr onset, 2wk half life!!!

*hepatotoxicity*- black box (FDA warning)

not used in pregnancy

5

Etanercept

bio DMARD
TNF inhibitor

dimeric fusion protein: human rec. P75 attached to Fc of IgG-->attaches TNF-a or B and inhibits their binding to TNF receptors

risks: *infections, sepsis and malignancies*

tx: RA, JRA

can use in combo with methotrexate

6

Infliximab (Remicade)

bio DMARD
TNF inhibitor

chimera: human Fc IgG, murine variable region-binds TNF-a (NOT TNF-B)

half life about 9.5 days

tox: hypersn to murine portion
immunosuppr: TB, fungal infections, OIs
infusion-rel. reactions: dev. human anti-chimeric Abs (HACAs)

tx: RA, Crohn's
used in combo with methotrexate

7

Anakinra

bio DMARD
non-TNF inhibitor
IL-1 receptor antagonist

8

non-bio DMARDs already know

Azathioprine (Imuran®)
Cyclosporine (Sandimmune, Neoral)

9

arthritis

assoc. with spondylitis
degen. joint disease
assoc. with infection

10

initial tx??


then move on to ??

*aspirin*, salicylates, NSAIDs (if do not tolerate/respond to salicylates)

disease‐modifying antirheumatic drugs (DMARDs)

11

use ?? for flares

glucocorticoids, don't want to use chronically

prednisone, prednisolone

12

ASA dosage

3 gs/day
3-6 for significant anti-inflam.
GI intolerance

13

NSAIDs

same affects as ASA
*indomethacin: less GI complaints

14

combo therapy of DMARDs

synergistic
reduce resistance and toxicity
*agent of choice det. by pt and physician

15

70-80% of individuals w. RA show...

RF
B‐cells that secrete immunoglobulins, including the autoantibody rheumatoid factor, which can be identified in 80% of affected individuals.

16

inflammatory mediators present in RA

complement cleavage products, leukotrienes, prostaglandins, histamine, serotonin, proteases, platelet‐activating factor and cytokines (TNF‐), IL‐1, IL‐6, etc)

neutrophils-->lysosomal enz. TOI, AA cascade products

17

progressive RA therapy


a. Reduce pain, swelling and inflammation
b. Maintain joint mobility and range of motion
c. Prevent deformity
d. Retard disease progression

18

start pt w. education, PT, OT...then

salicylates (*ASA*) and NSAIDS

19

use ??? btw 1st and 2nd line agents

low-dose corticosteroids
"bridge"

20

DMARDs

2nd line
slow onset, more toxic
agent det. by Dr., pt
consider: convenience, monitoring, costs, time of onset, adverse effects

21

early RA (

mild:
DMARD monotherapy: methotrexate/Cl on its own

mod or high:
DMARD combo
+/- TNF inhibitor

22

established RA (>6 mos)

mild:
DMARD combo

mod or high:
DMARD combo
+ TNF inhibitor OR
+ non-TNF inhibitor

23

JRA tx: ASA ?

*concern for Reyes w. ASA*

24

JRA tx: NSAIDs?

use Tolmetin and Naproxen

25

JRA tx: DMARDs?

use methotrexate
gen. well-tolerated

sulfasalazine
hydroxychloroquine (but ocular toxicity!)

26

JRA tx: if DMARDs fail

bio. agents: TNF inhibitors
Etanercept

27

JRA tx: corticosteroids

NO
potential adverse reactions, including growth retardation and problems associated with withdrawal

can use inj. 3-4/yr

28

OA

not systemic, typically 1 joint: cartilage
most common

29

OA tx

Acetaminophen
then NSAIDs: Ibuprofen, naproxen, COX-2 inhib.

NOT ketorolac or mefenamic acid
-don't work

intermittent corticosteroid intra-art. injections

30

OA initial tx

exercise, wl, PT

31

OA tx after NSAIDs

glucosamine and chondroitin: controversial

32

OA tx after glucosamine and chondroitin

opioids
then corticosteroid injection
hyaluronic injection

33

OA last resort

joint replacement

34

other major sulfasalazine adverse effects

anorexia, ha, N/V, GI distress (reversible)

along with rev. neutropenia