Drugs for Rheumatic Diseases - Linger Flashcards
agents that slow or stop progression of rheumatic disease, reduce pain and inflammation
-longer remission free phases and better quality of life
DMARDs
disease modifying antirheumatic drug
better disease outcome
referral to rheumatologist
non-biologic DMARDs
hydroxychloroquine
leflunomide
methotrexate
sulfalazine
hydroxychloroquine
non-biologic DMARD
leflunomide
non-biologic DMARD
methotrexate
non-biologic DMARD
sulfasalazine
non-biologic DMARD
rarely used DMARDs
azathioprine
cyclosporine
gold salts
minocycline
adalimumab
TNF-a blocker - biologic DMARD
mAb
certolizumab
TNF-a blocker - biologic DMARD
mAb
etanercept
TNF-a blocker - biologic DMARD
recombinant fusion protein**
golimumab
TNF-a blocker - biologic DMARD
mAb
infliximab
TNF-a blocker - biologic DMARD
mAb
anti-CD20 mAb
rituximab
T cell Fc-fusion
abatacept
domain of CTLA-4 receptor
anti-IL-6 mAb
tocilizumab
prevention of recurrent gout
allopurinol
febuxostat
pegloticase
probenecid
initial tx of rheumatoid arthritis
MTX or leflunomide
HCQ or sulfalazine - safer - if milder disease
NSAIDs
adjunct of pain relief for rheumatoid arthritis
corticosteroids
short term - for severe acute sx
biologic therapy for RA
after inadequate response to non-biologics
TNF-a inhibitors
no study to compare if one is more effective than another
etanercept
common first choice biologic
MOA methotrexate
inhibit dihydrofolate reductase
- impaired DNA synthesis
- causes cell death
MTX dosage
high - chemo
low - RA tx
high has myelosuppression - not a worry with RA tx and low dose
response time MTX
4-6 weeks to several months
adverse of methotrexate
nausea, upset stomach, diarrhea, stomatitis**, alopecia, fever, rash, HA, fatigue
elevation of hepatic enzymes - but cirrhosis rare - should monitor levels**
-screen those at risk for hepatitis, no alcohol
myelosuppression if high dose
supplement with methotrexate
folic acid or leucovorin
reduce adverse effects
MOA leflunomide
prodrug converted to active A77-1726
inhibits dihydroorotate dehydrogenase - reduced ribonucleotide synthesis and G1 arrest
inhibit B and T cell proliferation
response time leflunomide
6-12 weeks
adverse of leflunomide
diarrhea
elevated liver enzymes
category X pregnancy
leflunomide and methotrexate
MOA hydroxychloroquine
poorly understood - T cell suppression, decreased leukocyte chemotaxis, inhibit DNA/RNA synthesis, all possible causes
response time hydroxychloroquine
3-6 months
ocular toxicity
with hydroxychloroquine
need to monitor eyes**
MOA sulfasalazine
poorly understood - possibly decreased IgA and IgM rheumatoid factor production - suppression of T cell and B cell prolifeation, etc.
metabolized to 5-aminosalicylic acid
response time sulfasalazine
1-3 months
prevent rejection of transplant organs
azathioprine
rare used DMARD
pregnant transplant patient
cyclosporine
rare used DMARD
drug induced lupus
with minocycline
rare used DMARD
MOA TNF-a inhibitors
prevent binding of TNF-a to TNF receptors
-down-regulation of macrophages and T cells
biologic DMARD response time
1-2 weeks
faster than non-biologics**
biologic DMARDs
monotherapy - or combo (usually with MTX)
adverse of biologic DMARD
cytopenia
-monitor CBC**
opportunistic infection** - bacterial sepsis and TB
heart failure association
before starting biologic DMARD
screen for latent TB**
rare demyelinating disease
infliximab
NSAID MOA
inhibit COX - decreased prostaglandins
DMARD induction, transition to different DMARD, and during disease flare of RA
use NSAIDs
not acetaminophen - poor anti-inflammatory
adverse NSAIDs
GI ulcers and bleeds
can give ranitidine (H2 histamine antagonist)
less GI toxicity
with celecoxib - COX2 selective
third trimester pregnancy
no NSAIDs**
adverse of corticosteroids
osteoporosis, weight gain, fluid retention, cataracts, glaucoma, poor wound healing, hyperglycemia, HTN, adrenal suppression
should give Ca and Vit D supplements
first line for acute gout
NSAIDs
inhibit urate crystal phagocytosis
aspirin and gout
NO - because inhibit urate excretion at low doses
glucocorticoids
used in severe gout
colchicine MOA
binds tubulin and prevents polymerization - inhibit leukocyte migration and phagocytosis
decrease urate synthesis
xanthine oxidase inhibitor - allopurinol
increased renal excretion of urate
uricosuric agent - probenecid
colchicine
should not be repeated within 14 days - to avoid toxicity cumulation
allopurinol MOA
purine analog that inhibits xanthine oxidase
-decreased uric acid production
decreased recurrence of gout regardless of pathology
allopurinol
preferred for gout during periods between acute episodes
reduce dose of chemotherapy purines
if patient on allopurinol
febuxostat MOA
non-purine inhibitor of xanthine oxidase
probenacid MOA
organic acid - acts at anionic transport site of renal tubules to reduce reabsorption of uric acid
tx of hyperuricemia with gout - when tophi present
adverse of probenacid
increased likelihood of renal stone formation
