Rheumatic Drugs Flashcards
Hydroxycloroquine(HCQ)
Non biologic DMARD anti-inflammatory tissue bound - liver removal 45 day 1/2life 3-6 month response time ocular tox, N/V, abdominal, nightmares OK in pregnancy
Leflunomide
Non biologic DMARD converted to active in intestine/plasma inhibits T-cell proliferation and B-cell AB production Diarrhea Not in pregnancy
Methotrexate
Non biologic DMARD
inhibitor of dihydrofolate reductase inhibits DNA synth
folic acid or leucovorin supplementation
Conc incrased by HCQ
4-6 week response time
fast response time
GI toxicity, stomatitis
hepatotox, pulmonary tox, myelosuppression
not with pregnancy
Sulfasalazine
Non biologic DMARD
1-3 month response time
more toxic than HCQ 30% discontinue use
Azathioprine
Non biologic DMARD - rarely used anti inflammatory prevent rejection of transplant organs increased lymphoma risk not in pregnancy
Cyclosporine
Non biologic DMARD - rarely used
peptide antibiotic inhibits Tcell activation
nephrotox, many interactions
Gold Salts
Non biologic DMARD - rarely used
can induce complete remission
severe enterocolitis, anaplastic anemia, inters pneumonia
not in pregnancy
Minocycline
Non biologic DMARD - rarely used
tetracycline AB - mild RA only
drug induced lupus
not in kids or pregnancy
Adalimumab
Biologic DMARD - TNFa blocking agents SUbQ
1/2 life: 10-20 days
Certolizumab
Biologic DMARD - TNFa blocking agents SubQ
1/2 life: 14 days
Etanercept
Biologic DMARD - TNFa blocking agents SubQ
1/2 life: 4.5 days
Golimumab
Biologic DMARD - TNFa blocking agents SubQ
1/2 life: 14 days
Infliximab
Biologic DMARD - TNFa blocking agents IV
1/2 life: 8-10 days
Abatacept
Biologic DMARD - T cell Fc-fusion IV/SubQ
prevents t-cell activation
1/2 life: 13-16 days
relief of symptoms some after 1-2 doses - 6 months
Rituximab
Biologic DMARD - anti CD 20 mAb IV 1/2 life: 20 day response: 6 weeks lasts 9 months RA use with MTX AE: infusion reactions, infection risk
Tocilizumab
Biologic DMARD - anti IL-6 mAb IV/SubQ
1/2 life: 11-13 days
response - some early most in weeks 6-12
GI perf, infections, anaphylaxis
Celocoxib
Anti-inflammatory - NSAID
Ibuprofen
Anti-inflammatory - NSAID
Naproxen
Anti-inflammatory - NSAID
Prednisone
Anti-inflammatory - corticosteroid
oral
Methylprednisolone
Anti-inflammatory - corticosteroid
oral, depot IM, IV, intra articular
Triamcinolone
Anti-inflammatory - corticosteroid
intra-articular
NSAIDS
Acute gout
Colchicine
Acute gout
Corticosteroids
Acute gout
Allopurinol
Recurrent gout prevention
xanthine oxidase inhibitor - never stop it
Febuxostat
Recurrent gout prevention
xantine oxidase inhibitor
Pegloticase
Recurrent gout prevention
Probenecid
Recurrent gout prevention
Standard pharmacologic treatment for RA
DMARD + NSAID + corticosteroid to control symptoms
Recommended DMARDS for initial treatment
Methotrexate or leflunomide
Hydroxychloroquine or sulfasalazine - safer in mild disease
If inadequate response to biologic DMARDs:
1 non biologic added - usually TNFa inhibitor
Common first choice of TNFa inhibitor
Etanercept - rapid onset of action and short half life
or
infliximab switching to etanercept/adalimumab if needed
Actions of TNFa
pro inflammatory cytokine
fever, apoptotic cell death, inflammation
inhibit tumorigenesis and viral replication
AE of TNFa blockers
injection site reactions(SubQ) - fever, urticaria,
cytopenias - monitor CBCs
Serious Infections! - bacterial sepsis and TB(screen)
increase risk of viral/fungal/opportunistic pathogens
malignancies? (RA has increase lymphoma risk)
Heart failure - not with CHF class 3/4 and <50% EF
demyelinating(infliximab)
Safe up to 30 weeks in pregnancy
NSAIDs
MOA: reduce prostaglandin synthesis
aspirin irreversibly inhibits cox 1 and cox 2 others reverse
found in synovial fluid after repeated dosing
PAIN management - don’t alter course
NSAIDS - AE
gastric irritants - use PPI
nephrotox, hepatotox, CV events
not in third trimester
Choice of NSAIDS
All equal tolmetin - not for gout asprin less effective for ankylosising spondylitis ketorolac - gi and renal effects salsalate and ibuprofen - least toxic
