NSAIDS and DMARDs Flashcards
acetylsalisylic acid
aspirin
acetaminophen
tylenol
celecoxib: only COX2 inhibitor
celebrex
COX2 is inducible by …
cytokines
NSAIDs do not inhibit …
lipoxygenase
protection from cardiovascular disease is additional use of which NSAID
aspirin
which drug will close the ductus in neonates when it has remained patent
indomethacin
most common side effect of NSAIDs is …
gastric or intestinal ulceration
all NSAIDs except … tend to cause GI side effects
acetaminophen
aspirin covalently modifies both COX1 and COX2 … … cyclooxygenase activity
irreversibly inhibiting
aspirin … COX enzymes
acetylates
side effects of which NSAID?: GI ulceration, tinnitus, reyes syndrome
aspirin
hepatic toxicity is a major side effect of which NSAID?
acetaminophen
therapeutic doses of … do not produce gastric irritation or increase bleeding time
acetaminophen
antiinflammatory, analgesic, antipyretic; one of the more potent inhibitors of COX; useful for treatment of arthritis, gout; contraindicated in pregnancy
indomethacin
NSAID for postop pain and inflammation; administered intramuscularly or orally; inflammatory conditions in eye
ketorolac
potency is greater than indomethacin; non recommended for pregnant women; elevation of hepatic aminotransferase activities in plasma
diclofenac
approved as a transdermal NSAID
diclofenac
formulation of diclofenac and misoprotol (PGE1 analog) together that provides gastric protection
arthrotec
propionic acid derivatives
ibuprofen, naproxen, oxaprozin
half life of ibuprofen
2 hrs
half life of naproxen
14 hrs
half life of oxaprozin
40 hrs
equivalent of indomethacin or naproxen; principal advantage is its long half life of 50 hrs
piroxicam
more selective COX2 inhibitor although it will inhibit COX1
meloxicam
all NSAIDs … hypotensive effect of antihypertensives
decrease
all NSAIDs … natriuretic and diuretic effects of diuretic agents
decrease
all NSAIDs … anticoagulant effect of oral anticoagulants
increase
treatment of all NSAIDs with potassium sparing diuretics, ACE inhibitors, B blockers has potential for
hyperkalemia
selective COX2 inhibitor; potential for CV problems
celecoxib
very commonly used DMARD; inhibitor of dihydrofolate reductase and interferes with de novo purine biosynthesis; has been used in treatment of various leukemias; treamtent of psoriasis
methotrexate
therapeutic effects of methotrexate are within … weeks
4-6
…. supplements are recommended with methotrexate
folic acid
methotrexate can by co-administered with …
glucocorticoids
2nd line DMARD; oral pyrimidine synthesis inhibitor; side effect of hepatic toxicity and liver failure
leflunomide
antimalarial agent and 2nd live agent used for mild rheumatoid athritis
hydroxychloroquine
treats RA, ulcertive colitis, Crohn’s; prodrug; colonic bacteria release; 5-aminosalicylic acid–>therapeutic benefit
sulfasalazine
elevated … levels found in synovial fluid of RA patients
TNF
major side effect of which class?: increased risk of infections
TNF inhibitors
decrease TNFa levels; false receptor; may be used in combo with methotrexate, NSAIDs or other agents (except antibodies directed against cytokines)
etanercept (enbrel)
chimeric IgG1 monoclonal antibody; high affinity binding to TNFa; inhibits interaction of TNFa with its receptors
infliximab (remicade)
human monoclonal TNFa antibody with human IgG; may be administered with other DMARDs (except biologics) or NSAIDs
adalimumab (humira)
TNF human monoclonal antibody; administered as monthly SQ injection
golimumab
TNF antibody conjugated to polyethylene glycol; monthly SQ injection
certolizumab
interleukin 1 receptor antagonist; one amino acid difference from IL 1; competitively inhibits IL 1
anakinra
T cell co stimulatory blocker; CTLA4 binds CD80 on antigen presenting cell and prevents interaction with CD20 on T cell
abatacept
depletes B cells; chimeric monoclonal antibody against CD20 on B cell surface
rituximab
monoclonal antibody against the IL 6 receptor
tocilzumab
