NSaids antirheumatoids nonopioids and antigouts Flashcards
memorise (30 cards)
COX-1
homeostatic in function
COX 2
induced during inflammation anf tends to facilitate inflammatory response.
NSAIDs
Aspirin is the original NSAID.All Nsaids are weak organic acids except nabumetone which is a ketone prodrug that is metabolized to the acidic active drug.
MOA of NSAIDs
inhibition of biosynthesis of prostaglandins. Aspirin irreversibky acetylates and blocks platelet Cyclooxygenase .
Toxicity
all of them are gastric irritants .Can be nephrotoxic due to interference with autoregukation of renal blood flow which is regulated by prostaglandins.
positive effect
most appear to reduce the incidence of colon cancer when taken chronically.
cox2 selective inhibitors
have analgesic, antioyretic and antiinflammatory effects.eg…Celecoxib and meloxicam though not as selective as celecoxib.
Non selective cox inhibitors
diclofenac ,diflunisal, etodolac,flurbiprofen,ibuprofen(brufen)-closes patent ductus arteriosus in infants.,Indomethacin-also inhibits phospholipase A and C,,ketoprofen,ketolorac,nabumetone,naproxen,oxaprozin ,piroxicam,sulindac-prodrug and tolmetin.
DMARDs
disease modifying antirheumatic drugs.They are grouped into biologic and non biologic derived .
Non biologic dmards
methotrexate,salfasalazine, azathioprine,chloroquine and hydroxychloroquine , gold salts,leflunomide, cyclosporin and minocycline.
biologic dmards
eternercept ,infliximab ,adalimumab,rituximab,abatacept ,tocilizumab and golimumab.
abatacept
MOA:inhibits activation of Tcells…………………………………………………..Adverse effects:increased risk of infection.
Azathioprine
MOA:acts through its active metabolite ,6-thioguanine which suppresses inosinic acid synthesis,B-cell and T-cell function,immunoglobulin priduction and IL-2 secretion.Adverse effects:bone marriw suppression.
HCQ
MoA -trapping of free radicals,suppression of T lymphocyte respinses to mitogens
cyclosporine
inhibits IL2 and IL 1 receptor production .grapefruit juice increases its bioavailabiliy can cause nephrotoxicity
leflunomide
its metabolite inhibits dihydroorotate dehydrogenase also inhibits Tcell proliferation.it causes elevation of liver enzymes
methotrexate
inhibits dihrydrofolate reductase. its toxic effects are nausea and mucosal ulcers
Rituximab
its is an antibody that targets CD20 B lymohocytes
sulfasalazine
inhibits the release of inflammatory cytokines
TNF alfa blocking agents
adalimumab,infliximab,etanercept.
glucocoorticoids(corticosteroids)
they are used in rheumatoid arthritis patients
acetaminophen
weak cox1 and cox 2 inhibitor.treats mild to miderate pain such as headache
Drugs used to treat Gout
gout is associated with hyperuricemia.
drugs used to treat acute gout
colchicine,Nsaids,glucocorticoids.