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Pharm Lecture 3

QuestionAnswer
NSAIDs examples ibuprofen, indomethacin, diclofenac, celexocib, etoricoxib
NSAIDs adverse effects GI upsets, renal toxicity, cardiovascular events (COX-2 specific inhibitors)
Ibuprofen adverse effects few adverse effects
Indomethacin adverse effects GI upset and impaired renal function due to higher COX-1 selectivity
Diclofenac adverse effects GI upset and headaches (more potent than indomethacin)
COX-2 inhibitors adverse effects no GI upsets, heart attack and stroke
NSAIDs mechanism inhibit COX enzyme
NSAIDs effects antiinflammatory, analgesic, anti-pyretic
COX pathway Phospholipid --> (phospholipase A2) arachidonic acid --> (COX) PGG2 --> PGH2 --> PGE2, PGF2, PGI2, PGD2, TXA2
NSAID uses treatment of acute or chronic conditions where pain and inflammation e.g. rheumatoid arthritis, limited effects on RA disease progression, used as bridge therapy
Rheumatoid arthritis drug classes NSAIDs, glucocorticoids, DMARDs, immunosuppressants, biological agents
Glucocorticoid examples prednisone
Glucocorticoid adverse effects immunosuppresion, hyperglycaemia, muscle breakdown, osteoporosis, adrenal insufficiency (HPA axis suppression), poor wound healing, thinning of skin, fat redistribution
Prednisone adverse effects hyperglycaemia, insomnia, euphoria, cushing's syndrome, truncal weight gain, osteoporsis, glaucoma, type II diabetes
Glucocoritcoid mechanism increased synthesis of lipocortin-1 --> inhibits PLA2, down-regulation of pro-inflammatory cytokines, up-regulation of anti-infalmmatory cytokines
Glucocorticoid effects anti-inflammatory and immunosuppressive, metabolic effects
Glucocorticoid uses limited effects on RA disease progression, used as bridge therapy
DMARDs examples methotrexate, gold salts, D-penicillamine, hydroxychloroquine, sulfasalazine, (cyclosporin A, azathioprine, leflunomide, infliximab, etanercept, rituximab)
Methotrexate characteristics first choice DMARD, low cost, effective, quicker onset
Methotrexate adverse effects mucosal ulceration, hepatic and renal toxicity, skin reactions, nausea, teratogenic
Methotrexate mechanism inhibits metabolism of folic acid --> inhibits thymidine synthesis --> inhibits cell growth of pannus tissue
Gold salts mechanism inhibits IL-1 and TNF-alpha production, inhibits mitogen-induced lymphocyte proflieration, inhibits neutrophil chemotaxis and free radical production
Gold salts adverse effects decreased appetite, itchy skin, mouth sores, nausea, hair thinning, diarrhoea, thrombocytopenia
D-penicillamine mechanism metal chelator, reduces number of T-lymphocytes, inhibits macrophage function, decrease IL-1 and rheumatoid factor, pevents collagen cross-linking
D-penicillamine adverse effects hepatic and renal dysfunction, rash, nausea, vomiting
Hydroxychloroquine adverse effects rash, GI upset, headaches
Hydroxychloroquine characteristics 50% patients respond, low toxicity
Sulfasalazine adverse effects skin reactions, GI disturbances, headaches, nausea
Sulfasalazine mechanism may treat unrecognised UC --> reduces arthritis symptoms
Cyclosporin A adverse effects renal and hepatic toxicity
Cyclosporin A mechanism inhibits calicneurim --> inhibits IL-2 synthesis and activation
Cyclopsorin A characteristics most effective when combined with DMARDs --> decreased dose
Azathioprine adverse effects skin eruptions, nausea, suppress bone marrow --> thrombocytopenia, leukopenia
Azathioprine mechanism purine analog
Leflunomide adverse effects hepatic toxicity, diarrhoea, rash, teratogenic
Leflunomide mechanism inhibits enzyme involved in pyrimidine synthesis
Infliximab mechanism TNF-alpha inhibitor (monoclonal antibody)
Etanercept mechanism TNF-alpha receptor fusion protein
Biological agents administration only IV infusion or subcutaneous injection
TNF-alpha inhibitors adverse effects infusion-related reaction, blood dyscrasias, infections
Anakinra mechanism IL-1 receptor antagonist analog
Abatacept mechanism blocks co-stimulatory signal between APC and T cell
Rituximab mechanism depletes B cells
Created by: skyglow1
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