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Exam #4 - Antiarthritic Agents
N/A
19
Pharmacology
Graduate
11/10/2009

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Term
hydroxychloroquine sulfate [Plaquenil]
Definition
MoA: precise mechanism unknown, redaily absorbed from GI tract, half-life of 6-7 days, drug deposited in tissues (brain, liver, spleen, lung, kidney, heart, EYES); Toxicity: OCULAR TOXICITY - MOST SERIOUS (pts need periodic ophthalmologic exams), C/I in pregnant women, dermatologic rxns: pigmentation & psoriasis, hypersensitivity
Term
aurothioglucose (Solganal)
Definition
approximately 50% gold; MoA: inhibits macrophage phagocytosis & enzyme release, decreases conc. of rheumatoid factor & IgG, exact MoA in RA is unknown, effects take 3-6 months; Toxicity: diarrhea/loose stools, dermatologic, stomatitis
Term
auranofin (Ridaura)
Definition
approximately 29%; MoA: inhibits macrophage phagocytosis & enzyme release, decreases conc. of rheumatoid factor & IgG, exact MoA in RA is unknown, effects take 3-6 months; Toxicity: diarrhea/loose stools, dermatologic, stomatitis
Term
penicillamine [Cuprimine, Depen]
Definition
MoA: immunosuppressive - IgM rheumatoid factor & T- but not B-cells, effects are slow (2-3 months); Toxicity: hypersensitivity, GI, renal, hematological
Term
sulfasalazine [Azulfidine]
Definition
MoA: immunosuppressive, affinity for connective tissue, high conc. in liver & intestinal walls; Toxicities: Major: anorexia, HA, nausea, vomiting, gastric distress; Hematologic: reversible neutropenia;
Term
leflunomide [Arava]
Definition
MoA: inhibition of pyrimidine synthesis, inhibition of dihydroorotate dehydrogenase; Toxicity: GI: diarrhea, Hepatotoxicity: elevated ALT, AST, Hematological: immunosuppression potential, Hypersensitivity: rash & alopecia
Term
etanercept [Enbrel]
Definition
Structure: receptor for TNF: fusion protein of 75 kD TNF receptor to Fc portion of HUMAN IgG1; MoA: binds with TNF-alpha & -beta blocking interaction with TNF receptors, can modulate TNF-dependent biological responses; Toxicity: hypersensitivity, Caution: should be D/C'd in pts with serious infections or sepsis
Term
infliximab [Remicade]
Definition
Structure: monoclonal IgG1 Ab against TNF-alpha CHIMERIC Ab; MoA: neutralizes TNF-alpha only - does NOT neutralize TNF-beta, inhibits TNF-alpha dependent biological responses; Toxicity: hypersensitivity, immunosuppression, infections, HACA Abs
Term
Main Goals of RA Therapy
Definition
1) reduce pain, swelling, & inflammation; 2) maintain joint mobility & range of motion; 3) prevent deformitiy; 4) retard disease progression
Term
Early Stages of RA Therapy
Definition
"Pyramid Approach" - rest, emotional support & pt education, exercise, occupational therapy, salicylates & NSAIDs are 1st line drug therapy; corticosteroids used as 'bridge' between 1st line & 2nd line therapies; treat disease progression with 2nd line agents (DMARDs or SAARDs)
Term
prednisone & prednisolone
Definition
commonly used as "bridge" between 1st line & 2nd line; restricted to pts with severe, rapidly progressing RA
Term
aspirin
Definition
initial drug of choice to treat RA; do NOT use concurrent NSAIDs
Term
hydroxychloroquine sulfate [Plaquenil]
Definition
2nd most commonly used DMARD; antimalarial used in pts with mild or moderate disease unresponsive to conventional treatment; SEs: retinal toxicity, visual impairment
Term
methotrexate
Definition
most favored treatment of severe RA because of rapid response, high response rate, & longest sustained efficacy; most common & effective combo with hydroxychloroquine & sulfasalazine
Term
sulfazalazine
Definition
used for long-term treatment of severe RA most commonly in conjunction with methotrexate & hydroxychloroquine
Term
Treatment of Severe RA NOT responsive to methotrexate
Definition
azathioprine, gold compounds, penicillamine, leflunomide (DON'T COMBINE WITH METHOTREXATE), cyclophosphamide, cyclosporine
Term
Treatment of Juvenile Arthritis
Definition
Management: 1) prevent or correct loss of range & fcn, 2) encourage normal physical & emotional development, 3) control of inflammation with medicine: aspirin, NSAIDs [tolmetin & NSAID], DMARDs [methotrexate, sulfasalazine, hydroxychloroquine, gold, etanercept]; DO NOT ADMINISTER CORTICOSTEROIDS!!!
Term
Characterizations of Osteoarthritis
Definition
joint pain, tenderness, limitation of movement, occasional effusion, & variable degrees of local inflammation
Term
Pharmacologic treatment of Osteoarthritis
Definition
Simple analgesics: acetaminophen; NSAIDs: ibuprofen or naproxen and/or celecoxib [Celebrex]; intermittent corticosteroid intra-articular injections
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