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Anti-Inflammatory Drugs
PHAR340
21
Pharmacology
Undergraduate 3
12/06/2012

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Cards

Term
NSAIDs
Definition
Non-steroidal anti-inflammatory drugs
Suppress signs/symptoms of inflammation via inhibition of COX
Decreased inflammation, pain and fever
Term
Salicylates
Mechanism of action?
Definition
COX inhibition (reversible and irreversible)
Ab-Ag inhibition at high concentrations
Barrier formation → interfere with leukocyte migration
Block signal transduction in inflammatory cells
Term
Salicylates
Effect at low dose? Elimination?
Definition
Pain and fever relief
First order elimination
Term
Salicylates
Effect at high dose? Elimination?
Definition
Anti-inflammatory
Zero order elimination; enzymes become saturated
Term
Salicylates
Adverse Effects?
Definition
GI intolerance → inhibition of protective effects of prostaglandins
Increased formation of leukotrienes
Ulcer activity
Renal failure → RBF is regulated by PGs
Term
Misoprostol
Definition
PG analog
NSAIDs may cause ulcers
PG combats ulcer activity
Term
Indomethacin
Definition
Indole derivative
Efficacious COX inhibitor
Psychiatric effects, most commonly severe frontal headaches
Term
Naproxen
Definition
COX inhibitor → analgesic, antipyretic, anti-inflammatory
T1/2 of naproxen is 14 hours
Longer lasting effect
Problematic for toxicities
Term
Ibuprofen
Definition
COX inhibitor → analgesic, antipyretic, anti-inflammatory
T1/2 of ibuprofen = 2-6 hours
Term
DMARDs
Definition
Disease-modifying antirheumatic drugs
Slow the progress of rheumatoid arthritis
Block/release cytokine action
Lose effect (5 year benefit)
Toxic to skin, blood, liver, kidney and eye
Term
Methotrexate
Definition
Structural analogue of folic acid
Interferes with purine synthesis and pro-inflammatory cytokines
Anti-cancer drug
Teratogenic, causes birth defects
Term
Infliximab
Definition
Remicade
Monoclonal antibody to TNF-ɑ (pro-inflammatory cytokine)
IV infusion
Increased susceptibility to infection and lymphoma
Term
Etanercept
Definition
Recombinant protein that fuses 2 TNF-ɑ receptors with IgG1
Subcutaneous
Increased susceptibility to infection and lymphoma
Term
Rituximab
Definition
Monoclonal antibody, binds to CD20 on B cells
If anti-TNF-ɑ is ineffective
Term
Tofacitinib
Definition
Inhibitor of JAK expressed in immune cells
JAK-STAT cytokine signalling inhibited → altered transcription of genes
Term
Indomethacin
Definition
NSAID (anti-inflammatory) for acute gout attacks
Gout: sodium urate crystals in joints
Term
Colchicine
Definition
Anti-inflammatory for gout arthritis
Depolymerization of microtubules in granulocytes → inhibit migration
GI toxicity: nausea, vomiting, diarrhea
Term
Allopurinol
Definition
Xanthine oxidase inhibitor, non-competitive
Most common treatment for long-term gout
Decrease uric acid formation
Term
Alloxanthine
Definition
Xanthine oxidase inhibitor, non-competitive
Most common treatment for long-term gout
Decrease uric acid formation
Term
Probenecid
Definition
Uricosuric drug, organic acids
Inhibit renal tubular reabsorption of uric acid
Occupy anion transporter
Term
Sulfinpyrazone
Definition
Uricosuric drug, organic acid
Inhibit renal tubular reabsorption of uric acid
Occupy anion transporter
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