Anti-Inflammatory Agents Flashcards
Ibuprofen
Anti-Inflammatory Agent. NSAID.
Reversible inhibitor of COX 1 and 2, decreasing prostaglandin synthesis and resulting in an anti-inflammatory effect. Less PGE2 leads to decreased sensation to pain, set-point at hypothalamic thermoregulatory center, and synthesis of gastric mucus, with increase in gastric acid secretion (b/c less prostacyclin).
Use as an antipyretic, analgesic, and anti-inflammatory (RA and osteoarthritis). SE: GI bleeding, allergy, interstitial nephritis, tinnitus, hepatitis. Because reversible binding in platelets, NO big anti-platelet effect like aspirin b/c TXA2 is eventually replenished.
Other NSAIDs: Naproxen, Indomethacin, Diclofenac, Sulindac, Oxaprozin.
Indomethacin
Anti-Inflammatory Agent. NSAID.
Reversible inhibitor of COX 1 and 2, decreasing prostaglandin synthesis and resulting in an anti-inflammatory effect. Less PGE2 leads to decreased sensation to pain, set-point at hypothalamic thermoregulatory center, synthesis of gastric mucus, and uterine contractions with increase in gastric acid secretion (b/c less prostacyclin).
Use as an antipyretic, analgesic, and anti-inflammatory (gout and osteoarthritis), labor suppressor via decreasing uterine contractions (PGE effect), closes PDA.
Celecoxib
Anti-Inflammatory Agent. NSAID.
Irreversible inhibitor of COX 2, decreasing prostaglandin synthesis and leading to an anti-inflammatory effect. Selectively targets sites of inflammation (where COX 2 is upregulated) such as inflamed joints. COX 1 is in all tissues, so avoiding it = avoiding most NSAID side effects (like gastric ulcers).
Rx of RA, osteoarthritis, other acute pain. Reduces colonic polyps in FAP. SE: gI upset, interstitial nephritis, allergic rxn (sulfa drug), increased clot risk (stroke, MI) - why Rofecoxib removed from market.
Acetaminophen
Anti-Inflammatory Agent. NSAID.
Reversible inhibitor of COX 1 and 2 in the CNS (deactivated peripherally), decreasing prostaglandin synthesis and leading to an anti-inflammatory effect in the CNS. Decreased pain and set-point at hypothalamic thermoregulatory center.
Used as an antipyretic and analgesic. Good alternative in pts that cannot tolerate aspirin or other NSAIDs, or children with viral infections (Aspirin risks Reye syndrome). SE: dizziness, fatal hepatotoxicity in overdose (Acetylcysteine is antidote, binds and inactivates the toxic metabolite).
__lukast
Anti-Inflammatory Agent. NSAID.
Reversible inhibitor of cysteinyl leukotriene-1 receptor. Blocks LT4 (C, D, E) and their actions (broncoconstriction and increased mucus), resulting in bronchodilation and less mucus.
Preventative Rx of asthma. SE: abnormal LFTs, HA, eosinophilic vasculitis. P-450 activator.
Ex: Zafirlukast, Montelukast
Zileuton
Anti-Inflammatory Agent. NSAID.
Inhibits 5-lipooxygenase, decreasing conversion of arachidonic acid to leukotriene A4, thus downstream LTB4 decreased. LTB4 attracts neutrophils and eosinophils, leading to inflammation in tissues (lung), so blocking it leads to decreased airway inflammation.
Preventative Rx of asthma. SE: abnormal LFTs, HA, eosinophilic vasculitis.
Cromolyn
Anti-Inflammatory Agent. Inhaled.
Inhibits the release of histamine and inflammatory compounds from mast cells.
Prevents asthma exacerbations associated with allergies or exercise. Rx for allergic rhinitis or conjunctivitis.
Cyclosporine
Anti-Inflammatory Agent. Immunomodulator.
Binds cyclophilin in T-cell, inhibiting calcineurin (normally activates IL-2 transcription). IL-2 production decreased, resulting in decreased activation of T-cells and ultimately less cytokine production. Can block T-cell differentiation. Similar to Tacrolimus.
Immunosuppressant in transplant patients, Rx of GvH disease, autoimmune diseases (RA, psoriasis, IBD). SE: nephro/hepatotoxicity, increased infection risk, increased lymphoma incidence, hyperglycemia, HTN, hyperkalemia. Dose-dependent. Metabolized by P-450.
Tacrolimus
Anti-Inflammatory Agent. Immunomodulator.
Binds FKBP, inhibiting calcineurin (normally activates IL-2 transcription). IL-2 production decreased, resulting in decreased activation of T-cells and ultimately less cytokine production. Similar to Cyclosporine.
Immunosuppressant in transplant patients, autoimmune diseases (RA, psoriasis, IBD). SE: nephro/hepatotoxicity, increased infection risk, increased lymphoma incidence, hyperglycemia, HTN, hyperkalemia. Dose-dependent. Metabolized by P-450.
Mycophenolate Mofetil
Anti-Inflammatory Agent. Immunomodulator.
Metabolized to mycophenolic acid in liver, which acts in B and T-cells to inhibit inosine monophosphate dehydrogenase (GMP synthesis in purine synthesis pathway). Lack of GMP leads to decreased DNA synthesis in B and T cells, ultimately decreases proliferation.
Immunosuppressant in transplant patients, autoimmune diseases (RA, psoriasis, IBD). SE: allergic rxn, increased infection risk, pancytopenia, increased lymphoma incidence, GI upset and bleed.
Interferon a/B/g
Anti-Inflammatory Agent. Immunomodulator. Interferons.
Produced in response to a viral infection. Boost the immune system by increasing MHC expression, activation of natural killer and CD8 T-cells, increase ribonuclease activity (degrades viral mRNA), and inhibit elongation factor 2. Produced by: alpha - leukocytes, beta - fibroblasts, gamma - CD4 T-cells.
Rx of certain cancers (Kaposi sarcoma, melanoma), chronic Hep C, MS (reduces exacerbations). SE: fatigue, bone marrow suppression.
__prost__
Anti-Inflammatory Agent. Immunomodulator. Prostaglandins.
Alprostadil: PGE1 - vasodilator, smooth muscle relaxant. Rx of ED, maintain PDA.
Misoprostol: PGE1 - increase uterine contractions, inhibits gastric acid secretion, increases gastric mucosa. Prevents NSAID ulcers, abortifacient with Methotrexate.
Latanoprost: PGF2a - increases aqueous humor drainage. Rx of chronic glaucoma.
Dinoprostone: PGE2 - increases uterine contractions. Abortifacient, prepares for labor.
Carboprost: PGF2a - increases uterine contractions. Abortifacient, prepares for labor.
Epoprostenol: PGI2 - vasodilator. Rx of primary pulmonary HTN.
Etanercept
Anti-Inflammatory Agent. Immunomodulator.
Inhibits the binding of TNF-a and TNF-B to their receptors, decreasing their effects. Alpha is a cytokine from macrophages and T-cells, so blocking inhibits the release of more cytokines (IL-1, 6, 8). Result is an anti-inflammatory effect.
Rx of autoimmune diseases (RA, psoriatic arthritis, ankylosing spondylitis). SE: injection site rxn, URI, increased risk of malignancy development.
Gold salts
Anti-Inflammatory Agent. Immunomodulator.
Inhibit macrophage and lysosomal enzyme activity, leading to anti-inflammatory effects.
Rx of RA.
Infliximab, Adalimumab
Anti-Inflammatory Agent. Immunomodulator.
Chimeric (I) or monoclonal (A) antibody that binds to TNF-a and prevents its binding with receptor. TNF-a is a cytokine from macrophages and T-cells, so blocking inhibits the release of more cytokines (IL-1, 6, 8). Result is an anti-inflammatory effect.
Rx of autoimmune diseases (RA, IBD, psoriasis, ankylosing spondylitis). SE: risk of infection, infusion rxn, abnormal LFTs, increased risk of malignancy development.
