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36 Cards in this Set
- Front
- Back
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What 2 prostoglandins sensitize pain receptors to inflamatory agents?
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PGE2 and PGF2alpha
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ASA; mechanism
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irreversible, non-selective COX inh.
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ASA; kinetics
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pKa = 3.4 (low), adding NaCO3 to diet speeds up elimination. Enteric coating does not alter COX inh. Crosses placenta and breast milk. Not for 3rd trimester
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ASA; adverse
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Gastritis
GI ulcer development (PGE2 decreases acid secretion/ pumps up mucus production) Blood thining (TXA2/PGI2) Salicylism - N&V, tinnitus, vertigo, respiratory alkalosis, hepatitis OD - hepatic/nephro/cardio toxic, hyperthermia Reye's Syndrome - fatty liver, encephalopathy, kidney changes Gout attacks - causes retention of uric acid |
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Ibuprofen; mechanism
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reversable, non-selective COX inh.
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Ibuprofen; high dose vs. low dose
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high - analgesic and anti-inflamatory
low - analgesic but low anti-inflamatory |
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Ibuprofen; adverse
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GI ulcer
Edema HTN Agranulocytosis - rare Aplastic anemia - rare |
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Ibuprofen; kinetics
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interaction w/ ASA - reverses blood thining effect
interaction w/ Li - ups toxicity mimimal milk excretion |
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Naproxen; mechanism
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non-selective COX inh
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Naproxen vs. Ibuprofen
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longer-lasting/slower-onset analgesic. no interactions w/ coumadin or oral hypoglycemics
GI bleeding less common than w/ ASA GI bleeding more common than w/ ibuprofen |
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Etodolac
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(Lodine) COX2>COX1
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Nabumetone
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(Relafen) long-acting, once daily, avoid w/ renal dysfunction
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Piroxicam
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(Feldene) long-acting, every other day dosing, ok w/ renal dysfunction
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Diflunisal
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(Dolobid) long-acting, better analgesic than ASA/acetominophen, renal elimination
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Diclofenac
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(Cataflam) long-acting, ok w/ renal dysfunction
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Ketorolac
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(Toradol) non-selective COX inh. for short term systemic use
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Flurbiprofen
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(Ansaid) COX inh + TNF-alpha inh + NO synthase inh. good for gout/OA
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Indomethacin
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(Indocin) COX inh + phospholipase A/C inh + T & B cell migration inh.
for gout and RA and tocolytic |
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Celecoxib
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(Celebrex) COX2>>COX1
Less GI effects than ASA Doesnt inhibit TXA2 Long term use -> cardiotox |
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Meloxicam
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(Mobic) COX2>COX1.
does nto effect TXA2 |
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NSAID interactions
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MTX: decreased clearance
Oral Anti-coagulants: increased action Loop Diuretics: decreased action Cyclosporine: up tox w/ Diclofenac and naproxen no Ketorolac + ASA Lithium: up tox Steroids: peptic ulcer |
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Acetaminophen; mechanism
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COX3 inh. analgesic only
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Acetaminophen; interactions
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EtOH: more hepatotox
Phenothiazine: hypothermia INZ: more hepatotox |
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Acetaminophen; kinetics
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hepatic microsomal.
N-acetyl-p-benoquinone - hepato/nephro toxic metabolite |
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Acetylcysteine
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for acetaminophen OD, nutralizes NAPB to minimize damage
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MTX; mechanism
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aminoimidazolecarboxamide trasformylase (AICAR) inh. + thymidylate synthatase inh. + PMN chemotaxis inh.
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MTX; adverse
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N&V, mucosal ulcers, hepatotox.
w/ NSAIDs = bone marrow supression |
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Cyclophosphamide
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metabolized to phosphoramide mustard - cross links DNA.
Infertility and bone marrow supression |
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Cyclosporine
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decreases IL-1/IL-2 receptor production.
alters T-cell and B-cell function Nephrotox Hepatic metabolism (CYP3A) |
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Azathioprine
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metabolized to mercaptopurine
hepatotox, marrow supression, anemia |
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Adalimumab
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(Humira) rh-TNFalpha MAB. increases TB infection
for RA |
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Entanercept
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(Enbrel) binds TNF-alpha
for RA, JRA, UC |
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Sulfasalazine
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metabolized to sulfapyridine. Reduces IgA and IgM levels. supresses T-cells
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Leflunomide
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inhibits DiHydroOronate dh.
Adverse: diarreah, hepatotox, heme |
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Chloro/hydrocholoro quine
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suppresses T-cell response
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Which drug requires a 2 year washout period before contraception should be attempted? (DMARD)
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Leflunomide
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