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45 Cards in this Set
- Front
- Back
- 3rd side (hint)
Aspirin
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Irreversible COX inhibitor
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Ibuprofen (Advil, Motrin)
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Reversible COX inhibitor
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Naproxen
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Reversible COX inhibitor
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Diclofenac
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Reversible COX inhibitor
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Sulindac
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Reversible COX inhibitor
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Piroxicam
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Reversible COX inhibitor
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Indomethacin
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very strong reversible COX inhibitor, used for closing of patent ductus arteriosus, used for severe gout
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Ketorolac
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Reversible COX inhibitor
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Celecoxib (Celebrex)
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COX2 Inhibitor, used when pts cant tolerate nonselective inhibitors and need to stop gastric bleeding
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Rofecoxib (Vioxx)
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COX2 Inhibitor
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Infliximab (Remicade)
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Anti-TNF alpha AB (rh arthritis)
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Adalimumab (Humira)
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Anti-TNF alpha AB (rh arthritis)
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Etanercept (Enbrel)
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Soluble extracellular domain of TNFR1 (Rh athritis & Crohn's)
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Thalidomide (Thalomid)
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Block pathway of getting NFkB (used in Crohn's disease but can be teratogenic)
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Acetaminophen (Tylenol)
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only analgesic unknown mechanism
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COX inhibitor actions
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anti-inflam, analgesic, anti-pyretic, anti-thrombotic
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COX inhibitor Side effects
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GI ulcer/bleeding, induce remodelling of the heart (bad for CHF), inhibit the effects of thiazide drugs, salicylism (ASA only): tinnitus, dec hearing, vertigo.
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COX2 Inhibitor actions
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Prevent GI bleeding
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COX2 Inhibitor side effects
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Decrease PGI2 (which normally causes protective vasodilation in vessels with atherosclerotic plaque)
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Zileutin
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5-LOX inhibitor
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Zafirlukast
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Cysteine Leukotriene Blocker LTC4/LTD4
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Montellukast
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Cysteine Leukotriene Blocker LTC4/LTD5
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Promethazine
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1st Gen Anti histamine (less selective H1)
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Cross BBB: drowsiness/dry mouth
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Clopheniramine
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1st Gen Anti histamine (less selective H1)
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Cross BBB: drowsiness/dry mouth
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Loratidine
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selective H1 antagonist anti-histamine
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Desloratidine
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selective H1 antagonist anti-histamine
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Bradykinin effects
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hyperalgesia,hyperalludinia, inflammation, vasodilation (PGE production), release Arachidonic acid, bronchoconstriction
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steroid side effects
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water retention, muscle weakness, ostereoporosis, Euphoria, alkylosis, stomach ulcer, dec immunity
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steroid indications
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goat, osteo or rheumatoid arthritis, severe inflammation, organ transplant
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steroid mechanism
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turn on annexin(dec AA) block COX2 expression also decrease COX2 activity
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alprostidil
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PGE1 agonist- causes muscle relaxation
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misoprostol
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prostaglandin agonist: stomach protection and to maintain patent ductus arteriosus. Combined with RU486 to induce abortion.
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What are some of the actions of Prostaglandins
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1. magnify actions of histamine and bradykinin (secreted by neutrophils at inflammatory site) 2. raise core temperature setpoint (stimulated by IL-1/TNF in post-hypothalamus) 3. vasodilates vessels and prevents remodelling in the heart 4. stim Na reabsorption in the kidneys to prevent kidney failure. 5. stim replacement/proliferation of mucosa in stomach to prevent ulcers.
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How is bradykinin made and degraded
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kallikrein (serine protease) breaks down kininogen (floating in blood) to free bradykinin. Bradykinin is broken down by ACE (mainly in the lung)
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actions of PGI
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vasodilation, platelet disaggregation
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action of TXA
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vasoconstriction, platelet aggregation
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what cells usually make TXA
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platelets
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what cells usually make PGI
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endothelial cells
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actions of LTB4
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leukocyte chemotaxis
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actions of LTC4/LTD4
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bronchoconstriction, venule permeability
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which COX is constitutively on and and which is inducible
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COX1 constitutive and COX2 inducible
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name the receptors for PGE2, PGI2, and TXA2 and their associated G protein
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EP4 (Gs incr adenylate cyclase), IP (Gs incr adenylate cyclase), TP (Gi incr IP3 and Ca)
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what drugs have a synergistic effect w/ opioids and what is the effect
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NSAIDs and acetamenophen (they reduce the amount of opioids need to have the same analgesic action and therefore reduce the amount of side effects)
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what are the histamine receptors and their actions
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H1: inflammation (bronchoconstriction, allergic rhinitis, vasodilation, stim of itch neurons) but also in the brain. H2: acid secretion in the stomach. H3: NT release in the brain. H4: also in the brain
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what is the goal of inflammation
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to deliver blood component to target site
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