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45 Cards in this Set

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