Analgesics and NSAIDs Flashcards
Which drugs are used for pain? (3)
-narcotic / opioid analgesics
Non opioid:
-paracetamol
-NSAIDs
Which drugs are anti-inflammatory? (2)
- NSAIDs
- Steroids
cellular mediators of inflammation, pain and thermoregulation can…: (6)
- promote microcirculation blood flow
- increase permeability
- enhance action of other mediators
- sensitize nerve endings
- promote leukocyte infiltration
- pro-platelet aggreagtion
What is the mechanism of action for NSAIDs?
-nonselective inhibitor for COX-1 and COX-2 isoenzymes
Is the mechanism of action for NSAIDs reversible?
- competitively reversible
- varying degrees of reversibility
- EXCEPT asprin (irreversible)
Which NSAID is irreversible?
aspirin
What does the COX enzyme do? (3)
arachidonic acid–> prostaglandins + thromboxane
Where is arachidonic acid derived from? with what enzyme?
From phospholipid bilayer
-enzyme: phospholipase A2
What do prostaglandins do?(2)
- messenger in process of inflammation
- protection of stomach lining
What do steroids inhibit?
ENZ phospholipase A2
What do NSAIDs inhibit?
ENZ Cyclooxygenase (COX)
What are the derivatives of arachidonic acid? What enzymes produce them? (5)
COX enz:
- prostaglandins + thromboxane
- collectively called cyclic endoperoxides
5-lipooxygenase ENZ:
-leukotrienes
What are prostaglandins + thromboxane collectively called?
cyclic endoperoxides
inhibiting COX produces what therapeutic effects? (2)
- reduces inflammation
- reduces pain
What is the COX-1 expression?
constitutively (always) expressed
What are the derivatives of arachidonic acid called?
eicosanoids
what functions do COX-1 facilitate? (3)
- protection of stomach lining
- maintenance of renal function
- differentiation of marcophages
What is the COX-1 expression?
facultatively (when needed)
COX-1 inhibition produces..
side effects
COX-2 inhibition produces…
desirable NSAID effects
COX-2 functions facilitated? (4)
- inflammation
- pain
- fever
- normal/pathologic cell proliferation
COX-2 inhibition effects?
anti-inflammatory
discovery of COX2 led to the research of…
development of selective COX-2 inhibitors without gastric problems (characteristic of older NSAIDs)
What are the drug classes of the analgesics and antipyretics that are not NSAIDS?
- paraaminophenols
- pyraolones