NSAIDs Flashcards
Aspirin is unique among the NSAIDs for its ability to ______.
decrease clotting
Celecoxib is unique among the NSAIDs because it ______.
doesn’t have any gastric side effects
The COX1 pathway in platelets turns arachidonic acid into ______.
thromboxane
Eicosanoids are ________.
signaling molecules made from oxidizing 20-carbon fatty acids
List some of the effects of prostaglandins from the COX 1 pathway.
- GI: decreased acid production and increased mucous/bicarb secretion; increase smooth muscle contractions
- Platelets (TXA2): pro-aggregatory effect
- Kidneys: increased renal blood flow
On vascular endothelial cells, prostaglandins work to _________.
cause vasodilation and anti-clotting
COX1 is ___________, while COX2 is ________.
constitutively functioning; dependent of stimuli for induction
Acetaminophen does not function in the periphery, only in the ______. Thus it is not an anti-inflammatory.
CNS (on COX2, to be specific)
Glucocorticoids inhibit _____ and stimulate ______, thus leading to a strong anti-inflammatory effect.
COX; annexins (which inhibit phospholipase A, the enzyme that makes arachidonic acid)
Ketorolac is ________, as is Celebrex.
prescription only
The antiplatelet effect of aspirin is ______, while the antiplatelet effect of other NSAIDs is _______.
4 - 7 days; 2 days
If you have to recommend a tNSAID, for GI patients ______ is better, while for cardio patients ______ is better.
ibuprofen; naproxen
Celecoxib (Celebrex) is a ________ inhibitor.
selective COX2
Celecoxib is great for _________.
patients who cannot tolerate high doses of NSAIDs due to GI tract
Selective COX2 inhibitors have ________ effect on platelets.
no (because platelets are mediated by COX1)
What is inhibited by NSAIDs to induce analgesia?
Inhibition of COX-2 at site of inflammation
The antipyretic effect of NSAIDs is mediated by ______.
inhibition of COX-2 in the hypothalamus
The anti-inflammatory effect of NSAIDs occurs through _______.
inhibition of COX-2 at sites of inflammation
NSAIDs inhibit thrombogenesis by ______.
inhibiting COX-1 in platelets
Which isoform of COX is present in the stomach, and what does it do?
COX-1, and it produces PGE which decreases acid/pepsin secretions and increase mucous/bicarb secretions
Which isoform of COX is present in the kidneys?
Both!
Inhibiting ______ leads to bleeding problems, while inhibiting ______ leads to thrombosis.
COX-1 in platelets; COX-2 in vascular endothelial cells
The traditional NSAIDs are _______ and include the following drugs: _________.
reversible inhibitors of COX-1 and COX-2; ibuprofen, ketorolac, and naproxen
Acetaminophen does not _________, but does inhibit ______.
COX-1 or COX-2 in the peripheral system; COX-2 in the CNS, leading to antipyretic effect and analgesia
Celecoxib (Celebrex) is a ________.
selective reversible inhibitor of COX-2
Aspirin (acetyl salicylic acid) is an _________.
irreversible inhibitor of COX-1 and COX-2
________ mediates platelet aggregation.
Thromboxane A2 (produced by the COX-1 pathway)
In the kidneys, NSAIDs cause _______.
vasoconstriction and fluid retention
Celebrex is great for __________.
patients at risk of GI bleeds (still has renal risk)
Recommended maximum doses of acetaminophen are ______ for those without liver disease and ______ for those with.
4000 mg / day; 2000 mg/day (because alcohol induces CYP2E1)
Low-dose aspirin is essentially ______.
platelet COX-1 selective, thus it is antithrombotic
In the kidneys, PGE2 and PGI2 ________.
increase renal blood flow
In vascular smooth muscle, PGE2 and PGI2 lead to _______ while TXA2 leads to _______.
vasodilation; vasoconstriction
The anti-thrombotic enzyme on vascular endothelial cells is ______.
COX-2
Leukotrienes lead to _________.
vasoconstriction, bronchoconstriction, vascular permeability, and chemotaxis for phagocytic cells
The lowest GI-risk NSAID is _______ and the highest is ______.
ibuprofen; naproxen
The lowest CV-risk NSAID is ________ and the highest is _______.
naproxen; ibuprofen
Aspirin overdose first leads to _____ and then _______.
respiratory alkalosis; metabolic acidosis
Acetylsalicylic acid is rapidly hydrolyzed by _____.
esterases
