pharmacology part 1 Flashcards
what is COX1 stimulated by vs CX2
COX1 is stimulated by hormones/growth factors while COX2 is induced in response to inflammation
the expression of COX___is suppressed by corticosteroids
COX2
***explain what low dose aspirin inhibits and how it inhibits it
pseudoirreverisibly inhibits COX1 and thus also TXA2 because COX1 produces TXA2
TXA2 is involved with…
platelet aggregation and thrombus formation
______ is central prostaglandin synthase
COX3
______ inhibits PLA2
sterouds
what does PLA2 do
cleaves arachidonic acid from cell membrane
what do coxibs inhibit
COX2
true or false
NSAIDS inhibit both COX1 and COX2
true
_____ is a vasodilator that inhibits platelet aggregation
what produces it?
PG12
produced by COX2
differentiate between the locations of TXA2 and PGI2
TXA2 = platelet
PGI2 = endothelial cells
what is ASA
acetyl salicylic acid (aspirin)
true or false
low dose aspirin pseudoirreversibly inhibits COX2
false
COX1
What is the typical mg strength of low dose aspirin
75mg-81mg
taking _______ regularly abolishes the preventative effects of low dose aspirin
NSAIDS
explain the mechanism of how low dose aspirin as an antithrombotic effect
(3 components)
-inhibit PGH2 synthesis – reducing TXA2 formation
-promotes fibrinolysis (breakdown of clots)
-downregulates release of dense granules in platelets (they would promote platelet aggregation)
aspirin uncouples _________ and suppresses signaling through ______
uncouples MITOCHONDRIAL OXIDATIVE PHOSPHORYLATION and suppresses SIGNALING THROUGH NFKB (like an on switch for inflammation)
as mentioned, aspirin uncouples mitochondrial oxidative phosphorylation
what is the result of this
platelets less active
what specific amino acid on COX1 is acetylated by aspirin
serine 529
what is the antiplatelet dose of aspirin
75-81 mg
what does of aspirin is used for STROKE prophylaxis
325mg
name some side effects/adverse drug reactions of aspirin
NVD
GI upset
GI bleeds
tinnitus
hoarseness
heartburn
wheezing
asthma
tachycardia
as mentioned, aspirin can cause GI bleeds
how can you tell if the bleed is upper or lower
upper - vomit will look like coffee grounds
lower - dark or black tarry (sticky) stool
true or false***
NSAIDS inhibit both COX1 and COX2
true
name 4 NSAIDS that are a little more selective for COX2 than for COX1**
Diclofenac
Etodolac
Sulindac
Meloxicam
name an NSAID in which there is a limit on the max daily dose because it can become nephrotoxic
ketorolac
true or false
both ibuprofen and naproxen are nonselective NSAIDS
true
name 3 things that NSAIDS (nonselective) reduce the synthesis of
TXA2
PGI2 (prostacyclin)
prostaglandins (the whole point)
TRUE OR FALSE***
NSAIDS are not very highly bound to albumin
FALSE
they are HIGHLY bound
as mentioned, NSAIDS are highly bound to albumin. this limits their ___________
distribution
NSAIDS being highly bound to albumin makes them subject to….
drug-drug interaction
true or false
NSAIDS can be used to treat OA/RA
true
what can occur with high dose and chronic use of NSAIDS**
why?
analgesic induced nephropathy(kidney disease)
because of decreased glomerular filtration
NSAIDS can cause asymptomatic ______
hepatitis
state a respiratory side effect of NSAIDS
at high doses (overdose) they can stimulate respiration and result in alkalosis and later acidosis
name some GI effects of NSAIDS
NVD
gastric ulceration and bleeding
explain the mechanism in which NSAIDS can cause gastric ulcers
NSAIDS inhibit the production of prostaglandins (eicosanoids) — even the protective ones in the stomach. more prone to ulceration
name some blood changes that can occur as a result of NSAIDS
decrease in hemoglobin/hematocrit
thrombocytopenia (low platelet count)
what is a concern of pts with HTN taking NSAIDS
NSAIDS can cause fluid retention, increasing BP
what is AIN and what can cause it
analgesic induced nephropathy
can be caused by chronic use of high dose NSAIDS
***Acetaminophen MOA
inhibition of COX3 (central prostaglandin synthase)
another name for acetaminophen/tylenol
paracetamol
when COX2 inhibitors and ____ inhibitors are taken together, caution must be exercised because COX2 levels can be increased
CYP2D6 inhibitors
COX2 inhibitors may increase the risk of renal failure when taken with…
ACE inhibitors and diuretics
____ work in the brain AND body while ____ only in the brain
NSAIDS in both brain and body and tylenol only brain
what is the BLACK BOX WARNING for tylenol****
hepatotoxicity
true or false
acetaminophen has NO anti inflammatory effect
TRUE
which has a longer duration of action - tylenol or ibuprofen
ibupofen
another name for COX3
central prostaglandin synthase
briefly name 2 ways in which tylenol works in the brain (not just inhibit COX3)
inhibits reuptake of endocannabinoid
activates central serotonergic pain modulation
the biggest concern with tylenol is ________ toxicity
HEPATO (liver)
acetaminophen is a _____ and ______
analgesic and antipyretic
what is the antidote for acetaminophen overdose and why is it effective***
N-acetyl cysteine
substitute for endogenous GSH pathway of detoxification when the body runs out
besides n acetyl cysteine, name 2 other things that are hepato protective in the case of an acetaminophen overdose
silymarin and silibilin
what is the max daily dose of acetaminophen
generally 3000mg a day, but can go up to 4000mg
true or false
acetaminophen is relatively safe and effective
true
what is the most COMMON adverse effect associated with acetaminophen use**
GI bleeding in an alcoholic patient
hypo_____ is an adverse effect of acetaminophen
hypophosphatemia (low phosphate in blood)
name 3 types of drugs used in arthritis
NSAIDS
steroids
immunosuppressants (in case of RA)
what is gouty arthritis
excessive uric acid deposits in the joints
aside from inhibiting COX3, name another mechanism of acetaminophen
suppresses serotenergic and NE pain transmission
