WorksheetsNSAIDs Dr. Khan part 2
Total questions: 29
Worksheet time: 29mins
The solution: inhibit COX-2 selectively
high selectivity agents produced- increased MI and stroke risk, many pulled from market
low selectivity agents produced- increased MI and stroke risk, many pulled from market
high selectivity agents produced-low MI and stroke risk, many pulled from market
First NSAID marketed as a selective COX-2 inhibitor (COX-2I) is:
Celecoxib
Aspirin
Ibuprofen
Celecoxib up to 35% increased risk of CV events
True
False
COX-1:
TXA2
Promotes platelet aggregation and Hemostasis/Thrombosis
Platelets
Endothelial cells
COX-2:
PGI2: inhibit platelet aggregation
endothelial cells
platelets
•Uses: analgesic, antipyretic, CV conditions
•Oral, buffered, EC, chewable, rectal administration
Aspirin
Ibuprofen
Diclofenac
Meloxicam
Is utilized for cardioprotection
Aspirin
Diclofenac
Ibuprofen
Meloxciam
Unique amongst NSAIDs:
Having Irreversible inhibition and Inhibition of prostaglandin and thromboxane synthesis
Aspirin
Celecoxib
APAP
Ibuprofen
Covalently inhibit COX enzymes by ACETYLATION
Aspirin
Ibuprofen
Diclofenac
Nabumetone
Aspirin have Biosynthesis of both PGs and TX will be inhibited
True
False
Aspirin induced asthma: NSAIDS/ASA cause more severe attacks.
Mechanism -> due to increased leukotrienes
True
False
Avoid aspirin in children and teenagers with viral infections, because increase risk of Reye’s Syndrome (N/V, somnolence, hepatic encephalopathy, lethargy, confusion)
True
False
Acetaminophen is alternative to patients who can’t use NSAIDs or in situations when anti-inflammatory effect is undesirable
True
False
•Boxed warnings: risk of errors and hepatotoxicity
•Note: variable recommended MDD; always ≤4 grams/day
•FDA: not more than 325 mg of APAP per dose in combination products
APAP
ASA
Ibuprofen
Naproxen
APAP Kinetics:
–A: extensive absorption in intestine
–M: hepatic oxidation (minimal at therapeutic dose), conjugation*
–E: t1/2 = 2-3 hours, prolonged at toxic doses
–A: extensive absorption in intestine
–M: liver oxidation (minimal at therapeutic dose), conjugation*
–E: t1/2 = 2-3 hours, prolonged at toxic doses
–A: low absorption in intestine
–M: hepatic oxidation (minimal at therapeutic dose), conjugation*
–E: t1/2 = 2-3 hours, prolonged at toxic doses
–A: extensive absorption in intestine
–M: hepatic oxidation (minimal at therapeutic dose), conjugation*
–E: t1/2 = 2-3 hours, not prolonged at toxic doses
What are the ADRs cause APAP?
rash
insomnia
constipation
nausea
vomiting
Acetaminophen have a metabolism mostly ______________and sulfate conjugation (80-90%)
glucuronidation
glucorinic
sulfation
oxidation
Oxidative metabolism in APAP: 10% via 2E1 & 1A2 à toxic metabolite via 2E1 1A2 (NAPQIà ->toxic metabolite
Inactivated by glutathione
activated by glutathione
Inactivated by glucorinic acid
APAP: Ethanol induces CYP2E1-> increased risk of hepatotoxicity with >2 drinks/day
True
False
Acetaminophen can cause:
Hepatotoxicity
Livertoxicity
Neuromuscular blockers-used during surgical procedures and in intensive care units
True
False
Skeletal Muscle Relaxants-reduce spasticity in a variety of neurological conditions
True
False
Skeletal muscle relaxants
Soma
Flexeril
Zanaflex
Motrin
Carisoprodol (SOMA) Poor CYP2C19 metabolizers->Increase drug level
True
False
_______________ is structurally related to tricyclic antidepressants and possess antimuscarinic effects.
Sedative, dry mouth
Cyclobenzaprine
Carisoprodol
Tizanidine
Ibuprofen
MOA: Exerts effect at GABAB receptors (G protein coupled receptor)
Baclofen
Cyclobenzaprine
Carisoprodol
Diazepam
Baclofen: hyperpolarization causes presynaptic inhibition by reducing Ca influx ® reduces release of excitatory neurotransmitters in the brain and spinal cord
True
False
________________ is a congener of clonidine that has been studied for its spasmolytic actions. Has significant central alpha-2 agonist effect. Inhibits nociceptive transmission
Zanaflex
Lioresal
Soma
Valium
___________ Blocks neuromuscular transmission by entering the nerve terminals, and inhibiting the release of acetylcholine.
Botulinum toxin Type A (BOTOX)
Cyclobenzaprine (FLEXERIL)
Tizanidine (ZANAFLEX)
Carisoprodol (SOMA)
