NSAIDs Flashcards
Propionic acid derivatives
ibuprofen
naproxen
Ibuprofen/naproxen uses
- analgesic
- anti-pyretic
- anti-inflammatory
- fewer side effects than aspirin, less toxic
Ibuprofen/naproxen inhibition
reversible and competitive only
ibuprofen/naproxen has specific approval for what?
dysmenorrhea
Adverse effects of ibuprofen/naproxen
- GI similar to aspirin (less severe, more potent, lower dose)
- prolong bleeding (short term)
- high albumin binding
- cross sensitivity
- prevent low dose aspirin from exerting anti-platelet effects
ibuprofen/naproxen is ___% protein binding
98%
Ibuprofen/naproxen and aspirin
take 8 hr before or 30 min after taking low dose aspirin
All NSAIDs can cause what?
renal toxicity/failure
Ibuprofen/naproxen toxicity
- tinnitus
- N/V
- GI bleeding
- lethargy
- seizures
- coma
Treatment of OD ibuprofen/naproxen
- activated charcoal first 2 hr
- supportive therapy
- monitor respirations
- urine alkalization not effective! (because protein bound)
Low dose ibuprofen use
analgesia/anti-pyresis
high dose ibuprofen use
anti-inflammatory
Ibuprofen specifically approved for
patent ductus arteriosus
Naproxen additional approvals
Gout
migraine
Acetic acid derivatives
indomethacin
Indomethacin is ___ more potent than aspirin
10-20x
indomethacin use
- limited use for analgesia and antipyresis
- Severe inflammation (RA, gouty arthritis)
indomethacin side effects
- severe HA, vertigo, confusion
- seizures
- serious GI problems
Selective COX2 inhibitor
Celecoxib
Most inflammation effects are due to ___
COX2
Celecoxib is equal to naproxen for what?
osteoarthritis and RA
Celecoxib is poorer than naproxen for what?
acute pain
DI celecoxib
- may inhibit CYP2D6
- slow metabolism of tricyclic and SSRI
Adverse effects of celecoxib
- edema
- GI (less than with ibu/nap)
- increased risk of MI
Who cannot use celecoxib?
allergy to sulfonamides
pregnancy
Components of MI risk in celecoxib
- TX/PGI imbalance
- inhibition of renal COX and loss of renal PG
BBW celecoxib and all NSAIDs
MI risk
COX2 inhibitors increase what?
Tx
platelet aggregation
risk of thrombosis, MI,storke
APAP
acetyl para-amino phenol
How dose APAP work?
don’t know!
inhibit COX and PG synthesis
APAP used for
analgesic
antipyresis
- CNS for relaxation, drowsiness, euphoria
***no anti-inflammatory
APAP side effects vs aspirin
- No GI effects
- No hematologic effects
- No CV effects
- No respiratory effects
- No acid/base effects
- No association with Reye’s
What is used in place of aspirin in children?
APAP
Max of APAP recommended
4g/day
Adverse effects of APAP
- cross sensitivity with aspirin
- hepatic damage!!
- alcohol increase liver damage
- skin rash, drug fever
- chronic abuse –> nephrotoxicity
OD toxicity APAP
- GI distress: 24h
- hepatotoxicity: usually reversible
- jaundice 24-48h
High APAP depletes ____
glucuronic acid
- hepatotoxicity
Treatment OD APAP
- supportive therapy
- remove drug promptly (charcoal 4hr)
- vomiting/gastric lavage (4h)
- after 4 hour: N-acetyl-cysteine
- time and concentration dependent windows
N-acetyl-cysteine
- reverse toxicity
- restore endogenous glutathione
- react with NAPQI (AC*) toxic metabolite
