NSAIDs Flashcards
Acetyl Salicylic Acid
Asprin
salicylate ester, hydrolyzed in vivo
acidic
irreversibly acetylates and inactivates COX1
inhibits prostaglandin synthesis
may prolong bleeding time
platelet effects for 4-7 days
absorbed from the GI tract, dissolution is RLS
higher pH in stomach increases absorption but most occurs in small intestine where dissolution and large SA allow absorption
crosses placental, BBB
highly bound to albumin
more cleared with more alkaline urine
SE - GI, otic, hepatic, renal, CV, hematologic, hypersensitivity type 1, reye’s syndrome, pregnancy,
uses - mild pain, fever, inflammatory disease, venous thrombosis
- rheumatoid, jevenile, osteoarthritis -> 3 g daily
Mesalamine
salicylic acid
reversible COX1&2
uses - ulcerative colitis
SE - GI, CNS, Nasopharyngitis, hypersensitivity
Diflunisal
derivative of salicylic, not true salicylic
analgesic, antiinflammatory, no antipyretic
reversibly bind COX1 and 2
mild SE - GI, HA, renal impairment, hypersensitivity
use -anti-inflammatory, analgesic
indomethacin
NSAID reversible COX-1 and 2 use - arthritis EXCEPT juveline tocolytic agent SE - severe GI, bleeding, CV, CNS, close PDA
etodolac
NSAID
less sever GI than indomethacin
diclofenac
NSAID
dysmenorrhea
SE - GI, CNS
tolmetin
NSAID
juvenile and other arthritis
SE - GI, CNS, hypersensitivity
ketorolac
NSAID
not for RA or osteoarthritis
SE - GI, HA
ibuprofen
reversible COX1 and COX2
less GI than aspirin, indomethacin
ocular disturbances, hypersensitivity, not during late pregnancy or breast feeding
tx - fever, RA, osteoarthritis, pain, dysmenorrhea
naproxen
reversible COX1 and COX2
GI, CNS, hypersensitivity
used for juveline RA
ketoprofen
reversible COX1 and COX2
GI in 30% of pts
CNS
oxaprozin
reversible COX1 and COX2
once daily
GI
piroxican
oxicam - reversible COX1 and COX2
SE - GIA
RA and osteoarthritis
meloxicam
reversible COX1 and COX2 but COX2 selective
SE - GI
osteoarthritis
nabumetone
reversible COX1 and COX2 but COX2 selective
activated by liver
SE - GI, HA
acetaminophen
paracetamol
weakly inhibits COX-1 and 2
inhibits prostaglandins in CNS only
works of fever at hypothalamic level
no CV, respiratory, platelet, GI side effects
can form N-acetyl-p-benzoquinoneimine which is toxic to the liver and kidney when GSH depleted
use - analgesic-antipyretic
osteoarthritis
no more than 4 g/daily
overdoes- give mucomyst and gastric lavage
celecoxib
NSAId that has anti-inflammmatory, pyretic and analgesic activity
inhibits just COX2
highly protein bound
hepatic metabolism
uses - osteoarthritis, rheumatoid arthritis, acute pain, familial adenomatous polyposis
SE - GI, CNS< respiratory, skin, psychiatric
should not be given to pts with allergic rcns to sulfonamides, aspirin or other NSAIDs
aspirin toxicity
tinnitus and HL are first manifestation chronically in adults
kids - hyperventilation and CNS effects
metabolic acidosis, respiratory alkalosis
salicylate jab then CNS depression
tx - remove from GI tract via emesis, give charcoal to prevent further absorption, enhance salicylate elimination via sodium bicarbonate
aspirin drug interactions
corticosteroids increase renal clearance
others NSAIDs cause a potential for adverse effects
highly protein bound - interacts with other protein bound drugs - oral anticoagulants, PCN
NSAIDS
analgesic, antipyretic reversivle COX1 and 2 inhibition reduce prostaglandins and thromboxane B2 mostly used as anti-inflammatory agents mild analgesia rheumatoid arthritis, osteoarthritis, juvenile arthritis close patent ductus arteriousis rapidly absorbed, acidic
NSAIDs SE
hepatotoxicity in kids CV - edema, HTN CNS - cross BBB - dizziness, HA< dorwsiness, derm reations stronger reactions as you age GI - ucler hematologic hepatic hypersensitivity not to be used while pregnant or nursing renal impairment due to prostaglandin inhibition
