NSAIDs

Question 1

Acetyl Salicylic Acid

Answer 1

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

Question 2

Mesalamine

Answer 2

salicylic acid
reversible COX1&2
uses - ulcerative colitis
SE - GI, CNS, Nasopharyngitis, hypersensitivity

Question 3

Diflunisal

Answer 3

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

Question 4

indomethacin

Answer 4

NSAID
reversible COX-1 and 2
use - arthritis EXCEPT juveline
tocolytic agent
SE - severe GI, bleeding, CV, CNS, close PDA

Question 5

etodolac

Answer 5

NSAID

less sever GI than indomethacin

Question 6

diclofenac

Answer 6

NSAID
dysmenorrhea
SE - GI, CNS

Question 7

tolmetin

Answer 7

NSAID
juvenile and other arthritis
SE - GI, CNS, hypersensitivity

Question 8

ketorolac

Answer 8

NSAID
not for RA or osteoarthritis
SE - GI, HA

Question 9

ibuprofen

Answer 9

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

Question 10

naproxen

Answer 10

reversible COX1 and COX2
GI, CNS, hypersensitivity
used for juveline RA

Question 11

ketoprofen

Answer 11

reversible COX1 and COX2
GI in 30% of pts
CNS

Question 12

oxaprozin

Answer 12

reversible COX1 and COX2
once daily
GI

Question 13

piroxican

Answer 13

oxicam - reversible COX1 and COX2
SE - GIA
RA and osteoarthritis

Question 14

meloxicam

Answer 14

reversible COX1 and COX2 but COX2 selective
SE - GI
osteoarthritis

Question 15

nabumetone

Answer 15

reversible COX1 and COX2 but COX2 selective
activated by liver
SE - GI, HA

Question 16

acetaminophen

Answer 16

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

Question 17

celecoxib

Answer 17

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

Question 18

aspirin toxicity

Answer 18

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

Question 19

aspirin drug interactions

Answer 19

corticosteroids increase renal clearance
others NSAIDs cause a potential for adverse effects
highly protein bound - interacts with other protein bound drugs - oral anticoagulants, PCN

Question 20

NSAIDS

Answer 20

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

Question 21

NSAIDs SE

Answer 21

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