NSAIDs

Question 1

ASA dosing

Answer 1

Analgesic: 325mg q4-6h
Antipyretic: 325-650mg q4-6h
Aniplatelet: min. 60-80mg
Antiinflamm: 650mg

Question 2

ASA GI SEs is caused by?

Answer 2

Due to inhibition of prostacyclin PGEs, PGI2- inhibit gastric secretion
salicyclate GI SEs n&v epigastric discomfort, peptic ulcers- dyspepsia, heartburn

Question 3

ASA respiratory and renal SEs

Answer 3

Respiratory depression: toxicity resp. alkalosis and metabolic acidosis (inc. CO2 and dec pH)
Decrease RENAL BLOOD FLOW= acute renal failure

Question 4

Acute syndrome that may follow infuenza and chicken pox infections in children, only assoc. only ASA

Answer 4

Reye’s syndrome

SEs vomiting, violent headache, unusual behavior

Question 5

Sulfasalazine drug chemistry.

Answer 5

Azo bond, sulfonamide group may cause sulfa allergy. Metabolism phase 1-Azo reduction yields 5ASA (Mesalamine) + Sulfapyridine

Question 6

Sulfasalazine DOC and SEs

Answer 6

DOC for ulcerative colitis

SE megaloblastic anemia, infertility in men

Question 7

Diflurophenyl derivative of salicylic acid

Answer 7

Diflunisal- no salicylate toxicity, doesn’t produce salicylic acid
NO ANTIPYRETIC ACTION

Question 8

Propionic, acetic, Anthranilic acid and Oxicams drug derivatives.

Answer 8

Pro: Ketoprofen, Ibu, Naproxen, Carpro and Feno
AA: Indo, Diclo, Ketorolac, Etodolac and Sulindac- long t1/2 OD or BID
Antranilic acid: Mefenamic and Meclofenate acid
causes severe diarr and inflamm of bowels
Oxi: Piro, Melo, Teno, Piroxicam- t1/2 50h OD, more bleeding, CI in elderly

Question 9

Acetaminophen drug chemistry.

Answer 9

p-Aminophenil derivatives:
Acetaminophen from=
Phenacetin dealkylation
Acetanilid hydroxylation

Question 10

Acetaminophen metabolism

Answer 10

Undergoes phase 1 metabolism and glucuronidation, sulphate conjugation and glutathione conjugation

Question 11

Acetaminophen dosing and SEs

Answer 11

Antipyretic action: 325-650mg q4-6h PRN
SEs skin rash, hemolytic anemia -long term use of phenacetin
>4g/day renal dysf. and tubular necrosis hepatotoxicity.
max dose of 2g/d with excessive alcohol

Question 12

Toxic intermediate of phase 1 metabolism which is catalyzed by glutathione conjugation to what?

Answer 12

N-benzoquinoneimine = cysteine and mercapturic acid -end product

Question 13

Glutathione consists of what aa?

Saturation causes what toxicity?

Answer 13

Glutamic acid, cysteine and glycine

Glutathione saturation causes hepatotoxicity

Question 14

Acetaminophen antidote?

Answer 14

N-acetylcysteine

CH3CONH-CH-(COOH)-CH2SH

Question 15

Pyrazole drug derivatives and SEs

Answer 15

COX2 inhibitors: Celecoxib, Velde
have sulfonamide functional group
SEs arrhythmias GI upset diarr back pain resp probs nephrotoxicity

Question 16

Drugs that have sulfa allergy.

Answer 16

Celecoxib HCTZ Sulfonamide antibiotics Acetazolamide Furosemide Sulfasalazine Rosuvastatin