NSAIDs, Acetaminophen, DMARDs, Drugs used in Gout

Question 1

Class and MOA of aspirin

Answer 1

antiplatelet drug

nonselective COX 1 and 2 inhibitor; reduce platelet production of thromboxane A2

Question 2

Class and MOA of Ibuprofen

Answer 2

nonselective NSAID

reversible inhibitor of COX 1 and 2; inhibits PG synthesis

Question 3

Class and MOA of Ketorolac

Answer 3

IV NSAID nonselective

reversible inhibitor of COX 1 and 2; inhibits PG synthesis

Question 4

Class and MOA of indomethacin

Answer 4

NSAID nonselective

reversible inhibitor of COX 1 and 2; inhibits PG synthesis

Question 5

Class and MOA of Celecoxib

Answer 5

NSAID Highly COX-2 selective

Selective COX-2 inhibitor; inhibits PG synthesis

Question 6

Class and MOA of Paracetamol

Answer 6

Analgesic (COX-3 inhibitor)

selectively inhibits COX-3; weakly inhibits COX-1 and 2; inhibits PG synthesis

Question 7

SE of phenacitin

Answer 7

interstitial nephritis

Question 8

Mechanism of Paracetamol overdose

Answer 8

oxidation to a cytotoxic intermediate N-acetyl-p-benzoquinoneimine (NAPQI) by phase 1 cyt P450 enzymes (CYP2E1)

Question 9

Toxic and lethal dose for paracetamol

Answer 9

Toxic: 150mg/kg = 21 tabs
Lethal: 15g = 30 tabs

Question 10

DMARD of first choice to treat RA

Answer 10

Methotrexate

Question 11

Rescue agent for methotrexate

Answer 11

Leucovorin (folinic acid)

Question 12

Class and MOA of Methotrexate

Answer 12

DMARD, Cancer chemo drug

inhibits AICAR transformylase, and thymidylate synthetase

Question 13

Class and MOA of Infliximab

Answer 13

DMARD

Binds to TNF-a and prevents it from activating TNF-a receptor

Question 14

Class and MOA of Azathioprine

Answer 14

DMARD

Forms 6-Thioguanine -> suppressing inosinic acid synthesis, B and T cell function, Ig production and IL-2 secretion

Question 15

why you cannot give allopurinol with azathioprine?

Answer 15

allopurinol reduces xanthine oxidase catabolism of purine analogs -> inc 6-thioguanine nucleotides -> leukopenia

Question 16

Class and MOA of Chloroquine

Answer 16

DMARD, antimalarial
suppression of T-lymphocyte responses to mitogens, dec leukocyte chemotaxis, stabilization of lysosomal enzymes, inhibition of DNA/RNA synthesis, trapping of free radicals

Question 17

Class and MOA of cyclophosphamide

Answer 17

DMARD, cancer chemo drug
forms phosphoramide mustard -> crosslinks with DNA preventing cell replication
Suppresses B and T cell function

Question 18

Rescue agent for cyclophosphamide

Answer 18

MESNA

Question 19

Class and MOA of Cyclosporine

Answer 19

DMARD
inhibits IL-1 and IL-2 receptor production
secondarily inhibits macrophage T-cell interaction and T-cell responsiveness

Question 20

Class and MOA of mycophenolate mofetil

Answer 20

DMARD
active product (mycophenolic acid) inhibits inosine monophosphate DH (imp for guanin nucleotide synthesis)
inhibits T-cell lymphocyte proliferation

Question 21

Class and MOA of sulfasalazine

Answer 21

DMARD 
active metabolite (sulfapyridine) inhibits release of inflammatory cytokines

Question 22

Class and MOA of Colchicine

Answer 22

Antigout Drug (microtubule assembly inhibitor) 
inhibits microtubule assembly and LTB4 production -> dec macrophage migration and phagocytosis

Question 23

Class and MOA of probenecid

Answer 23

Antigout drug (uricosuric agent)
compete with uric acid for reabsorption in the PT
inc uric acid excretion

Question 24

1st line tx for chronic gout

Answer 24

Allopurinol

Question 25

Class and MOA of allopurinol

Answer 25

Antigout drug (xanthine oxidase inhibitor)
Active metabolite (alloxanthine) irreversibly inhibits xanthine oxidase and lowers production of uric acid

Question 26

Class and MOA of Febuxostat

Answer 26

antigout (xanthine oxidase inhibitor)

nonpurine reversible inhibitor of xanthine oxidase