NSAIDs, Acetaminophen, DMARDs, Drugs used in Gout Flashcards
Class and MOA of aspirin
antiplatelet drug
nonselective COX 1 and 2 inhibitor; reduce platelet production of thromboxane A2
Class and MOA of Ibuprofen
nonselective NSAID
reversible inhibitor of COX 1 and 2; inhibits PG synthesis
Class and MOA of Ketorolac
IV NSAID nonselective
reversible inhibitor of COX 1 and 2; inhibits PG synthesis
Class and MOA of indomethacin
NSAID nonselective
reversible inhibitor of COX 1 and 2; inhibits PG synthesis
Class and MOA of Celecoxib
NSAID Highly COX-2 selective
Selective COX-2 inhibitor; inhibits PG synthesis
Class and MOA of Paracetamol
Analgesic (COX-3 inhibitor)
selectively inhibits COX-3; weakly inhibits COX-1 and 2; inhibits PG synthesis
SE of phenacitin
interstitial nephritis
Mechanism of Paracetamol overdose
oxidation to a cytotoxic intermediate N-acetyl-p-benzoquinoneimine (NAPQI) by phase 1 cyt P450 enzymes (CYP2E1)
Toxic and lethal dose for paracetamol
Toxic: 150mg/kg = 21 tabs
Lethal: 15g = 30 tabs
DMARD of first choice to treat RA
Methotrexate
Rescue agent for methotrexate
Leucovorin (folinic acid)
Class and MOA of Methotrexate
DMARD, Cancer chemo drug
inhibits AICAR transformylase, and thymidylate synthetase
Class and MOA of Infliximab
DMARD
Binds to TNF-a and prevents it from activating TNF-a receptor
Class and MOA of Azathioprine
DMARD
Forms 6-Thioguanine -> suppressing inosinic acid synthesis, B and T cell function, Ig production and IL-2 secretion
why you cannot give allopurinol with azathioprine?
allopurinol reduces xanthine oxidase catabolism of purine analogs -> inc 6-thioguanine nucleotides -> leukopenia
Class and MOA of Chloroquine
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
Class and MOA of cyclophosphamide
DMARD, cancer chemo drug
forms phosphoramide mustard -> crosslinks with DNA preventing cell replication
Suppresses B and T cell function
Rescue agent for cyclophosphamide
MESNA
Class and MOA of Cyclosporine
DMARD
inhibits IL-1 and IL-2 receptor production
secondarily inhibits macrophage T-cell interaction and T-cell responsiveness
Class and MOA of mycophenolate mofetil
DMARD
active product (mycophenolic acid) inhibits inosine monophosphate DH (imp for guanin nucleotide synthesis)
inhibits T-cell lymphocyte proliferation
Class and MOA of sulfasalazine
DMARD active metabolite (sulfapyridine) inhibits release of inflammatory cytokines
Class and MOA of Colchicine
Antigout Drug (microtubule assembly inhibitor) inhibits microtubule assembly and LTB4 production -> dec macrophage migration and phagocytosis
Class and MOA of probenecid
Antigout drug (uricosuric agent)
compete with uric acid for reabsorption in the PT
inc uric acid excretion
1st line tx for chronic gout
Allopurinol