NSAIDs, Acetaminophen, DMARDs, and Drugs used in Gout Flashcards
classification of NSAIDs
- Salicylates: irreversible
- Non-Selective NSAIDs: reversible
- COX2 selective
prevents uric acid excretion
therefore NOT USED IN GOUT
aspirin/ASA/acetylsalicylic acid
salsalate, sodium salicylate, choline salicylate, magnesium salicylate
low range dose of aspirin (<300 mg/d) follow what type of elimination kinetics?
first-order
effective in reducing platelet aggregation
intermediate dose of aspirin (300 - 400 mg/d) is effective as?
antipyretic and analgesic
high doses of aspirin (2400-4000 mg/d) follows what type of elimination kinetics?
zero-order
anti-inflammatory effect
NSAID propionic acid derivatives
Ibuprofen, Naproxen, Fenoprofen, Carprofen, Ketoprofen, Dexketoprofen, Oxaprozin
non-selective NSAID
for analgesia
long-term use reduces risk of colon Ca
Ibuprofen
diclofenac, diflunisal, etodolac, fenoprofen, fluribuprofen, ketoprofen, nabumetone, naproxen, oxaprozin, piroxicam, sulindac, tolmetin, mefenamic acid, bromfenac, meclofenamate, suprofen
prevents NSAID-induced gastritis
misoprostol
non-selective NSAID, IV
inhibits prostaglandin synthesis
post-surgical analgesic control
use generally restricted to 72 hours only
ketorolac
dexketoprofen
non-selective NSAID
reversible COX-1 > COX-2 inhibitor
for PDA closure
SE: aplastic anemia, thrombocytopenia
indomethacin
highly COX-2 selective NSAID
for analgesia
SE: reduced risk of GI bleeding, MI, stroke
celecoxib
etoricoxib, parecoxib
rofecoxib & valdecoib: withdrawn from market due to MI and stroke development
MELOXICAM IS PREFERENTIALLY COX-2 SELECTIVE INHIBITOR
COX-3 inhibitor
analgesic (mild)
SE: hepatotoxicity (increased with alcohol use)
preferred antipyretic in children (does NOT cause Reye Syndrome)
paracetamol
acetaminophen
phenacetin
antidote to paracetamol
N-Acetylcysteine
will donate -SH to reduce glutathione and reuse it vs. NAPQI (toxic paracetamol metabolite)
stages of paracetamol overdose
time period and manifestations
stage I: 0.5-24 hours: nausea, vomiting, diaphoresis, pallor, lethargy, malaise
stage II: 24-72 hours: elevated liver enzymes, oliguria, azotemia, increased PT, hyperbilirubinemia
stage III: 72-96 hours: jaundice, hepatic encephalopathy, bleeding diatheses, acute tubular necrosis, HAGMA, coma, death
stage IV: 4 days-2 weeks: recovery
DMARD
cancer chemotherapeutic drug
DMARD of first choice to treat rheumatoid arthritis
SE: mucosal ulcers, pseudolymphomatous reaction
RESCUE AGENT: LEUCOVORIN (folinic acid)
methotrexate
DMARD binds to TNF alpha for Crohn's disease, rheumatoid arthritis SE: reactivation of latent TB synergistic with methotrexate
infliximab
adalimumab, etanercept, certolizumab, golimumab
DMARD
forms 6-thioguanine
for rheumatoid arthritis
SE: bone marrow suppression, increased incidence of lymphoma
azathioprine
CANNOT BE GIVEN WITH ALLOPURINOL
reduces xanthine oxide metabolism of purine analogs
increasing 6-thioguanine nucleotides –> myelosuppression
DMARD
anti-malarial
for rheumatoid arthritis
SE: OCULAR TOXICITY
chloroquine
hydroxychloroquine
DMARD forms phosphoramide mustard for rheumatoid arthritis SE: bone marrow suppression, HEMORRHAGIC CYSTITIS RESCUE AGENT: MESNA
cyclophosphamide
DMARD
inhibits IL-1 and IL-2 receptor production
inhibits macrophage T-cell interaction and T-cell responsiveness
for rheumatoid arthritis, tissue transplantation
SE: NEPHROTOXICITY, GINGIVAL HYPERPLASIA, HIRSUTISM
cyclosporine
DMARD
for SLE nephritis, vasculitis Wegener’s granulomatosis, rheumatoid arthritis
SE: reversible myelosuppression (neutropenia)
mycophenolate mofetil
DMARD
for rheumatoid arthritis, IBD
SE: HEMOLYTIC ANEMIA, METHEMOGLOBINEMIA, REVERSIBLE INFERTILTY FOR MEN
Sulfasalazine
co-stimulation modulator
inhibits T-cell activation by binding to CD80 and CD86 on APC
for moderate to severe rheumatoid arthritis
NOT RECOMMENDED TO USE WITH TNF-ALPHA BLOCKER: increased incidence of serious infection
abatacept
non-biological DMARD
leflunomide
anti-gout
microtubule assembly inhibitor
for gout, familial mediterranean fever
SE: diarrhea, hepatic necrosis, acute renal failure, agranulocytosis
colchicine
5 agents that can inhibit microtubule function
- colchicine
- vinca-alkaloids
- taxanes
- griseofulvin
- azole anti-helminthics
commonly used in initial treatment of gout as replacement for colchicine
indomethacin
anti-gout
uricosuric agent: competes with uric acid for reabsorption
SE: GI irritation, aplastic anemia
may precipitate acute gout during early phase of drug action (hence co-administer with colchicine or indomethacin)
inhibits secretion of other weak acids (e.g. penicillin, methotrexate)
probenicid
sulfinpyrazone
anti-gout
xanthine oxidase inhibitor (irreversible)
1st LINE TREATMENT FOR CHRONIC GOUT, TUMOR LYSIS SYNDROME
SE: CATARACTS
inhibits metabolism of mercaptopurine and azathioprine
allopurinol
withheld for 1-2 weeks after acute episode of gouty arthritis
anti-gout
xanthine oxidase inhibitor (reversible)
NONPURINE REVERSIBLE INHIBITOR OF XANTHINE OXIDASE (MORE SELECTIVE THAN ALLOPURINOL)
for chronic gout, tumor lysis syndrome
Febuxostat
