NSAIDS & DMARDS Flashcards
Aspirin
NSAID, 80% protein bound, 325 mg tablets,
low dose inhibits only COX-1 (irreversible acetylation)(decreases TX/platelets)
anti-analgesic, anti-pyretic
anti-inflammatory in higher doses (reversible)
no for kids, Reye’s syndrome
COX-1
Thromboxanes (TX) INCREASE, platelets INCREASE
Clotting INCREASE
Fever, pain, protect stomach mucosa
COX-2
PGs INCREASE, Clotting DOWN, Platelets DECREASE
pain, inflammation, protect stomach mucosa
Metabolism of salicylate
LOW; liver, glucuronic acid, first order
HIGH: kidneys OATS, zero order
Metabolism of salicylate
LOW; liver, glucuronic acid, first order
HIGH: kidneys OATS, zero order
Salicylate Toxicity
Low: acidosis, breathe more,
Mid: breathe more from above causes alkalosis, excrete bicarb in urine
Extreme: respiratory paralysis, become acidosis, renal failure, acidic plasma causes major organ failure
RESPIRATORY FAILURE IS FINAL CAUSE OF DEATH
Ibuprofen
propionic acid
not as severe side effects as salicylates
specifically approved for menstrual cramps,
98% protein/albumin-bound
200 mg /4-6 hrs
treats ductus arteriosis
Naproxen
propionic acid
goat and migraine
for sharper pain
Indomethacin
causes severe headaches and GI issues
treats ductus arteriosis
only use for severe rheumatoid or gouty arthritis
Indomethacin
causes severe headaches and GI issues
Celecoxib
Only inhibits COX-2
more for chronic pain
contrained with sulfonamide allergy
can’t take while pregnant
Acetaminophen
NO ANTI-INFLAMMATORY ACTION
aka non-opioid analgesic
no bad aspirin side effects (like GI/asthma issues) but can cause terrible liver toxicity (NADQI and no glutathione to take it)
kids can take
N-Acetylcysteine
Treats acetaminophen toxicity
Replenishes lost glutathione stores
Methotrexate/MTX
oral or SC injection
uses folate membrane transporters, poly-glutamate
inhibited AICAR purines
inhibited thymidine pyrimidines
inhibits inflammation immune cell proliferation^^
increases adenosine (prevents inflammation)
anti-cancer: kills DHFR and FH4
cant be pregnant/or a nursing mother
give folate to prevent issues
Hydroxychloroquine
ok while preggo antimalarial and anti-inflammatory alters cell pH risk of retinal damage decrease blood glucose
Sulfasalazine
oral
often used w MTX and HCN (triple Nebraska therapy)
modifies GI immune system
don’t use w a sulfonamide allergy
Leflunomide
inhibits pyrimidine synthesis
inhibits T-cell and reduce antibodies from B-cells
is a prodrug
very long half life, repeat enterohepatic circulation is an issue
cant be preggo
need cholestyramine to be ok before pregnancy
Minocycline
tetracycline antibiotic
inhibits degradation of collagen
General Biological Response Modifiers
work better w MTX
increased risk of infections and cancer
etanercept
binds to and prevents TNF from binding to cellular receptors
cause PML/brain disease
infliximab
mouse-human
is a monoclonal antibody against TNF
can cause hypotension
adalimumab
full-human
anti-TNF antibody
Can cause demyelination
adalimumab
full-human
anti-TNF antibody
Can cause demyelination
Abatacept
CD28, T-CELL!!!!!!!!!
don’t combine w other TNF inhibitors, can’t use with COPD
