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Non-steroidal anti-inflammatory drugs : drugs of other than aspirin or…
Non-steroidal anti-inflammatory drugs : drugs of other than aspirin or paracetamol
pryazolone derivative
phenylbutazone
non-selective COX inhibitor
active metabolite-> oxyphenbutazone
Effect
Weak analgesic & antipyretic effects
anti-inflammatory effect : marked -> limited to acute gouty arthritis
inhibition of phagocytosis of urate crystal -> relevant for gout
side effect
Low dose
May lead to uric acid retention by competitive inhibition of urate secretion in the proximal tubule
High dose
increase renal urate excretion by inhibiting urate reabsorption (not a side effect)
Special
agranulocytosis
Aplastic anemia
High plasma protein binding
displacement of other drugs
Metamizol-Na
Effect:
analgesic & antipyretic effects with unknown mechanism
act in colic pain as well
anti-inflammatory effect
only in high dose with weak effect
Advantage
lack of peripheral COX inhibition
no gastric damage & no acute renal function-diminishing
Side effect
allergic reactions
nephropathy in long-term treatment
hypotension and convulsion
agranulocytosis
Sulfinpyrazone
Chemically related to pyrazolone
but has no analgesic, antypyretic or anti-inflammatory effect
Inhibit platelet aggregation
its uricosuric acction is exploited in treatment of gout
Acetic acid derivate
indomethacin
Non-selective COX inhibitor
produrg: acemetacin
Effect
analgesic & antipyretic effects
anti-inflammatory effect
special effect
inhibition of phagocytosis of urate crystal -> relevant for gout
for closure of persistent ductus arteriosus
Side effect
Severe gastric damage
Diclofenac
Non-selective COX inhibitor
Effect
Analgesic & antipyretic effect
Anti-inflammatory
I.m, eyedrops, ointment
Accumulate in synovial fluid -> sustained local effect
Side effect:
less gastric damage but hepattoxic
Etodolac
COX-2 preferential inhibitor
Less GI side effect
99% binding to plasma protein
Ketoloac
Non selective COX inhibitor
analgesic effect : postoperative
anti-inflammatory effect : eyedrops in ocular inflammatory disease
Propionic acid derivative
naproxen
ibuprofen
flurbiprofen
Non-selective COX inhibitor
Effect
analgesic & antipyretic effects
anti-inflammatory effect
special effect
inhibitory effect on neutrophils’ activity
Side effect
less GI side effects than other non-selective COX inhibitors
99% binding to plasma protein
naproxen : cardioprotective effect
Enolic acid derivative
Prioxicam
Non-selectiveCOX inhibitor
Effect
marked anti-inflammatory effect
inhibit chemotaxis of neutrophil
T1/2: days
Side effect
Mild GI side effect
Meloxicam
COX-2 preferential inhibitor
Effect
Marked anti-inflammatory effect
Long half life
Side effect
Mild GI side effect
Fenamic acid derivative
niflumic acid
mefenamic acid
non-selective COX inhibitor
Effect
analgesic & antipyretic
anti-inflammatory
special effect
some have PG effect
Special side effect
Diarrhea
Coxibs
Cox 2 specific
Effect
analgesic but no antipyretic effects
anti-inflammatory effect
Advantage
. strongly reduced GI toxicity compared to non-selective COX inhibitors
do not alter the bleeding time
no aspirin asthma
high degree of plasma protein binding
Side effect
similar renal side effects as with non-selective COX inhibitors
acute myocardial infarction & stroke upon long-term treatment
Others
nabumetone
COX-2 preferential inhibitor
T1/2: 1 day
Prodrug
converted to COX-2 preferential metabolite
Nimesulide
COX-2 preferential inhibitor
may cause hepatotosicity