Non-Narcotic Analgesics (NSAID’s) 91Paracetamol is given orally and is well ab-
sorbed, peak plasma concentration is reached
in 30 to 60 minutes. About 1/3rd is bound to
plasma proteins and the drug is inactivated in
the liver, being conjugated to give the glucu-
ronide or sulphate which are excreted in urine.
Adverse effects include nausea, epigas-
tric distress. Rarely it can cause skin rash.
Acute toxicity may result in hepatic failure.
Paracetamol is used for the rapid relief
of fever, pains and aches such as headache,
earache, toothache, fibrositis, myalgia, neu-
ralgia, arthralgia, osteoarthritis and postop-
erative pain.
NEWER COX-2 INHIBITORSKETOROLAC
Ketorolac is a NSAID chemically related
to indomethacin and tolmetin.
Ketorolac has antiinflammatory and an-
tipyretic action that, together with its anal-
gesic effects.
The absorption is rapid with maximum
plasma concentration being attained 30 to
40 minutes after oral administration. Highly
plasma protein bound and metabolised by
glucuronidation. 60% is excreted unchanged
in urine.
Adverse effects include, nausea, vom-
iting, epigastric distress, diarrhoea, drowsi-
ness, dizziness, skin rash etc.
It is indicated in short term management
of acute pain, pain associated with surgical
procedures.
NIMESULIDE
Nimesulide is a NSAID of the sulfonanilide
class. Nimesulide has exhibited potency
similar to or greater than that of indometha-
cin, diclofenac, piroxicam and ibuprofen in
standard animal models of inflammation.
Oral drug absorption is nearly complete
and concomitant administration of food may
decrease the rate, but not the extent of ab-
sorption. The drug is 99% bound to plasma
proteins and metabolised (1 to 3% of a dose
is excreted unchanged in the urine) to sev-
eral metabolites which are excreted mainly
in the urine or the faeces.
The adverse effects are gastrointestinal
disturbances (epigastralgia, heart burns,
nausea, diarrhoea and vomiting). It can also
lead to rash, pruritus, dizziness, somnolence
and headache.
There were reports of hepatotoxicity es-
pecially in children, due to which it should
not be used in children and in the presence
of hepatic dysfunction.
It is indicated in the treatment of a vari-
ety of painful inflammatory conditions, in-
cluding osteoarthritis, oncology, postopera-
tively, trauma, sports injuries, ear, nose and
throat disorders, dental surgery, bursitis/
tendinitis, thrombophlebitis, upper airways
inflammation and gynaecological disorders.
Nimesulide has shown to be well tolerated
even by aspirin sensitive asthmatic patients.CELECOXIB
It is a NSAID which has COX-2 selec-
tivity. It is a diaryl substituted pyrazole.
It exhibits antiinflammatory, analgesic
and antipyretic activities which are believed
to be due to inhibition of COX-2. At thera-
peutic concentrations in humans, celecoxib
does not inhibit COX-1 enzyme.