Download NONSTEROIDAL ANTIINFLAMATORY DRUGS(NSAIDS)

NONSTEROIDAL ANTIINFLAMATORY
DRUGS(NSAIDS)
• Definition :Non steroidal anti inflammatory drugs is a
class of analgesic medication that reduces pain, fever
& inflammation .
• Pain: It is a neurophysiological sensation arising from
noxious stimulus.
• Fever : It is a elevation of body temperature.
• Inflammation : It is a localized physical condition in
which part of the body becomes reddened , swollen
,hot & often pain full ,especially as a reaction to
infection
Classification:
Non selective
Cox inhibitors
Preferential
Selective
cox2 inhibitors cox2inhibitors
Cox3
inhibitors
• Non selective COX inhibitors:
1. Salicylates : aspirin
2. Propionic acid derivatives : ibuprofen
3. Anthranillic acid derivative : mephenamicacid
4. Aryl acetic acid derivatives : diclofenac
•
•
•
Preferential cox2 inhibitors : nimesulide , meloxicam
nabumetone
Selective cox2 inhibitors :celecoxib , etoricoxib
Cox3 inhibitors : para acetamido phenol
Mechanism of action:
Cell wall phospholipids
phospho lipase A2
Arachidonic acid
COX enzyme
cyclo endo
peroxides
prostaglandins
Hydroxy acid
of arachdonic acid
leuko trienes
• Cox 1:This activity is constitutively present in nearly
all cell types at constant level .
• Cox 2: This activity is normally absent from cells
except those of kidneys & brain but it is inducible by
bacterial lyposaccharides IL2 &TNF in activated
leucocytes &other inflammatory cells.
• Cox 1 is a physiological while Cox 2 is usually
pathological
• SALICYLATES:
• Aspirin: it is a acetyl salicylic acid it is rapidly
converted in the body to salicylic acid which is
responsible for most of the actions . Other actions
are the result of acetylation of certain macro
molecules including COX it is the of the oldest
analgesic, anti inflammatory drugs & is still widely
used
• Pharmacological actions:
 Analgesic , anti pyretic , anti inflammatory actions
of aspirin:
aspirin is weaker analgesic than
morphine like drugs aspirin 600mg similar to
codeine 60mg .how ever it effectively relives anti
inflammatory action.
 Respiration:
the effects are dose dependent . at anti
inflammatory doses , respiration is stimulated by
peripheral &central actions further rising of Salicylate
level causes respiratory depression , death is due to
respiratory failure
 Acid base electrolyte balance:
anti inflammatory doses produce
significant changes in the acid base &electrolyte
composition of body fluids. initially respiratory
stimulation predominates &tends to wash out CO2
CVS:
aspirin has no direct effect in therapeutic
doses larger dose increase in cardiac output and
increased oxygen levels and cause direct
vasodilation .
GIT:
aspirin and released salicylic acid irritate
gastric mucosa
BLOOD:
Aspirin having anti coagulent property
.long term intake of large dose decreases
synthesis of clotting factors in liver
 USES:
Its is used as analgesic, anti pyretic &treatment
of acute rheumatic fever &rheumatoid arthritis &
osteoarthritis
 Adverse effects:
Ibuprofen & all its congeners are better
tolerated than aspirin . side effects are milder and
their incidence is lower
gastric discomfort , nausea ,and vomiting ,
though less than aspirin or indomethacin.
CNS side effects include headache, dizziness.
Precautions :
•
aspirin is contraindicated in patients who are
sensitive to it and in peptic ulcer ,bleeding tendencies
In children suffering from chicken fox or influenza.
• In chronic liver disease cases of hepatic necrosis have
been reported .
• Aspirin should be stopped one week before electric
surgery
• Given during pregnancy it may be responsible for low
birth weight babies
• It should be avoided by breast feeding methods &also
in diabetics
• Conclusion:
Inhibition of COX-1& COX-2 by NSAIDS
in gastro intestinal track has been associated
with both adverse and beneficial effects. The
effects of NSAIDS & COX-2 inhibitors in
patients with inflammatory bowel disease are
still unclear. New nitric oxide-NSAIDS
derivates, may prevent the colon cancer.
• References:
• Abenavoli L, capasso R ,Millic N ,et al
• A Book on pharmacology by NM agarwal