Nonsteroidal Nonsteroidal
Antiinflammatory Drugs Antiinflammatory Drugs
(NSAIDs)(NSAIDs)
Under The Guidance Of – Presented By -Under The Guidance Of – Presented By -
Mr. Sudhakar Singh Mohd Asad FarooquiMr. Sudhakar Singh Mohd Asad Farooqui
(ASST.PROFESSOR ) B.Pharm 3(ASST.PROFESSOR ) B.Pharm 3
rdrd
year year
CHANDRA SHEKHAR SINGH COLLEGE OF PHARMACY CHANDRA SHEKHAR SINGH COLLEGE OF PHARMACY
ALLAHABADALLAHABAD
What are NSAIDs and how do they What are NSAIDs and how do they
work?work?
Drug with analgesic( without impairing Drug with analgesic( without impairing
consciousness ), antipyretic, and anti- consciousness ), antipyretic, and anti-
inflamammatory effectsinflamammatory effects
weak acids, PH 3-5, well absorbed weak acids, PH 3-5, well absorbed
from stomach and intestinal mucosafrom stomach and intestinal mucosa
protein-bound in plasma ( albumin),protein-bound in plasma ( albumin),
metabolised in the livermetabolised in the liver
ProstaglandinsProstaglandins
Prostaglandins : produced by the cells, Prostaglandins : produced by the cells,
promote inflammation, pain, and fever; blood promote inflammation, pain, and fever; blood
clotting function of platelets; protect the lining clotting function of platelets; protect the lining
of the stomach from damaging effects of acid.of the stomach from damaging effects of acid.
two COX enzymes, COX-1 and COX-2. two COX enzymes, COX-1 and COX-2.
produce prostaglandins that promote produce prostaglandins that promote
inflammation, pain, and fever inflammation, pain, and fever
What are NSAIDs and how do they What are NSAIDs and how do they
work work ??
NSAIDs block the COX enzymes , reduce NSAIDs block the COX enzymes , reduce
prostaglandins, inflammation, pain, and fever are prostaglandins, inflammation, pain, and fever are
reduced. reduced.
COX-1 produced prostaglandins that support platelets COX-1 produced prostaglandins that support platelets
and protect the stomach.and protect the stomach.
Reduced prostaglandins that protect the stomach and Reduced prostaglandins that protect the stomach and
support blood clotting, so NSAIDs can cause ulcers support blood clotting, so NSAIDs can cause ulcers
in the stomach and promote bleeding. in the stomach and promote bleeding.
For what conditions are NSAIDs For what conditions are NSAIDs
used?used?
Infalmmatory arthritis, Infalmmatory arthritis,
AS, psoriatic arthritis, AS, psoriatic arthritis,
ReterReter’’s syndromes syndrome
Acute goutAcute gout
Metastatic bone painMetastatic bone pain
Headache, migrainHeadache, migrain
Postoperative painPostoperative pain
Pyrexia ( fever)Pyrexia ( fever)
Renal colicRenal colic
For what conditions are NSAIDs For what conditions are NSAIDs
used?used?
AspirinAspirin (also an NSAID) : inhibit the clotting (also an NSAID) : inhibit the clotting
of blood( platelet aggregation ) ,prevent of blood( platelet aggregation ) ,prevent
strokes and cardiovascular attacksstrokes and cardiovascular attacks
Classification of NSAIDClassification of NSAID
Mode of action of NSAIDMode of action of NSAID
COXCOX
Cyclooxygenase (COX) is found bound to the
endoplasmatic reticulum. It exists in 3 isoforms:
• COX-1 (constitutive) acts in physiological
conditions.
• COX-2 (inducible) is induced in inflammatory
cells by pathological stimulus.
• COX-3 (in brain).
Side effects of NSAIDsSide effects of NSAIDs
GastrointestinalGastrointestinal
Direct irritation : acidic molecules Direct irritation : acidic molecules
Indirect irritation: inhibit COX-1, reduce Indirect irritation: inhibit COX-1, reduce
protective prostaglandinsprotective prostaglandins
nausea, vomiting, dyspepsia, gastric nausea, vomiting, dyspepsia, gastric
ulcer/bleeding, diarrheaulcer/bleeding, diarrhea
Duration of therapy, doseDuration of therapy, dose
Side effects of NSAIDsSide effects of NSAIDs
CardiovascularCardiovascular
80% increase risk with newer COX-2 and high 80% increase risk with newer COX-2 and high
dose traditional NSAIDdose traditional NSAID
Heart failure risk Heart failure risk
Side effects of NSAIDsSide effects of NSAIDs
RenalRenal
Decrease prostaglandinsDecrease prostaglandins→→ constriction of constriction of
afferent arteriole afferent arteriole →→ decreased renal perfusion decreased renal perfusion
→→alter renal functionalter renal function
: salt and fluid retension, hypertension: salt and fluid retension, hypertension
Caution: NSAID with ACE inhibitor, diureticCaution: NSAID with ACE inhibitor, diuretic
Rare: ARF, ATN, nephrotic syn.Rare: ARF, ATN, nephrotic syn.
Side effects of NSAIDsSide effects of NSAIDs
OthersOthers
Allergy: shortness of breath Allergy: shortness of breath
Asthma : a higher risk for serious allergic Asthma : a higher risk for serious allergic
reactionreaction
with a serious allergy to one NSAID are likely with a serious allergy to one NSAID are likely
to have similar reaction to a different NSAID to have similar reaction to a different NSAID
photosensitivityphotosensitivity
Combinational RiskCombinational Risk
If COX-2 inhibitor taken, should not use a If COX-2 inhibitor taken, should not use a
traditional NSAID concomitantlytraditional NSAID concomitantly
With daily aspirin therapy, should use other With daily aspirin therapy, should use other
NSAID carefully, they may block the NSAID carefully, they may block the
cardioprotective effect of aspirincardioprotective effect of aspirin
During pregnancyDuring pregnancy
Not recommended during pregnancy, Not recommended during pregnancy,
particular 3rd trimesterparticular 3rd trimester
Cause early closure of fetal ductus arteriosus, Cause early closure of fetal ductus arteriosus,
and fetal renal toxicity, premature birthand fetal renal toxicity, premature birth
Acetaminophen ia more safe during pregnancyAcetaminophen ia more safe during pregnancy
In France, NSAID and aspirin is contra-In France, NSAID and aspirin is contra-
indicated after 6 months of pregnancyindicated after 6 months of pregnancy