Pests of castor_Binomics_Identification_Dr.UPR.pdf
NSAIDs Mechanism of Action and Side Effects
1. NonsteroidalNonsteroidal
Antiinflammatory DrugsAntiinflammatory 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 3rdrd
yearyear
CHANDRA SHEKHAR SINGH COLLEGE OF PHARMACYCHANDRA SHEKHAR SINGH COLLEGE OF PHARMACY
ALLAHABADALLAHABAD
2. What are NSAIDs and how do theyWhat are NSAIDs and how do they
work?work?
Drug with analgesic( without impairingDrug with analgesic( without impairing
consciousness ), antipyretic, and anti-consciousness ), antipyretic, and anti-
inflamammatory effectsinflamammatory effects
weak acids, PH 3-5, well absorbedweak 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
3. ProstaglandinsProstaglandins
Prostaglandins : produced by the cells,Prostaglandins : produced by the cells,
promote inflammation, pain, and fever; bloodpromote inflammation, pain, and fever; blood
clotting function of platelets; protect the liningclotting 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 promoteproduce prostaglandins that promote
inflammation, pain, and feverinflammation, pain, and fever
4. What are NSAIDs and how do theyWhat are NSAIDs and how do they
workwork ??
NSAIDs block the COX enzymes , reduceNSAIDs block the COX enzymes , reduce
prostaglandins, inflammation, pain, and fever areprostaglandins, inflammation, pain, and fever are
reduced.reduced.
COX-1 produced prostaglandins that support plateletsCOX-1 produced prostaglandins that support platelets
and protect the stomach.and protect the stomach.
Reduced prostaglandins that protect the stomach andReduced prostaglandins that protect the stomach and
support blood clotting, so NSAIDs can cause ulcerssupport blood clotting, so NSAIDs can cause ulcers
in the stomach and promote bleeding.in the stomach and promote bleeding.
5.
6. For what conditions are NSAIDsFor 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
7. For what conditions are NSAIDsFor what conditions are NSAIDs
used?used?
AspirinAspirin (also an NSAID) : inhibit the clotting(also an NSAID) : inhibit the clotting
of blood( platelet aggregation ) ,preventof blood( platelet aggregation ) ,prevent
strokes and cardiovascular attacksstrokes and cardiovascular attacks
11. 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).
20. Side effects of NSAIDsSide effects of NSAIDs
GastrointestinalGastrointestinal
Direct irritation : acidic moleculesDirect irritation : acidic molecules
Indirect irritation: inhibit COX-1, reduceIndirect irritation: inhibit COX-1, reduce
protective prostaglandinsprotective prostaglandins
nausea, vomiting, dyspepsia, gastricnausea, vomiting, dyspepsia, gastric
ulcer/bleeding, diarrheaulcer/bleeding, diarrhea
Duration of therapy, doseDuration of therapy, dose
21. Side effects of NSAIDsSide effects of NSAIDs
CardiovascularCardiovascular
80% increase risk with newer COX-2 and high80% increase risk with newer COX-2 and high
dose traditional NSAIDdose traditional NSAID
Heart failure riskHeart failure risk
22. Side effects of NSAIDsSide effects of NSAIDs
RenalRenal
Decrease prostaglandinsDecrease prostaglandins→→ constriction ofconstriction of
afferent arterioleafferent arteriole →→ decreased renal perfusiondecreased 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.
23. Side effects of NSAIDsSide effects of NSAIDs
OthersOthers
Allergy: shortness of breathAllergy: shortness of breath
Asthma : a higher risk for serious allergicAsthma : a higher risk for serious allergic
reactionreaction
with a serious allergy to one NSAID are likelywith a serious allergy to one NSAID are likely
to have similar reaction to a different NSAIDto have similar reaction to a different NSAID
photosensitivityphotosensitivity
24. Combinational RiskCombinational Risk
If COX-2 inhibitor taken, should not use aIf COX-2 inhibitor taken, should not use a
traditional NSAID concomitantlytraditional NSAID concomitantly
With daily aspirin therapy, should use otherWith daily aspirin therapy, should use other
NSAID carefully, they may block theNSAID carefully, they may block the
cardioprotective effect of aspirincardioprotective effect of aspirin
25. 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