This document provides an overview of nonsteroidal anti-inflammatory drugs (NSAIDs), including their classification, mechanisms of action, examples of drug classes, and key properties. NSAIDs are widely used analgesic, antipyretic and anti-inflammatory drugs. They work by inhibiting the cyclooxygenase (COX) enzymes and subsequent prostaglandin synthesis. The document describes both non-selective COX inhibitors like aspirin, ibuprofen, and naproxen, as well as selective COX-2 inhibitors. Common adverse effects and clinical uses are summarized for different NSAID classes.

1. Dr ABHINAND
MALABAR DENTAL COLLEGE
NONSTEROIDAL ANTI-
INFLAMMATORY DRUGS

2. CONTENT
 Introduction
 Classification
 Mechanism of action
 Ibuprofen
 Acetyl salicylic acid
 Pyrazolone derivatives
 Other non selective cox 2 inhibitors
 Cox 2 selective inhibitors

3. INTRODUCTION
 Most widely used therapeutic agent in world wide
 They are also called 1.aspirin like analgesics
2.non narcotics
3.non opioids
 Analgesics
 Antipyretics
 Anti-inflammatory actions
 Uricosuric properties

4. CLASSIFICATION
1. Non seletive COX inhibitors
 Salicylic acid derivatives
( aspirin , sodium salicylate ,diflunisal)
 Para-aminophenol derivatives
( paracetamol)
 Pyrazolone derivatives
(phenylbutazone)
 Indole acetic acid derivatives
(Indomethacin, sulindac)
 Arylacetic acid derivatives
(Diclofenac, aciclofenac, ketorolac)

5.  Propoinic acid derivatives
(ibuprofen,fenoprofen,naproxen,flurbiprofen)
 Anthranilic acids(fenamate)
(flufenamic acid,mefenamic acid,enfenamic
acid)
 Oxicams
(piroxicam ,tenoxicam)
 Alkanones
(nabumetone)

6. 2. Selective cox2 inhibitors
(celocoxib,rofecoxib)
3.Preferential cox-2inhibitors
(nimesulide,meloxicam)
4 nsaids that do not inhibit PG synthesis
(metamizol ,nefopam)

7. MODE OF ACTION
 During inflammation , arachidonic acid liberated from
membarane phospholipids is converted to PGs
catalysed by enzyme COX
 PGs sensitize nerve endings and produce hyperalgia
by mediators like bradykinin and histamine
 NSAIDs inhibit PG synthesis by blocking the enzyme
cyclo-oxygenase
 Two types COX enzyme ,COX1 and COX2
 COX1 seen in normal cell to mainatin
hemostasis(costitutive)
 COX 2 induced by inflammatory cell(inducible)

9. NON SELECTIVE COX
INHIBITORS

10. SALICYLATES
 Salts of salicylic acid
 Aspirin is taken as the prototype
PHARMOCOLOGICAL ACTION
1. Analgesia-(300-600mg/day)
 Relief pain in inflammatory orgin
 Pain orginating from integumentary structure
like muscle,bone joints,muscle,and pain in
connective tissue is releived
 Relif without euphoria and hypnosis, so less
chance to developmnt of dependence and
tolerance

11. 2.Antipyretics-(300-600mg/day)
 in the presence of fever salicylates bring down
the temperature to normal.
 In fever ,pyrogen increase the PGs synthesis in
hypothalamus and disturbs the thermostat
 Aspirin inhibit PGs synthesis and reset the
temperature.
 Increase the sweating and cutaneous
vasodialation assist the antipyretic action

12. 3.Anti-inflammatory action
 At higher doses of 4-6g/day
 It reduces the inflammatory signs like
tenderness ,swelling ,erythema , and pain
 But actually disease is progressing
 In addition,Aspirin interfere with the formation
of chemical mediators of kallilerin system.

13. 4.Respiration
 In therapeutic doses,it increase the consumption of
O2 by skeltal muscles.→↑co2
 It stimulates the respiratory center-→co2 washed out
and leads to respiratory alkalosis and increase in
pH→compensated by excretion of HCO3→known as
compensated respiratory alkalosis
 With toxic dose,direct stimulation of centres -
Depression of respiratory center& cardiovascular
centre→↑bp,respiratory acidosis,no compensations
&metabbolic acidosis also-so called uncompensated
respiratory acidosis
 Renal failure

14. 5.acid-base &electrolyte balance
 In anti inflammatory dose ,it produce significant
respiratory stimulation-co2 washed out resulting
in respiratory alkalosis,pH become alkaline.
 It compensated by secretion of HCO3+
 In toxic doses produce respiratory acidosis
 Effects accompanied by dehydration

15. 6.Metabolic effect
 Enhance the cellular metabolism due to
uncoupling of oxidative phosphyration
 More of o2 is used more co2 is produced ,leading
to incresed heat production
7.GIT
Aspirin blocks the PGs in stomach that leads to
increase the hcl in stomach
 Also salicylic acid increase HCl directly. This
leads to peptic ulcer.
 Also it affect CTZ and induce emesis

16. ADVERSE EFFECT
1. GIT. Nausea ,epigastric
distress,vomitting,erosive gastrirtis,peptic
ulcer,increased occult blood loss in stools
2. CNS-headache,diziness
3. ALLERGIC REACTION
4. RESPIRATORY SYSTEM
5. HEMOLYSIS
6. NEPHROTOXICITY
7. REYE’S SYNDROME
8. PREGNANCY AND INFANCY
9. SALICYLISM

17. ACUTE SALICYLATE
INTOXICATION
 Poisoning may be accidental or suicidal
 More common in childrens
 15-30 g is the fatal dose
 Symptoms and signs-
dehydration,hyoerpyrexia,GI
irritation,vomitting,acid base
imbalance,restlessness,deliriumhalucination,meta
bolic acidosis,tremors,convulsions,coma,death
due to resoiratory failure

18.  TREATMENT-
 Gastric lavage to eliminate unabsrobed drugs
 Iv fluid to correct the acid base imbalance and
dehydration
 T is brouht down by external cooling with alcohole
or cold water sponges
 If hemorragic complications are seen ,blood
transfusion and vit K are needed
 In severe cases,forced alkaline diuresis with
NaHCO3 and diuretic like frusemides is given
along with iv fluid.

19. PRECAUTION
&CONTRAINDICATION
1. Peptic ulcer
2. Sensitive pt.
3. Children suffering from influenza &chickenpox
4. Chronic liver disease
5. Diabetics
6. Pregnancy-delayed labour,premature closure
of ductus arterioles,bleeding
7. G6PD deficiency

20. INTERACTION
 Aspirin competes for pp sites and displacesdrug
molecules resulting in toxicity like
warfarin,heparin,naproxen,phenytoin
 Inhibit the tubular scretion of uric acid and
antogonizes the actions of uricosuric agent

21. USES
1. As analgesics(300-400 mg/day in every 6-8 hrs)
2. Fever
3. For anti inflamatory conditions(4-6g/day)
4. Acute rheumatic fever(4-6g/day in 4-6 devided
intrvl)
5. Rheumatoid arthritis
6. To delay labour
7. Prevention of colon cancer
8. PDA
9. Bartter s syndrom
10. Cataract
11. Osteoarthritis

22. PARA-AMINOPHENOL
DERIVATIVES
 Eg;-paracetamol(acetoaminophen)
 It has analgesics,antipyreticand weak anti-
inflamatory properties
 Uses-analgesics in painful condition like
toothache,headache,myalgia
 Used in chronic pulpitis,periodontal
abcess,postextraction –used as combination
 Adverse effect is hepatotoxic

23. PYRAZOLONE DERIVATIVES
 Eg;-phenylbutazone ,azapropazone,metamizol
phenylbutazone
 Good antiinflamatory and uricosuric agent
 More toxic than aspirin
 Uses are rheumatoid arthritis ,ankylosing
spondylatis, gout,muskuloskeltal disorder
 DOSE-100-200mg

24. INDOLE DERIVATIVES
 Eg:-indomethacine,sulindac,etodolac
 It is a potent antiinflamatory agent ,antipyretic,and
good analgesics
 USES-1.rheumatoid arthrits
2.gout
3.closure of PDA
4.eye drops in inflamatoin
5.mouth rinsers in gingival inflammation
 Side effects-CNS,GIT,and hyoersensitive reaction

25. ARYLACETIC ACID
DERIVATIVES
Eg;-diclofenac,aciclofenac,keterolac
 Aciclofenac-long acting ,more gastric
friendly,COX2 selective
 Used for acute musculoskeltal pain,painful dental
lesions,post operatively for relief pain
 Dose-100mg BD
 Diclofenac-analgesics,antipyretics,and anti-
inflamatory agent
 Dose is 50 mg BD and gel are available for
topical applications

26. PROPONOIC ACID
DERIVATIVES
Eg:-Ibuprofen,naproxen,carprofen
Ibuprofen
 Analgesics,antipyretics,anti-inflamtory action
 Acts by inhibits the PGs synthesis
 Uses 1.Contol post surgical pain,
2.in fever
3.impacted tooth removal
4.gout.
 Side effect -nausea ,vomitting,fluid
retention,hypertensive reactionand gastric distress
 Dose -400-800 mg TDS

27.  NAPROXEN
 Mode of action-NSAIDs reduces PGs activity.
 Anti-inflamatory and antipyretic poperty
 Contraindication-allergic pts.
 Precaution-pts. With decreased renal function
and liver function,heart failure or diuretic therapy
can be risk for liver dysfunctionfluid retention
while taking naproxen

28. ANTHRANILIC ACIDS
(FENAMATES)
Eg;-flufenamic acid,mefenamic acid enfenamic acid
 They are anagesics,antipyretic,antiinflamatory
drugs
 Contraindicated in children
 They are not generally preferred
 Diarrhea is common side effect
 Mefenamic acid is used in dysmenorrhea(250-
500mg TDS)
 Mefenamic acid exert peripheral and central
analgesic action

29. OXICAMS
 EG;-piroxicam ,meloxicam
 Piroxicam- Reversible cox inhibitor
 Dose 20 mg OD
 Used for rheumatoid arthritis ,osteoarthritis,painful
dental lesions
 Meloxicam-similar to piroxicam
 Dose-7.5-15 mg once daily

30. ALKANONES
Eg;-nabumetone
 It is antiinflamatory agent with significant efficacy
in rheumatoid arthritis and osteoarthritis
 Less uricogenic proprty
 Used in rheumatoid and osteoarthritis

31. SELECTIVE COX2
INHIBITORS
 Eg;-celocoxib,rofecoxib,valdecoxib,etoricoxib
 Celecoxib 100-200mg
 Rofecoxib 12.5-25mg OD
 Valdecoxib 20mg BD
 Low uricogenic potential
 Pedal edema &rise in BP occurs as result of salt
and water retention due to the inhibition of
consitutive COX2
 Use for long term analgesics in chronic pain

32. PREFERENTIAL COX2
INHIBITORS
 Eg;-nimesulide
 Used for short lasting painful conditions-sinusitis
,dental surgery ,backache , dysmenorrhea
 Side effect-fuminant hepatitis
-bronchospasm
 Dose-50-100mg BD

33. NSAIDS THAT DONOT INHIBIT
PGs SYNTHESIS
 Eg;-metamizol
 analgin.,novalgin
 Potent analgesics and antipyretics
 Dose-500mg 3-4 times a day
 Not recommended in childresns upto 6 years

34. REFERENCE
 TEXT BOOK OF PHARMOCOLOGY
-TRIPATI
 TEXT BOOK OF ORAL AND MAXILLOFACIAL
SURGERY
- SM BALAJI
TEXT BOOK OF DENTAL PHARMACOLOGY
- PADMAJA
UDAYAKUMAR