NON-STEROIDAL

ANTI-INFLAMMATORY
DRUGS
PRESENTOR
SUMOLLY ANAK DAVID
22 JULY 2009
 INTRODUCTION
Pain is an unpleasant sensation that is
caused by actual or perceived injury to body
tissues and produces physical and emotional
reactions.
Acute pain is of sudden onset and is usually
the result of a clearly defined cause such as
an injury
Chronic pain persists for weeks or months
and is usually associated with an underlying
condition
Non Steroidal Anti-Inflammatory Drugs
(NSAIDs) are medications which, as well as
 MECHANISM OF ACTION
♠ Prostaglandin are chemicals released by
the body at the site of injury
♠ They are responsible for producing
inflammation and pain following tissue
damage & in immune response
♠ NSAIDs blocks the production of PG &
thus reduce pain and inflammation.
♣ Cyclooxygenase inhibition

– COX-1 is expressed in most tissues,

described as a "housekeeping" enzyme,
regulating normal cellular processes
(gastric cytoprotection, vascular
homeostasis, platelet aggregation &
kidney function), stimulated by
hormones or growth factors.
– COX-2 is usually undetectable in most
tissues; its expression is increased
during states of inflammation.
 NON SELECTIVE
NSAIDs
♣ Salycylates:
– Acetylsalicylic acid (aspirin)
♣ Fenamates:
– Mefenamic acid
♣ Acetic acid:
– Diclofenac
– Indomethacin
♣ Propionic acid:
– Ibuprofen -Ketoprofen -
 COX-2 SELECTIVE

♠ Celecoxib
♠ Etoricoxib
♠ Valdecoxib
♠ Parecoxib
♠ Rofecoxib
♣ Developed in attempt to inhibit prostacyclin
synthesis by the COX-2 isoenzyme without
affecting the of he constitutively active
“housekeeping” COX-1 isoenzyme found in
GIT, kidneys & platelets.
♣ Have analgesic, antipyretic &
antiinflammatory effect with improved
gastrointestinal safety, no impact on platelet
aggregation
♣ Increased incidence of edema &
hypertension
♣ The principal benefit with the selective COX-
2 inhibitors is the production of comparable
analgesia and antiinflammatory effects to
 PHARMACOKINETIC/
DYNAMIC
All NSAIDs are
Absorbed completely,
have negligible first-pass
hepatic metabolism,
tightly bound to albumin,
&
have small
volumes of distribution
 INDICATION
• NSAIDs are used primarily to treat inflammation,
mild to moderate pain, and fever. Specific uses
include the treatment of headaches, arthritis,
sports injuries, and menstrual cramps.
• Aspirin (also an NSAID) is used to inhibit the
clotting of blood and prevent strokes and heart
attacks in individuals at high risk.
• Migraine
• Dental pain & post-operative pain
 SIDE EFFECT/ ADR
• Gastrointestinal toxicity, including
dyspepsia, peptic ulcer disease, and
bleeding
• Development of acute renal failure
due to renal vasoconstriction
• Hepatotoxicity , Elevations of serum
aminotransferases (transaminases)
• Hypersensitivity reactions: rashes,
angioedema, bronchospasm.
 DRUG INTERACTION

Agents Description of interaction

ACEi ↑ risk of renal impairment
NSAIDs, ↑ side effect
aspirin
Anticoagulant Enhance anticoagulant effect

Corticosteroid ↑ risk of GI bleeding &

s ulceration
Diuretics Risk of NSAIDs nephrotoxicity
is increased by diuretics
 RISK OF GI TOXICITY

• Duration of therapy.
• Increasing age, particularly >60
• Higher NSAID dose
• A past history of gastroduodenal
toxicity from NSAIDs or peptic ulcer
disease
• Concurrent use of glucocorticoids,
anticoagulants, bisphosphonates, or
other NSAIDs
 NSAID & USUAL DOSAGE
NSAIDs USUAL DOSAGE
Aspirin 2.4-6 g/24h in 4-5 divided doses
Ibuprofen OTC:200-400 mg QID; Rx: 400-800 mg;
max 3200 mg/24h
Naproxen 250, 375, 500 mg BID; 225 mg BID
Ketoprofen 75 mg TDS
Indomethacin 25, 50 mg TDS-QID
Diclofenac 50, 75 mg BID (50 mg BID)
Mefeamic acid 250 mg QID
Celebrex 100, 200 mg a day
Etoricoxib 60mg daily (OA)
9omg daily (RA)
120mg daily for max of 8 days (acute pain
in gouty arthritis)
CONTRAINDICATION
• Allergy to aspirin or any NSAID
• Aspirin should not be used under
the age of 16 years , elderly
• During pregnancy & During breast
feeding
• On blood thinning agents
• Suffering from a defect of the blood
clotting system (coagulation)
• Active peptic ulcer
♠ Care is needed if you have:
– Asthma
– Kidney impairment
– Heart impairment
– Liver impairment

♣ COX2 selectives are

contraindicated in
IHD, cerebrovascular disease,
peripheral arterial disease &
CHF.
Choosing an anti-
inflammatory
 CONCLUSION
♣ Before treatment is started,the prescriber
should weigh efficacy against possible side effect.
♣ Differences in antiinflammatory action between
NSAIDs are small, but individual response and
tolerance varies.
♣ The effect of non-aspirin NSAID on MI protection is
of lower significant compared to aspirin alone, yet
the use of both concurrently will increase the side
effect without producing additional benefit on MI.
So non-aspirin NSAIDs should not be considered
alternatives for aspirin for prevention .
 REFERENCES
• http://www.uptodate.com
• Katzung, B.G. 2004. Nonsteroidal antiiflammatory Drugs, DMARDs, Nonopioid
Analgesics & Drugs Used in Gouts. Basic & Clinical Pharmacology.
• Dipiro, J.T., Wells, B.G., Schwinghammer, T.L. & Hamilton, C.W. 2006. Pain
management. Pharmacotherapy Handbook. 6th Edtion.
• http://www.medinfo.co.uk/drugs/nsaids.html
• Pain Management – Pain Medications and Over-The-Counter (OTC) Drugs
• Kimmel et.al. 2004. The Effects of Nonselective Non-Aspirin Non-Steroidal
Anti-Inflammatory Medications on the Risk of Nonfatal Myocardial Infarction
and Their Interaction With Aspirin. Journal of the American College of
Cardiology. Vol. 43, No. 6, 2004.
• British National Formulary. 50th edition. 2005.