Non Steroidal Anti Inflammatory Drugs

1. NSAID
By: Mrs. Kalaivani Sathish, M. Pharm.
Assistant Professor – PIMS
Panipat

2. NSAID
• NSAIDs means.. “Non Steroidal Anti
Inflammatory Drugs”
• What is inflammation ?...
– “Response of the body to injurious stimuli”
• Features of Inflammation
1. Heat/fever
2. Swelling
3. Pain
4. Redness
5. Loss of function

3. • NSAIDS addresses mainly FEVER, PAIN AND SWELLING.
• CLASSIFICATION OF NSAIDS
A.Nonselective COX inhibitors (traditional
NSAIDs)
1.Salicylic acid derivatives – Aspirin, Sodium
Salicylate.
2.Para Amino Phenol Derivatives –
Paracetamol
3.Pyrazolone Derivatives – Phenyl butazone

4. 4. Indole Acetic Acid Derivatives –
Indomethacin
5. Aryl Acetic Acid Deivatives – Diclofenac,
Aceclofenac
6. Propionic Acid Derivatives – Ibuprofen,
Fenoprofen.
7. Anthranilic Acid – Mefenamic acid
8. Oxicams – Piroxicam
9. Alkanones - Nabumetone

5. B. Selective COX – 2 Inhibitors
1. Celecoxib
2. Nimesulide

6. MECHANISM OF
ACTION
• During Inflammation, Arachidonic acid
Liberated from Membrane Phospholipid is
converted to prostaglandins (PG’s),
Catalyzed by the enzymes Cyclo –
Oxygenase (COX).
• These NSAID’s inhibits the PG’s synthesis
by inhibiting the enzyme COX.
• There are 2 forms of COX (COX – 1 &
COX – 2)

7. • COX – 1 is found in most of the normal
cells. It is involved in maintaining Tissue
Homeostasis.
• COX – 2 is induced in the inflammatory
cells, by cytokinin and other mediators of
inflammation.
• Most NSAID’s inhibits both COX – 1 and
COX – 2.

8. Membrane Phospholipids
Phospholipase A2
Arachidonic Acid
COX LOX
PG’S Leukotrines

9. SALICYLATES
• They are salts of salicylic acids. e.g. Methyl
Salicylate.
• Pharmacological Action
• Analgesia – Aspirin is a good analgesics and
relieves pain of inflammatory origin.
Aspirin inhibits PG’s synthesis and there by
acts as analgesics. The pain is relieved w/o
euphoria and hypnosis.

10. SALICYLATES
• Antipyretic Action – In fever, salicylate
reduce the temp to normal level. In normal
individual there is no change in temp.
Aspirin inhibits PG’s synthesis in the
hypothalamus and reset the thermostat at
the normal level.
* Anti Inflammatory Action – PG’s present in
inflammatory tissues are responsible for
edema, erythema and Pain. Aspirin acts
asanti inflamatory agents.

11. SALICYLATES
• Respiration – Saliyclates increase
consumption of O2 by skeletal muscle, as a
result there is an increased CO2
Production, this stimulates Respiration. In
toxic doses the respiratory centre is
depressed leading to respiratory failure.
• Acid – Base Balance – Salicylate normal
dose ph becomes alkaline. In toxic dose ph
decreases.

12. • Metabolic Effect – it enhances the cellular
metabolism as a result more O2 is used and
More Co2 is produced.
• GIT – Aspirin is a gastric irritant, it
produce epigastric distress, nausea and
vomiting.
• CVS – in normal dose CVS effect are seen.
Toxic dose it depresses the circulation
• Immunological Effect – in higher dose
salicylate suppress the several antigen –
antibody reaction and antibody production.

13. • Uric Acid Excretion – Aspirin increases the
plasma urate level by urate retention.
• Blood – Aspirin interferes with platelet
aggregation and prolongs the bleeding time.
• Local Effects – Salicylates when applied
locally, it is a keratolytic.
(A substance that promotes the softening and peelin
g of epidermis). It also has mild antiseptic and
fungistatic property.

14. PHARMAKOKINETICS
Absorption (Stomach & Small Intestine)
Bounds to Plasma Protein
Metabolized in Liver
Excretion by urine

15. ADVERSE EFFECTS
• GIT – Nausea, Vomiting, Peptic Ulcer, blood loss
in stool.
• CNS – Headache, Confusion, Allergic Reactions,
Rashes, Photosensitivity, Urticaria
• Respiratory System – Bronchial Asthma
• Hemolysis, Nephrotoxicity, Hepatotoxicity
• Reye’s syndrome – A rare condition in children
which causes swelling in brain and Liver.
• Pregnancy and Labour – Delays onset of labour,
Portal hypertension, increase Post Partum
Bleeding

16. • Salicylism – Higher dose given for a
long time in the treatment of
Rheumatoid arthritis may cause
chronic salicylate intoxication.
• Treatment : Symptoms & Signs
– Dehydration, Hyperpyrexia, GI
Irritation, Vomiting, Tremor, Delirium,
Convulsion, Coma and Death due to
respiratory failure and CV Collapse.

17. • Treatment includes
– Gastric Lavage to eliminate unabsorbed drugs
– IV Fluids to correct acid base imbalance and
dehydration
– Cold water sponge to bring down elevated body
temp.
– Blood transfusion and Vitamin – K are
administerd for haemorrhagic complications
– IV Fluids should contain (Na, K, HCO3 & Glucose).
– Blood ph should be monitored.
– In severe cases administer diuretics.

18. PRECAUTIONS & CONTRA
INDICATIONS
• Peptic ulcer, Liver diseases, Viral fever in
children's are contra Indicate the use of
aspirin and salicilate.
• During Pregnancy aspirin should be
avoided.
• NSAID should be stopped one week before
surgery due to anti platelet effect.

19. USES
• Analgesics – Headache, Backache, Myalgia,
Dysmennorhea, arthralgia.
• Fever – used as antipyretic
• Inflammation – Effective in arthritis and
fibromyositis
• Acute Rheumatic Fever – Aspirin is used very
effectively.
• Rheumatoid Arthritis – Aspirin release pain,
reduces swelling and redness of joints in RA.
• Osteoarthritis
• Post Myocardial Infraction & Post Stroke

20. USES
• Inflammatory Bowel Disease
• 0ther Uses
• To Delay labour,
• Prevention of colon cancer.
• Eclampsia
• Locally used as Keratolytic and Fungistatic and
Mild antiseptic

21. PARAMINO PHENOL
DERIVATIVES
• Paracetamol
• it has analgesics, good anti pyretic and weak anti
inflammatory properties.
• Adverse Effects – Nausea, Rashes, when large dose
taken acute paracetamol poisoning occurs.
• Symptoms – Nausea, Vomiting, Anorexia,
abdominal pain during first 24 Hrs,
Nephrotoxicity and cause severe Hepatic damage.

22. • Treatment for acute paracetamol poisoning:
– Gastric Lavage, Activated charcoal prevents
further absorption.
– Anti dote is N – Acetyl cysteine is more
effective, when given early.
Uses :
Analgesics in painful condition like, tooth ache,
headache and myalgia.
Antipyretic

24. Pyrazolone Derivatives – Phenyl
butazone
• Has good anti inflammatory activity.
• It is more potent, but has poor analgesic
and anti pyretic effect.
• It is a uricosuric agent.

25. PHARMACOKINETICS
• Oral absorption (Complete)
98 % bound to plasma protein
Metabolized in liver
• Excreted in Kidney

26. • Dose : 100 – 200 mg Bd.
• Adverse Effects: it is more toxic than
aspirin.
• Nausea, Vomiting, Epigastric Pain,
Dyspepsia, Peptic ulcer and Diarrhoea.
Anemia etc.
• Uses: Rheumatoid Arthritis, Ankylosing
spondolytis. Osteo arthritis, Gout and
other musculo skeletal disorders.

27. Indole Acetic Acid Derivatives –
Indomethacin
• It is a potent anti inflammatory agent, anti pyretic
and good analgesic.
• It is well absorbed, 90 % bound to plasma protein.
• Dose : 25 to 50 mg Bd, tds.
• Adverse Effects: Nausea, Vomiting, GI Bleeding
and Diarrhoea and peptic ulcer.
• CNS Effect: Headache, Ataxia, Confusion,
Depression and psychosis, Hypersensitivity etc.
• Uses: Rheumatoid arthritis, Gout, Ankylosing
spondolyits etc.

28. Aryl Acetic Acid Deivatives –
Diclofenac, Aceclofenac
• It is an analgesic and anti pyretic and anti
inflammatory agent. With mild adverse
side effects.
• Uses: Rheumatoid arthritis, Osteoarthritis,
Musculo Skeletal Pain, in eye to reduce
occular inflammation.
• Dose: 50 mg bd or tds

29. Propionic Acid Derivatives –
Ibuprofen
• It is better tolerated than aspirin. It has an
analgesic, anti pyretic and anti
inflammatory action.

30. PHARMACOKINETICS
• Oral absorption (Complete)
90 % bound to plasma protein
Crosses BBB
Metabolized in Liver
Excreted in Kidney & Bile

31. Anthranilic Acid – Fenamates
• It has an analgesic, anti pyretic and anti
inflammatory action.less efficay and more
toxic.
• Adverse Effects – Similar to Aspirin.
• Uses – Analgesics in Myalgia. Mefenamic
acid is used in dysmenorrhoea.
• Dose – 250 – 500 Mg tds.

32. Oxicams – Piroxicam
• It is long acting good analgesic, anti
pyretic and anti inflammatory action.
• Dose: 20 mg.
• Uses: Rheumatoid arthritis, Osteoarthritis.
Ankylosing spondolytis. Musculo Skeletal
Pain and Post Operative pain.

33. Alkanones - Nabumetone
• good analgesic, anti pyretic and anti
inflammatory action. It is good for
osteoarthritis.

34. Selective COX – 2 Inhibitors
Celecoxib
• It can cause HT and edema in CV
Problem patient
• It is used for post operative pain and
dysmennorhea and osteoarthritis and
rheumatoid arthrits.
• Dose – 100 – 200 Mg.

35. Nursing Implications
• BP Checked regularly
• Regulate Sodium intake
• Body weight is checked everyday