The presentation gives information about NSAID's.

2. Introduction
Non-steroidal anti-inflammatory drugs is a class of
analgesic medication that reduces pain, fever and
inflammation.
NSAIDs are cleared from the blood stream by the
kidney thus, precautions should be taken to avoid
kidney damage and disease when NSAIDs are taken
over an extended period.
Side effects of NSAIDs include stomach ulcers and
kidney and platelet dysfunction.
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3. Classification of NSAID’S
The NSAID’S are classified into the following
categories-
Non selective COX Inhibitors
Preferential COX Inhibitors
Selective COX Inhibitors
Analgesic anti pyretic and poor inflammatory
drugs
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4. A] Non selective COX Inhibitors
 Salicylates – Aspirin(acetylsalicylic acid), Diflunisal,
Salicylic acid and its salt, Salsalate.
 Pyrazolone derivatives – Phenyl butazone ,
Oxyphenbutazone .
 Indole derivatives- Indomethacin, Sulindac
 Propionic acid derivatives –
Ibuprofen,Dexibuprofen,Naproxen,Fenoprofen,
Ketoprofen,Dexketoprofen, Flurbiprofen,
Oxaprozin,Loxoprofen
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5. A] Non selective COX Inhibitors
Anthranilic acid derivatives - Mefenamic acid
Meclofenamic acid, Flufenamic acid, Tolfenamic acid
Aryl acetic acid derivatives- Etodolac, Ketorolac,
Diclofenac
Oxicam derivatives- Pyroxicam, Tenoxicam
Pyrrolo- pyrrole derivatives- Ketorolac
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6. B] Preferential COX 2 Inhibitors
Nemesulide
Meloxicam
Nabumetone
C] Selective COX 2 Inhibitors
Celecoxib
Rafecoxib
Valdecoxib
D] Analgesic anti pyretic and poor inflammatory drugs
 Para aminophenol derivative- Paracetamol
 Pyrazolone derivatives - metamizol, propiphenazone
 Benzoxazocine derivatives- Nefopam
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7. Mechanism of action of NSAID’S
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8. Medicinal Uses
NSAIDs are generally used for the symptomatic relief of the following
conditions:
Osteoarthritis
Rheumatoid arthritis
Mild-to-moderate pain due to inflammation and tissue injury
Low back pain
Inflammatory arthropathies Tennis elbow
Headache
Migraine
Acute gout
Muscle stiffness and pain due to Parkinson's disease
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9. Aspirin
It is a non selective COX inhibitor.
Aspirin is a acetylsalicylic acid converts to salicylic acid in the
body, which I responsible for action.
Aspirin is the weaker analgesic than morphine.
It effectively relives inflammation, tissue injury, integumental
pain, but it is ineffective in various ischemic pain.
No sedation, tolerance and physical dependence is produced.
Acetyl salicylic acid

10. Aspirin is the weaker analgesic than morphine.
Aspirin600mg< codeine 60mg<morphine 6mg
Anti- inflammatory action of aspirin is exerted at higher
doses 3-6gm/day or 100mg/kg/day.
Aspirin and released salicylic acid cause irritation in gastric
mucosa and can cause vomiting & nausea.
Aspirin at higher doses renal tubular excretion of urate.
Aspirin even at small doses inhibits TXA2 synthesis of
platelets.
Long term intake of higher doses can cause the depletion
in clotting factors in the blood.
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11. Pharmacokinetics
Aspirin is absorbed from small intestine.
Acetylsalicylic acid is quickly absorbed through the cell
membrane in the acidic conditions of the stomach.
As much as 80% of therapeutic doses of salicylic acid
is metabolized in the liver.
It slowly acts on brain but freely crosses the placenta.
The metabolites are excreted by glomerular filtration
as well as tubular secretion.
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12. Mechanism of Action
Essential fatty acids
Membrane phospholipids
Arachidonic acid
Prostaglandin(PG)
{doesn't form due to the action of aspirin}
Prostacycline Thromboxanes Prostaglandin
{Doesn’t form}
Aspirin
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13. Pharmacological actions of aspirin
Analgesic - Useful to treat mild to moderate pain.
In the treatment of osteoarthritis.
Antipyretic - In the treatment of fever.
To treat rheumatoid arthritis.
Have anticoagulant action.
Anti – inflammatory action- for acute and chronic
inflammation.
Thromboembolic disorders.
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14. Adverse effects
1) Gastro intestinal tract:
vomiting,
diarrhea,
constipation,
epigastric pain,
dyspepsia(impaired digestion),
bleeding,
ulceration
2) Hypersensitivity reactions:
Edema,
rash,
bronchospasm ,
Anaphylactic shock may be life threatening
3) CNS
Nausea,
Headache
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15. Drug Interactions
Drug Interaction result
Diuretics Effect of diuretics
Beta blockers Antihypertensive effects
ACE Inhibitors blood pressure
Sulphonyl Urea's hypoglycemic risk
Spironolactone Effect
Alcohol GI bleeding
Anticoagulant Action
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16. Ibuprofen
It is a Propionic acid derivative.
It have analgesic, antipyretic & anti inflammatory effects.
Compared to other NSAIDs, it may have fewer side effects.
Ibuprofen was discovered in 1961 by Stewart Adams and
initially marketed as Brufen.
 In 2016, it was the 35th-most prescribed medication in
the United States, with more than 21 million prescriptions.
2-(4-Isobutylphenyl)Propionic acid

17. At high doses it may cause heart attack.
 Ibuprofen can also worsen asthma
 While it is unclear if it is safe in early pregnancy
 It appears to be harmful in later pregnancy and
therefore is not recommended.
 It works by inhibiting the production
of prostaglandins by decreasing the activity of the
enzyme cyclo-oxygenase.
the lysine salt of ibuprofen called Ibuprofen
lysinate is used because it is more water-soluble.
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18. Pharmacokinetics
Well absorbed orally.
Highly bound to plasma protein(90-99%).
Its use with the anticoagulants must be avoided as
they interact with it.
It crosses BBB as well as the placental membrane.
It is metabolized in the liver by the process of
hydroxylation & glucuronide conjugation.
Excreted through urine and bile.
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19. Mechanism of action
It is the non-selective, reversible inhibition of the
cyclo-oxygenase enzymes COX-1 and COX-2 (coded
for by PTGS1 and PTGS2, respectively).
Ibuprofen exerts its anti-inflammatory and
analgesic effects through inhibition of both COX
isoforms.
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20. Adverse Effects
1) Gastro intestinal tract:
Stomach pain
Acidity
Constipation
Indigestion
Vomiting
Ulcers
2) CNS
Nausea
Dizziness
Blurring of vision
Depression
3) Hypersensitivity
Rashes
Itching
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21. Drug Interactions
Pharmacological actions
 Act as analgesic.
Act as antipyretic- used to treat fever.
 Weak anti- inflammatory action then other NSAID’s.
Used to treat rheumatoid arthritis, osteoarthritis, musculoskeletal
disorders.
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Drug Interaction Result
Ibuprofen + Phenytoin Action of phenytoin
Ibuprofen + sulphonamide Action of sulphonamide
Ibuprofen + Salicylates Action of salicylates

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