NSAIDS ppt.ppt analgesics used in humans

NSAIDs - drugs, MOA, uses, ADR

1. NON-STEROIDAL ANTI-
INFLAMMATORY DRUGS

2. Non-Selective COXs
Inhibitor
Selective COX2
Inhibitor

3. NON- SLECTIVE -NON -STEROIDAL
ANTI-INFLAMMATORY DRUGS
Group of drugs that sharing the capacity to
induce the following pharmacological
actions :
Analgesic
Antipyretic
Anti-inflammatory
Anti-platelet
Effect on the kidney function

4. ANALGESIC
Drug that relieve pain.

5. ANTIPYRETIC
Drug that lower
the elevated body
temperature to
normal.

6. PHARMACOKINETIC

9. GENERAL MECHANISM OF
ACTION OF NS-NSAIDS
Reversible inhibition of both COX-1 &
COX-2 enzymes

EXCEPT Aspirin is the only NS-NSAID that
irreversible inhibitor of both enzymes
Resulting in inhibition of the synthesis of
prostaglandins & thromboxane A2

10. MECHANISM OF ACTION

11. ( CONTINUE)

12. EFFECT ON THE KIDNEY
Inhibition of both COX-1& COX-2 enzymes
(mainly COX-2)
( inhibit synthesis of PGE2 & PGI2 that are
responsible for maintaining renal blood flow)
Salt &water retention & edema of lower limbs
Hyperkalemia
Interstitial nephritis



13. Antipyretic
Analgesic ( Which type of
pain?)
Dull, mild , moderate
e.g. Headache, Migraine,
Dental pain ,common cold

14. CONTINUE
Anti-inflammatory
Rheumatic / Rheumatoid
arthritis / myositis or other
forms of inflammatory
conditions.
Dysmenorrhea

15. ADVERSE EFFECTS SHARED
BY NS-NSAIDS
GIT upsets ( nausea, vomiting)
GIT bleeding & ulceration
Bleeding
Hypersensitivity reaction
Inhibition of uterine
contraction
Salt & water retention

17. CLINICAL USES OF ASPIRIN
Acute rheumatic fever
Low doses used as cardioprotective
to reduce the incidence of myocardial
infarction & unstable angina

19. ( CONTINUE)
Large doses ( 5gm)used to treat
chronic gouty arthritis
Chronic use of small doses of aspirin
used as protective to reduce the
incidence of colorectal cancer

20. Adverse Effects Related to
(A) Therapeutic Doses Of Aspirin
Nausea & vomiting
Hypersensitivity
( Aspirin asthma)
Acute Gouty arthritis
Reye's syndrome

21. ( B) LARGE DOSES OR
CHRONIC USE OF ASPIRIN
Salicylism ( ringing of ear( tinnitus) ,
vertigo)
Hyperthermia
Gastric ulceration & bleeding
Respiratory depression

22. ADVERSE EFFECTS RELATED TO
HIGH DOSES

23. CONTRAINDICATIONS
Peptic ulcer
Pregnancy
Hemophilic patients
Patients taking anticoagulants
Children with viral infections
Gout ( small doses )

24. PARACETAMOL
IS commonly used as
analgesic antipyretic

25. CONDITIONS IN WHICH
PARACETAMOL IS A
SUITABLE DRUG

26. In patients with :
Peptic or gastric ulcers.
Bleeding tendency.
Allergy to aspirin.
Viral infections especially
in children .
o During Pregnancy.

27. ADVERSE EFFECTS
Due to its active metabolite
( N-acetyl-p-benzoquinone)
Therapeutic doses
elevate liver enzymes
Chronic administration causes kidney
failure ( necrosis)
Large doses cause
Acute toxicity :{liver failure ( necrosis) }
Treatment Of acute toxicity
by : N- acetylcysteine ( SH- donor) to
neutralize the toxic metabolite

28. DICLOFENAC
( accumulate in synovial fluid)
Clinical uses
oRheumatoid arthritis , osteoarthritis
& ankylosing spondylitis
oAnalgesic
oAntipyretic
oAcute gouty arthritis
oLocally to prevent post-opthalmic
inflammation

29. PREPARATIONS OF DICLOFENAC
Oral
Oral with misoprostol to decrease
upper gastrointestinal ulceration .
0.1% opthalmic ( eye drops) to
decrease postoperative opthalmic
inflammation.
A topical gel 3% .
Rectal suppository

30. CONTINUE
Oral mouth wash.
Intramuscular preparations.

31. SELECTIVE COX-2
INHIBITORS
General advantages :
oPotent anti-inflammatory
oAntipyretic & analgesic
oLower incidence of gastric
upset
o( recommneded in patients
with a history of gastric
ulceration )

32. CONTINUE
No effect on platelet aggregation
( have no inhibitory effect on
(COX-1 enzyme) so can be
given in hemophilic patients

33. GENERAL ADVERSE
EFFECTS
Renal toxicity
Dyspepsia & heartburn
Allergy
Increase incidence of myocardial
infarction
( lack cardioprotective effect of
NS-NSAIDs as they have no
effect on COX-1 enzyme)

34. GENERAL CLINICAL USES
Commonly used as
antiinflammatory drugs
Rheumatoid arthritis
Osteoarthritis
Acute gouty arthritis
Acute musculoskeletal pain
Ankylosing spondylitis
Dysmenorrhea

35. EXAMPLE :CELECOXIB
Half-life 11 hours
(twice/day)
Food decrease its
absorption
Highly bound to plasma
proteins

36. CLINICAL USES & ADVERSE
EFFECTS
Discussed before with general uses and
general adverse effects of selective COX-2
inhibitors

37. DRUG INTERACTIONS

With warfarin ( anticoagulant )
celecoxib inhibits warfarin metabolism so it
potentiates its action resulting in bleeding.