7/27/2019 NSAIDS (2)

1/47

PPT

on

Non steroidal anti- inflammatory drugs.

NSAIDS

by

Dr.Saloni Gupta ,Dr. Prashant ,MD

drprashantw@gmail.com

www.pharmacology4students.com

mailto:drprashantw@gmail.commailto:drprashantw@gmail.com

7/27/2019 NSAIDS (2)

2/47

INTRODUCTION

These are weaker analgesis and

non narcotic in nature i.e. do notdepress CNS.

7/27/2019 NSAIDS (2)

3/47

CLASSIFICATION

1.Nonselective cox inhibitors-

Salicylates-aspirin,diflunisal

Pyrazolone derivatives-

phenylbutazone,

oxyphenbutazone

7/27/2019 NSAIDS (2)

4/47

Indole derivatives-

indomethacin,sulindac

Proionic acid derivatives-

ibuprofen,naproxen,ketoprofen

Anthranilic acid derivatives-

mephenamic acid

Aryl acetic acid derivatives-

diclofenac

7/27/2019 NSAIDS (2)

5/47

Oxicam derivatives-

piroxicam,tenoxicam

Pyrrolo pyrrole derivatives-

ketorolac

2.Prefential COX-2 inhibitors-

nimesulide,meloxicam,nabumetone

7/27/2019 NSAIDS (2)

6/47

3.Selective COX-2 inhibitors-

celecoxib, rofecoxib, valdecoxib

4.Analgesic antipyretic with poor

antiinflammatory action-

Paraaminophenol derivatives-

paracetamol

7/27/2019 NSAIDS (2)

7/47

Pyrazolone derivatives-metamizol,

propiphenzone

Benzoxazocine derivatives- nefopam

7/27/2019 NSAIDS (2)

8/47

MECHANISMOF

ACTION

Inhibits COX due to which there isdecrease in synthesis of

prostaglandin, thromboxane.

Due to this there is analgesic,

antipyretic, anti inflammatory action

7/27/2019 NSAIDS (2)

9/47

It is acetylsalicylic acid. it is one of the oldest analgesic.

it is converted into salicylic acid inour body

ASPIRIN

7/27/2019 NSAIDS (2)

10/47

PHARMACOLOGICAL

ACTION

1.Analgesic action

Relieves inflamation, tissue injury,

integumental connective tissue

No effect on visceral pain, ishaemic

pain

7/27/2019 NSAIDS (2)

11/47

2.Antipyretic

decrease fever by sweating and

cutaneous dilatation

3.Antiinflammatory

Decrease pain, tenderness,

swelling. Redness, leucocysticinfilteration

7/27/2019 NSAIDS (2)

12/47

4.Antiplatlet action

Inhibits platlet aggregation and

decreases thromboxaneA2

synthesis

5.Metabolic action

Decreases cell metabolism sodecrease utilization of glucose and

blood sugar therefore there is

7/27/2019 NSAIDS (2)

13/47

decrease in liver glycogen

6.Respiratory action

By periphral action it increases CO2

production

And by central action increases

sensitivity of respiratory center

7/27/2019 NSAIDS (2)

14/47

7.Acid base balance

Causes compensatory respiratory

alkalosis

8.GIT

Irritates mucosa due to which

pain in epigastric region

Stimulates CTZ which causes

7/27/2019 NSAIDS (2)

15/47

7/27/2019 NSAIDS (2)

16/47

PHARMACOKINETICS

absorb from stomach and small

intestine

alkalization of urine tend to

increase elimination of aspirin

freely crooses placenta

7/27/2019 NSAIDS (2)

17/47

7/27/2019 NSAIDS (2)

18/47

2. Hypersensitivity reaction- rashes,

dermatitis, angiodema, asthma,rhinitis, urticaria, rarely anaphylactic

shock

3. Acute salicylic poisoning- caused

by anti inflammatory dose

Causes rhinitis, vertigo, dizziness,

head ache, impairment in hearing

7/27/2019 NSAIDS (2)

19/47

Blurring of vision, mental confusion,

exitement, electrolyte imbalance,sound in ear

4.Ryes syndrome- occurs inchildren

Causes hepatic encephalopathyduring viral influenza

7/27/2019 NSAIDS (2)

20/47

INDICATION

Post MI and post stroke patient

As an analgesic in bodyache, jointpain, tooth ache, neuralgic pain,

dysmennorhea

As an antipyretic

As an antiinflammatory in

7/27/2019 NSAIDS (2)

21/47

Rheumatic arthritis, osteoarthritis,

acute rheumatic fever

Potential use in patent ductus

arteriosus. Premature labour,

pregnancy induce HTN

7/27/2019 NSAIDS (2)

22/47

CONTRAINDICATION

Hypersensitivity

Peptic ulcer

Chronic liver disease

During normal pregnancy at full

time

7/27/2019 NSAIDS (2)

23/47

Avoided 1 week before surgery

Patient having bleeding disorder

7/27/2019 NSAIDS (2)

24/47

NIMESULIDE

Relatively weak inhibitor of PGsynthesis

Used primarily for short long lasting

painful inflamatory conditions like

sport injuries, sinusitis, dentalsurgery, post operative pain and

fever

7/27/2019 NSAIDS (2)

25/47

Adverse effects are epigastralgia,

heart burn, nausea, loose motions,

rashes, pruritis, somnolence,

dizziness.

7/27/2019 NSAIDS (2)

26/47

PARACETAMOL

It is a deethylated active metabolite

of phenacetin

ACTIONS

It raises pain threshold but has weakperipheral antiinflammatory

component

7/27/2019 NSAIDS (2)

27/47

Poor inhibitor of PG synthesis

PHARMACOKINETICS

Well absorbed orally

Excreted rapidly in urine

Plasma t1\2 is 2-3 hours

Effect of oral dose last for 3-5hrs

7/27/2019 NSAIDS (2)

28/47

ADVERSE EFFECTS

It is well tolerated, nausea and

rashes occur occasionally

Analgesic nephropathy occurs after

years of heavy dose

USES

Commonly use as an analgesic for

7/27/2019 NSAIDS (2)

29/47

headache, musculoskeletal pain,

dysmenorrheaMuch safer than aspirin as does not

cause any hypersensitivity reactionIt is the first choice for osteoarthritis

Best drug to be used as antipyretic

ACUTE PARACETAMOL

7/27/2019 NSAIDS (2)

30/47

ACUTE PARACETAMOL

POISONING

Occurs specially in small children

Early manifestations are nausea,vomiting, abdominal pain and liver

tenderness, jaundice starts after 2

days

Mechanism of toxicity

N-acetyl-p-benzoquinoneimine is a

7/27/2019 NSAIDS (2)

31/47

highly reactive arylating minor

metabolte of paracetamol which isdetoxified by congugation with

glutathione

this binds covalently to protiens in

liver cells causing necrosis

So paracetamol is not recommended

in premature infants for fear of

hepatotoxicity

7/27/2019 NSAIDS (2)

32/47

Treatment

Early vomiting should be induced

Gastric lavage should be done

Activated charcoal is given orally

Nacetylcysteine should be infused

i.v. over 15min

7/27/2019 NSAIDS (2)

33/47

DICLOFENAC

Potent analgesic antipyretic and

antiinflammatory drug

May also inhibit lipoxygenase

Plasma half life is 2-3hours

7/27/2019 NSAIDS (2)

34/47

INDOMETHACIN

As an analgesic mainly relieves

tissue injury and inflammatory pain

Adverse effects- aggravate pre

existing renal disease and induce

mental confusion

Plasma half life is 2-3hours

7/27/2019 NSAIDS (2)

35/47

7/27/2019 NSAIDS (2)

36/47

PHENYLBUTAZONE

Uricosuric by virtue of a metabolite

which inhibits renal tubular

reabsorption of uric acid

Plasma half life is 50-100hours

Clinical use is limited due to bone

marrow depression

7/27/2019 NSAIDS (2)

37/47

OXYPHENBUTASONE

It is a biotransformation product of

phenylbutazone

Clinical use is limited because is

causes bone marrow depression

Plasma half life is 10-14hours

7/27/2019 NSAIDS (2)

38/47

PIROXICAM

long acting potent antiinflammatory,

antipyretic and analgesic drug

It has enterohepatic circulation

Plasma half life 45hours

7/27/2019 NSAIDS (2)

39/47

KETOROLAC

Potent analgesic and modest

antiinflammatory agent

In post operative pain efficacy is

equal to morphine

Used for short term management of

moderate pain

7/27/2019 NSAIDS (2)

40/47

IBUPROFEN

Better tolerated than aspirin

Drug of choice for rheumatoidarthritis

Plasma half life is 2-3 hours

7/27/2019 NSAIDS (2)

41/47

NAPROXEN

Better tolerated than aspirin

Second choice after ibuprofen inthe treatment of rheumatoid

arthritis

Plasma half life is 12-14hours

7/27/2019 NSAIDS (2)

42/47

KETOPROFEN

Inhibits both cycloxygenase and

lipoxygenase

MEPHENAMIC ACID

Lower efficacy as analgesic,antipyretic and antinflammatory

agent

7/27/2019 NSAIDS (2)

43/47

NEFOPAM

Non opoid analgesic

It does not inhibit prostaglandin

synthesis

Useful to relieve traumatic and

musculoskeletal pain

Side effects are blurred vision,

tachycardia,urinary retention

7/27/2019 NSAIDS (2)

44/47

TOPICAL NSAIDS

Preparations are being used forosteoarthritis, sprains, sports

injuries, tenosinovitis, backache,and other forms of soft tissue

rheumatism

the drug would penetrate to the

subjacent tissues attaining high

concentrations in the affected

7/27/2019 NSAIDS (2)

45/47

muscles or joint while maintaining

low blood levelsTopical NSAIDs preparations are

slow taking~10 times longer time to

attain peak concentration compared

to oral dosing.

Better response have generally

been obtained in short lasting

musculo-skeletal pain.

7/27/2019 NSAIDS (2)

46/47

7/27/2019 NSAIDS (2)

47/47