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PPT
on
Non steroidal anti- inflammatory drugs.
NSAIDS
by
Dr.Saloni Gupta ,Dr. Prashant ,MD
www.pharmacology4students.com
mailto:[email protected]:[email protected]7/27/2019 NSAIDS (2)
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INTRODUCTION
These are weaker analgesis and
non narcotic in nature i.e. do notdepress CNS.
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CLASSIFICATION
1.Nonselective cox inhibitors-
Salicylates-aspirin,diflunisal
Pyrazolone derivatives-
phenylbutazone,
oxyphenbutazone
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Indole derivatives-
indomethacin,sulindac
Proionic acid derivatives-
ibuprofen,naproxen,ketoprofen
Anthranilic acid derivatives-
mephenamic acid
Aryl acetic acid derivatives-
diclofenac
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Oxicam derivatives-
piroxicam,tenoxicam
Pyrrolo pyrrole derivatives-
ketorolac
2.Prefential COX-2 inhibitors-
nimesulide,meloxicam,nabumetone
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3.Selective COX-2 inhibitors-
celecoxib, rofecoxib, valdecoxib
4.Analgesic antipyretic with poor
antiinflammatory action-
Paraaminophenol derivatives-
paracetamol
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Pyrazolone derivatives-metamizol,
propiphenzone
Benzoxazocine derivatives- nefopam
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MECHANISMOF
ACTION
Inhibits COX due to which there isdecrease in synthesis of
prostaglandin, thromboxane.
Due to this there is analgesic,
antipyretic, anti inflammatory action
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It is acetylsalicylic acid. it is one of the oldest analgesic.
it is converted into salicylic acid inour body
ASPIRIN
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PHARMACOLOGICAL
ACTION
1.Analgesic action
Relieves inflamation, tissue injury,
integumental connective tissue
No effect on visceral pain, ishaemic
pain
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2.Antipyretic
decrease fever by sweating and
cutaneous dilatation
3.Antiinflammatory
Decrease pain, tenderness,
swelling. Redness, leucocysticinfilteration
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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
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decrease in liver glycogen
6.Respiratory action
By periphral action it increases CO2
production
And by central action increases
sensitivity of respiratory center
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7.Acid base balance
Causes compensatory respiratory
alkalosis
8.GIT
Irritates mucosa due to which
pain in epigastric region
Stimulates CTZ which causes
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PHARMACOKINETICS
absorb from stomach and small
intestine
alkalization of urine tend to
increase elimination of aspirin
freely crooses placenta
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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
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Blurring of vision, mental confusion,
exitement, electrolyte imbalance,sound in ear
4.Ryes syndrome- occurs inchildren
Causes hepatic encephalopathyduring viral influenza
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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
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Rheumatic arthritis, osteoarthritis,
acute rheumatic fever
Potential use in patent ductus
arteriosus. Premature labour,
pregnancy induce HTN
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CONTRAINDICATION
Hypersensitivity
Peptic ulcer
Chronic liver disease
During normal pregnancy at full
time
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Avoided 1 week before surgery
Patient having bleeding disorder
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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
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Adverse effects are epigastralgia,
heart burn, nausea, loose motions,
rashes, pruritis, somnolence,
dizziness.
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PARACETAMOL
It is a deethylated active metabolite
of phenacetin
ACTIONS
It raises pain threshold but has weakperipheral antiinflammatory
component
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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
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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
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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
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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
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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
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Treatment
Early vomiting should be induced
Gastric lavage should be done
Activated charcoal is given orally
Nacetylcysteine should be infused
i.v. over 15min
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DICLOFENAC
Potent analgesic antipyretic and
antiinflammatory drug
May also inhibit lipoxygenase
Plasma half life is 2-3hours
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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
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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
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OXYPHENBUTASONE
It is a biotransformation product of
phenylbutazone
Clinical use is limited because is
causes bone marrow depression
Plasma half life is 10-14hours
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PIROXICAM
long acting potent antiinflammatory,
antipyretic and analgesic drug
It has enterohepatic circulation
Plasma half life 45hours
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KETOROLAC
Potent analgesic and modest
antiinflammatory agent
In post operative pain efficacy is
equal to morphine
Used for short term management of
moderate pain
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IBUPROFEN
Better tolerated than aspirin
Drug of choice for rheumatoidarthritis
Plasma half life is 2-3 hours
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NAPROXEN
Better tolerated than aspirin
Second choice after ibuprofen inthe treatment of rheumatoid
arthritis
Plasma half life is 12-14hours
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KETOPROFEN
Inhibits both cycloxygenase and
lipoxygenase
MEPHENAMIC ACID
Lower efficacy as analgesic,antipyretic and antinflammatory
agent
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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
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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
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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.
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