NON NON- -STEROIDAL ANTI STEROIDAL ANTI- -

INFLAMMATORIES DRUGS INFLAMMATORIES DRUGS

(NSAIDs) (NSAIDs)
THE !NFLANNATORY RESPONSE
The inflammatory response is a normal (desirable) defense The inflammatory response is a normal (desirable) defense
mechanism. mechanism.
The side effects are undesirable. The side effects are undesirable.
Normal inflammatory response has an on/off switch. Normal inflammatory response has an on/off switch.
!n chronic inflammation something has gone wrong with !n chronic inflammation something has gone wrong with
the the OFF OFF switch switch
Therefore we need drugs to control the inflammatory Therefore we need drugs to control the inflammatory
reaction. reaction.
Complement system
Histamine
Serotonin
Bradykinin - major contributors to symptoms oI inIlammation
Leukotrienes - increase vascular permeability
- increase mobilization oI endogenous mediators oI inIlammation
Prostaglandins PGE
2
- promote edema and leukocyte inIiltration
PGI
2
- increase vascular permeability, enhance pain producing
properties oI bradykinin
NED!ATORS OF THE
!NFLANNATORY RESPONSE
S!CNS OF !NFLANNAT!ON S!CNS OF !NFLANNAT!ON
Redness Redness due to local vessel dilatation due to local vessel dilatation
Heat Heat due to local vessel dilatation due to local vessel dilatation
Swelling Swelling due to influx of plasma proteins and due to influx of plasma proteins and
phagocytic cells into the tissue spaces phagocytic cells into the tissue spaces
Pain Pain due to local release of enzymes and increased due to local release of enzymes and increased
tissue pressure tissue pressure
NA]OR PATHWAYS NA]OR PATHWAYS
OX 1 and OX 2 OX 1 and OX 2
The key enzyme in the The key enzyme in the cyclooxygenase pathway cyclooxygenase pathway
is the enzyme cyclooxygenase (COX). is the enzyme cyclooxygenase (COX).
There are two forms of cyclooxygenase, COX1 (the There are two forms of cyclooxygenase, COX1 (the
predominant form) and COX2. predominant form) and COX2.
The basic pharmaceutical reasons to use NSA!Ds The basic pharmaceutical reasons to use NSA!Ds
are : are :
Anti Anti inflammatory inflammatory
Analgesic Analgesic
Antipyretic Antipyretic
Anti Anti coagulant coagulant
The anti The antiinflammatory properties of the NSA!Ds insure inflammatory properties of the NSA!Ds insure
that the release of the prostaglandins, histamines, that the release of the prostaglandins, histamines,
thromboxanes and leukotrienes is inhibited in the area thromboxanes and leukotrienes is inhibited in the area
of tissue injury. of tissue injury.
NSA!Ds Are Analgesic Agents NSA!Ds Are Analgesic Agents
They produce analgesia by : They produce analgesia by :
reducing capillary permiability reducing capillary permiability
stabilizing the mast cell stabilizing the mast cell
inhibit prostaglandin production inhibit prostaglandin production
inhibits bradykinin from stimulating pain inhibits bradykinin from stimulating pain
receptors receptors
NSA!Ds Are Antipyretic NSA!Ds Are Antipyretic
!nhibit the effects of prostaglandins on the
thermoregulatory center's (TRC) set point lowering the
TRC set point
NSA!Ds Are Anti NSA!Ds Are Anti oagulants oagulants
These medications have varying capabilities to prolong the
clotting time. They all inhibit one of the clotting factors as well
as inhibit platelet aggregation.
ADvERSE EFFETS OF THE NSA!DS ADvERSE EFFETS OF THE NSA!DS
NS : NS :
Headaches Headaches
Tinnitus Tinnitus
Dizziness Dizziness
ADvERSE EFFETS OF THE NSA!DS ADvERSE EFFETS OF THE NSA!DS
ardiovascular:
Fluid retention hypertension Fluid retention hypertension
dema dema
Congestive cardiac failure (Rarely) Congestive cardiac failure (Rarely)
Hepatic: Hepatic:
Abnormal liver function test Abnormal liver function test
iver failure iver failure
ADvERSE EFFETS OF THE NSA!DS ADvERSE EFFETS OF THE NSA!DS
C! Tract : C! Tract :
Abdominal pain Abdominal pain
Dyspepsia Dyspepsia
Nausea Nausea
vomiting vomiting
Bleeding Bleeding
Ulcer Ulcer
ADvERSE EFFETS OF THE NSA!DS ADvERSE EFFETS OF THE NSA!DS
Hematopoietic Effects : Hematopoietic Effects :
Thrombocytopenia (low platelet count) Thrombocytopenia (low platelet count)
Neutropenia Neutropenia
Aplastic anemia Aplastic anemia bone marrow bone marrow
dysfunction dysfunction
ADvERSE EFFETS OF THE NSA!DS ADvERSE EFFETS OF THE NSA!DS
Kidneys : Kidneys :
Renal !nsufficiency Renal !nsufficiency
Renal Failure Renal Failure
Hyperkalemia Hyperkalemia
Proteinuria Proteinuria
ADvERSE EFFETS OF THE NSA!DS ADvERSE EFFETS OF THE NSA!DS
Pulmonary: Pulmonary:
Asthma Asthma
Rashes: Rashes:
All types All types
Pruritus Pruritus
Thank you Thank you