Nonsteroidal Anti-Inflammatory Drugs

s ()
() NSAIDs Not an NSAID (Acetaminophen)

1.
(1)
(2)
(3)
(4)
2.

Histamine ++ - -
Serotonin +/-
Bradykinin +++ - +++
Prostaglandins +++ +++ +
Leukotrienes - +++ -
3. Prostaglandins
(1) (Arachidonic acid) (Cyclooxygenase)
(2)
A. Prostaglandins
(C-fiber dorsal horn cell)

B. Prostaglandins ( 37 39
)

C.
D.
E.
(3) NSAIDs Prostaglandins
A.
B.
C.
D.
E.

1
NSAIDs (Non-steroidal anti-inflammatory drugs)

NSAIDs 1 Cyclooxygenase (Prostaglandins

Thromboxane) 1 Arachidonic acid
2 Leukotrienes
1.
(1) (Anti-inflammatory) ()
(2) (Analgesic)
(3) (Antipyretic)
(4) NSAIDs
2.
(1) abc
A. Thromboxane
a.
b. NSAIDs () Aspirin Acetyl group
Cyclooxygenase
Cyclooxygenase

2
 B. Prostaglandins
a.
b.
c.
d.
e.
(2)
A. Leukotriene (LTC4)
a.
b.
B. Prostanoids ()
a.

3
Salicylates
1. (Salicylates)

2. Salicylates
(1) Aspirin Acetyl group (Acetylsalicylic acid ; ASA)
(2) Non-acetylated salt of salicylate Acetyl group
Acetyl group

Aspirin
Acetyl group
Cyclooxygenase

4
3. Salicylates
(1) (Antiplatelet)

(2) (Analgesic) (Antipyretic)

(3) (Anti-inflammatory)

(4)

4. Salicylates
(1) (Reyes syndrome)


(2)


(3)
(4) Prostaglandin Aspirin

5.
(1) Probenecid Aspirin
Aspirin
(2) Antacids () Aspirin
Aspirin
(3) Aspirin Aspirin
(4) BilirubinPhenytoinNaproxenSulfinpyrazoneThiopentalThyroxine
Triiodothyronine Aspirin
()

5
 NSAIDs
1. Salicylic acids
(1) Aspirin
(2) Diflunisal
(3) Benorylate
2. Propionic acids
(1) Ibuprofen
(2) Naproxen
(3) Flurbiprofen
(4) Fenbufen
(5) Ketoprofen
3. Acetic acids
(1) Indomethacin Cyclooxygenase Lipoxygenase



(2) Sulindac
4. Fenamates
(1) Mefenamic acid (Ponstan)
(2) Meclofenamic acid
5. Oxicams
(1) Piroxicam
(2) Tenoxicam
6. Paracetamol (Acetaminophen)

6
Cyclooxygenase

Cyclooxygenase1 (COX1) Cyclooxygenase2 (COX2)

Constitutive Inducible

Mucous secretion Peripheral and central
Renal function Sensitization(Pain)
Erythema ()
Platelet aggregation Edema formation
Fever
1. COX2 COX2
2. NSAIDs Cyclooxygenase (COX)
COX-2

COX2
COX1 COX2 COX2
(Constitutive) (Constitutive) (Inducible)

7
3. COX1COX2
(1) COX2

(2) COX2 COX2 () COX1

(3) COX1 COX1 COX2( COX2)

8
4. COX2
(1) NSAIDs COX1
(2) COX2
A. Nabumetone (Relafen)
B. Etodolac (Lodine)
C. Meloxicam: ()
(3) COX2 COX2
A. Celecoxib (Celebrex)

B. Rofecoxib (Vioxx)
()
a. PGI 2 PGI 2

b.

9
Acetaminophen (Paracetamol)
1.

2. Peripheral cyclooxygenase
3. Prostaglandin
4. Cyclooxygenase
(1) Prostaglandin
(2) (,)
5. NSAIDs ()

() ()

6.
(1)
(2) ()
(3) ()

10
7.
(1) Glutathione
(2) (Activated charcoal) :
(3) (Antidote) : Acetylcysteine (Mucomyst, Mucosol)
()

11
 NSAIDs

1. ()

2.

12
( COX2 )

13

103-1-65.
Rofecoxib( COX-2 selective inhibitors) PGI 2
TXA 2
(A) (B) (C) (D)
(D)
( p.9)

99-1-69.
(NSAIDs) (cyclooxygenaseCOX)
(COX-1) (COX-2)
(whole blood assay) 50% COX-2
50% COX-1 LogIC50 ratio WBA (COX-2/COX-1)
(A) Aspirin (B) Ketorolac (C) Ketoprofen (D) Meloxicam
(D)
50% COX-2 50% COX-1 LogIC50 ratio WBA
(COX-2/COX-1) , 50% COX-2 COX-2
Meloxicam COX-2 COX-2
D ( p.9)
(A) Aspirin : non selective
(B) Ketorolac : NSAIDs
(C) KetoprofenPropionic acid ( p.6)

103-1-67.
,,

(A) Paracetamol (B) Aspirin (C) Indomethacin (D) Ibuprofen

(A)
COX-2
() ( p.10)

101-2-65.
Acetaminophen
(A) Alcohol (B) Water (C) Electrolytes (D) N-acetylcysteine
(D)
N-acetylcysteine acetaminophen ( p.11)

14
103-2-65.
Indomethacin
(A) (B) Cyclooxygenase
(C) (D)
(D)
( p.6)

100-2-66.
Propionic acid
(A) Ibuprofen (B) Naproxen (C) Flurbiprofen (D) Mefenamic acid (Ponstan)
(D)
Mefenamic acid (Ponstan) Fenamates ( p.6)

98-2-69.
Mefenamic acid (Ponstan)
(A) Para-aminophenol (B) Propionic acid derivative (C) Fenamates (D) Indole derivative
(C)
( p.6)

15