By : IG

Derifat

asam asetic heterocyiclic

Analgesic potent tapi anti inflamasi
moderat
gol.
NSAID
menghasilkan
efek
analgesi
melalui
penghambatan
sintesis prostaglandin
Struktur kimia :

Sebagian besar NSAIDs bekerja sbg nonselective inhibitors dari enzyme

cyclooxygenase,
Menghambat :
cyclooxygenase-1 (COX-1)
cyclooxygenase-2 (COX-2) isoenzymes.
Cyclooxygenase mengkatalisa formasi
prostaglandins & thromboxane dari arachidonic
acid (itself derived from the cellular
phospholipid bilayer by phospholipase A2).
Prostaglandins act (among other things) as
messenger molecules in the process of
inflammation. This mechanism of action was
elucidated by John Vane (1927-2004), who later
received a Nobel Prize for his work

Diindikasikan untuk manajemen nyeri jangka

pendek (<5 hari)
Sangat berguna untuk manajemen nyeri post
operatif yg segera
Efek analgesinya pada dosis terapi setara 6-12
mg morfin dgn onset yang sama (20-30menit)
tapi durasi lebih panjang (6-8jam)
Bekerja di perifir dan tidak menembus sawar
darah otak sehingga efek ke SSP minimal
Spesifik : tidak mendepresi pernapasan, mual,
muntah,mengantuk.
Sering digunakan untuk manajemen nyeri
operasi ortopedi dan obgyn tapi lebih jarang
digunakan pada operasi intra abdominal

Menghambat
agregasi
platelet,
memperpanjang bleeding time
Penggunaan jangka panjang bisa berakibat
toksis ke ginjal (nekrosis papiler)
GIT bisa berakibat perdarahan dan ulserasi
bahkan perforasi
Karena eliminasinya di ginjal tidak disarankan
diberikan pd pasien dgn ggn fungsi ginjal
Kontra indikasi pada pasien yang alergi aspirin
atau NSAID lainya
Pasien dg rwyt asma insiden hipersensitif
terhadap
aspirin
meningkat
(10%)polip
nasal(20%)

Lo
of ss
ac of
id PG
se E
cr 2 a
et
i o nd
P
n
an GI
d 2m
cy
to edi
pr at
ot ed
ec i n
tiv hi
e e bi t
ffe ion
ct

NSAID
Loss of PGI2 induced inhibition of LTB4 mediated
endothelial adhesion and activation of neutrophils

Leukocyte-Endothelial
Interactions

Capillary
Obstruction

Proteases +
Oxygen Radicals

Ischemic
Cell Injury

Endo/Epithelial
Cell Injury

Mucosal Ulceration

 Dosis

awal 60mg IM atau 30mg IV

loading dose
Maintenance 15-30mg /6jam
Pasien
usia
tua
perlu
dosis
penyesuaian / pengurangan dosis
karena fx ginjal menurun

 Aspirin

menurunkan protein binding

ketorolac sehingga perlu dosis yang
lebih besar.
Ketorolac tidak mempengaruhi MAC
agen
anestesi inhalasi serta tidak
mempengaruhi hemodinamic pasien
yang dibius
Ketorolac bisa menurunkan kebutuhan
analgetik opiat post operatif

 Non

spesifik COX inhibitor (ketorolac,

diclofenac dosis : 1mg/kgbb IV)
Selectif COX-2 inhibitor (parecoxib)
punya toxicitas lebih rendah dan
efek ke GIT yang lebih rendah,serta
efek ke agregasi platelet yang lebih
rendah pula dosis (20-40mg IV)

NSAIDs are effective analgesics for

the acute pain of surgery, low back
pain and renal colic (Level I*).
2. NSAIDs are effective adjunct to
opioids (Level I).
3. NSAIDs given in addition to
paracetamol improve analgesia
(Level I).
1.

I Evidence obtained from a systematic

review of all relevant randomised controlled
trials.
II Evidence obtained from at least one
properly designed randomised controlled
trial
III-1 Evidence obtained from well-designed
pseudo-randomised controlled trials
(alternate allocation or some other method)
NHMRC 1999

NNT (95%CI)
Codeine 60 mg
16.7 (11-48)
Paracetamol 1000 mg 3.8 (3.4-4.4)
Morphine 10 mg (IM) 2.9 (2.6-3.6)
Ketorolac 10 mg
2.6 (2.3-3.1)
Ibuprofen 400 mg
2.4 (2.3-2.6)
Diclofenac 50 mg
2.3 (2.0-2.7)
Paracetamol 1G/ Codeine 60 mg
2.2
(1.7-2.9)
Parecoxib 40 mg (iv) 2.2 (1.8-2.7)
Lumiracoxib 400mg 2.1 (1.7-2.5)
Diclofenac 100mg
1.9 (1.6-2.2)
Oxford acute pain league table
www.jr2.ox.ac.uk/bandolier/booth/painpag/Ac
utrev/Analgesics/Leagtab.html

 Small

increased risk of thrombotic

attacks.
Diclofenac (150 mg ) = etoricoxib.
Ibuprofen 1200mg or below - no
increase of myocardial infarction.
Naproxen - lower incidence of
thrombotic risk than coxibs.
All NSAIDs - risk greater with high
doses, long term Rx.

 Clinical

anestesiology,G
Edward
MORGANJr,
Fourt
edition.2006
chapter 15 page 282-283
Pharmakology
&
physiology
in
Anesthetic practice,fourt edition,
Robert K STOELTING, lipincot &
walkins chapter 11 page 287-288