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Presented by:
Rozaimah Zain-Hamid
• Pulse
• Blood pressure Pain:
• Temperature Vital Signs
• Respiratory rate
American Pain Society Web site.
1
VAS
0 1 2 3 4 5 6 7 8 9 10
Mild Moderate Severe
Pain threshold
Pain tolerance
Department of Pharmacology & Therapeutics
Faculty of Medicine, Universitas Sumatera
Pain Management
• Elimination of the cause of the pain
• Lowering sensitivity nociceptors: antipyretic
analgesics, local anesthetics
• Interrupting nociceptive conduction in
sensory nerves: local anesthetics
• Supression of transmission of nociceptive
impulses in the spinal medulla:opioids
• Inhibition of pain perception: opioids, general
anesthetics
• Altering emotional responses to pain:
antideppresants
Department of Pharmacology & Therapeutics
Faculty of Medicine, Universitas Sumatera
Origin and effects of prostaglandin
Antipyretic analgesics
• Acetaminophen (paracetamol):
toothaches and headaches
• Acetysalicylic acid (ASA):
antiinflammatory effect (+)
• Ibuprofen
• Pyrazolone derivates
(aminopyrine and dypirone):
metamizole displays the highest efficacy
inflammation severe
neurophatic
CNS origin
PAIN KILLER
adjuvant opioid
analgesic NSAID analgesic
COX LOX
COX-2 COX-1
cyclic
endoperoxides 5-HPETE
NSAIDs
PGI2
inhibits platelet TXA2 LTA4
aggregation, stimulates platelet
vasodilator, aggregation,
vasoconstriction LTB4
hyperalgesia chemotaxis
LTC4
PGD2 PGE2 PGF2alfa
inhibits platelet bronchoconstriction LTD4 brochoconstriction
vasodilator, myometrial contr. increase
aggregation,
vasodilator hyperalgesia hyperalgesia vascular
LTE4
permeability
Department of Pharmacology & Therapeutics
Faculty of Medicine, Universitas Sumatera
The evolution of NSAID chemistry
for the control of pain
Coxib
Class
Acetic
Oxicam Acid Celecoxib
Class Class Rofecoxib
Propionic
Acid Valdecoxib
Salicylic Piroxicam Diclofenac Etoricoxib
Acid Class Etodolac
Meloxicam Parecoxib
Class Lumiracoxib
Ibuprofen
Aspirin ketoprofen
anti-inflammatory
analgesic
Diclofenac Celecoxib
Acetosal Indomethacin Ibuprofen
Ketorolac Piroxicam Ketoprofen
Meloxicam
Nimesulide
COXIB
Rofecoxib
Valdecoxib
AA
NSAIDs
LTs PGs
vaso- constriction vaso-dilatation
fluid & electrolyte
AA
NSAID
LTs PGs
vaso- vaso-
constriction dilatation
temporary
reversible
color-blindness
Department of Pharmacology & Therapeutics
Faculty of Medicine, Universitas Sumatera
TOXICITY IN PREGNANCY
AA
NSAID
LTs PGs
utero-
contraction
NSAIDs
deplete folic acid levels and then prolong
increase the risks of birth defects gestation & labor
increase risk of miscarriage Department of Pharmacology & Therapeutics
Faculty of Medicine, Universitas Sumatera
RESPIRATORY TOXICITY
AA
NSAID
LTs PGs
bronchoconstriction bronchodilatation
NSAID-induced asthma
Department of Pharmacology & Therapeutics
Faculty of Medicine, Universitas Sumatera
OPIOID ANALGESICS
• Opioid receptors
– Binding sites not only for endogenous opiates
but also for opioid analgesics to relieve pain
• Several types of receptors:
– Mu, Kappa, Delta, Epsilon & Sigma.
• Tramadol • Morphine
• Codein: 1/10 morphine • Fentanyl
• Dihydrocodeine • Oxycodone
• Buprenorphine
• Hydromorphone
• Methadone
• Tapentadol
Department of Pharmacology & Therapeutics
Faculty of Medicine, Universitas Sumatera
Choosing pain killer
and its combinations
10 Pain Intensity Scale
0 1 2 3 4 5 6 7 8 9 10
Mild Moderate Severe
paracetamol NSAID Strong opioid
or/+ ± ±
NSAID weak opioid NSAID
± ± ±
adjuvant adjuvant adjuvant
analgesic analgesic analgesic
Department of Pharmacology & Therapeutics
Faculty of Medicine, Universitas Sumatera
Thank You