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PAIN definition
Noxious
Stimulus
Stimulus nyeri yang
disebabkan oleh :
• Kimia
• Mekanik
• Termal
• Panas (>42̊ C)
• Dingin (<10̊ C)
3
Klasifikasi berdasarkan lama nyeri
Klasifikasi berdasarkan asalnya
Pain pathway
TATA LAKSANA TERAPI
• Menghilangkan rasa nyeri
• Membuat perasaan lebih nyaman
• Dapat beraktivitas secara normal
• Meningkatkan kualitas hidup
Tujuan Terapi
Pharmacotherapy
1. Non-opioid analgesics
2. Opioid analgesics
3. Adjuvant analgesics
LA = Local anesthetic
ASA = Asetil salysilic acid
TCA = Tricyclic Antidepressant
SSRI = Selective serotonin reuptake inhibitor
SNRI = Selective norepinephrine reutake inhibitor
Target Terapi
PAIN SCALE
adjuvan
non-opioid adjuvan
non-opioid adjuvan
NON-OPIOID ANALGESIC
(NSAID, asetaminophen)
• Analgesik
1
• Antipiretik
2
• Antiinflamasi
3 (kec.parasetamol)
Pharmacology Effects
• depression of cyclooxygenases activity
• decreasing of prostaglandins synthesis in peripheral
tissues and in central nervous system
• decreasing of sensitivity of nervous endings and
depression of transmission of nociceptive impulses
on the level of CNS structures
• pain-relieving action of non-opioid analgesics is
partly connected with their anti-inflammatory
activity
Potency of NSAID
onset NSAID T-max (hr)
Rapid Diclofenac 0.8
Nimesulide 1.2 – 2.7
Slow Celecoxib 2–4
Meloxicam 6
• Efek samping
• Pada dosis terapi normal bebas dari efek samping bermakna
• Kemerahan pada kulit dan reaksi alergi yang lain sering terjadi
• Penggunaan dosis besar jangka lama dapat menyebabkan nekrosis
tubular ginjal dan nekrosis hati
• Hepatotoksik
• In adults, hepatotoxicity may occur after ingestion of a single dose of 10
to 15 g (150 to 250 mg/kg) of acetaminophen; doses of 20 to 25 g or
more are potentially fatal Symptoms occur during the first 2 days of
acute poisoning by acetaminophen reflect gastric distress (nausea,
abdominal pain, and anorexia)
OPIOID ANALGESIC
Opioid Receptors
• Group of G-protein coupled receptors with opioids as
ligands.
• Subtypes of opiod receptors:
mu, delta, kappa, epsilon, sigma
Physical Dependence
Mania, hallucination
• Opium is extracted from poppy seeds (Papaver
somniforum)
• Used for thousands of years to produce:
• Euphoria
• Analgesia
• Sedation
• Relief from diarrhea
• Cough suppression
History of Opioids
Morpheus
is the Greek god of
dreams and sleep.
Classification
Tolerance and
Dependence
Depressant effects Stimulate effects
• Sedation Analgesia • CTZ (nausea, vomiting)
• Indifference to surroundings
• Edinger Wesphal nucleus
• Mood and subjective effects
• Depression of respiration (III nerve –producing
• Cough centre miosis)
• Vasomotor centre dilatation • Vagal centre
• Decrease GI motility (bradycardia)
constipation
• Urine retention
1. Morphine
MORPHINE HYDROCHLORIDE
routes of administration
subcutaneously and intramuscularly
(analgesic action after 10-15 min)
oral administration – presystemic elimination
( 20-60 % enters general blood circulation)
sublingually – quick absorption
i.v. is indicated even in emergency
Epidural or intrathecal ( into the spinal canal ) injection
produces segmental analgesia lasting 12 hours without
affecting other sensory, motor or autonomic modalities
Duration of analgesic action – 4-6 hours
Maximum single dose of morphine is 0,02 g,
maximum daily dose – 0,05 g
2. Fentanyl
• synthetic opioid analgesic of short action
• analgesic activity is 300 times higher than of morphine
• analgesic effect after intravenous introduction – after 1-3
min, lasts for 15-30 min
• Transdermal route: should be used for long-term (chronic)
pain requiring continuous narcotic pain
• Is designed to release the drug into the skin at a constant rate
ranging from 25 to 100 micrograms/h,
3. Codeine
opium alkaloid
analgesic action is not strong, but anticough effect is
considerable
administered as an anticough drug of central action
combination with non opiod analgesics
(eg. Paracetamol) is supra-additive
• Central analgesic
• Terikat pada reseptor N opiat dan secara lemah
menghambat reuptake norepinefrin dan serotonin
• ESO = opioid lain, tetapi potensi depresi pernafasan <<
• Digunakan untuk nyeri kronis (neuropati), bukan akut.
4. Tramadol
• Terapi tambahan bukan analgesik, tetapi dapat
meningkatkan respon terhadap analgesik
• Contoh:
• Antidepresan, misal: gol. Amin trisiklik/TCA (amitriptilin,
imipramin), Inhibitor MAO, SSRI, SNRI
• Antikonnvulsan, misal : phenobarbital, diazepam
• Anestesi lokal, misal: lidokain
Adjuvan Analgesic
AAFP, 2013