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Referat Analgesik Opioid

Oxycodone is an opioid analgesic that acts on mu-opioid receptors to provide pain relief. It has higher oral bioavailability than morphine, resulting in more predictable effects. Studies show oxycodone provides effective acute and chronic pain relief, with some evidence of reduced side effects like hallucinations and itching compared to morphine. Both drugs cause typical opioid side effects. Oxycodone may be preferred for oral administration while morphine is better for epidural use due to its strong spinal analgesic effects.

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43 views25 pages

Referat Analgesik Opioid

Oxycodone is an opioid analgesic that acts on mu-opioid receptors to provide pain relief. It has higher oral bioavailability than morphine, resulting in more predictable effects. Studies show oxycodone provides effective acute and chronic pain relief, with some evidence of reduced side effects like hallucinations and itching compared to morphine. Both drugs cause typical opioid side effects. Oxycodone may be preferred for oral administration while morphine is better for epidural use due to its strong spinal analgesic effects.

Uploaded by

Deny Prima O
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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OPIOID ANALGESICS

“OXYCODONE “

Deny Prima Oktaviyanti


30101206766
FK Unissula
OPIOID RECEPTORS

Opioid receptors are a group of G-protein coupled


receptors with opioids as ligands
MECHANISM OF ACTION
OF OPIOID ANALGESICS
Effects are mediated via opioid
receptors :
•  (Mu) : mediate analgesia at
the supraspinal level.
•  (Kappa ): analgesia at the
spinal level.
•  (Delta) : analgesia in the periphery.
MU-RECEPTOR : TWO TYPES

• Mu-1 • Mu-2
– Located outside – Located
spinal cord throughout CNS
– Responsible – Responsible for
for central respiratory
interpretation depression, spinal
analgesia, physical
of pain dependence, and
euphoria
KAPPA RECEPTOR

• Only modest analgesia


• Little or no respiratory depression
• Little or no dependence
• Dysphoric effects
DELTA RECEPTOR

• It is unclear what delta’s responsible


for.
• Delta agonists show poor
analgesia and little addictive
potential.
• May regulate Mu receptor activity.
ENDOGENOUS ANALGESIC

There are endogenous analgesic


substances peptide structure and
with
morphine-like action.
They are called endogenous peptides and
were discovered during the investigation
of the mechanism of analgesic action of
morphine.
ENDOGENOUS ANALGESIC

Endogenous opioid peptides are :


a) enkephalins activate μ and δ-receptors;
b) endorphins activate μ, κ and δ-receptors;
c) dynorphins activate μ, κ and δ-receptors.
d) nociceptin – ORL1 (opioid like receptor) 
tolerance
Opioid peptides act in CNS as :
- neurotransmitters
- modulators of response (usually inhibitory)
OPIOID RECEPTORS
DISTRIBUTION AND
PHYSIOLOGICAL EFFECTS :
CERTAIN CELLS IN THE CNS
 Brainstem : mediate respiration, cough,
nausea and vomiting, maintain blood pressure,
pupillary diameter and control of stomach
secretions.
 Medial thalamus : modulate deep pain that
is poorly localized and emotionally
influenced.
OPIOID RECEPTORS

CERTAIN CELLS IN THE CNS


 Spinal cord : involved in the reception and
integration of incoming sensory information
and attenuate painful afferent stimulation.
 Hypothalamus : affect
neuroendocrine secretion.
 Limbic system: influence emotional
behavior.
OPIOID RECEPTORS
PERIPHERY
 Inhibit the release of excitatory,
proinflammatory substances from nerve
endings, contribute to the
which
inflammatory effect of opioids. anti-

IMMUNE CELLS
 Immune depression
MU AND KAPPA RECEPTOR
ACTIVATION
Response Mu-1 Mu-2 Kappa

Analgesia

Respirator
y
Depression
Euphoria

Dysphoria

Decrease GI
motility
Physical
Dependenc
e
Mainly agonist action at μ receptors,
but some actions on other receptors
•Morphine Agonist action at κ receptors,
•Heroin with partial antagonist action
•Codeine at μ receptors
•Fentanyl •Pentazocine

⊕ ⊕

μ⊕
opioid κ opioid 
opioid
receptor receptor

receptor

Analgesia Analgesia

Analgesia Respiratory depression

Sedation/dysphoria Euphoria/sedation Pupil

constriction
CLASSIFICATION OF OPIATES
 NATURAL OPIATES : morphine (alcaloid),
codeine,
 papaverine and thebaine; OPIATES
SEMI-SYNTHETIC : hydromorphone,
hydrocodone, oxycodone,
oxymorphone,
diacetylmorphine desomorphine,
(heroin), nicomorphine,
dipropanoyl- morphine, benzylmorphine and
ethylmorphine;
 FULLY SYNTHETIC OPIOIDS : fentanyl,
pethidine,
methadone, tramadol and propoxyphene;
 ENDOGENOUS OPIOID PEPTIDES :
endorphins, enkephalins, dynorphins, and endomorphins.
Semisynthetic derivative (opioid analogs)
Morphine derivatives
•Ethylmorphine, Heroin
Codeine derivatives
•Dextromethorphan
(antitusive agent)
•Dihydrocodeine
•Hydrocodone
•Oxycodone: p.o.
Thebaine derivatives
•Buprenorphine,
SYNTHETIC DERIVATIVES
PHENYLPIPERIDINES
pethidine, fentanyl
METHADONES
methadone, dextropropoxyphene
BENZOMORPHANS
pentazocine
TRAMADOL
GENERAL PHARMACOKINETICS
 LATENCY TO ONSET
 Oral (15 – 30 minutes)
 Intranasal (2 – 3 minutes)
 Intravenous (15 – 30 seconds)
 Pulmonary – inhalation (6 – 12 seconds)
 DURATION OF ACTION : anywhere between
4 and 72 hours depending on the substance
in question.
 METABOLISM : hepatic via phase 1 and
phase 2 biotransformations to form a diverse
array of metabolites (eg., morphine to
morphine-6-glucuronide).
OXYCODONE

Oksikodon telah digunakan dalam praktik klinis sejak tahun 1917

Obat ini diberikan secara intravena (i.v.), intramuskuler (i.m.), intranasal


(i.n.), subkutaneus (s.c.), perrektal, epidural, dan peroral menggunakan
larutan, larutan immediate-release, dan tablet immediate-release
dan controlled-release

Pemberian transdermal
juga telah diuji pada
binatang coba
Pendahuluan

Saat ini, oksikodon terutama digunakan sebagai tablet


controlled-release untuk nyeri kronik
Larutan dan tablet immediate-release digunakan untuk
nyeri akut

Oksikodon parenteral merupakan alternatif yang baik


ketika opioid tidak dapat diberikan secara peroral
Struktur Kimia

Molekul oksikodon (6-deoxy-7,8-dehydro-


14-hydroxy-3-O-methyl-6-oxomorphine)
terdiri dari dua planar (A dan B) dan dua
cincin alifatik (C dan D)

Kelompok penting untuk aksi


analgesik fenantrenen
terhubung dengan
posisi C3, C6, dan N

Struktur kimia oksikodon


Efikasi pada Nyeri Pascaoperatif Akut

Kalso et al.

Oksikodon dalam jumlah yang lebih sedikit secara signifikan lebih


dibutuhkan daripada morfin, keduanya untuk mencapai “first state of pain
relief” (13.2 mg vs. 24.9 mg) dan selama 2 jam periode penelitian (21.8 mg
vs. 34.2 mg)

Keadaan “first state of pain relief” dicapai lebih cepat (28 min vs. 46
min) dan bertahan lebih lama (39 min vs. 27 min) dengan oksikodon
daripada morfin

Morfin menyebabkan sedasi yang lebih tinggi dan penurunan MAP


yang lebih besar daripada oksikodon

Dalam hal lain, keduanya setara


Efikasi pada Nyeri Pascaoperatif Akut

Silvasti et al.
• Morfin dan oksikodon dalam jumlah sama dikonsumsi
pasien selama penelitian 24 jam
• Tidak ada perbedaan kualitas analgesia atau insidensi
ESO

Silvasti et al.
• Membandingkan oksikodon dengan tramadol patient-
controlled analgesia (PCA) i.v.
• Radio dosis equianalgesik tramadol terhadap oksikodon
ditemukan sekitar 8:1
• Tidak ada depresi respiratorik yang ditemukan
• Insidensi mual sedikit lebih tinggi pada kelompok
tramadol daripada oksikodon (44% vs. 28%, ns).
Efikasi pada Nyeri Terkait-Kanker

Oksikodon dan morfin Rasio dosis


memberikan analgesik yang equianalgesik harian
adekuat pada nyeri skala oksikodon:morfin =
sedang hingga berat 3:4 hingga 1:2

Halusinasi, mual dan


ESO yang dilaporkan  pruritus yang lebih
ESO opioid tipikal rendah dilaporkan
pada oksikodon
Efikasi pada Nyeri Non-Kanker Kronik

Caldwell et al.  OA Roth et al  OA


Intensitas nyeri menyeluruh
rerata setelah 2-4 minggu lebih Dibandingkan plasebo,
rendah pada oksikodon daripada oksikodon menghasilkan pain
plasebo relief yang lebih baik
(2.9 ± 1.2 vs 1.8 ± 1.1 dalam
Namun tingkat intensitas nyeri skala 0 hingga 5)
cenderung meningkat pada akhir
perlakukan
Reduksi signifikan pada nyeri
Kualitas tidur membaik secara menetap, allodinia, dan nyeri
signifikan pada oksikodon spontan paroksismal
daripada plasebo
Morphine atau oksikodon?

Baik morfin maupun oksikodon memberikan analgesik efektif pada nyeri akut
dan kronik

Oksikodon memiliki profil farmakokinetik yang lebih disukai

Bioavailabilitas oksikodon lebih tinggi sehingga variasi bioavailabilitas


interindividual dan konsentrasi plama yang diharapkan leih sedikit

Keduanya menimbulkan efek samping khas terkait-opioid

Beberapa laporan mengindikasi oksikodon menyebabkan lebih sedikit


halusinasi
Lebih sedikit rasa gatal pada oksikodon mungkin berkaitan dengan
pelepasan histamin yang lebih sedikit daripada morfin
Oksikodon tidak terutama efektif secara epidural, sementara morfin memiliki
efek analgesik spinal yang kuat

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