BMS-K 10

Opioid
Analgesics
Aznan Lelo
Dep. Farmakologi & Terapeutik,

Fakultas Kedokteran
Universitas Sumatera
Utara
31 Januari 2010, KBK BMS-10, FK USU

ANALGETIKA OPIAT

Peptida endogen opioid

FD/FK opioid
Efek samping, antidiare, antitussiva
Interaksi

Analgesics
Decrease in sensation of pain.
Classes:
Opioid.
Agonist.
Antagonist.
Agonist-antagonist.

Non-opioids.
Salicylates.
NSAIDs.
Adjuncts.

Opioids
Generic reference to morphine-like
drugs/actions
Opiate: derivative of opium

Prototype: morphine
Morpheus: god of dreams

Act on endorphin receptors:

Mu (most important)
Kappa

Actions of Opioid
Receptors
Response

Mu

Kappa

Analgesia

Respiratory Depression

Sedation

Euphoria

Physical Dependence

GI motility

Actions at Opioid
Receptors
Drugs
Pure Agonists

Mu
Agonist

Kappa
Agonist

-morphine, codeine, meperidine (Demerol),

fentanyl (Sublimaze), remifentanil (Ultiva),
propoxyphene (Darvon), hydrocodone
(Vicodin), oxycodone (Percocet)

AntaAgonist-Antagonist
-nalbuphine (Nubaine), butorphanol (Stadol) gonist

Agonist

Pure Antagonist

Antagonist

-naloxone (Narcan)

Antagonist

General Actions of
Opioids
Analgesia
Respiratory
depression
Constipation
Urinary retention
Cough suppression
Emesis
Increased ICP
Indirect through CO2
retention

Euphoria/Dysphoria
Sedation
Miosis
Pupil constriction

Preload &
afterload
Watch for
hypotension!

Opioid Receptors
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 and
Sigma.

Mu Receptors
Location:
CNS incl. brainstem, limbic system,
dorsal horn of spinal cord
Morphine sulfate and morphine
sulfate agonists bind to Mu receptors
Bind to opioid receptors in brain and
SC and even in periphery

Narcotic Analgesics
Relieve moderate to severe pain by
inhibiting release of Substance P in
central and peripheral nerves;
reducing the perception of pain
sensation in brain,
producing sedation and
decreasing emotional upsets
associated with pain

Narcotic Analgesics
Can be given orally, IM, sub q, IV or
even transdermally
Orally are metabolized by liver,
excreted by kidneycaution if
compromised
Morphine and meperidine produce
metabolites
Widespread effects: CNS, Resp., GI

Indications for Use

Before and during surgery
Before and during invasive diagnostic
procedures
During labor and delivery
Tx acute pulmonary edema
Treating severe, nonproductive cough

Contraindications to Use

Respiratory depression
Chronic lung disease
Chronic liver or kidney disease
BPH
Increased intracranial pressure
Hypersensitivity reactions

Management
Considerations
age-specific considerations
Morphine often drug of choicenonceiling. Other nonceiling drugs
include: hydromorphone, levorphanol
and methadone
Use non-narcotic when able
Combinations may work by different
mechanisms thus greater efficacy
(e.g. Tylenol w/codeine)

Route selections
Oral preferred
IV most rapidPCA allows self
administration. Basal dosage. More
effective, requires less dosing.
Epidural, intrathecal or local injection
Can use rectal suppositories or
transdermal routes

Dosage
Dosages of narcotic analgesics
should be reduced for clients
receiving other CNS depressants
such as other sedative-type drugs,
antihistamines or sedating
antianxiety medications

Scheduling
Give narcotics before encouraging
turning, coughing and deep
breathing in post-surgical patients
Automatic stop orders after 72h
In acute pain, narcotic analgesics are
most effective when given
parenterally and at start of pain

Individual Drugs
Agonists have activity on mu and
kappa opioid receptors
Agonist/antagonists have agonist
activity in some receptors;
antagonists in others. Have lower
abuse potential than pure agonists;
because of antagonismcan produce
withdrawal symptoms
Antagonists are antidote drugs

Agonists
Alfenta (alfentanil)short duration
Codeine
Sublimaze or Duragesic (Fentanyl)short
duration
Dilaudid (hydromorphone)
Demerol (meperidine)preferred in urinary and
biliary colic, less resp. depression newborns
Morphine
OxyContin
Darvon (propoxyphene)
Ultram (tramadol)
Methadone

Agonists/Antagonists
Have lower abuse potential than pure
agonists
Buprenex (buprenorphine)
Nubain (nalbuphine)
Talwin (pentazocine)
Stadol (butohanol)also in nasal
spray

Antagonists
Revex (nalmefene)longer duration
of action than Narcan
Narcan (naloxone)
ReVia (naltrexone)-used in
maintenance of opiate-free states in
opiate addicts

Narcotic (Opioid)
Antagonists
Purpose: Reverse CNS depression and
respiratory depression from excessive
opioid usage.
Action: Block the effects of opioid
analgesics from binding with receptor sites
or displacing those already on sites.
Ex.: Narcan
Uses: Reverse post-op opioid depression,
relieve CNS and respiratory depression by
therapeutic doses or overdoses of opioids.

FARMAKOLOGI SSP
Kanal ion
Tapak kerja obat dan mekanisme
modulasi transmisi sinap
Excitatory and inhibitory neurotransmitter

Inhibitory and Facilitatory

Mechanisms
Neurotransmitterschemicals that
exert inhibitory or excitatory activity
at post-synaptic nerve cell
membranes. Examples include:
acetylcholine, norepinehprine,
epinephrine, dopamin, and serotonin.
Neuromodulatorsendogenous
opiates. Hormones in brain. Alpha
endorphins, beta endorphins and
enkephalins. Help to relieve pain.

Topics

Analgesics and antagonists

Anesthetics
Anti-anxiety and sedative-hypnotics
Anti-seizure / anti-convulsants
CNS stimulators
Psychotherapeutics
ANS/PNS/SNS agents