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History of Opioids
Opium is extracted from poppy seeds
(Paper somniforum)
Used for thousands of years to
produce:
Euphoria
Analgesia
Sedation
Relief from diarrhea
Cough suppression
Terminology
opium is a Greek word meaning
juice, or the exudate from the
poppy
opiate is a drug extracted from the
exudate of the poppy
opioid is a natural or synthetic drug
that binds to opioid receptors
producing agonist effects
Mechanism of Action
bind to G-protein-coupled neural receptors (
Opioid Receptors
Mu-1
Mu-2
Kappa
Effects of opioids
Opiods: dose-response
relationship
Morphine
Alfentanil
Fentanyl
Heroin
Meperidine
Methadone
Morphine
Remifentanil
Sufentanil
MODERATE/LOW AGONISTS
Codeine
Oxycodone
Propoxyphene
MIXED AGONIST-ANTAGONISTS AND PARTIAL AGONISTS
Buprenorphine
Butorphanol
Nalbuphine
Pentazocine
ANTAGONISTS
Naloxone
Naltrexone
(according to
OTHER ANALGESICS
Lippincotts
Tramadol
Pharmacology, 2006
Morphine
CNS effects
Respiratory depression and
suppression of cough: reducing the
responsiveness of the respiratory
centers in the brain stem to blood
levels of carbon dioxide and inhibiting
directly the respiratory center.
Morphine
CNS effects
Nausea and vomiting: stimulating the
chemoreceptor trigger zone. In most
cases, after therapeutic dose,
subsequent doses of morphine do not
produce vomiting.
Miosis: pinpoint pupils are indicative
of toxic dosage prior to asphyxia. It
can be block with atropine.
Morphine
Cardiovascular effects:
Orthostatic hypotention can occur
due to vasomotor medullary
depression and histamine release.
Gastrointestinal effect:
Reduces gastrointestinal motility,
causing constipation
Decreases biliary and pancreatic
secretions.
Constriction at the spincter of Oddi
causes an increase in biliary pressure.
Morphine
Other systemic effects:
Increases detrusor muscle tone in the
urinary bladder, producing a feeling
of urinary. Vesical sphincter tone is
also increased, making voiding
Inhibits the cellular immunity and
humoral immunity, which is
significant in withdrawal syndrome
and tolerant in chronic administration.
Farmakokinetik Opioid
Adverse effects
Respiratory depression is the most important effect.
Contraindications and
cautions
Use in patients with head injures
Interaksi Obat
Obat yang bekerja secara sentral
seperti barbiturat, fenotiazin,
penghambat MAO, antidepresan
trisiklikefek sedatif dan
depresi pernafasan
Fenotiazinefek menurunkan
tek.darah
Amphetamineanalgesia dari
morphin dan mengurangi efek sedasi
dan depresi pernafasan
Methadone
Fentanyl
Has a shorter duration of action than morphine.
Meperidine
Pharmacokinetics:
Meperidine is well absorbed from the
gastrointestinal tract, and is useful
when an orally administered
However, meperidine is most often
administered parenterally
The drug has a duration of action of 2
to 4 hours, which is shorter than that
of morphine
Adverse effects:
Large or repetitive doses of
meperidine can cause anxiety,
tremors, muscle twitches, and rarely,
convulsions due to the accumulation
of a toxic metabolite, normeperidine.
Codeine
Pethidine
Tramadol
a centrally acting analgesic that
binds to the -opioid receptor
it weakly inhibits reuptake of
norepinephrine and serotonin
It is used to manage moderate to
moderately severe pain
Its respiratory-depressant activity is
less than that of morphine
Opioid Antagonists
Opioid Antagonists
Naloxone
ALHAMDULILLAH.