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Opioid Analgesics &

Antagonists
Nur Hesti Kusumasari, dr
Opioid Analgesics
Classification :
Spectrum of Clinical Uses :
Analgesics
Antitussive
Antidiarrheal drugs
Strength of Analgesia :
Strong analgesia
Moderate analgesia
Weak Analgesia
Ratio of Agonists to Antagonist Effects :
Agonists (receptor activator)full or partial
Antagonists (receptor blocker)
Mixed agonist-antagonists (capable of activating one
opioid receptor subtype & blocking another subtype)
Pharmacokinetics
Most drugs are well absorbed orally
& can be given parenterally
Opioid drugs are widely distributed
to body tissues
They cross the placental barrier &
exert effects on the fetus
The opioid are metabolized by
hepatic enzymes
Mechanism of action
Interaction with specific opioid receptors in the
CNS & peripheral tissues
Three major opioid receptors are , ,
& receptor : contributed to analgesia,
respiratory depression, physical dependence
receptor : contributed to spinal analgesia &
sedative effects of opioid drugs
Opioid receptors are thought to be activated by
endogenous peptides under physiologic
conditions.
these peptides are enkephalins, dynorphin,
beta-endorphin
Ionic mechanisms


The Effects
Acute Effects
Analgesia :
Strong agonists (morphine, methadone, meperidone,
fentanyl, levorphanol, heroin)
Mild to moderate agonists (codeine, hydrocodone,
oxycodone)
Weak agonists (propoxyphene)
Sedation & euphoria :
These effects occur at doses below maximum
analgesia doses
At higher doses, the drugs may cause mental
clouding, stuporous, or comatose state
Respiratory depression :
Decreased response to carbondioxide challenge
Antitussive actions :
Suppression of the cough
The Effects
Nausea & vomitus
Caused by activation of the chemoreceptor trigger
zone & are increased by ambulation
Gastrointestinal effects :
Constipation (decreased intestinal peristalsis, which
is probably mediated by effects on opioid receptors in
the en teric nervous system
Smooth muscle :
Contraction of biliary tract muscle
Increased uretral & bladder sphincter tone
Reduction in uterine tone
Miosis :
Pupillary coonstriction, is a characteristics effects of
all opioid except meperidine
The Effects
Chronic Effects
Tolerance
Involve receptor uncoupling
Physical dependence
Is an anticipated physiologic responese
to chronic therapy with drugs in this
group, particularly the strong agonists
Abstinence syndrome (rinorrhea,
lacrimation, chills, gooseflesh, muscle
aches, diarrhea, yawning, anxiety, &
hostility
Clinical Uses
Analgesia
To treatment of moderate to severe pain
Cough suppression
Include codein & dextromethorphan (orally)
Treatment of diarrhea
Include diphenoxylate & loperamide (selective antidiarrheal
opioids)
Management of acute pulmonary edema
Morphine (parenterally) is useful in acute pulmonary edema
because its hemodynamics action & its calming effects to
relief of the pulmonary symptoms
Anesthesia
Are used as preoperative medications & intraoperaive
adjuntive agents
Opioid dependence
Methadone is used in the management of opioid withdrawal
states & in maintenance programs for addicts
Toxicity
Overdose
Coma with marked respiratory deppression
& hypotension
Treatment : naloxone, ventilatory support
Drug interactions
Interaction with ethanol, sedative hypnotic,
anesthetic, antipsychotics drugs, tricyclic
antidepressants, & antihistamine (additive
CNS deppression)
Mixed agonist-antagonists
& Partial Agonist drugs
Mixed agonist-antagonists drugs :
Prototype : butorphanol, nalbuphine,
pentazocine
Are agonists with weak
antagonists activity
Partial Agonists drugs :
Prototype : buprenorphine
Is a partial agonists at receptor
Mixed agonist-antagonists
& Partial Agonist drugs
Effects :
Sedation at analgesic doses
Dizzines, sweating, nausea, anxiety,
hallucinations, nightmares
Less intense respiratory deppression
than with pure agonists
Less tolerance
Less physical dependence
Opioid Antagonists
Prototype : naloxone (duration
of action 1-2h), naltrexone (24-
48h)
Clinical uses : management of
acute opioid overdose
Given intravenously

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