Chapter 26 Opioid agonist, opiod antagonist, and antimigraine agents Flashcards
(48 cards)
Opioid agonists MEDS
Morphine, Codeine, Fentanyl, Hydrocodone, Hydromorphone, Meperidine, Methadone, Oxycodone, Oxymorphone, Tapentadol ,Tramadol
MOA opioid agonist
Opioid agonists stimulate opioid receptors in the CNS, specifically mu and kappa receptors.
Mu-receptor effects:
Analgesia, euphoria, respiratory depression, pupil constriction, and physical dependence.
Kappa-receptor effects:
Analgesia, sedation, and dysphoria.
Opioids alter pain perception by modulating pain signal transmission in the brain and spinal cord.
Indications for opioid agonists
Relief of moderate to severe acute or chronic pain.
Preoperative medication to reduce anxiety and pain.
Adjunct to anesthesia
for additional sedation and pain control.
Management of severe pain conditions, including cancer pain and post-surgical pain
Pharmacokinetics opioid agonists
Absorption: Well absorbed through oral, IM, IV, subcutaneous, transdermal, and intrathecal routes.
Metabolism: Mostly in the liver.
Excretion: Primarily through urine and bile.
Half-life of Morphine: 1.5 to 2 hours.
CI opioid agonist
Allergy to opioids.
Severe respiratory disorders (e.g., COPD, asthma, emphysema) due to respiratory depression risk.
Acute or severe GI conditions (e.g., paralytic ileus, biliary tract disease) as opioids slow motility.
Head injuries, cerebral vascular disease, alcohol use disorder, or delirium tremens (opioids may exacerbate CNS depression).
Preg and lactation: Use with caution due to risk of neonatal opioid withdrawal syndrome
AE opioid agonists
CNS Effects: Light-headedness, dizziness, sedation, confusion, psychoses, anxiety, hallucinations.
Respiratory Depression: Apnea, circulatory depression, respiratory arrest, shock.
Cardiovascular (CV) Effects:
Orthostatic hypotension, tachycardia, cardiac arrest.
Gastrointestinal (GI) Effects:
Nausea, vomiting, constipation, biliary spasm.
Genitourinary (GU) Effects:
Urinary retention, ureteral spasms, loss of libido.
Pupil Constriction: Causes miosis.
Physical Dependence: Long-term use can lead to opioid addiction and withdrawal syndrome.
DDI opioid agonists
CNS Depressants (barbiturates, benzodiazepines, alcohol, phenothiazines, MAOIs): Increased risk of respiratory depression, sedation, and coma.
Tapentadol + SSRIs, MAOIs, TCAs, St.
John’s Wort: Risk of serotonin syndrome, a potentially fatal condition.
Anticholinergic Agents: May exacerbate constipation and urinary retention.
Antihypertensive Drugs: Increased risk of hypotension and orthostatic hypotension.
Nursing interventions for opioid agonists
Assessment:
- Assess for contraindications, including respiratory
dysfunction, liver or kidney disease, head trauma, and
pregnancy.
- Monitor CNS effects, such as sedation, confusion,
dizziness, and hallucinations.
- Check vital signs (respiratory rate, blood pressure, heart
rate) to detect respiratory depression or hypotension.
- Evaluate bowel function to monitor for constipation.
- Assess urinary output to detect urinary retention.
Interventions:
- Administer IV opioids slowly to reduce risk of
hypotension and respiratory depression.
- Monitor respiratory rate (hold if < 12 breaths/min).
- Encourage fiber intake and hydration to prevent
constipation.
- Ensure patient safety (fall precautions due to sedation
and dizziness).
- Educate patients on opioid dependence risks and the
importance of gradual tapering.
Patient Teaching:
- Take opioids exactly as prescribed to avoid addiction and overdose.
- Do not mix opioids with alcohol or other CNS depressants.
- Report signs of respiratory distress, confusion, or extreme drowsiness.
- Increase fiber and fluids to prevent constipation.
- Avoid operating heavy machinery due to drowsiness and
dizziness risks.
Opioid Agonist- Antagonists MEDS
Buprenorphine(Buprenex)
Butorphanol (generic)
Nalbuphine (generic)
Pentazocine (available only in combination with naloxone)
MOA opioid agonist-antagonist
These drugs act as partial agonists at mu-opioid receptors and antagonists at kappa-opioid receptors.
They produce analgesia, sedation, and euphoria but can also cause hallucinations and impaired mental function.
Their antagonistic properties may induce withdrawal in opioid- dependent patients.
Indications Opioid Agonist- Antagonists
Moderate to severe pain requiring opioid therapy.
Treatment of opioid use disorder (buprenorphine).
Pain relief during labor and delivery (nalbuphine).
Pharmacokinetics Opioid AA
Buprenorphine: Available in IM, IV, oral, transdermal, and transmucosal forms.
Butorphanol: Available IM, IV, and as a nasal spray.
Nalbuphine: Administered parenterally (subcutaneous, IM, IV).
Pentazocine: Only available in oral combination form with naloxone.
Metabolized in the liver, excreted in urine or feces.
Crosses the placenta and enters breast milk.
CI to Opioid AA
Allergy to opioid agonist-antagonists.
Sulfite allergy (for nalbuphine).
Physical dependence on opioids (can trigger withdrawal syndrome).
Use with caution in:
- Respiratory disorders (COPD,
asthma, sleep apnea) due to risk
of respiratory depression.
- Cardiac conditions (MI, CAD,
hypertension) due to stimulatory
effects.
- Renal or hepatic dysfunction
(may affect drug metabolism and
clearance).
- Pregnancy and lactation (risk of
neonatal opioid withdrawal syndrome).
AE opioid AA
Central Nervous System (CNS):
Light-headedness, dizziness, sedation, hallucinations, psychoses, anxiety, fear.
Respiratory Effects: Respiratory depression, apnea, suppression of cough reflex.
Gastrointestinal (GI): Nausea, vomiting, constipation, biliary spasms.
Genitourinary (GU): Urinary retention, ureteral spasms, loss of libido.
Physical and psychological dependence are possible, but less likely than with full opioid agonists.
DDI Opioid AA
CNS depressants (barbiturates, alcohol, benzodiazepines): Increased risk of respiratory depression, sedation, and coma.
Use in opioid-dependent patients: May precipitate withdrawal symptoms, including hypertension, vomiting, anxiety, and fever.
Patients switching from opioid agonists to opioid agonist-antagonists require careful monitoring.
Nursing interventions Opioid AA
Assessment:
- Assess for contraindications, including opioid dependence, respiratory disorders, cardiovascular conditions, and hepatic/renal dysfunction.
- Monitor CNS effects, including hallucinations, sedation, and dizziness.
- Check respiratory rate and oxygen saturation (hold if respiratory rate < 12 breaths/min).
- Assess bowel function (constipation risk) and urinary output (urinary retention risk).
Interventions:
- Monitor for withdrawal symptoms in opioid-dependent patients.
- Educate on avoiding alcohol and CNS depressants.
- Ensure fall precautions due to dizziness and sedation.
- Titrate doses carefully to prevent severe sedation or
withdrawal reactions.
- Monitor pain relief effectiveness and adjust treatment if
necessary.
Patient Teaching:
- Take the medication exactly as prescribed.
- Avoid alcohol and sedatives to prevent excessive CNS
depression.
- Report any signs of withdrawal, hallucinations, or
difficulty breathing.
- Use caution when driving or operating heavy
machinery.
- Maintain hydration and fiber intake to prevent
constipation.
Opioid Antagonists MEDS
Naloxone (generic)
Naltrexone (Vivitrol)
Methylnaltrexone and other opioid antagonists for opioid- induced constipation
MOA opioid antagonist
Block opioid receptors to reverse opioid effects such as respiratory depression, sedation, and hypotension.
Do not produce analgesic effects but can induce withdrawal symptoms in opioid-dependent individuals.
Indication opioid antagonist
Reversal of opioid- induced respiratory depression and sedation.
Treatment of opioid overdose.
Management of opioid dependence (naltrexone).
Pharmacokinetics opioid antagonist
Naloxone: Administered parenterally (IM, IV, or subcutaneous); not absorbed orally.
Naltrexone: Well absorbed orally.
Metabolism: Hepatic metabolism.
Excretion: Primarily in the urine.
Half-Life: Shorter than most opioids, so repeat dosing may be required.
CI opioid antagonist
Known hypersensitivity to opioid antagonists.
Use with caution in pregnancy and lactation, as it may cause withdrawal symptoms in the fetus or newborn.
Use with caution in patients with a history of opioid dependence, as it can precipitate acute withdrawal.
AE opioid antagonist
Opioid Withdrawal Symptoms (Opioid Abstinence Syndrome): Nausea, vomiting, sweating, tachycardia, hypertension, tremors, and anxiety.
CNS Effects: Agitation, restlessness, nervousness.
Cardiovascular (CV) Effects: Tachycardia, dysrhythmias, blood pressure fluctuations, pulmonary edema.
DDI opioid antagonist
Higher doses of opioid antagonists may be required to reverse the effects of:
- Buprenorphine
- Butorphanol
- Nalbuphine
- Pentazocine (opioid
agonist-antagonists).
Nursing interventions opioid antagonist
Assessment:
- Assess for opioid overdose signs (respiratory depression, pinpoint pupils, unresponsiveness).
- Monitor respiratory status and oxygen levels closely.
- Evaluate cardiovascular status, including heart rate and
blood pressure.
- Check for opioid dependence history, as administration
may trigger withdrawal.
Interventions:
- Ensure airway patency and provide artificial ventilation if necessary.
- Monitor continuously for opioid withdrawal symptoms.
- Be prepared for repeated dosing, as opioid antagonists
have shorter half-lives than most opioids.
- Provide comfort and support to help patients cope with
withdrawal symptoms.
Patient Teaching:
- Inform patients and families about opioid reversal effects.
- Warn about potential withdrawal symptoms in opioid- dependent individuals.
- Educate caregivers on how to use naloxone auto- injectors in emergency settings.
- Ensure opioid-dependent patients are aware that opioid antagonists block opioid effects and may reduce pain relief from prescribed opioids.
