Opioid Analgesics

Drug ClassSchedulePrimary UseAntidote
Opioid agonistsDEA Schedule IIModerate–severe acute and chronic painNaloxone (Narcan)

Key Points

  • Mechanism: Bind to mu, delta, and kappa opioid receptors in the CNS → alter pain perception, raise pain threshold, produce CNS depression
  • Primary adverse effect: Respiratory depression — monitor respiratory rate; rate <12/min → withhold and notify provider; keep naloxone at bedside
  • Constipation is the most persistent adverse effect — does NOT develop tolerance; requires proactive bowel management
  • Morphine is the prototype opioid; no ceiling effect → appropriate for cancer pain and end-of-life care
  • Meperidine (Demerol): NOT recommended for routine analgesia — toxic metabolite causes delirium and seizures, especially in elderly and renal-impaired patients
  • Avoid opioid-first strategies for chronic noncancer pain when effective alternatives exist, and avoid routine opioid-first use in patients younger than 18 years
  • All opioids are Schedule II controlled substances — require double-count documentation, witnessed waste
  • IM opioid onset is slower and more variable than IV; low-perfusion states (for example shock or chilled tissue) can delay absorption and later increase overdose risk as circulation recovers.

Mechanism of Action

Opioid agonists bind to opioid receptors (primarily mu receptors) located throughout the CNS and peripheral tissues. Receptor activation:

  • Analgesia: Modulates painful signals from peripheral tissues; raises pain threshold
  • Euphoria/sedation: CNS depression through limbic and cortical pathways
  • Cough suppression: Suppresses cough center in medulla
  • Respiratory depression: Decreases responsiveness of brain stem respiratory centers to CO2 — primary life-threatening adverse effect

Key Opioid Agents

DrugRouteTypical Adult DoseNotes
MorphineIV, POIV PCA: 1–2 mg per bolus; PO: 15–30 mg q4h IRPrototype opioid; no ceiling effect; used for cancer/end-of-life; common in PCA
Morphine concentrate (Roxanol)Sublingual, POConcentration often 20 mg/mL; dose individualizedCommon in end-of-life care for pain or air hunger when swallowing is limited; reassess comfort-alertness balance
Fentanyl (Sublimaze, Duragesic)IV, transdermalAcute: 25–50 mcg IV q30–60 min; Patch: 25–100 mcg/hrSynthetic — safe alternative for morphine allergy; extremely potent; major contributor to opioid overdose deaths
Hydromorphone (Dilaudid)IV, POIV: 0.2–1 mg q2–3h; PO: 2–4 mg q4–6hSemisynthetic; potent; available in both forms for in/out-hospital use
Tramadol (Ultram)PO (IR/ER)IR: 50 mg; ER: 100/200/300 mgIR for short pain episodes when other options are not tolerated/effective; ER for chronic ongoing pain
Oxycodone (OxyContin, Xtampza ER)POIR: 5–15 mg q4–6h; ER: individualizedLess pruritus than morphine; often combined with acetaminophen (monitor total APAP dose ≤4 g/day)
CodeinePO15–60 mg q4h; max 360 mg/dayRequires CYP2D6 conversion to morphine; unpredictable response; NOT recommended in children
Methadone (Dolophine)PO, IVIndividualizedHalf-life up to 59 hours; used for opioid use disorder and chronic pain; neuropathic pain benefit
Meperidine (Demerol)IM, SQ50–150 mg q3–4h; max 600 mg/dayNOT for routine analgesia — toxic metabolite (normeperidine) causes CNS excitability, delirium, seizures; use limited to shivering (rigors) management

Adverse Effects

SystemAdverse EffectClinical Action
RespiratoryRespiratory depression (RR <12/min)Withhold opioid; stimulate patient; administer naloxone
CNSSedation, confusion, dizziness, lightheadednessFall precautions; side rails up; assist ambulation
CardiovascularHypotension (vasodilation)Position changes slowly; monitor BP; avoid in hypovolemia
GIConstipation (no tolerance develops), nausea, vomitingBowel regimen (stool softener + stimulant laxative); anti-emetics
UrinaryUrinary retention (higher risk in opioid-naive or spinal-route opioid use)Monitor urine output; assess for bladder distention; catheterize if needed
DermatologicPruritus (especially with spinal-route opioids)Antihistamines; monitor for added sedation if diphenhydramine is used

Respiratory Depression

Respiratory depression is the primary life-threatening risk of opioid use. Risk is highest in:

  • Elderly and debilitated patients
  • Patients with COPD, sleep apnea, or decreased respiratory reserve
  • When combined with other CNS depressants (benzodiazepines, alcohol, sedative-hypnotics)
  • When opioid-naive patients receive first doses

Naloxone (Narcan) — Opioid Antidote

Mechanism: Competitive opioid receptor antagonist — rapidly displaces opioids from receptors and reverses CNS/respiratory depression.

Indications: Complete or partial reversal of opioid-induced respiratory depression; suspected opioid overdose.

Administration: IV push (fastest) or IM; repeat every 2–3 minutes until adequate respiratory response; effect lasts 30–90 minutes (shorter than most opioids → re-sedation can occur, requiring repeat doses or infusion).

Naloxone Cautions

  • Precipitates acute withdrawal in opioid-dependent patients — signs: sweating, tachycardia, hypertension, vomiting, severe agitation, seizures
  • Withdrawal may also present with diarrhea and tremors after abrupt reversal
  • Neonates of opioid-dependent mothers: Do NOT administer naloxone — precipitates neonatal withdrawal with convulsions
  • Abrupt reversal in postoperative opioid-dependent patients → severe hypertension, ventricular dysrhythmias, pulmonary edema

Nursing Monitoring Priorities

Before Administering:

  • Assess pain using validated scale (0–10, FACES, behavioral)
  • Prefer oral/IV/subcutaneous/rectal/transdermal routes as appropriate; intramuscular opioid administration is typically avoided when alternatives are available
  • If IM opioid dosing is required, monitor closely in low-perfusion states because delayed absorption can lead to later rebound sedation/respiratory depression.
  • Assess baseline respiratory rate, LOC, blood pressure
  • Review current medications for CNS depressants (benzodiazepines, alcohol history)
  • Verify opioid history and tolerance status
  • Confirm controlled substance documentation (count, witness)

During Therapy:

  • Respiratory rate — q1–4h depending on route; RR <12/min → withhold and notify provider
  • Level of consciousness — sedation scale assessment
  • Pain reassessment — 30–60 min after IV dose; 60 min after PO dose
  • In final-hours comfort care, reassess dyspnea relief and ability to interact, and titrate toward the patient-defined comfort-alertness goal.
  • Bowel function — daily; start prophylactic bowel regimen with initial opioid order
  • Urinary output — especially with epidural or intrathecal opioids

Safety:

  • Fall precautions — bed in lowest position, call light within reach, non-skid footwear
  • Side rails elevated when sedated
  • Naloxone immediately available at bedside during IV opioid use

Patient Education:

  • Do not drive or operate heavy machinery
  • Avoid alcohol and CNS depressants
  • Change positions slowly (orthostatic hypotension)
  • Report: RR <12/min, extreme drowsiness, inability to be woken
  • Take with food to reduce nausea
  • Constipation expected — take prescribed laxative/stool softener

Self-Check

  1. A postoperative patient receiving IV morphine via PCA has a respiratory rate of 10/min and is difficult to arouse. What is the immediate nursing priority?
  2. A nurse administers naloxone to a patient with suspected opioid overdose. The patient’s respirations improve, but 45 minutes later the nurse reassesses and finds renewed sedation and RR of 11. Why does this occur, and what should the nurse do?
  3. An elderly patient with COPD and moderate-to-severe cancer pain is prescribed around-the-clock morphine. What special monitoring parameters apply to this patient?