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Meperidine (demerol®)?

See the DrugPatentWatch profile for Meperidine

Meperidine (trade name Demerol®)
A short‑acting synthetic opioid analgesic that has largely been replaced by other agents (e.g., morphine, fentanyl, oxycodone) in most settings because of its side‑effect profile and the risk of accumulation of a toxic metabolite (normeperidine).

Feature Details
Class Opioid (μ‑receptor agonist)
Indication Moderate to severe pain (post‑operative, acute, or inflammatory) in adults and children. Also used for severe cough (rare) and as part of anesthesia in some settings.
Typical adult dose 25–100 mg IV/IM every 3–4 h (maximum 200 mg/day). For IV infusion, 100 mg over 10–30 min every 3–4 h.
Pediatric dose 0.3–0.5 mg/kg IV/IM every 3–4 h (max 0.3–0.5 mg/kg/day).
Route of administration IV, IM, SC (injections). Oral formulations are available but not common in the U.S.
Mechanism Binds to μ‑opioid receptors in the central and peripheral nervous system, inhibiting ascending pain pathways, increasing pain threshold, and producing analgesia, sedation, and respiratory depression.
Metabolism Hepatic amidation to meperidine‑1‑hydrogen‑cysteine (MHC), then N‑demethylation to normeperidine (a neurotoxic metabolite). Excreted mainly by the kidneys.
Half‑life Meperidine: ~4 h; normeperidine: ~15–24 h.
Key safety concerns
• Normeperidine accumulation Especially in renal impairment; can cause seizures, myoclonus, delirium, and neurotoxicity.
• Respiratory depression Dose‑dependent; caution in elderly, patients with COPD, or concomitant CNS depressants.
• Serotonin syndrome When combined with serotonergic drugs (SSRIs, MAOIs, triptans, etc.).
• Seizures Rarely, especially with high doses or chronic use.
• Tolerance and dependence Potential for physical dependence and withdrawal if used >5–7 days.
• Drug interactions MAO inhibitors, SSRIs, SNRIs, duloxetine, tramadol, other opioids, alcohol, benzodiazepines, muscle relaxants, anticholinergics.
Contraindications Known hypersensitivity to meperidine or other opioids; uncontrolled seizures; severe respiratory depression; severe hepatic/renal dysfunction (risk of normeperidine accumulation).
Precautions Use lowest effective dose for shortest duration. Monitor for signs of neurotoxicity, especially in patients with renal disease. Avoid in patients on serotonergic drugs.
Common adverse events Nausea, vomiting, constipation, pruritus, dizziness, somnolence, hypotension, urinary retention.
Rare but serious Seizures, severe CNS depression, serotonin syndrome, hypersensitivity reactions, renal impairment exacerbation.
Discontinuation/withdrawal Taper gradually if used >5 days to avoid abrupt withdrawal. Monitor for symptoms: agitation, anxiety, tremor, sweating, nausea, diarrhea.
Alternative agents Morphine, hydromorphone, fentanyl, oxycodone, tramadol (if neuropathic pain), NSAIDs, acetaminophen, regional techniques.
Why it’s less used now 1) Normeperidine risk → seizures and neurotoxicity. 2) Better alternatives with longer duration, fewer side effects. 3) Risk of dependence. 4) Regulatory warnings and black‑box label.
Special populations • Elderly: Increased sensitivity, risk of CNS depression. • Pregnancy: Category C; use only if benefits outweigh risks. • Pediatric: Dose adjustments for weight; monitor for neurotoxicity. • Renal impairment: Reduce dose, increase interval, or avoid.
Monitoring • Vitals (BP, HR, RR, O₂ sat). • Pain scores. • Mental status (alertness, confusion). • Urine output if renal dysfunction. • Electrolytes, especially if seizures suspected.
Patient counseling • Take exactly as prescribed. • Do not exceed prescribed dose. • Avoid alcohol and other sedatives. • Report dizziness, confusion, seizures, or breathing problems. • Store in a safe place out of reach of children/others.

Quick Reference Table

Situation Recommendation
Acute postoperative pain 25–100 mg IV/IM q3‑4 h; monitor for respiratory depression.
Renal impairment Consider dose reduction, longer intervals, or alternative analgesic.
Concurrent SSRI/MaOI use Avoid due to serotonin syndrome risk.
Severe hepatic dysfunction Use caution; monitor for normeperidine.
Long‑term use (>7 days) Generally avoid; switch to alternative opioid or multimodal pain management.

Bottom‑line

Meperidine remains a useful short‑acting opioid for specific acute pain scenarios but is generally reserved for situations where other agents are unsuitable (e.g., when a brief, rapid onset is needed and other opioids cannot be used). Its risk of normeperidine accumulation and seizure potential, particularly in patients with renal impairment, limits its widespread use. Always weigh the benefits against the potential for neurotoxicity, respiratory depression, and dependence.



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