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ACUTE EXPOSURE INFORMATION
- USES: Meperidine is a narcotic analgesic used for the relief of moderate to severe pain, obstetrical analgesia, as a preoperative medication, and for support of anesthesia.
- PHARMACOLOGY: Meperidine is a mu and kappa opioid agonist. In therapeutic doses, it produces euphoria and analgesia.
- TOXICOLOGY: Therapeutic and toxic effects are mediated by different opioid receptors. Mu 1: Supraspinal and peripheral analgesia, sedation, and euphoria. Mu 2: Spinal analgesia, respiratory depression, physical dependence, GI dysmotility, bradycardia and pruritus. Kappa 1: Spinal analgesia and miosis. Kappa 2: Dysphoria and psychotomimesis. Kappa 3: Supraspinal analgesia. Chronic opioid users develop tolerance to the analgesic and euphoric effects, but not to the respiratory depression effects. Meperidine has an active metabolite (normeperidine) which may accumulate after repeated high doses or in patients with renal failure and cause seizures and myoclonus. Meperidine inhibits serotonin uptake and may also precipitate serotonin syndrome in combination with other serotonergic drugs.
- EPIDEMIOLOGY: Meperidine overdose is uncommon as the medication is decreasingly used. Severe toxicity can occur.
- WITH THERAPEUTIC USE
- COMMON: Lightheadedness, dizziness, sedation, nausea, vomiting, and sweating. OTHER EFFECTS: Asthenia, confusion, headache, weakness, syncope, constipation, dry mouth, seizures, tremors, myoclonus, delirium, euphoria, dysphoria, agitation, transient hallucinations and disorientation, urinary retention, hypotension, tachycardia, bradycardia, palpitations, pruritus, flushing, urticaria, injection site pain and irritation, visual disturbances, anaphylactic reactions, muscle rigidity, biliary tract spasm, and respiratory depression. Histamine release, leading to hypotension and/or tachycardia, flushing, sweating, and pruritus, has been reported in patients receiving meperidine.
- WITH POISONING/EXPOSURE
- MILD TO MODERATE TOXICITY: Lightheadedness, dizziness, nausea, vomiting, urinary retention, sedation, and disorientation.
- SEVERE TOXICITY: Higher doses and longer-term administration have been associated with central nervous system excitatory effects such as agitation, tremors, myoclonus, motor weakness, and seizures. Excitatory symptoms are thought to be due to the metabolite, normeperidine, which has a longer half-life than the parent compound and thus accumulates with frequently repeated high dose use of meperidine. Respiratory and CNS depression can occur from large doses. Meperidine can cause signs of serotonin toxicity such as muscle rigidity, tremor, confusion, behavioral changes, and autonomic instability usually when used with other serotonergic drugs. A syndrome closely resembling moderate to severe idiopathic Parkinson's disease has been described in intravenous and intranasal drug users following use of a derivative of meperidine, 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Orofacial dyskinesias, arm flexion, and stiffening of the legs have been observed.
- DRUG INTERACTION: Concomitant administration with monoamine oxidase inhibitors can cause a severe reaction (eg, hyperthermia, hypertension, muscle rigidity, coma, mental status changes, seizures, death). Meperidine may precipitate serotonin syndrome when administered with other serotonergic drugs.
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