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BackMeperidine Data - Uses, Dosage, Drug class, Brand name, Warnings, etc
| Pharmacology | Meperidine is a phenylpiperidine opioid agonist with important antimuscarinic activity and negative inotropic effects on the heart. Its major metabolite, normeperidine, has excitant effects that can precipitate tremors, myoclonus, or seizures. Meperidine’s antimuscarinic activity might negate the miosis that occurs with other opioids. |
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| Administration and Adult Dosage |
- PO, IV, or SC for analgesia: 50–150 mg every 3–4 hr; oral doses ~50% as effective as parenteral - IV for shaking caused by general anesthesia or amphotericin B: 25–50 mg - Reduce dosage when given with phenothiazines or other drugs that potentiate depressant effects - IM administration not recommended |
| Special Populations - Pediatric Dosage |
- PO, IV, or SC for analgesia (≥1 yr): 1–1.8 mg/kg every 3–4 hr, maximum 100 mg/dose - IM administration painful and not recommended in children |
| Special Populations - Geriatric Dosage | Same as adult dosage. |
| Dosage Forms |
- Syrup: 10 mg/mL - Tablet: 50, 100 mg - Injection: 10, 25, 50, 75, 100 mg/mL |
| Patient Instructions |
- Take as directed; do not exceed recommended dosage - May cause drowsiness; avoid driving or operating machinery until effects are known - Avoid alcohol and other CNS depressants - Report severe constipation, difficulty breathing, twitching, or seizures to your physician |
| Missed Doses |
- If taken on a regular schedule, take a missed dose as soon as remembered - If near the time for the next dose, take that dose only; do not double the dose or take extra |
| Pharmacokinetics - Onset and Duration |
- PO onset: ~15 min; duration 2–3 hr - SC or IM onset: ~10 min; peak analgesia 0.5–1 hr; duration 2–3 hr |
| Pharmacokinetics - Serum Levels | - Analgesia: 500–700 µg/L (2–2.8 µmol/L) |
| Pharmacokinetics - Fate |
- Bioavailability: ~52 ± 3%; 80–90% in cirrhosis due to decreased first-pass metabolism - Serum Levels (100 mg IM): 670 µg/L (2.7 µmol/L) at 1 hr, 650 µg/L (2.6 µmol/L) at 2 hr - Protein Binding: 58 ± 9%, largely to α1-acid glycoprotein; decreased in elderly and uremia - Distribution: Vd = 4.4 ± 0.9 L/kg, increased in elderly and premature infants - Clearance: Cl = 1.02 ± 0.3 L/hr/kg; reduced by 25% in surgical patients, 50% in cirrhosis, and in acute viral hepatitis - Metabolism: Hepatic hydrolysis and metabolism to normeperidine (active metabolite) - Excretion: 2% unchanged, 1–21% (average 6%) normeperidine in urine |
| Pharmacokinetics - t¹⁄₂ |
- Meperidine: α phase 12 min, β phase 3.2 hr; increases to 7 hr in cirrhosis/acute liver disease, 14–21 hr in moderate to severe renal dysfunction - Normeperidine: 14–21 hr in normals, up to 35 hr in renal failure |
| Adverse Reactions & Side Effects |
- Sedation, dizziness, nausea, vomiting, constipation, respiratory depression - Normeperidine-induced seizures with: dosage >400–600 mg/day, renal failure, seizure history, long-term use in cancer patients, or co-administration of agents increasing N-demethylation - Local irritation and induration with repeated SC injection |
| Contraindications |
- MAO inhibitors within the past 14–21 days - Chronic pain - Hypersensitivity to meperidine or other opioids |
| Precautions & Warnings |
- Avoid in patients with reduced renal function or continuous administration for more than a few days - Use with caution in patients with respiratory disease, head injury, increased intracranial pressure, or hepatic impairment - Combination with promethazine and chlorpromazine (DPT) not recommended due to poor efficacy and high adverse effects |
| Drug Interactions |
- MAO inhibitors may cause marked blood pressure alterations, sweating, excitation, and rigidity - Barbiturates, chlorpromazine, and phenytoin decrease meperidine levels and increase normeperidine, reducing analgesia and increasing seizure risk - Ritonavir increases meperidine AUC via CYP2D6 inhibition - CNS depressants (e.g., alcohol, benzodiazepines) increase sedation and respiratory depression risk |
| Parameters to Monitor |
- Monitor vital signs and pain scores regularly - Watch for jerking/twitching movements indicating normeperidine accumulation and potential toxicity |
| Class and Drug Brand Name |
- Class: Opioids - Brand Names: Demerol, Various |
| Notes |
- Meperidine may cause less sphincter of Oddi spasm than morphine, but clinical relevance is limited - Useful for treating shaking/shivering from general anesthesia or amphotericin B - Reserve for brief courses in healthy patients with untoward effects from other opioids (e.g., morphine, hydromorphone) due to low therapeutic index - IM administration unreliable; IV preferred for rapid, predictable effect - Oral meperidine not recommended for cancer pain due to CNS toxicity risk at high doses |
References
Hand of Clinical Drug Data