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MEPERIDINE
Meperidine is an opioid agonist that binds to mu-opioid receptors to produce analgesia and sedation.
Meperidine is a marketed opioid analgesic primarily indicated for acute pain management, competing in a crowded market of established opioids. Its key strength lies in its ability to provide effective analgesia and sedation through binding to mu-opioid receptors. The primary risk is the strong competition from widely used alternatives such as morphine, hydromorphone, fentanyl, oxycodone, and tramadol, each offering distinct advantages in potency, duration, and safety profile.
At a glance
| Generic name | MEPERIDINE |
|---|---|
| Also known as | pethidine |
| Drug class | opioid analgesic |
| Target | mu-opioid receptor |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 1942 |
Mechanism of action
Meperidine works by binding to mu-opioid receptors in the central nervous system and organs composed of smooth muscle. This binding leads to a reduction in pain perception and induces sedation. However, it also has the potential to cause respiratory depression and other side effects, which are mediated through the same receptors.
Approved indications
- Acute Pain Management
Boxed warnings
- WARNING: SERIOUS AND LIFE-THREATENING RISKS FROM USE OF MEPERIDINE HYDROCHLORIDE TABLETS AND ORAL SOLUTION Risk of Medication Errors Ensure accuracy when prescribing, dispensing, and administering Meperidine Hydrochloride Oral Solution. Dosing errors due to confusion between mg and mL, and other Meperidine Hydrochloride Oral Solutions of different concentrations can result in accidental overdose and death [see Dosage and Administration ( 2.1 ), Warnings and Precautions ( 5.1 )] . Addiction, Abuse, and Misuse Because the use of Meperidine Hydrochloride Tablets and Oral Solution exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death, assess each patient’s risk prior to prescribing and reassess all patients regularly for the development of these behaviors and conditions [see Warnings and Precautions ( 5.2 )] . Life-Threatening Respiratory Depression Serious, life-threatening, or fatal respiratory depression may occur with use of Meperidine Hydrochloride Tablets and Oral Solution, especially during initiation or following a dosage increase. To reduce the risk of respiratory depression, proper dosing and titration of Meperidine Hydrochloride Tablets or Oral Solution are essential [see Warnings and Precautions ( 5.3 )]. Accidental Ingestion Accidental ingestion of Meperidine Hydrochloride Tablets and Oral Solution, especially by children, can result in a fatal overdose of meperidine [see Warnings and Precautions ( 5.3 )] . Risks From Concomitant Use with Benzodiazepines Or Other CNS Depressants Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of Meperidine Hydrochloride Tablets and Oral Solution and benzodiazepines or other CNS depressants for use in patients for whom alternative treatment options are inadequate [see Warnings and Precautions ( 5.4 ), Drug Interactions ( 7 )] . Neonatal Opioid Withdrawal Syndrome (NOWS) Advise pregnant women using opioids for an extended period of time of the risk of Neonatal Opioid Withdrawal Syndrome, which may be life-threatening if not recognized and treated. Ensure that management by neonatology experts will be available at delivery [see Warnings and Precautions ( 5.5 )] . Opioid Analgesic Risk Evaluation and Mitigation Strategy (REMS) Healthcare providers are strongly encouraged to complete a REMS-compliant education program and to counsel patients and caregivers on serious risks, safe use, and the importance of reading the Medication Guide with each prescription [see Warnings and Precautions ( 5.6 )]. Cytochrome P450 3A4 (CYP3A4) Interaction The concomitant use of Meperidine Hydrochloride Tablets or Oral Solution with all cytochrome P450 3A4 (CYP3A4) inhibitors may result in an increase in meperidine plasma concentrations, which could increase or prolong adverse reactions and may cause potentially fatal respiratory depression. In addition, discontinuation of a concomitantly used cytochrome P450 3A4 (CYP3A4) inducer may result in an increase in meperidine plasma concentration. Monitor patients receiving Meperidine Hydrochloride Tablets or Oral Solution, and any CYP3A4 inhibitor or inducer [see Warnings and Precautions ( 5.7 ), Drug Interactions (7 )]. Concomitant use of Meperidine Hydrochloride Tablets and Oral Solution with Monoamine Oxidase Inhibitors (MAOIs) Concomitant use of Meperidine Hydrochloride Tablets or Oral Solution with monoamine oxidase inhibitors (MAOIs) can result in coma, severe respiratory depression, cyanosis, and hypotension. Use of Meperidine Hydrochloride Tablets or Oral Solution with MAOIs within last 14 days is contraindicated [see Contraindications ( 4 ), Warnings and Precautions ( 5.8 ), Drug Interactions ( 7 )]. WARNING: SERIOUS AND LIFE-THREATENING RISKS FROM USE OF MEPERIDINE HYDROCHLORIDE TABLETS AND ORAL SOLUTION See full prescribing information for complete boxed warning. • Ensure accuracy when prescribing, dispensing, and administering Meperidine Hydrochloride Oral Solution. Dosing errors due to confusion between mg and mL, and other Meperidine Hydrochloride Oral Solutions of different concentrations can result in accidental overdose and death. ( 2.1, 5.1 ) • Meperidine Hydrochloride Tablets and Oral Solution expose users to risks of addiction, abuse, and misuse, which can lead to overdose and death. Assess patient’s risk before prescribing and reassess regularly for these behaviors and conditions. ( 5.2 ) • Serious, life-threatening, or fatal respiratory depression may occur, especially upon initiation or following a dosage increase. To reduce the risk of respiratory depression, proper dosing and titration of Meperidine Hydrochloride Tablets or Oral Solution are essential. ( 5.3 ) • Accidental ingestion of Meperidine Hydrochloride Tablets or Oral Solution, especially by children, can result in a fatal overdose of meperidine. ( 5.4 ) • Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing for use in patients for whom alternative treatment options are inadequate. ( 5.7 , 7 ) • Advise pregnant women using opioids for an extended period of time of the risk of Neonatal Opioid Withdrawal Syndrome, which may be life-threatening if not recognized and treated. Ensure that management by neonatology experts will be available at delivery . ( 5.5 ) • Healthcare providers are strongly encouraged to complete a REMS-compliant education program and to counsel patients and caregivers on serious risks, safe use, and the importance of reading the Medication Guide with each prescription. ( 5.6 ) • Concomitant use with CYP3A4 inhibitors (or discontinuation of CYP3A4 inducers) can result in fatal overdose of meperidine. ( 5.6 , 7 ) • Concomitant use of Meperidine Hydrochloride Tablets or Oral Solution with monoamine oxidase inhibitors (MAOIs) can result in coma, severe respiratory depression, cyanosis and hypotension. Use of Meperidine Hydrochloride Tablets or Oral Solution with MAOIs within the last 14 days is contraindicated. ( 4 , 5.8 , 6 )
Common side effects
- Lightheadedness
- Dizziness
- Sedation
- Nausea
- Vomiting
- Sweating
- Headache
- Agitation
- Tremor
- Involuntary muscle movements
- Seizures
- Constipation
Drug interactions
- Monoamine Oxidase Inhibitors (MAOIs)
- Inhibitors of CYP3A4 and CYP2B6
Key clinical trials
- TEAS for Sedation During ERCP: A Multicenter Trial (NA)
- Postoperative Analgesia and Ventilation After Cardiac Surgery
- E7 TCR T Cells for Human Papillomavirus-Associated Cancers (PHASE1, PHASE2)
- Sacral Erector Spinae Plane Block in Transurethral Prostate Resection Surgery (NA)
- The Effect of Parental Anxiety Level on the Child's Anxiety Level and Postoperative Pain in Children Undergoing Surgery.
- Interscalene Block vs Serratus Posterior Superior Intercostal Plane Block (NA)
- Ultrasound-Guided Regional Blocks for Postoperative Analgesia After Laparoscopic Cholecystectomy (NA)
- Ultrasound Guided TAPB vs Surgical TAPB With Bupivacaine in Cesarean Section (NA)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- MEPERIDINE CI brief — competitive landscape report
- MEPERIDINE updates RSS · CI watch RSS