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NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Phenylpiperidine derivatives
pethidine
N02AB02
Forms & Strengths
- Injection: 50 mg/mL, 100 mg/mL
- Oral Syrup: 50 mg/5 mL
- Oral Tablet: 50 mg, 100 mg
Adult Dosing
- Acute pain (IM/SC/IV): 50-150 mg every 3-4 hours as needed
- Obstetric analgesia (IM/SC): 50-100 mg when labor is well established
- Max daily dose: Generally not to exceed 600 mg/24 hours due to neurotoxic metabolite accumulation
Pediatric Dosing
- Pain (IM/SC/IV): 1-1.5 mg/kg every 4-6 hours as needed
- Max single dose: 100 mg
Indications
- Management of moderate to severe acute pain
- Rigors associated with transfusion reactions
- Obstetric analgesia during labor
Mechanism of Action
- Full agonist at mu-opioid receptors in the central nervous system
- Weak serotonin reuptake inhibitor
- Possesses local anesthetic properties via sodium channel blockade
Contraindications
- Concomitant monoamine oxidase inhibitor (MAOI) use or use within the past 14 days
- Significant respiratory depression
- Acute or severe bronchial asthma in an unmonitored setting
- Known or suspected gastrointestinal obstruction, including paralytic ileus
Adverse Reactions
- Respiratory depression
- Central nervous system excitation (seizures, tremors, myoclonus due to normeperidine accumulation)
- Serotonin syndrome (when combined with serotonergic agents)
- Hypotension, dizziness, and sedation
- Nausea, vomiting, and constipation
Drug Interactions
- MAOIs: Severe, fatal reactions including hyperpyrexia, excitation, and hypertension
- Serotonergic drugs (SSRIs, SNRIs, TCAs): Increased risk of serotonin syndrome
- CNS depressants (alcohol, benzodiazepines, general anesthetics): Profound sedation, respiratory depression, and hypotension
- CYP3A4 inducers (phenytoin, ritonavir, rifampin): Increased formation of the toxic metabolite normeperidine
Curated Content: Needs Vetting Before Put to Clinical Use