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NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Phenylpiperidine derivatives
pethidine, combinations with psycholeptics
N02AB72
Forms & Strengths
- Pethidine combined with psycholeptic agents (e.g., phenothiazines)
- Parenteral injection solutions
- Oral tablet formulations containing fixed-dose narcotic-psycholeptic combinations
Adult Dosing
- Individualized based on severity of pain and patient response
- Pethidine component typically 50 mg to 150 mg per dose
- Administered orally or intramuscularly as needed at 4-hour intervals
- Maximum daily dose restricted to limit cumulative toxicity of active metabolites
Pediatric Dosing
- Not generally recommended for pediatric use due to risks of neurotoxicity and respiratory depression
- If used, dosing must be strictly calculated based on body weight under specialist supervision
Indications
- Management of moderate to severe acute pain unresponsive to non-opioid analgesics
- Short-term adjunctive relief where sedation and analgesia are concurrently required
Mechanism of Action
- Pethidine acts as a mu-opioid receptor agonist producing central analgesia and sedation
- Psycholeptic component acts as a central nervous system depressant to augment sedation and reduce anxiety
Contraindications
- Hypersensitivity to pethidine, psycholeptics, or any component of the formulation
- Concomitant use with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing them
- Severe respiratory depression or acute bronchial asthma
- Paralytic ileus or significant gastrointestinal obstruction
- Severe hepatic impairment
Adverse Reactions
- Central nervous system depression, excessive sedation, dizziness, and confusion
- Respiratory depression and hypoventilation
- Hypotension, orthostatic hypotension, and syncope
- Nausea, vomiting, constipation, and dry mouth
- Neurotoxicity, tremors, myoclonus, and seizures due to normeperidine accumulation
- Extrapyramidal symptoms related to the psycholeptic component
Drug Interactions
- Severe risk of serotonin syndrome or fatal CNS excitation with MAOI antidepressants
- Profound CNS depression, respiratory depression, and hypotension when combined with alcohol, barbiturates, or other CNS depressants
- Potentiation of anticholinergic effects when combined with drugs possessing anticholinergic properties
- Inhibition of pethidine metabolism by CYP3A4 and CYP2B6 inhibitors
Curated Content: Needs Vetting Before Put to Clinical Use