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NERVOUS SYSTEM › ANALGESICS › OPIOIDS › Opioids in combination with antispasmodics
ketobemidone and antispasmodics
N02AG02
Forms & Strengths
- Combination product: Ketobemidone hydrochloride combined with antispasmodic agents (e.g., benzylpenicillin derivative spasmo-ketobemidone)
- Parenteral injection solution
- Oral tablets/suppositories (jurisdiction-dependent)
Adult Dosing
- Severe acute pain with visceral spasm: 2.5 mg to 5 mg subcutaneously or intramuscularly, repeated every 4 to 6 hours as needed
- Intravenous administration: Slow IV injection under close hemodynamic monitoring
- Maximum daily dose: Determined by individual opioid tolerance and clinical response
Pediatric Dosing
- Safety and efficacy in pediatric patients not established
- Use generally avoided in children due to potent opioid agonist risks and lack of standardized dosing guidelines
Indications
- Management of severe acute pain accompanied by visceral smooth muscle spasm
- Renal colic and biliary colic
Mechanism of Action
- Ketobemidone: Potent mu-opioid receptor agonist providing central analgesia and altering pain perception
- Antispasmodic component: Relaxes visceral smooth muscle via anticholinergic or direct relaxant mechanisms, synergizing with opioid analgesia
Contraindications
- Hypersensitivity to ketobemidone or any antispasmodic components
- Acute respiratory depression or severe chronic obstructive airway disease
- Paralytic ileus or gastrointestinal obstruction
- Acute angle-closure glaucoma (due to antispasmodic component)
- Severe hepatic impairment
- Concomitant use with MAO inhibitors or within 14 days of cessation
Adverse Reactions
- Respiratory depression and apnea
- Sedation, dizziness, and cognitive impairment
- Hypotension and orthostatic hypotension
- Constipation, nausea, and vomiting
- Urinary retention (compounded by antispasmodic effect)
- Dry mouth, blurred vision, and tachycardia (antispasmodic-related)
- Opioid dependence, tolerance, and withdrawal syndrome with prolonged use
Drug Interactions
- Central nervous system depressants (alcohol, benzodiazepines, barbiturates): Enhanced sedation, respiratory depression, and hypotension
- MAO inhibitors: Risk of severe, potentially fatal CNS excitation or depression (serotonergic crisis)
- Anticholinergic drugs: Increased risk of severe constipation, urinary retention, and dry mouth
- Potent CYP inhibitors/inducers: Potential alteration of ketobemidone metabolism
Curated Content: Needs Vetting Before Put to Clinical Use