ZEMURON
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZEMURON (ZEMURON).
Rocuronium is a nondepolarizing neuromuscular blocking agent that competitively binds to nicotinic acetylcholine receptors at the motor endplate, preventing acetylcholine from inducing muscle contraction.
| Metabolism | Primarily hepatic via CYP3A4; minor metabolism via CYP2C9; also undergoes deacetylation. Approximately 30% excreted unchanged in urine. |
| Excretion | Primarily renal (70-80% as unchanged drug and metabolites) and biliary (20-30% as unchanged drug and metabolites). |
| Half-life | Terminal elimination half-life is approximately 2.3 hours (range 1.7-3.1 hours) in adults with normal renal function. Clinical context: May be prolonged in hepatic or renal impairment. |
| Protein binding | Approximately 30% bound, mainly to albumin and globulins. |
| Volume of Distribution | Vd: 0.3-0.6 L/kg. Clinical meaning: Indicates extensive distribution into extracellular fluid. |
| Bioavailability | Not applicable; only administered IV, thus bioavailability is 100%. |
| Onset of Action | IV: 60-90 seconds (intubating dose 0.6 mg/kg). |
| Duration of Action | IV: Approximately 30-45 minutes (clinical duration of neuromuscular block) after initial intubating dose; longer with higher doses or after multiple maintenance doses. Recovery to 25% of control twitch height: ~20-30 min. |
0.6-1.2 mg/kg IV bolus for intubation; maintenance 0.1-0.2 mg/kg IV as needed for neuromuscular blockade.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment; prolonged effect may occur in renal impairment; monitor recovery. |
| Liver impairment | Child-Pugh A/B: No adjustment; Child-Pugh C: Caution, may have prolonged duration. |
| Pediatric use | Infants 1-12 months: 0.15 mg/kg IV; Children 1-12 years: 0.6 mg/kg IV for intubation; maintenance 0.075-0.125 mg/kg IV. |
| Geriatric use | Consider lower doses; increased sensitivity and prolonged recovery; monitor neuromuscular function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZEMURON (ZEMURON).
| Breastfeeding | Excretion in human milk unknown. Caution advised. M/P ratio not documented. Consider discontinuing nursing or drug, taking into account importance of drug to mother. |
| Teratogenic Risk | Pregnancy Category C. No adequate and well-controlled studies in pregnant women. Fetal risk cannot be ruled out. Use only if potential benefit justifies potential risk to fetus. In animal studies, no teratogenic effects observed at doses up to 0.2 mg/kg IV in rats and rabbits. |
| Fetal Monitoring |
■ FDA Black Box Warning
Appropriate administration and monitoring of rocuronium require the availability of resuscitative equipment and trained personnel. Use only by individuals skilled in airway management and respiratory support.
| Serious Effects |
["Known hypersensitivity to rocuronium or any component of the formulation"]
| Precautions | ["Can cause anaphylaxis","May potentiate neuromuscular blockade in patients with neuromuscular diseases (e.g., myasthenia gravis)","Risk of residual paralysis","Acid-base or electrolyte disturbances may alter effects","Prolonged use in ICU may result in prolonged paralysis and myopathy"] |
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| Monitor maternal vital signs, oxygen saturation, and neuromuscular function with train-of-four monitoring. Fetal heart rate monitoring recommended if used during cesarean section. |
| Fertility Effects | No human data on fertility effects. In animal studies, no impairment of fertility observed at doses up to 0.2 mg/kg IV. |