CISATRACURIUM BESYLATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CISATRACURIUM BESYLATE (CISATRACURIUM BESYLATE).
Competitive antagonist at nicotinic acetylcholine receptors at the neuromuscular junction, blocking neurotransmission and causing muscle paralysis.
| Metabolism | Undergoes Hoffman elimination (pH- and temperature-dependent degradation) and ester hydrolysis; metabolites are primarily inactive. |
| Excretion | Renal (77%) and fecal/biliary (23%); unchanged drug eliminated primarily via renal excretion; Hofmann elimination (non-enzymatic degradation) accounts for ~80% of clearance. |
| Half-life | Terminal elimination half-life is 22–29 minutes in patients with normal renal and hepatic function; prolonged to ~30–40 minutes in elderly or patients with renal impairment; independent of hepatic function. |
| Protein binding | ~32% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Steady-state volume of distribution (Vdss) is 0.11–0.18 L/kg (approximately 8–12 L in adults), indicating distribution primarily in extracellular fluid. |
| Bioavailability | Intravenous: 100%; not available for oral or intramuscular use. |
| Onset of Action | Intravenous: 1–2 minutes to achieve good intubating conditions; maximum neuromuscular block within 2–3 minutes. |
| Duration of Action | Clinical duration (time to 25% recovery of T1) is 45–60 minutes after an intubating dose of 0.15–0.2 mg/kg; recovery index (25–75% recovery) is 10–20 minutes; suitable for continuous infusion with rapid recovery regardless of infusion duration. |
Initial IV bolus: 0.15-0.2 mg/kg (2×ED95) for intubation; maintenance: 0.03 mg/kg as needed or continuous infusion at 1-2 mcg/kg/min adjusted to twitch response. Titrate to train-of-four count of 1-2 twitches.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min or renal failure, consider monitoring neuromuscular blockade duration; no specific dose reduction recommended. Cisatracurium undergoes Hofmann elimination independent of renal function. |
| Liver impairment | No dose adjustment required for Child-Pugh A or B. For Child-Pugh C, consider slightly prolonged duration; no specific dose reduction recommended. Metabolism via Hofmann elimination not affected by hepatic function. |
| Pediatric use | Infants 1-23 months: initial 0.15 mg/kg IV; maintenance 1-2 mcg/kg/min. Children 2-12 years: initial 0.1-0.15 mg/kg; maintenance 1-2 mcg/kg/min. Adolescents ≥13 years: same as adult dosing. |
| Geriatric use | Elderly patients may have slower onset and prolonged duration; reduce initial dose to 0.1-0.15 mg/kg and titrate infusion rate (start at 1 mcg/kg/min). Monitor neuromuscular function closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CISATRACURIUM BESYLATE (CISATRACURIUM BESYLATE).
| Breastfeeding | Unknown if excreted in human milk; minimal risk expected due to low oral bioavailability and short half-life. M/P ratio not determined. |
| Teratogenic Risk | No evidence of teratogenicity in animal studies; limited human data. Use only if clearly needed in all trimesters. Neuromuscular blocking agents are not expected to cause structural anomalies. |
| Fetal Monitoring |
■ FDA Black Box Warning
Appropriate administration by experienced clinicians; only with adequate facilities for intubation, ventilation, and oxygen supplementation; risk of prolonged paralysis; anaphylaxis risk.
| Serious Effects |
Hypersensitivity to cisatracurium or other bis-benzylisoquinolinium agents; known anaphylaxis to similar agents.
| Precautions | Risk of residual neuromuscular blockade; anaphylaxis; history of malignant hyperthermia; prolonged use may lead to muscle weakness; caution in patients with neuromuscular diseases, electrolyte disturbances, acidosis, or hypothermia. |
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| Monitor maternal vital signs, oxygen saturation, and neuromuscular blockade with train-of-four monitoring. Continuous fetal heart rate monitoring if viable fetus. |
| Fertility Effects | No known adverse effects on human fertility; no reproductive toxicity studies available. |