CISATRACURIUM BESYLATE PRESERVATIVE FREE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CISATRACURIUM BESYLATE PRESERVATIVE FREE (CISATRACURIUM BESYLATE PRESERVATIVE FREE).
Competitive antagonist at nicotinic acetylcholine receptors at the neuromuscular junction, blocking acetylcholine binding and preventing muscle contraction.
| Metabolism | Hofmann elimination (pH- and temperature-dependent spontaneous degradation) forming laudanosine and monoquaternary acrylate; lauded by ester hydrolysis (nonspecific plasma esterases). |
| Excretion | Renal (77%) and fecal (11%) as unchanged drug. Minor hepatic metabolism via Hofmann elimination (non-enzymatic) and ester hydrolysis. No active metabolites. |
| Half-life | Terminal elimination half-life is approximately 22-29 minutes in patients with normal renal and hepatic function. Clinical context: Recovery of neuromuscular function is predictable and independent of organ function due to Hofmann elimination. |
| Protein binding | Approximately 37-44% bound to plasma proteins (mainly albumin). |
| Volume of Distribution | Volume of distribution at steady state is approximately 0.15-0.2 L/kg. Clinical meaning: Indicates limited distribution outside the vascular space. |
| Bioavailability | Intravenous: 100% (only route used). Not administered orally or via other routes. |
| Onset of Action | Intravenous: 1.5-2 minutes (intubating dose 0.15-0.2 mg/kg). Onset is similar to atracurium but with less histamine release. |
| Duration of Action | Clinical duration (25% recovery of T1) is 25-35 minutes after intubating dose. Spontaneous recovery to 95% T1 in 45-55 minutes. Reversible with neostigmine or sugammadex (non-depolarizing relaxant). |
Initial bolus: 0.15-0.2 mg/kg IV; maintenance infusion: 1-3 mcg/kg/min IV titrated to desired neuromuscular blockade.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment (GFR >10 mL/min); for severe renal impairment (GFR <10 mL/min), monitor for prolonged recovery. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B); for severe hepatic impairment (Child-Pugh C), consider reduced initial dose and titrate carefully due to prolonged duration. |
| Pediatric use | Infants (1-23 months): initial bolus 0.15 mg/kg IV; Children (2-12 years): initial bolus 0.1-0.15 mg/kg IV; maintenance infusion: 1-2 mcg/kg/min IV; Adolescents: same as adult dosing. |
| Geriatric use | Elderly patients (>65 years): consider reduced initial bolus (0.1-0.15 mg/kg IV) and lower infusion rates (1-2 mcg/kg/min IV) due to prolonged recovery time and reduced clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CISATRACURIUM BESYLATE PRESERVATIVE FREE (CISATRACURIUM BESYLATE PRESERVATIVE FREE).
| Breastfeeding | It is unknown if cisatracurium is excreted in human breast milk. The manufacturer recommends caution. Due to its quaternary ammonium structure and low lipid solubility, excretion into breast milk is expected to be minimal. No M/P ratio is available. The short half-life and intravenous administration further limit systemic exposure to the infant. |
| Teratogenic Risk | Cisatracurium besylate is a non-depolarizing neuromuscular blocker. Animal studies have not demonstrated teratogenicity. In pregnant women, there are no adequate and well-controlled studies. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Since it is a quaternary ammonium compound, placental transfer is limited, but minimal amounts may cross the placenta, especially in the third trimester. No specific fetal risks have been identified. |
■ FDA Black Box Warning
Cisatracurium should be administered only by adequately trained individuals familiar with its actions, characteristics, and hazards. Facilities for intubation, artificial respiration, oxygen therapy, and an antagonist must be immediately available. Cisatracurium has no known effect on consciousness, pain threshold, or cerebration.
| Serious Effects |
Known hypersensitivity to cisatracurium or other bisbenzylisoquinolinium agents; conditions in which the use of neuromuscular blocking agents is contraindicated (e.g., after acute phase of tetanus).
| Precautions | Risk of profound and prolonged neuromuscular blockade; potential for histamine release (less than other neuromuscular blockers); caution in patients with neuromuscular diseases (e.g., myasthenia gravis); extravasation may cause tissue damage; anaphylaxis risk. |
| Food/Dietary | No known food interactions. No dietary restrictions. |
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| Fetal Monitoring | Monitor maternal vital signs, oxygen saturation, and neuromuscular function with a peripheral nerve stimulator. Continuous fetal heart rate monitoring is recommended during cesarean section to assess fetal well-being. Prepare for neonatal resuscitation as residual neuromuscular blockade could occur. |
| Fertility Effects | No data are available on the effect of cisatracurium on human fertility. Animal studies have not reported adverse effects on fertility. |
| Clinical Pearls | Cisatracurium is a nondepolarizing neuromuscular blocker that undergoes Hofmann elimination, making it safe in patients with renal or hepatic impairment. It does not cause histamine release, so minimal hemodynamic changes occur. Reversal with sugammadex is effective. Use 2x ED95 for intubation; duration ~45-60 min. Monitor train-of-four for recovery. |
| Patient Advice | This medication causes temporary paralysis and requires mechanical ventilation. · You will be unconscious and not feel pain during surgery due to anesthesia. · After surgery, the effects will be reversed, and you will regain muscle control. · Inform your doctor if you have kidney or liver disease, as no dose adjustment is needed. · Report any history of allergic reactions to muscle relaxants. |