Medication Guide App

Cisatracurium Besylate

Pronunciation: SIS-at-ra-KURE-ee-um BES-i-late
Class: Nondepolarizing neuromuscular blocker

Trade Names

Nimbex
- Injection, solution 2 mg/mL
- Injection, solution 10 mg/mL

Pharmacology

Binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in block of neuromuscular transmission.

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Pharmacokinetics

Distribution

Vd at steady state is 145 mL/kg.

Metabolism

Undergoes Hofmann elimination (a pH- and temperature-dependent chemical process) to form laudanosine and a monoquarternary acrylate metabolite (both metabolites are inactive).

Elimination

Cl is 4.5 to 5.7 mL/min/kg; 80% is a result of Hofmann elimination and 20% by renal and hepatic elimination. 95% of the dose is recovered in the urine (less than 10% is unchanged drug); 4% is recovered in the feces. Half-life is 22 to 29 min.

Special Populations

Renal Function Impairment

The times to 90% block were approximately 1 min slower in patients with ESRD. The half-life values of the metabolites are longer in patients with renal failure and concentrations may be higher after long-term administration.

Hepatic Function Impairment

The times to max block were approximately 1 min faster in liver transplant patients compared with healthy adults. The half-life values of the metabolites are longer in patients with hepatic disease and concentrations may be higher after long-term administration.

Elderly

The times to max block were approximately 1 min slower in elderly patients.

Children

Minor differences in pharmacokinetic/pharmacodynamic parameters in children resulted in a faster time to onset and a shorter duration of neuromuscular block.

Indications and Usage

For inpatients and outpatients as adjunct to general anesthesia, to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation in the intensive care unit (ICU).

Contraindications

Hypersensitivity to the product or its components.

Multiple-dose vial

Premature infants.

Dosage and Administration

Bolus
Adults

IV Initial doses of 0.15 and 0.2 mg/kg, as components of a propofol/nitrous oxide/oxygen induction-intubation technique, may produce generally good or excellent conditions for tracheal intubation in 2 and 1.5 min, respectively. Maintenance dose of 0.03 mg/kg sustains neuromuscular block for approximately 20 min; for shorter or longer durations of action, smaller or larger maintenance doses may be administered.

Children 2 to 12 y of age

IV 0.1 to 0.15 mg/kg over 5 to 10 sec during either halothane or opioid anesthesia. When given during stable opioid/nitrous oxide/oxygen anesthesia, 0.1 mg/kg produces max neuromuscular block in an average of 2.8 min and clinically effective block for 28 min, while 0.15 mg/kg produces max neuromuscular block in an average of 3 min and clinically effective block for 36 min.

Children 1 to 23 mo of age

IV 0.15 mg/kg administered over 5 to 10 sec during halothane or opioid anesthesia. When given during stable opioid/nitrous oxide/oxygen anesthesia, 0.15 mg/kg produces max neuromuscular block in an average of 2 min and clinically effective block for 43 min.

Continuous Infusion in the Operating Room
Adults and Children 2 y and older

IV Initiate the infusion only after early evidence of spontaneous recovery from the initial bolus dose; an initial rate of 3 mcg/kg/min may be needed to rapidly counteract spontaneous recovery. A rate of 1 to 2 mcg/kg/min should be adequate to maintain continuous neuromuscular block. Adjust rate of administration according to the patient's response as determined by peripheral nerve stimulation. Consider reduction of the infusion rate by 30% to 40% when administered during stable isoflurane or enflurane anesthesia.

Infusion in ICU
Adults

IV Approximately 3 mcg/kg/min (range, 0.5 to 10.2 mcg/kg/min) should provide adequate neuromuscular block. Following recovery from neuromuscular block, readministration of a bolus dose may be necessary to quickly reestablish neuromuscular block prior to reinstitution of the infusion. Use in the ICU for longer than 6 days has not been studied.

Neuromuscular disease

A dose of no more than cisatracurium 0.02 mg/kg is recommended to assess the level of neuromuscular block and to monitor dosage requirements.

Elderly patients/renal function impairment

Extending the interval between administration of cisatracurium and the intubation attempt may be required to achieve adequate intubation condition.

General Advice

  • Individualize dose, especially in patients with preexisting conditions and/or in burn patients.
  • Use of a peripheral nerve stimulator will permit the most advantageous use of cisatracurium, minimize the possibility of overdosage or underdosage, and assist in the evaluation of recovery.
  • Administer IV only. Follow manufacturer's instructions for preparation and storage of solutions for continuous IV infusion. Refer to the manufacturer's prescribing information for infusion rates.
  • Cisatracurium is compatible with dextrose 5% injection; sodium chloride 0.9% injection; dextrose 5% and sodium chloride 0.9% injection; and sufentanil, alfentanil, fentanyl, midazolam, and droperidol, diluted as directed.
  • Cisatracurium may not be compatible with alkaline solutions having a pH greater than 8.5 (eg, barbiturate solutions) and should not be diluted with Ringer's lactate injection. Not compatible with propofol or ketorolac for Y-site administration.
  • Inspect solution visually before administration. Solution may have a slightly yellow or greenish-yellow color. Do not administer if solution is cloudy or discolored, or contains particulate matter.

Storage/Stability

Store between 36° and 46°F in original carton. Do not freeze. Protect from light. May be removed from refrigerator and stored at 77°F but injection must be used within 21 days even if re-refrigerated.

Drug Interactions

Antibiotics (eg, aminoglycosides [eg, kanamycin], bacitracin, clindamycin, lincomycin, polymyxins, sodium colistimethate, tetracyclines), cyclosporine, ketamine, lithium, local anesthetics (eg, lidocaine), magnesium salts, procainamide, quinidine, verapamil

May enhance the neuromuscular blocking action of cisatracurium. Use with caution. Carefully titrate the dose of cisatracurium and closely monitor neuromuscular function. Provide mechanical respiratory support as needed.

Carbamazepine, hydantoins (eg, phenytoin)

Resistance to neuromuscular blocking action of cisatracurium may occur. Monitor for decreased cisatracurium effect and adjust the dose as needed.

General anesthetics (eg, enflurane, isoflurane)

May potentiate the action of cisatracurium. In long surgical procedures during enflurane or isoflurane anesthesia, less frequent maintenance dosing, lower maintenance doses, or reduced infusion rates may be necessary. The average infusion rate requirement may be decreased as much as 30% to 40%.

Theophyllines

Neuromuscular blocking effects of cisatracurium may be decreased. Cardiac arrhythmia may occur. Dosing requirements of cisatracurium may be increased. Consider avoiding coadministration.

Thiazide diuretics (eg, chlorothiazide)

The neuromuscular blocking effects of cisatracurium may be increased because of thiazide diuretic–induced hypokalemia. Prolonged respiratory depression with extended periods of apnea may occur. If hypokalemia cannot be corrected, a lower cisatracurium dose may be needed.

Adverse Reactions

Cardiovascular

Bradycardia, hypotension.

Dermatologic

Rash; itching (postmarketing).

Hypersensitivity

Histamine release, hypersensitivity reactions including anaphylactic or anaphylactoid reactions, itching, laryngospasm, wheezing (postmarketing).

Musculoskeletal

Inadequate neuromuscular block, muscle weakness, myopathy, prolonged neuromuscular block (postmarketing).

Respiratory

Bronchospasm.

Miscellaneous

Flushing.

Precautions

Monitor

A peripheral nerve stimulator should be used to measure neuromuscular function during the administration of cisatracurium in order to monitor drug effect, determine the need for additional doses, and confirm recovery from neuromuscular block.


Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 1 mo.

Elderly

The time of max block is approximately 1 min slower in patients older than 65 y.

Hypersensitivity

Severe anaphylactic reactions, in some cases fatal and life-threatening, to neuromuscular blocking agents, including cisatracurium, have been reported.

Renal Function

The onset time was approximately 1 min slower in patients with renal dysfunction compared with healthy adults.

Hepatic Function

The onset time was approximately 1 min faster in patients with end-stage liver disease compared with healthy adults.

Administration

Use under the supervision of experienced clinicians who are familiar with cisatracurium action and complications. Personnel and facilities for resuscitation and life support and an antagonist of cisatracurium should be immediately available. Cisatracurium has no effect on consciousness, pain threshold, or cerebration; to avoid distress to the patients, do not induce neuromuscular block before unconsciousness.

Benzyl alcohol

The 10 mL multiple-dose vial contains benzyl alcohol, which has been associated with neurological and other complications that are sometimes fatal in neonates.

Endotracheal intubation

Because of intermediate onset, not recommended for rapid sequence endotracheal intubation.

Malignant hyperthermia

May occur.

Neuromuscular function

To avoid inaccurate dosing in patient with hemiparesis or paraparesis, monitor neuromuscular function on a nonparetic limb.

Special populations

May have profound effect in patients with neuromuscular disease (eg, myasthenia gravis). Patients with burns, hemiparesis, or paraparesis may have resistance to cisatracurium. Acid-base or serum electrolyte imbalance may potentiate or antagonize the action of cisatracurium.

Overdosage

Symptoms

Prolonged neuromuscular block.

Patient Information

  • Advise patient, family, or caregiver that medication will be prepared and administered by a health care provider in a health care setting.
  • Reassure patient, family, or caregiver that breathing will be closely monitored and supported while medication is being administered and that breathing and muscle function will return to normal after medication has been discontinued.
  • Inform patients that severe anaphylactic reactions to neuromuscular blocking agents, including cisatracurium, have been reported; request information about previous anaphylactic reactions to other agents.

Copyright © 2009 Wolters Kluwer Health.

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