Drug information of Cis atracurium

Cis atracurium

Drug group:

Cisatracurium is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium is used to relax the muscles. It works by blocking the signals between your nerves and your muscles.

Cisatracurium is given before general anesthesia in preparing you for surgery. Cisatracurium helps keep your body still during surgery. It also relaxes your throat so a breathing tube can be more easily inserted before the surgery.

As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action.

Mechanism of effect

Cisatracurium besylate binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in block of neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine.

Pharmacokinetics

 Onset of action: IV: 2-3 minutes

Peak effect: 3-5 minutes

Duration: Dose dependent, 35 to 45 minutes after a single 0.1 mg/kg dose; recovery begins in 20-35 minutes when anesthesia is balanced

Distribution: Vdss: 145 mL/kg

Protein binding: Not studied due to rapid degradation at physiologic pH

Metabolism: Undergoes rapid nonenzymatic degradation in the bloodstream (Hofmann elimination) to laudanosine and inactive metabolites

Half-life elimination: 22-29 minutes

Excretion: Urine (95%; <10% as unchanged drug); feces (4%)

Clearance: Children: 5.89 mL/kg/minute; Adults: 4.57 mL/kg/minute

Dosage

 Neuromuscular blockade: IV (not to be used IM):

Operating room administration:

Intubating dose: 0.15-0.2 mg/kg as components of propofol/nitrous oxide/oxygen induction-intubation technique.

 (Note: May produce generally good or

excellent conditions for tracheal intubation in 1.5-2 minutes with clinically effective duration of action during propofol anesthesia of 55-61 minutes.)

Initial dose after succinylcholine for intubation: 0.1 mg/kg; maintenance dose: 0.03 mg/kg 40-60 minutes after initial dose, then at ~20-minute intervals

based on clinical criteria.

 

Continuous infusion: After an initial bolus, a diluted solution can be given by continuous infusion for maintenance of neuromuscular blockade during extended

surgery; adjust the rate of administration according to the patient's response as determined by peripheral nerve stimulation. An initial infusion rate of 3

mcg/kg/minute (0.18 mg/kg/hour) may be required to rapidly counteract the spontaneous recovery of neuromuscular function; thereafter, a rate of 1-2

mcg/kg/minute (0.06-0.12 mg/kg/hour) should be adequate to maintain continuous neuromuscular block in the 89% to 99% range in most pediatric

and adult patients. Consider reduction of the infusion rate by 30% to 40% when administering during stable isoflurane, enflurane, sevoflurane, or

desflurane anesthesia. Spontaneous recovery from neuromuscular blockade following discontinuation of infusion of cisatracurium may be expected to

proceed at a rate comparable to that following single bolus administration.

 

Intensive care unit administration:

Loading dose: 0.15-0.2 mg/kg; at initial signs of recovery from bolus dose, begin the infusion at a dose of 3 mcg/kg/minute (0.18

mg/kg/hour) and adjust rate accordingly (follow the principles for infusion in the operating room); dosage ranges of 0.5-10 mcg/kg/minute (0.03-0.6

mg/kg/hour) have been reported. If patient is allowed to recover from neuromuscular blockade, readministration of a bolus dose may be necessary to

quickly re-establish neuromuscular block prior to reinstituting the infusion.

Alerts

  • Bradycardia: May be more common with cisatracurium than with other neuromuscular-blocking agents since it has no clinically-significant effects on heart

rate to counteract the bradycardia produced by anesthetics.

  • Cross-sensitivity with other neuromuscular-blocking agents may occur; use extreme caution in patients with previous

anaphylactic reactions to other neuromuscular-blocking agents.

  • Burn injury: Resistance may occur in burn patients (≥20% of total body surface area), usually several days after the injury, and may persist for several

months after wound healing

  • Conditions which may antagonize neuromuscular blockade: Respiratory alkalosis, hypercalcemia, demyelinating lesions, peripheral neuropathies,

denervation, and muscle trauma may result in antagonism of neuromuscular blockade

  • Conditions which may potentiate neuromuscular blockade: Electrolyte abnormalities (eg, severe hypocalcemia, severe hypokalemia, hypermagnesemia),

neuromuscular diseases, metabolic acidosis, metabolic alkalosis, respiratory acidosis, Eaton-Lambert syndrome and myasthenia gravis may result in

potentiation of neuromuscular blockade

Points of recommendation

Administer IV only; give undiluted as bolus injection over 5-10 seconds. Continuous infusion requires the use of an infusion pump. The 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.

Do not administer IM (excessive tissue irritation).

Pregnancy level

B


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