Rocuronium (Esmeron) - Uses, Dose, Side effects, MOA, Brands

Rocuronium Bromide (Esmeron) is a widely used neuromuscular blocking drug in patients undergoing mechanical ventilation, tracheal intubations, and surgical procedures.

Rocuronium (Esmeron) Uses:

  • Neuromuscular blockade for endotracheal intubation, surgery, or mechanical ventilation:

    • As an adjunct to general anesthesia to help rapid sequence and routine tracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation in appropriately sedated ICU patients

Note:

  • The neuromuscular blockade does not provide pain control, sedation, or amnestic effects.
  • Appropriate analgesic and sedative mediations should be used before and during the administration of neuromuscular blockade to achieve deep sedation.
  • Off Label Use of Rocuronium in Adults:

    • Acute respiratory distress syndrome;
    • Intensive care unit paralysis:;
    • Preinduction defasciculation:;
    • Shivering due to therapeutic hypothermia following cardiac arrest

Rocuronium (Esmeron) Dose in Adults

Note:

  • Dose to effect; doses will vary due to interpatient variability.
  • Ensure adequate pain control and sedation before and during the administration of neuromuscular blockade to achieve deep sedation.

Rocuronium (Esmeron) Dose in the Intensive care unit for paralysis (eg, use for up to 48 hours in patients with early ARDS with PaO2 /FiO2 <150, to facilitate mechanical ventilation, or for shivering from therapeutic hypothermia) (off-label dosing):

  • Initial bolus of 0.6 to 1 mg/kg.
  • Followed by continuous IV infusion of 8 to 12 mcg/kg/minute (0.48 to 0.72 mg/kg/hour);
  • monitor the depth of blockade every 2 to 3 hours initially until a stable dose, then every 8 to 12 hours.
  • Adjust the rate of administration by 10% up-titration according to the desired clinical response and possibly with peripheral nerve stimulation.

Note:

  • When possible, minimize the depth and duration of paralysis.
  • Stop the infusion for some time until forced to restart based on a patient condition is recommended to reduce postparalytic complications (eg, acute quadriplegic myopathy syndrome [AQMS]).
  • Intermittent dosing:

    • Initial loading dose: 50 mg followed by 25 mg given when peripheral nerve stimulation returns.

Rocuronium (Esmeron) Dose in the treatment of Neuromuscular blockade for endotracheal intubation, surgery, or mechanical ventilation (as an adjunct to general anesthesia):

  • Rapid sequence intubation:

    • IV: 0.6 to 1.2 mg/kg
  • Dose in Obese patients:
    • In adult patients with morbid obesity (BMI >40 kg/m²), the use of 1.2 mg/kg using ideal body weight (IBW) provided a short onset of action and excellent or good intubating conditions at 60 seconds in one study.

Rocuronium (Esmeron) Dose for Tracheal intubation: IV:

  • Initial: 0.45 to 0.6 mg/kg;
  • administration of 0.3 mg/kg may also provide optimal conditions for tracheal intubation.

Rocuronium (Esmeron) Dose in Obese patients:

  • May use ideal body weight (IBW) for morbidly obese (BMI >40 kg/m²) adult patients.
  • The onset time may be slightly prolonged using IBW.
  • The manufacturer recommends dosing based on actual body weight in all obese patients.
  • Maintenance for continued surgical relaxation:

    • 1 to 0.2 mg/kg; repeat as needed or a continuous infusion of 10 to 12 mcg/kg/minute (0.6 to 0.72 mg/kg/hour) only after recovery of neuromuscular function; infusion rates range from 4 to 16 mcg/kg/minute (0.24 to 0.96 mg/kg/hour)

Note: Inhaled anesthetic agents prolong the duration of action of rocuronium. Use the lower end of the dosing range; redosing interval guided by monitoring with a peripheral nerve stimulator.

Rocuronium (Esmeron) Dose in the treatment of Pre-induction defasciculation (off-label):

  • IV: 0.03 to 0.06 mg/kg given 1.5 to 3 minutes before the administration of succinylcholine.

Rocuronium (Esmeron) Dose in Children

Note:

  • Dose to effect; doses will vary due to interpatient variability.
  • Dosing depends on the anesthetic technique and age of the patient.
  • In general, the onset of effect is shortened and duration is prolonged as the dose increases.
  • The time to maximum nerve block is shortest in infants 1 to 3 months; the duration of relaxation is shortest in children 2 to 11 years and longest in infants.
  • The manufacturer recommends dosing based on actual body weight in all obese patients; however, some have recommended dosing based on ideal body weight (IBW) in obese patients.

Rapid sequence intubation:

  • Children and Adolescents:

    • IV: 0.9 to 1.2 mg/kg;
    • Note:
      • Lower doses of 0.6 mg/kg have been reported in the literature; however, some studies found this dosing resulted in a prolonged time to onset, shortened duration of neuromuscular blockade, and less favorable intubating conditions.

Tracheal intubation, surgical:

  • Infants, Children, and Adolescents:

Note:

  • Inhaled anesthetic agents prolong the duration of action of rocuronium;
  • Use the lower end of the dosing range; dosing interval guided by monitoring with a peripheral nerve stimulator.
    • Initial: IV: 0.45 to 0.6 mg/kg
    • IM administration: Limited data available:

Note:

  • Due to the prolonged time to onset in some patients, IM dosing may not be ideal for rapid sequence intubation for the general population and should be reserved for case scenarios where alternative agents are not appropriate.
      • Infants ≥3 months:
        • 1 mg/kg administered as a single dose
      • Children 1 to 6 years:
        • 8 mg/kg administered as a single dose
    • Maintenance for continued surgical relaxation:

      • Intermittent IV dosing: Infants, Children, and Adolescents:
        • 0.075 to 0.15 mg/kg;
        • The dose may be repeated as required
      • Continuous IV infusion: Infants, Children, and Adolescents:
        • 7 to 12 mcg/kg/minute (0.42 to 0.72 mg/kg/hour); the manufacturer recommends using the lower end of the dosing range for infants and the upper end for children >2 to ≤11 years of age;
        • higher doses have been reported with prolonged infusions.

Pregnancy Risk Category: B

  • Animal reproduction studies did not show any adverse events.
  • Rocuronium crosses into the placenta. The umbilical vein plasma levels are approximately 18% of the maternal concentration following a maternal dose of 0.6% mg/kg.
  • Manufacturer does not recommend rapid sequence induction during a cesarean section.

Use of rocuronium while breastfeeding

  • We have not found any information regarding rocuronium and breastfeeding. A nursing infant should not absorb rocuronium if it is present in breast milk.

Dose in Kidney Disease:

  • No dosage adjustment is necessary.
  • The duration of neuromuscular blockade may vary in patients with renal dysfunction.

Rocuronium (Esmeron) Dose in Liver disease:

  • The manufacturer's labeling does not provide any dosage adjustments.
  • Patients with liver disease may need to adjust their dosage.
  • An increased volume of distribution may prolong the duration of neuromuscular blocking.
  • Adult patients suffering from ascites may require rapid sequence intubation.
  • In this case, it is possible to use a higher dose of the medication in order to provide adequate neuromuscular blockade.

Side effects of Rocuronium (Esmeron):

  • Cardiovascular:

    • Increased Peripheral Vascular Resistance
    • Tachycardia
    • Hypertension
    • Transient Hypotension
  • Hypersensitivity:

    • Anaphylaxis

Contraindications to Rocuronium (Esmeron):

  • Hypersensitivity to rocuronium or other neuromuscular-blocking drugs, or any component in the formulation, can lead to anaphylaxis.

Warnings and precautions

  • Anaphylactoid reactions and hypersensitivity reactions

    • You have been treated immediately for hypersensitivity reactions and anaphylactoid symptoms (epinephrine 1mg/mL)
  • Cross-sensitivity of neuromuscular neurons:

    • Cross-sensitivity may occur with other neuromuscular-blocking drugs; contraindicated for patients who have had anaphylactic reactions.
  • Paralysis for a prolonged period

    • Patients may experience prolonged recovery of neuromuscular function following administration, especially after prolonged use. Before extubation, patients should be fully recovered. You should also consider other factors that can prolong recovery, such as corticosteroid use and patient condition.
  • Burn injury

    • Patients with burn injuries may develop resistance (>=20% total body surface area). This usually occurs within a few days of the injury and can last several months.
  • Cardiovascular disease

    • Patients with heart disease, such as heart failure, should be cautious. The onset and duration may be longer.
  • Conditions that could lead to neuromuscular blockade (decreased parity)

    • Antagonism of neuromuscular blocking may be caused by hypercalcemia, respiratory alkalosis and peripheral neuropathies.
  • Conditions that can cause neuromuscular blockade (increased parity):

    • An electrolyte imbalance (eg, severe hypercalcemia, severe hypokalemia or hypermagnesemia), can lead to neuromuscular blockade.
  • Hepatic impairment

    • Patients with hepatic impairment should be cautious; the clinical duration could be longer.
  • Hypertension in the lungs:

    • Patients with pulmonary hypertension should be cautious; it may worsen right-heart failure symptoms.
  • Respiratory disease

    • Patients with respiratory diseases should be cautious.
  • Heart disease of the valvular kind:

    • Patients with valvular disease should be cautious; it may cause an increase in pulmonary vascular resistance.

Rocuronium: Drug Interaction

Risk Factor C (Monitor therapy)

Acetylcholinesterase Inhibitors

May diminish the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).

Aminoglycosides

May enhance the respiratory depressant effect of Neuromuscular-Blocking Agents.

Bacitracin (Systemic)

May enhance the neuromuscular-blocking effect of NeuromuscularBlocking Agents.

Botulinum Toxin-Containing Products

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Bromperidol

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Calcium Channel Blockers

May enhance the neuromuscular-blocking effect of NeuromuscularBlocking Agents (Nondepolarizing).

Capreomycin

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

CarBAMazepine

May decrease the serum concentration of Neuromuscular-Blocking Agents (Nondepolarizing).

Cardiac Glycosides

Neuromuscular-Blocking Agents may enhance the arrhythmogenic effect of Cardiac Glycosides.

Clindamycin (Topical)

May enhance the neuromuscular-blocking effect of NeuromuscularBlocking Agents.

CycloSPORINE (Systemic)

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

EPHEDrine (Systemic)

May enhance the therapeutic effect of Rocuronium.

Fosphenytoin-Phenytoin

May diminish the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). Fosphenytoin-Phenytoin may enhance the neuromuscular blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). Fosphenytoin-Phenytoin may decrease the serum concentration of Neuromuscular-Blocking Agents (Nondepolarizing).

Inhalational Anesthetics

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).

Ketorolac (Nasal)

May enhance the adverse/toxic effect of Neuromuscular-Blocking Agents (Nondepolarizing). Specifically, episodes of apnea have been reported in patients using this combination.

Ketorolac (Systemic)

May enhance the adverse/toxic effect of Neuromuscular-Blocking Agents (Nondepolarizing). Specifically, episodes of apnea have been reported in patients using this combination.

Lincosamide Antibiotics

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Lithium

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Local Anesthetics

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Exceptions: Benzocaine; Benzydamine; Cocaine (Topical); Dibucaine; Dyclonine; Ethyl Chloride; Hexylresorcinol; Lidocaine (Ophthalmic); Lidocaine (Topical); Pramoxine; Proparacaine; Tetracaine (Ophthalmic); Tetracaine (Topical).

Loop Diuretics

May diminish the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Loop Diuretics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Magnesium Salts

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Minocycline

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Pholcodine

May enhance the adverse/toxic effect of Neuromuscular-Blocking Agents. Specifically, anaphylaxis has been reported.

Procainamide

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

QuiNIDine

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Spironolactone

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).

Tetracyclines

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Thiazide and Thiazide-Like Diuretics

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).

Trimebutine

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing).

Vancomycin

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Risk Factor D (Consider therapy modification)

Colistimethate

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Corticosteroids (Systemic)

Neuromuscular-Blocking Agents (Nondepolarizing) may enhance the adverse neuromuscular effect of Corticosteroids (Systemic). Increased muscle weakness, possibly progressing to polyneuropathies and myopathies, may occur.

Polymyxin B

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Risk Factor X (Avoid combination)

QuiNINE

May enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents.

Monitoring parameters:

  • Vital signs (heart rate and blood pressure, respiratory rate)
  • The degree of muscle paralysis (eg., presence of spontaneous movements, ventilator asynchrony and shivering) and whether a peripheral nerve stimulator is used with monitoring and clinical assessments.
  • If the level of blockade is properly monitored in the ICU, prolonged paralysis or generalized myopathy may be reduced.

How to administer Rocuronium (Esmeron)?

It may be administered as a bolus intravenous undiluted injection or via a continuous infusion.

Mechanism of action of Rocuronium (Esmeron):

Depolarization is inhibited by blocking acetylcholine binding to motor endplate receptors

The beginning of action:

  • Children =3 months, Infants =3 Months: 30 seconds to 1 Minute
  • Adults: Excellent intubation conditions within 1 - 2 minutes, depending on the dose given; maximum neuromuscular blockade within four minutes

Time:

  • Infants 3-12 months: 40 minutes
  • Children 1-12 years old: 26-30 minutes
  • Adults: 30 minutes with standard doses. The duration may be extended if you take inhalational or intramuscular anesthetics. Hypothermia can prolong the action.

Protein binding:

  • ~30%

Metabolism:

  • Minimally hepatic; 17-desacetylrocuronium (5% to 10% activity of parent drug)

Half-life elimination:

  • Alpha elimination:
    • 1 to 2 minutes
  • Beta elimination:
    • Infants 3 to 12 months: 1.3 ± 0.5 hours
    • Children 1 to <3 years: 1.1 ± 0.7 hours
    • Children 3 to <8 years: 0.8 ± 0.3 hours
    • Adults: 1.4 to 2.4 hours
    • Hepatic impairment: 4.3 hours
    • Renal impairment: 2.4 hours

Excretion:

  • Feces (31%);
  • urine (26%).

International Brands of Rocuronium:

  • Zemuron
  • Curionialis
  • Desproxyl
  • Eslax
  • Esmeron
  • Kabiroc
  • Noveron
  • Rocon
  • Rocoron
  • Rocum
  • Rocumeron
  • Rocur
  • Rocuron
  • Rocuronio
  • Rocuthesia
  • Romeron

Rocuronium Brands Names in Pakistan:

Rocuronium Bromide Injection 50 mg in Pakistan

Esmeron OBS

 

Rocuronium Bromide Injection 100 mg in Pakistan

Esmeron OBS