Zemuron

Generic Name: Rocuronium Bromide
Class: Neuromuscular Blocking Agents
VA Class: MS200
Chemical Name: 1-[(2β,3α,5α,16β,17β)-17-(acetyloxy)-3-hydroxy-2-(4-morpholinyl) androstan-16-yl]-1-(2-propenyl)-pyrrolidinium bromide
Molecular Formula: C₃₂H₅₃N₂O₄•Br
CAS Number: 119302-91-9

• 
  

  Should be administered only under supervision of qualified clinicians experienced in the administration of neuromuscular blocking agent therapy.¹

  
  

Introduction

Nondepolarizing neuromuscular blocking agent.^{1 9}

Uses for Zemuron

Skeletal Muscle Relaxation

Production of skeletal muscle relaxation during surgery after general anesthesia has been induced.¹

Facilitation of endotracheal intubation.^{1 2 3 6 7}

Treatment to increase pulmonary compliance during assisted or controlled respiration.¹

Zemuron Dosage and Administration

General

• 
  

  Adjust dosage carefully according to individual requirements and response.¹

  
  


• 
  

  Assess neuromuscular blockade and recovery in patients undergoing anesthesia; a peripheral nerve stimulator is recommended to accurately monitor the degree of muscle relaxation and to minimize the possibility of overdosage.¹

  
  


• 
  

  To avoid patient distress, administer only after unconsciousness has been induced.¹

  
  

Facilitation of Endotracheal Intubation

• 
  

  Endotracheal intubation for nonemergency surgical procedures generally can be performed in about 1 minute following administration of 0.6-mg/kg dose.¹ (See Onset and also Duration under Pharmacokinetics.)

  
  


• 
  

  Good to excellent conditions for rapid sequence intubation result in <2 minutes following dose of 0.6–1.2 mg/kg in appropriately premedicated and adequately anesthetized patients.¹

  
  

Maintenance of Neuromuscular Blockade

• 
  

  Repeated administration of maintenance doses does not have a clinically important, cumulative effect on neuromuscular blockade.¹

  
  


• 
  

  Rate of spontaneous recovery from neuromuscular blockade following discontinuance of maintenance infusion usually is comparable to that following administration of intermittent IV injections.¹

  
  

Reversal of Neuromuscular Blockade

• 
  

  To reverse neuromuscular blockade, administer a cholinesterase inhibitor (e.g., neostigmine, pyridostigmine, edrophonium), usually in conjunction with an antimuscarinic (e.g., atropine, glycopyrrolate) to block adverse muscarinic effects of the cholinesterase inhibitor.^a

  
  

Administration

IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administer IV only.¹ Administer initial (intubating) dose by rapid IV injection; administer maintenance dosage by intermittent IV injection or continuous IV infusion.¹

Consult specialized references for specific procedures and techniques of administration.^a

Do not mix in the same syringe or administer through the same needle as an alkaline solution.¹

Dilution

For continuous IV infusion, dilute rocuronium bromide injection to the desired concentration (usually 0.5 or 1 mg/mL) in a compatible IV infusion solution (see Solution Compatibility under Stability).¹ Use within 24 hours.¹

Dosage

Available as rocuronium bromide; dosage expressed in terms of the salt.¹

Pediatric Patients

Skeletal Muscle Relaxation

Initial (Intubating) Dosage

IV

Children 3 months to 14 years of age: 0.6 mg/kg when used concomitantly with halothane anesthesia.¹ (See Onset and also Duration under Pharmacokinetics.)

Maintenance Dosage

Intermittent IV Injection

Children 3 months to 14 years of age: 0.075–0.125 mg/kg provides clinically sufficient neuromuscular blockade for about 7–10 minutes.¹ Initiate intermittent maintenance doses once neuromuscular blockade has returned to 25% of control.¹ (See Onset and also Duration under Pharmacokinetics.)

Children 1–12 years of age may require more frequent doses than adults.¹

Continuous IV Infusion

Children 3 months to 14 years of age: 12 mcg/kg per minute; initiate continuous IV infusion once neuromuscular blockade has returned to 10% of control.¹

Adults

Skeletal Muscle Relaxation

Initial (Intubating) Dosage

IV

0.6 mg/kg.¹ May use smaller initial dose (i.e., 0.45 mg/kg).¹ If a larger initial dose is considered necessary, 0.9 or 1.2 mg/kg.¹ (See Onset and also Duration under Pharmacokinetics.)

0.6–1.2 mg/kg for rapid sequence intubation in appropriately premedicated and adequately anesthetized patients.¹

Maintenance Dosage

Intermittent IV Injection

0.1, 0.15, or 0.2 mg/kg when used concomitantly with balanced anesthesia.¹ (See Onset and also Duration under Pharmacokinetics.)

Initiate intermittent maintenance doses once neuromuscular blockade has returned to 25% of control.¹

Continuous IV Infusion

Initially, 10–12 mcg/kg per minute.¹ Individualize dosage when desired level of neuromuscular block is attained; 4–16 mcg/kg per minute usually is required.¹

Initiate continuous IV infusion once neuromuscular blockade has returned to 10% of control.¹

May need to reduce infusion rate by about 30–50% approximately 45–60 minutes following the initial IV dose if steady-state anesthesia has been induced with enflurane or isoflurane.¹

Special Populations

Hepatic Impairment

Increased initial dosage may be required during rapid sequence induction to achieve effective neuromuscular blockade (however, doses >0.6 mg/kg have not been evaluated); once blockade is established, duration may be prolonged.¹ (See Hepatic Impairment under Cautions.)

Renal Impairment

Dosage adjustments not required.¹ (See Renal Impairment under Cautions.)

Geriatric Patients

Dosage adjustments not required.¹ (See Geriatric Use under Cautions.)

Burn Patients

Substantially increased doses may be required due to development of resistance.^a (See Burn Patients under Cautions.)

Obese Patients

Base dosage on actual body weight.¹

Patients with Neuromuscular Disease

Administer small test dose; monitor degree of neuromuscular blockade with a peripheral nerve stimulator to determine dosage requirements.¹ (See Neuromuscular Disease under Cautions.)

Other Populations

Patients in whom potentiation of neuromuscular blockade or difficulties with reversal of blockade may occur (e.g., patients with carcinomatosis, cachectic or debilitated patients): Consider reduced initial dosage.¹

Cautions for Zemuron

Contraindications

• 
  

  Known hypersensitivity to rocuronium bromide or any ingredient in the formulation.¹

  
  

Warnings/Precautions

Warnings

Respiratory Effects

Potential for severely compromised respiratory function and respiratory paralysis.^a

Should be used only by individuals experienced in the use of neuromuscular blocking agents and in the maintenance of an adequate airway and respiratory support.¹ Facilities and personnel necessary for intubation, administration of oxygen, and assisted or controlled respiration should be immediately available.¹

IV cholinesterase inhibitor (e.g., neostigmine, pyridostigmine, edrophonium) should be readily available.¹ (See Reversal of Neuromuscular Blockade under Dosage and Administration.)

Use with caution in patients with pulmonary impairment or respiratory depression.^a

Neuromuscular Disease

Possible profound neuromuscular blockade in patients with neuromuscular disease (e.g., myasthenia gravis, Eaton-Lambert syndrome).¹

Administer small test dose; monitor degree of neuromuscular blockade with a peripheral nerve stimulator.¹

Sensitivity Reactions

Hypersensitivity Reactions

Serious and occasionally fatal hypersensitivity reactions, including anaphylaxis, reported.¹

Caution in patients with a history of anaphylactic reaction to other neuromuscular blocking agents; potential for cross-sensitivity.¹

General Precautions

Burn Patients

Resistance to therapy with neuromuscular blocking agents can develop in burn patients,¹ particularly those with burns over 25–30% or more of body surface area.^a

Resistance generally becomes apparent ≥1 week after the burn,^a peaks ≥2 weeks after the burn,^a persists for several months or longer,^a and decreases gradually with healing.^a

Consider possible need for substantially increased doses.^a

Histamine Release

Histamine release or adverse effects associated with histamine release (e.g., bronchospasm, urticaria, flushing) reported rarely.¹

Cardiovascular Effects

Possible increased pulmonary vascular resistance; use with caution in patients with pulmonary hypertension or valvular heart disease.¹

Intensive Care Setting

Possible development of tolerance to neuromuscular blocking agent therapy.¹ Possible prolonged paralysis and/or muscle weakness and atrophy.¹

Continuous monitoring of neuromuscular transmission recommended during neuromuscular blocking agent therapy in intensive care setting.¹ Do not administer additional doses before there is a definite response to nerve stimulation tests.¹

Impaired Circulation

Possible delayed onset of action in patients with impaired circulation (e.g., cardiovascular disease).¹ Larger-than-usual initial doses generally are not recommended; when feasible, allow additional time for onset of clinically sufficient neuromuscular blockade.¹

Electrolyte Disturbances

Possible increased or decreased neuromuscular blockade in patients with electrolyte disturbances (e.g., diarrhea, adrenocortical insufficiency) or acid/base imbalances.^{1 a}

Malignant Hyperthermia

Malignant hyperthermia is rarely associated with use of neuromuscular blocking agents and/or potent inhalation anesthetics.^a Be vigilant for its possible development and prepared for its management in any patient undergoing general anesthesia.¹

Rocuronium has not been evaluated in patients susceptible to malignant hyperthermia.¹

Local Effects

Possible local irritation; discontinue injection and restart in another vein if extravasation occurs.¹

Specific Populations

Pregnancy

Category C.¹

Possible poor or inadequate intubating conditions following rapid sequence induction in cesarean section patients; use not recommended for rapid sequence induction in such patients.¹

Lactation

Not known whether rocuronium is distributed into milk.¹

Pediatric Use

Safety and efficacy not established in children <3 months of age or >14 years of age.¹

Geriatric Use

Slightly slower onset and slightly increased duration of neuromuscular blockade; however, recovery time in patients ≥65 years of age does not appear to differ from that in younger adults.¹

Hepatic Impairment

Possible incomplete neuromuscular blockade; increased initial dosage may be required.¹ See Hepatic Impairment under Dosage and Administration.

Use with caution.¹ Possible increase in half-life, duration of neuromuscular blockade, and recovery time.¹ (See Special Populations under Absorption and also under Elimination, in Pharmacokinetics.)

Renal Impairment

No substantial differences in pharmacokinetic profile relative to patients without renal impairment.¹ (See Absorption: Special Populations, under Pharmacokinetics.)

Common Adverse Effects

Skeletal muscle weakness.^a

Interactions for Zemuron

Specific Drugs

Drug	Interaction	Comments
Anesthetics, general (enflurane, isoflurane)	Increased potency and prolonged duration of neuromuscular blockadea	Reduced rocuronium infusion rate may be required1 (See Dosage under Dosage and Administration)
Anesthetics, local	Possible increased neuromuscular blockade1	Reduced initial rocuronium dosage may be required1
Anticonvulsants (carbamazepine, phenytoin)	Possible decreased duration and degree of neuromuscular blockade1	Higher rocuronium infusion rates may be required1
Anti-infectives (e.g., aminoglycosides, bacitracin, polymyxins, tetracyclines, vancomycin)	Possible prolonged duration of neuromuscular blockade1	Reduced initial rocuronium dosage may be required1
Lithium	Possible increased neuromuscular blockade1	Reduced initial rocuronium dosage may be required1
Magnesium salts	Increased neuromuscular blockade1	Use with caution; reduce rocuronium dosage if necessary a
Procainamide	Possible increased neuromuscular blockade1	Reduced initial rocuronium dosage may be required1
Propofol	Change in duration of, or recovery from, neuromuscular blockade unlikely1
Quinidine	Possible increased neuromuscular blockade; possible recurrence of paralysis1	Reduced initial rocuronium dosage may be required1
Succinylcholine		Administer rocuronium only after patient has recovered form succinylcholine-induced neuromuscular blockade1

Zemuron Pharmacokinetics

Absorption

Bioavailability

Poorly absorbed from the GI tract.^a

Onset

Onset of action is slower than that of succinylcholine but more rapid than that of most other currently available nondepolarizing agents.^{2 3 4 5 6 7 8}

Onset of neuromuscular blockade is more rapid in pediatric patients than adults.¹

Following IV administration of 0.45 or 0.6 mg/kg in adults, neuromuscular blockade is clinically sufficient in about 1.3 (range 0.8–6.2) or 1 (range: 0.4–6) minute, respectively, and is maximal in <4 or <3 minutes, respectively.¹

Maximum neuromuscular blockade generally occurs within 1 minute in children 3 months to 12 years of age.¹

Duration

Following initial dose of 0.45 or 0.6 mg/kg under balanced anesthesia in adults, clinically sufficient neuromuscular blockade persists for about 22 (range: 12–31) or 31 (range: 15–85) minutes, respectively.¹ Following initial adult dose of 0.9 or 1.2 mg/kg, clinically sufficient neuromuscular blockade persists for about 58 (range: 27–111) or 67 (range: 38–160) minutes, respectively.¹

Following initial dose of 0.6 mg/kg under halothane anesthesia in children 3–12 months of age or >1–12 years of age, clinically sufficient neuromuscular blockade generally persists for about 41 (range: 24–68) or 26 (range: 17–39) minutes, respectively.¹

Following maintenance doses of 0.1, 0.15, or 0.2 mg/kg in adults receiving balanced anesthesia, clinically sufficient neuromuscular blockade persists for about 12 (range: 2–31), 17 (range: 6–50), or 24 (range: 7–69) minutes, respectively.¹

Following maintenance doses of 0.075–0.125 mg/kg in children, clinically sufficient neuromuscular blockade persists for 7–10 minutes.¹

The time necessary for 25–75% recovery from neuromuscular blockade in adults is about 13 minutes.¹

Spontaneous recovery from neuromuscular blockade in children 3–12 months of age generally proceeds at a rate comparable to that in adults; recovery is more rapid in children 1–12 years of age.¹

Special Populations

In patients with hepatic impairment, prolonged duration of neuromuscular blockade.¹

In patients with renal failure, no substantial change in onset or duration of neuromuscular blockade; however, interindividual variation in duration may be greater.¹

In geriatric patients, slightly slower onset and slightly prolonged duration of neuromuscular blockade.¹

Distribution

Plasma Protein Binding

About 30%.¹

Special Populations

In patients with hepatic impairment, increased volume of distribution.¹

Elimination

Metabolism

Metabolized to a less active metabolite, 17-desacetyl-rocuronium.¹

Elimination Route

Eliminated primarily by the liver.¹

Half-life

Triphasic; terminal half-life is 1.4 or 2.4 hours during balanced anesthesia or isoflurane anesthesia, respectively.¹

Special Populations

In patients with hepatic impairment, terminal half-life is 4.3 hours during isoflurane anesthesia.¹

Stability

Storage

Parenteral

Injection

2–8°C; do not freeze.¹

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility¹

Compatible
Dextrose 5% in water
Sodium chloride 0.9%
Dextrose 5% in sodium chloride 0.9%
Ringer's injection, lactated

Drug Compatibility

Y-Site CompatibilityHID

Compatible
Dexmedetomidine HCl
Fenoldopam mesylate
Hetastarch in lactated electrolyte injection (Hextend)
Milrinone lactate

ActionsActions

• 
  

  Produces skeletal muscle relaxation by causing a decreased response to acetylcholine (ACh) at the myoneural (neuromuscular) junction of skeletal muscle.^a

  
  


• 
  

  Exhibits high affinity for ACh receptor sites and competitively blocks access of ACh to motor end-plate of myoneural junction; may affect ACh release.^{1 a}

  
  


• 
  

  Blocks the effects of both the small quantities of ACh that maintain muscle tone and the large quantities of ACh that produce voluntary skeletal muscle contraction; does not alter the resting electrical potential of the motor end-plate or cause muscular contractions.^a

  
  


• 
  

  Appears to have little, if any, histamine-releasing activity.^{1 a}

  
  

Advice to Patients

• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.¹

  
  


• 
  

  Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular disease, neuromuscular disease).¹

  
  


• 
  

  Importance of informing patients of other important precautionary information.¹ (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Rocuronium Bromide

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	Injection, for IV use only	10 mg/mL	Zemuron	Organon

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions July 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Organon. Zemuron (rocuronium bromide) injection prescribing information. West Orange, NJ: 2002 Jun.

2. Puhringer FK, Khuenl-Brady KS, Koller J et al. Evaluation of the endotracheal intubating conditions of rocuronium (ORG 9426) and succinylcholine in outpatient surgery. Anesth Analg. 1993; 76:904-5.

3. Huizinga AC, Vandenbrom RH, Wierda JM et al. Intubating conditions and onset of neuromuscular block of rocuronium (Org 9426); a comparison with suxamethonium. Acta Anaesthesiol Scand. 1992; 36:463-8. [PubMed 1321542]

4. Magorian T, Flannery KB, Miller RD. Comparison of rocuronium, succinylcholine, and vecuronium for rapid-sequence induction of anesthesia in adult patients. Anesthesiology. 1993; 79:913-8. [IDIS 322375] [PubMed 7902034]

5. Bartkowski RR, Witkowski TA, Azad S et al. Rocuronium onset of action: a comparison with atracurium and vecuronium. Anesth Analg. 1993; 77:574-8. [IDIS 319830] [PubMed 8103649]

6. Cooper R, Mirakhur RK, Clarke RS et al. Comparison of intubating conditions after administration of Org 9246 (rocuronium) and suxamethonium. Br J Anaesth. 1992; 69:269-73. [IDIS 302324] [PubMed 1389845]

7. Mirakhur RK. Newer neuromuscular blocking drugs: an overview of their clinical pharmacology and therapeutic use. Drugs. 1992; 44:182-99. [PubMed 1382013]

8. Agoston S, Vandenbrom RHG, Wierda JMKH. Clinical pharmacokinetics of neuromuscular blocking drugs. Clin Pharmacokinet. 1992; 22:94-115. [PubMed 1551294]

9. Organon, West Orange, NJ: Personal communication.

a. AHFS Drug Information 2004. McEvoy GK, ed. Neuromuscular Blocking Agents General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2004:1303-6.

HID. Trissel LA. Handbook on injectable drugs. 14th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2007:1463-4.

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