ROCULAX®
Description
Roculax® is a nondepolarizing neuromuscular blocking agent, supplied as a sterile, nonpyrogenic,
isotonic solution for intravenous injection only.
Composition
Each ampoule of Roculax® contains Rocuronium bromide 10 mg/mL.
Pharmacology
Pharmacodynamics :
Rocuronium bromide acts by competing for cholinergic receptors at the motor end-plate. This
action is antagonized by acetylcholinesterase inhibitors, such as neostigmine and edrophonium. The
recovery of neuromuscular function is satisfactory. The neuromuscular blocking action of
rocuronium bromide may be enhanced in the presence of potent inhalation anaesthetics.
Pharmacokinetics :
Rocuronium is a nondepolarizing neuromuscular agent with rapid to intermediate onset depending
on dose, and intermediate duration. The rapid distribution half-life is 1-2 minutes and the slower
distribution half-life is 14-18 minutes. Rocuronium is approximately 30% bound to human plasma
proteins. Rocuronium is eliminated primarily by the liver. The metabolite of rocuronium,17desacetyl-rocuronium, has been rarely observed in the plasma or urine of humans administered
single doses of 0.5-1 mg/kgBW with or without a subsequent infusion of rocuronium.
Indications
Roculax® is indicated as an adjunct to general anesthesia to facilitate endotracheal intubation, and to
provide skeletal muscle relaxation during surgery.
Contraindications
Roculax® is contraindicated in :
- Patients known to have hypersensitivity to rocuronium bromide or to bromide ion.
- Pregnancy.
Warnings and Precautions
- Roculax® should be administered in carefully adjusted dosages under the supervision of
experienced clinicians who are familiar with the drug’s actions and the possible complications
of its use. Roculax® should not be administrated unless facilities for intubation, artificial
respiration, oxygen therapy, and an antagonist are immediately available. It is recommended
that administration of Roculax® employ a peripheral nerve stimulator to monitor drug response,
need for additional relaxant, and adequacy of spontaneous recovery or antagonism.
- Roculax® administration must be accompanied by adequate anaesthesia or sedation.
- In patients with myasthenia gravis, small doses of nondepolarizing neuromuscular blocking
agents may have profound effects.
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Roculax®, which has an acid pH, should not be mixed with alkaline solutions (e.g. barbiturate
solutions) in the same syringe or administered simultaneously during intravenous infusion
through the same needle.
In the use of Roculax®, increases or decreases in MAP (Mean Arterial Pressure) and
tachycardia may occurred. Most of the pediatric patients developed tachycardia were
anaesthetized with halothane and who did not receive atropine for induction. Laryngoscopy and
tracheal intubation following Roculax® administration were accompanied by transient
tachycardia (≥ 30 % increment) in adult patients under opioid/ N2O/O2 anaesthesia. The
tachycardia observed in some patients may result from this vagal blocking activity.
Prolonged paralysis and/or skeletal muscle weakness may be noted during initial attempts to
wean from the ventilator patients who have chronically received neuromuscular blocking drugs
in the ICU. So Roculax® should only be used if the specific advantages of the drug outweigh the
risk.
Roculax® is not recommended for rapid induction in cesarean section patients.
Roculax® should be used with caution in patients with clinically significant hepatic disease
because clinial duration and the recovery was moderately prolonged in these patients.
Both respiratory and metabolic acidosis prolonged the recovery time. The potency of Roculax®
was significantly enhanced in metabolic acidosis and alkalosis, but was reduced in respiratory
alkalosis.
Severe acid-base and/or electrolyte abnormalities may potentiate or cause resistance to the
neuromuscular blocking action of Roculax®.
Extravasation of Roculax® may result signs or symptoms of local irritation; the injection or
infusion should be terminated immediately and restarted in another vein.
Burns, disuse atrophy, denervation, direct muscle trauma, and cerebral palsy may result the
development of resistance to nondepolarizing muscle relaxants.
Other nondepolarizing neuromuscular blocking agents exhibit profound neuromuscular blocking
effects in cachectic or debilitated patients, patients with neuromuscular diseases, and patients
with carcinomatosis. In these patients a decrease from the recommended initial dose should be
considered.
Roculax® may be associated with increased pulmonary vascular resistance so caution in patients
with pulmonary hypertension or valvular heart disease.
Anaphylactic reactions to neuromuscular blocking agents in general have been reported
Because Roculax® is always used with other agents and because the occurrence of malignant
hyperthermia during anaesthesia is possible, even in the absence of known triggering agents,
clinicians should be familiar with early signs, confirmatory diagnosis and treatment of
malignant hyperthermia prior to the start of any anaesthesia.
Roculax® should be used with caution in patients with clinically significant hepatic and/ or
billiary tract diseases and/ or renal failure.
Conditions associated with prolonged circulation time such as cardiovascular disease, old age,
and oedematous state resulting in an increased volume of distribution, may contribute to a
slower onset of action.
Like other neuromuscular blocking agents, Roculax® should be used with extreme caution in
patients with a neuromuscular disease or after poliomyelitis since the response to neuromuscular
blocking agents may be considerably altered in these cases.
In surgery under hypothermic condition, the neuromuscular blocking effect of Roculax® is
increased and the duration prolonged.
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Roculax® may exhibit a prolonged duration and a prolonged spontaneous recovery in obese
patients.
Roculax® should be given to lactating women only when the physician decides that the benefits
outweigh the risk.
It is not recommended to use potentially dangerous machinery or drive a car within 24 hours
after the full recovery from the neuromuscular blocking action of Roculax®.
Adverse Effects
Prolonged neuromuscular block is associated with neuromuscular blockers.
Adverse experiences with probable or unknown relationship:
Cardiovascular
: arrhythmia, abnormal electrocardiogram, tachycardia, hypotension,
hypertension.
Digestive
: nausea, vomiting.
Respiratory
: asthma (bronchospasm, wheezing, or rhonchi), hiccup.
Skin and Appendages : allergic reactions (rash, pruritus, anaphylactic and anaphylactoid),
injection site edema.
Dosage and Administration
- Endotracheal Intubation :
The dose is 0.6-1.2 mg/kgBW.
- Maintenance Dose:
The maintenance dose is 0.1- 0.2 mg/kgBW.
- Use by Continuous Infusion:
It is recommended to give loading dose of 0.6 mg Roculax®/kgBW, when neuromuscular block
starts to recover, to start administration by infusion. In adults under i.v anaesthesia, the infusion
rate required to maintain neuromuscular block at this level ranges from 5-10 g/kgBW/min
(0,3-0,6 mg/kg/h). Continuous monitoring of neuromuscular block is essential since infusion
rate requirements vary from patient to patient and with the anaesthetic method used.
- Pediatrics :
The initial dose is 0.6 mg/kgBW. The maintenance dose is 0.075-0.125 mg/kgBW.
A continuous infusion of Roculax initiated at a rate of 0.012 mg/kgBW/min may also be used to
maintain neuromuscular blockade in pediatric patients.
There are no data to support the recommendation for the use of rocuronium bromide in neonates
(0-3 months).
- Geriatrics ( ≥ 65 years) and patients with hepatic and/or biliary tract disease and/or renal
failure :
The dose is 0.6 - 1.2 mg/kgBW. The maintenance dose is 0.075-0.1 mg/kgBW.
The recommended infusion rate is 5-6 g/kgBW/min.
- Obese Patients :
When used in overweight or obese patients (defined as patients with a body weight of 30% or
more above ideal body weight) doses should be reduced taking into account a lean body mass.
Administration: Roculax® administered intravenously either as a bolus injection or as a continuous
infusion.
Presentation
Ampoules 5 mL in box @ 10 ampoules.
Roculax® should be stored under refrigeration (2 - 8)°C. Do not freeze. Upon removal from
refrigeration to room temperature storage conditions (25°C), use Roculax® within 60 days. Do not
use solution if particulate matter is present.