It is a non-depolarizing neuromuscular blocking drug , of intermediate action and with a rapid onset of action, which exhibits all the pharmacological actions characteristic of this class of drugs (curariform). It acts by competing for the nicotinic cholinergic receptors of the terminal motor plate; this action is antagonized by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine.
International non-proprietary name
Rocuronium bromide.
Composition
Each bulb contains 50 mg of rocuronium bromide.
Pharmacokinetics
- Following IV administration of a single bolus dose, the plasma concentration follows 3 exponential phases. In normal adults, the mean (95% CI) elimination half-life is 73 (66-80) min, the apparent Vd at equilibrium is 203 (193-214) mL / kg, and plasma clearance is 3.7 (3.5-3.9) mL / kg / min. In controlled studies, plasma clearance in geriatric patients and in patients with renal impairment was reduced. * In patients with hepatic impairment, the mean elimination half-life is prolonged by 30 min and the mean plasma clearance is reduced by 1 mL / kg / min.
- When given as a continuous infusion to facilitate mechanical ventilation for 20 h or longer, the mean elimination half-life and apparent Vd at steady state (mean) are increased. In controlled clinical studies, great variability is observed between patients, depending on the nature and importance of multiorgan failure and the characteristics of the patients.
- The drug is excreted in the urine and bile . Urinary excretion is approximately 40%, from 12 to 24 hours. Following injection of a dose of radioisotope-labeled rocuronium bromide, the mean excretion is 47% in the urine and 43% in the faeces after 9 days. Approximately 50% is recovered in its unaltered form. No metabolites are detected in plasma.
Indications
As an adjunct to general anesthesia to facilitate tracheal intubation during routine and rapid sequence induction, as well as to achieve skeletal muscle relaxation during surgery . It is also indicated as an adjunct in the intensive care unit, for short-term use, with the aim of facilitating tracheal intubation and mechanical ventilation.
Contraindications
Hypersensitivity to the drug or to the bromide ion or to any of the excipients.
Precautions
- E: data on drug use are limited .
- Work delivery , delivery and cesarean section : limited studies report that can be used in the technique of rapid sequence induction in patients undergoing surgery for cesarean section, provided that no difficulties are foreseen in the intubation has been administered a dose sufficient anesthetic or after suxamethonium intubation; In addition, it does not modify the assessment of the Apgar index, nor the fetal muscle tone or the cardiorespiratory adaptation.
- LM: avoid, no known human data. Other similar drugs show small levels of excretion in breast milk and therefore a slight reabsorption from the infant. Animal studies show negligible levels of the drug in breast milk. In making the decision to continue or discontinue breastfeeding, the benefit of breastfeeding should be considered against the potential risk to the child.
- Children: there are studies of use in endotracheal intubation and routine anesthesia. The average onset time in infants and children with the 0.6 mg / kg intubation dose is slightly shorter than in adults. The duration of relaxation and recovery time tend to be shorter in children compared to infants and adults. In general, in infants (3 months to 1 year), the apparent Vd under steady-state conditions is increased, compared to adults and children (1-8 years). In older children (3-8 years), the trend is for greater clearance and a shorter elimination half-life (approximately 20 min.) Relative to adults, younger children, and infants. It is not recommended for rapid sequence intubation or for ICU ventilation in this type of patient.
- Older adult: in clinical studies it has been administered to a group of patients, with which a similar pharmacokinetics was demonstrated in the young adult, even though the onset and duration of the effect was slightly longer. They are not recommended to facilitate mechanical ventilation due to the lack of safety and efficacy data.
- DR: reduce maintenance dose. Risk of prolonged paralysis.
- DH: should be administered with extreme caution in patients with liver and / or biliary tract disorders.
- It requires anticipation of intubation difficulties, particularly when used in rapid sequence induction. Causing respiratory paralysis requires ventilatory support. Extubate only when the patient has recovered from the neuromuscular block, due to the danger of a residual effect. Due to the frequency of anaphylactic reactions, it is recommended to create conditions in case of occurrence. Prolongation of neuromuscular blockade with the appearance of paralysis and muscle weakness may appear in patients in the ICU, therefore monitoring of neuromuscular transmission is recommended. * Use cautiously in obese patients, hypothermic conditions, neuromuscular disease or poliomyelitis , hypokalemia (e.g. after severe vomiting ,diarrhea and diuretic treatment), hypermagnesemia , hypocalcemia (after massive transfusions), hypoproteinemia, dehydration , acidosis, hypercapnea, cachexia . Using dangerous machinery or driving is not recommended for the first 24 hours after complete recovery from the neuromuscular blocking action of the drug.
Adverse reactions
Frequent
Common are pain / reaction at the injection site, changes in vital signs, and prolonged neuromuscular block.
Rare
Hypersensitivity reactions, rash and erythematous eruption, angioedema , urticaria , itching, rash, anaphylactic reactions, flaccid paralysis, tachycardia , hypotension , circulatory collapse and shock ; bronchospasm, apnea , respiratory failure, skeletal muscle weakness, steroid myopathy, increased histamine level , prolonged neuromuscular blockade.
Interactions
- Volatile halogenated anesthetics: they potentiate neuromuscular blockade, an effect only apparent with the maintenance dose and that may not be reversed with anticholinesterase inhibitors, it can also be inhibited.
- Thiopental, methohexital, ketamine , fentanyl, gammahydroxybutyrate, etomidate and propofol: suxamethonium (succinylcholine): increase its effect.
- Corticosteroids: prolonged and joint use causes prolonged duration of neuromuscular blockade or myopathy.
- Antibiotics (aminoglycosides, lincosamides and polypeptide antibiotics, acylaminopenicillins), diuretics, quinidine, quinine, magnesium salts, CCBs, lithium salts, local anesthetics ( intravenous lidocaine , epidural bupivacaine) and acute administration of phenytoin or beta-blockers: increased neuromuscular blocking effect .
- Phenytoin or carbamazepine: its chronic administration causes a decrease in its effect.
- Neostigmine, edrophonium, pyridostigmine, aminopyridine derivatives, protease inhibitors, norepinephrine, theophylline , chloride of calcium chloride , potassium : decreased neuromuscular blocking effect.
- Azathioprine: transient and limited decrease in the effect of rocuronium.
- Other non-depolarizing neuromuscular blocking drugs: they usually attenuate or enhance neuromuscular blockade, depending on the order of administration and the neuromuscular blocker used.
- Suxamethonium (succinylcholine): administered after rocuronium can enhance or attenuate its neuromuscular blocking effect.
- Lidocaine: usually induces the quickest onset of its action.
Posology
Intubation, adult and child older than 1 month, by IV initially 600 µg / kg; maintenance dose IV, 150 µg / kg (older adult 75-100 µg / kg) or for continuous infusion IV, 300-600 µg // kg / h (older adult up to 400 µg // kg / h) adjusted according to answer. Intensive care, by IV injection, adult initially 600 µg / kg, maintenance dose by IV infusion 300-600 µg / kg / h for the first hour, then adjust according to response.
Treatment of acute overdose and serious adverse effects
Stay under mechanical ventilation and sedation. Administer an acetylcholinesterase inhibitor (example: neostigmine, edrophonium, pyridostigmine) in appropriate doses, until spontaneous recovery begins.
Basic information to the patient
The ability to drive or operate dangerous machinery may be affected for at least 24 hours after drug administration.
Distribution level
Exclusive use of hospitals
Regulation to prescription
Does not have.
VEN classification
Special medicine
Producer laboratory
International
ATC code
M03AC09.