RECORUM 10MG/ML

Indications

• Facilitation of tracheal intubation
• Muscle relaxation during surgical procedures
• Adjunct to general anesthesia
• Facilitation of mechanical ventilation in intensive care settings

Dosage

Children: Refer to BNF for Children for specific dosing information in paediatric patients.

Adults: The dosage of rocuronium for adults typically ranges from 0.6 to 1.2 mg/kg for intubation, with maintenance doses of 0.1 to 0.2 mg/kg as needed during surgery.

Mechanism of action

Rocuronium acts by competing for cholinergic receptors at the motor end-plate, binding to nicotinic cholinergic receptors. This prevents acetylcholine from binding to its receptor, inhibiting depolarization and calcium ion release, which are essential for muscle contraction. The action of rocuronium can be reversed by acetylcholinesterase inhibitors such as neostigmine and edrophonium.

Pharmacodynamics

As a neuromuscular blocking agent, rocuronium causes skeletal muscle relaxation by decreasing the response to acetylcholine at the myoneural junction. By inhibiting the normal depolarization process of the postjunctional membrane, it effectively prevents muscle contraction. Rocuronium has a rapid to intermediate onset of action and an intermediate duration, varying with dosage and patient population, particularly acting longer in infants compared to children.

Pharmacokinetics

Rocuronium undergoes hepatic and renal metabolism, with a portion of the drug being excreted unchanged in the urine. It has a relatively rapid onset, typically within 1-2 minutes, and the duration of action is influenced by the dosage administered. Rocuronium's effects can be reversed with specific antagonists, and its pharmacokinetic properties can vary depending on patient factors such as age and organ function.

Contra-indications

• Hypersensitivity to rocuronium or any of its components
• Conditions where neuromuscular blockade is contraindicated, such as myasthenia gravis or Eaton-Lambert syndrome

Adverse effects

• Muscle weakness
• Prolonged neuromuscular blockade
• Hypotension
• Bradycardia
• Respiratory depression
• Anaphylactic reactions

Interactions

• Increased neuromuscular blockade with aminoglycosides, tetracyclines, and other neuromuscular blockers
• Acetylcholinesterase inhibitors (e.g., neostigmine, edrophonium) can reverse the effects of rocuronium

Precautions

• Use with caution in patients with neuromuscular disorders
• Monitor respiratory function closely in patients receiving rocuronium
• Consider dosage adjustments in elderly patients or those with hepatic or renal impairment

Pregnancy

Rocuronium should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Its safety profile in pregnancy is not well established.

Breast-feeding

It is not known whether rocuronium is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store at 2-8 degrees Celsius. Protect from light. Do not freeze.

Formulations

• Rocuronium bromide injection

Indications

• Neuromuscular blockade during surgery
• Neuromuscular blockade for intubation
• Neuromuscular blockade in intensive care settings

Dosage

Children: For children aged 2–5 months, the initial dose is 150 micrograms/kg by intravenous injection, followed by 100 micrograms/kg every 6–9 minutes as required. Alternatively, an infusion can be administered at 8–10 micrograms/kg/minute, adjusted as needed.

Adults: Initially, 100 micrograms/kg by intravenous injection, followed by 20 micrograms/kg as required. For maintenance, doses of 60 micrograms/kg can be given every 60–90 minutes. Adjustments may be necessary based on patient response and specific clinical circumstances.

Mechanism of action

Rocuronium bromide works by competitively inhibiting nicotinic acetylcholine receptors at the neuromuscular junction. This prevents the binding of acetylcholine, leading to muscle relaxation. The blockade can be reversed by cholinesterase inhibitors, which increase acetylcholine levels at the neuromuscular junction.

Pharmacodynamics

The onset of action for rocuronium is typically rapid, with effects observed within 1-2 minutes after administration. The duration of action is intermediate, lasting approximately 30-60 minutes, depending on the dose. The effect can be monitored using neuromuscular transmission monitoring to tailor dosing accurately.

Pharmacokinetics

Rocuronium is primarily eliminated through hepatic metabolism, with a significant portion excreted in the bile. It has a volume of distribution of about 0.3 L/kg and a clearance rate that is influenced by liver function. In patients with hepatic impairment, the duration of neuromuscular blockade may be prolonged. Rocuronium does not cross the blood-brain barrier significantly.

Contra-indications

• Hypersensitivity to rocuronium bromide or any of its components
• Neuromuscular disorders that may exacerbate neuromuscular blockade
• Conditions where neuromuscular blockade may be contraindicated

Adverse effects

• Apnoea
• Respiratory depression
• Cardiovascular effects such as hypotension and tachycardia
• Allergic reactions including anaphylaxis
• Malignant hyperthermia
• Prolonged neuromuscular blockade

Interactions

• Inhalational anaesthetics may enhance the neuromuscular blocking effect
• Aminoglycoside antibiotics may potentiate neuromuscular blockade
• Calcium channel blockers may increase the effects of neuromuscular blocking agents
• Cholinesterase inhibitors may antagonize the effects of rocuronium

Precautions

• Use with caution in patients with hepatic impairment as dose adjustment may be necessary
• Use with caution in patients with renal impairment due to the potential for prolonged neuromuscular blockade
• Monitor cardiovascular status in patients with cardiovascular disease
• Careful consideration of dosing in obese patients; doses should be calculated based on ideal body weight

Pregnancy

Rocuronium bromide should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised; it is recommended to monitor the infant for any adverse effects if rocuronium is administered during breastfeeding.

Storage

Store in a cool, dry place, protected from light. Keep out of reach of children. Do not use after the expiry date printed on the packaging.

Formulations

• Rocuronium bromide 10 mg per 1 ml solution for injection
• Rocuronium bromide 20 mg/10 ml solution for injection

Mechanism of action

Rocuronium acts by competing for cholinergic receptors at the motor end-plate. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine and edrophonium. Rocuronium acts by competitively binding to nicotinic cholinergic receptors. The binding of vecuronium decreases the opportunity for acetylcholine to bind to the nicotinic receptor at the postjunctional membrane of the myoneural junction. As a result, depolarization is prevented, calcium ions are not released and muscle contraction does not occur. Evidence also suggests that nondepolarizing agents can affect ACh release. It has been hypothesized that nondepolarzing agents bind to postjunctional ("curare") receptors and may therefore interfere with the sodium and potassium flux, which is responsible for depolarization and repolarization of the membranes involved in muscle contraction.

Pharmacodynamics

Neuromuscular blocking agents are drugs that cause skeletal muscle relaxation primarily by causing a decreased response to the neurotransmitter acetylcholine (ACh) at the myoneural (neuromuscular) junction of skeletal muscle. At that site, ACh normally produces electrical depolarization of the postjunctional membrane of motor end-plate, which leads to conduction of muscle action potential and subsequently induces skeletal muscle contraction. Neuromuscular agents are classified as depolarizing or nondepolarizing. Rocuronium is a nondepolarizing neuromuscular blocking agent with a rapid to intermediate onset depending on dose and intermediate duration. Rocuronium, like vecuronium is longer acting in infants than in children. However, unlike vecuronium, rocuronium retains the characteristics of an intermediate-acting NMBD in infants.