remimazolam besylate: clinical use

Prescribing considerations

• Use only in an appropriately equipped setting with personnel trained in airway management, ventilation and cardiovascular resuscitation.
• Exercise additional caution in older or frail patients and those with respiratory or cardiac impairment.
• Severe hepatic impairment can reduce clearance and prolong clinical effects; titrate carefully to response.
• Chronic benzodiazepine or other CNS-depressant exposure may produce tolerance.
• Consider abuse and dependence potential when relevant.
• The dextran excipient can cause anaphylactic or anaphylactoid reactions.

Contraindications and cautions

• Hypersensitivity to remimazolam, another benzodiazepine or a listed excipient
• Unstable myasthenia gravis

Monitoring

• Continuously assess respiratory function, oxygenation, circulation and depth of sedation or anaesthesia.
• Ensure airway, ventilation and resuscitation equipment is immediately available.
• For procedural sedation, a separate trained professional should have sole responsibility for monitoring the patient.
• Keep flumazenil available where required, while recognising that it does not reverse opioid effects and observation remains necessary.

Clinical pharmacology

Remimazolam is an intravenous benzodiazepine agonist at GABA-A receptor benzodiazepine sites. It is rapidly hydrolysed predominantly by hepatic carboxylesterase-1 to CNS7054, with no meaningful cytochrome P450 contribution and low CYP-, transporter- or protein-binding-mediated interaction potential.

Formulation and product differences

• The procedural-sedation presentation is a powder reconstituted as a solution for intravenous injection.
• The general-anaesthesia presentation is a powder for concentrate that requires reconstitution and further dilution before intravenous injection or infusion.
• Both selected formulations contain dextran 40 and are incompatible with Hartmann's and other specified alkaline Ringer-type solutions.

Injection

Route: Parenteral

Strengths: 20 mg, 50 mg