Remimazolam
Remimazolam Uses, Dosage, Side Effects, Food Interaction and all others data.
Remimazolam is an ultra short-acting benzodiazepine used in the induction and maintenance of sedation during short (6 Recent trends in anesthesia-related drug development have touted the benefits of so-called "soft drugs" - these agents, such as remifentanil, are designed to be metabolically fragile and thus susceptible to rapid biotransformation and elimination as inactive metabolites. These "soft drugs" are useful in the context of surgical procedures, wherein a rapid onset/offset is desirable, enabling anesthesiologists to manipulate drug concentrations as needed. Remimazolam was the first "soft" benzodiazepine analog to be developed and was approved for use by the FDA in July 2020 under the brand name Byfavo.
Remimazolam modulates the effects of GABA(A) receptors in order to enhance the effects of GABA. It is considered an "ultra short-acting" benzodiazepine that achieves peak sedation within 3 to 3.5 minutes following intravenous administration, a property that makes it desirable for use during short procedures. Hepatic impairment can result in elevated serum levels of remimazolam - patients with severe hepatic impairment should be carefully titrated to effect. As of its approval date, remimazolam has not received a scheduling action by the DEA under the Controlled Substances Act. As benzodiazepines as a class have been implicated in the development of drug dependence and have a known potential for abuse, remimazolam should be used with caution in patients with a history of drug dependence or abuse.
| Trade Name | Remimazolam |
| Availability | Prescription only |
| Generic | Remimazolam |
| Remimazolam Other Names | Remimazolam |
| Related Drugs | trazodone, hydroxyzine, lorazepam, promethazine, fentanyl, Ativan, lidocaine, ketamine, hyoscyamine, propofol |
| Weight | 20mg, |
| Type | Intravenous Powder For Injection, Intravenous |
| Formula | C21H19BrN4O2 |
| Weight | Average: 439.313 Monoisotopic: 438.069139 |
| Protein binding | Remimazolam is >91% protein-bound in plasma, primarily to serum albumin. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Remimazolam is an ultra short-acting benzodiazepine used for the induction and maintenence of procedural sedation during short procedures.
Remimazolam is indicated for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less.
Remimazolam is also used to associated treatment for these conditions: Procedural Sedation
How Remimazolam works
Like other benzodiazepines, remimazolam exerts its therapeutic effects by potentiating the effect of gamma-aminobutyric acid (GABA) on GABA(A) receptors, the main inhibitory neurotransmitter receptors in the mammalian brain. GABA(A) receptors are a component of GABA-gated ionotropic chloride channels that produce inhibitory postsynaptic potentials - following activation by GABA, the channel undergoes a conformational change that allows the passage of chloride ions through the channel. The inhibitory potentials produced by GABA neurotransmission play an integral role in the suppression and control of epileptiform nerve firing such as that seen in epilepsy, which makes the GABA system a desirable target in the treatment of epilepsy.
Benzodiazepines are positive allosteric modulators of GABA(A) function. They bind to the interface between alpha (α) and gamma (γ) subunits on the receptor, commonly referred to as the benzodiazepine binding site, and modulate the receptor such that its inhibitory response to GABA binding is dramatically increased.
Toxicity
Symptoms of remimazolam overdoses, as with other benzodiazepines, are likely to be consistent with its adverse effect profile and may therefore involve significant CNS depression, respiratory depression, ataxia, and hypotension. The benzodiazepine receptor antagonist flumazenil may be used for reversal of the sedative effects associated with benzodiazepine overdose, though it is not a substitute for proper supportive care.
Food Interaction
- Avoid alcohol. The sedative effects of benzodiazepines may be exacerbated by the co-administration of alcohol.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.
Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.
Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.
Remimazolam Drug Interaction
Moderate: ramipril, zolpidem, nebivolol, furosemide, pregabalinUnknown: fexofenadine, orlistat, citric acid/magnesium oxide/sodium picosulfate, ubiquinone, rosuvastatin, dehydroepiandrosterone, dapagliflozin, levocarnitine, lysine, pitavastatin, omega-3 polyunsaturated fatty acids, methylprednisolone, omega-3 polyunsaturated fatty acids, semaglutide, polyethylene glycol 3350 with electrolytes
Remimazolam Disease Interaction
Major: drug dependence, respiratory depression, prolonged hypotension
Volume of Distribution
The volume of distribution is approximately 0.76 - 0.98 L/kg.
Elimination Route
The Cmax and AUC0-inf following intravenous administration of 0.01 to 0.5 mg/kg were 189 to 6,960 ng/mL and 12.1 to 452 ng∙h/mL, respectively, and appear to be relatively dose proportional. The Tmax of the inactive CNS7054 metabolite is approximately 20-30 minutes and its AUC0-inf ranges from 231 to 7,090 ng∙h/mL.
Half Life
Following intravenous administration, the distribution half-life is of remimazolam is 0.5 - 2 minutes and the terminal elimination half-life is 37 - 53 minutes. Half-life is increased in patients with hepatic impairment necessitating careful dose titration in this population. The half-life of remimazolam's major inactive metabolite, CNS7054, is 2.4 - 3.8 hours.
Clearance
The clearance of remimazolam is approximately 24 - 75 L/h and is independent of body weight.
Elimination Route
In patients undergoing colonoscopy, approximately 0.003% of the administered dose is excreted in the urine as unchanged parent drug and 50-60% is excreted in the urine as CNS7054. In healthy subjects, >80% of the administered dose is excreted in the urine as CNS7054.
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