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Remimazolam | CAS No: 308242-62-8 | GMP-certified suppliers
A medication that provides rapid and controlled procedural sedation in adults undergoing brief medical procedures, enhancing patient comfort and safety during interventions lasting 30 minutes or less.
Therapeutic categories
BenzazepinesBenzodiazepine hypnotics and sedativesBenzodiazepines and benzodiazepine derivativesCentral Nervous System DepressantsGABA AgentsGABA Modulators
Generic name
Remimazolam
Molecule type
small molecule
CAS number
308242-62-8
DrugBank ID
DB12404
Approval status
Approved drug, Investigational drug
ATC code
N05CD14
Primary indications
- Remimazolam is indicated for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less
Product Snapshot
- Remimazolam is an intravenous injectable benzodiazepine formulation available as powder for solution and lyophilized powder
- It is primarily used for procedural sedation induction and maintenance in adult patients undergoing short-duration procedures
- The compound holds regulatory approvals in key markets including the US (FDA) and the European Union (EMA), with both approved and investigational statuses
Clinical Overview
Remimazolam (CAS number 308242-62-8) is an ultra short-acting benzodiazepine indicated for the induction and maintenance of procedural sedation in adults undergoing brief procedures lasting 30 minutes or less. It belongs to the chemical class of 1,4-benzodiazepines, characterized by a fused benzene and 1,4-azepine ring structure.
Pharmacologically, remimazolam acts as a positive allosteric modulator of gamma-aminobutyric acid A (GABA(A)) receptors. By binding to the benzodiazepine site at the interface of the alpha and gamma subunits, it enhances the inhibitory effects of GABA, the primary inhibitory neurotransmitter in the central nervous system. This potentiation results in increased chloride ion influx and hyperpolarization of neurons, leading to sedative and anxiolytic effects. Sedation onset typically occurs within 3 to 3.5 minutes of intravenous administration, consistent with its classification as a “soft drug” designed for rapid onset and offset.
The defining pharmacokinetic advantage of remimazolam is its rapid metabolism by tissue esterases to inactive metabolites, resulting in a short context-sensitive half-life and predictable recovery times. This metabolic pathway resembles that of other soft drugs such as remifentanil, facilitating fine-tuned control during anesthesia. Hepatic impairment can elevate plasma concentrations and prolong sedation, necessitating cautious titration in patients with severe liver dysfunction.
Safety considerations include the potential for drug dependence and abuse inherent to all benzodiazepines. Although remimazolam was approved by the FDA in July 2020 under the brand name Byfavo, it has not yet been scheduled under the U.S. Controlled Substances Act at the time of approval. Clinical use should therefore incorporate standard benzodiazepine precautions, especially in individuals with a history of substance misuse.
For active pharmaceutical ingredient (API) procurement, sourcing remimazolam requires stringent quality controls to ensure chemical purity and consistent ester bond integrity, given that metabolic fragility underpins its clinical profile. Manufacturers and suppliers must adhere to established pharmacopeial standards and regulatory guidelines to guarantee batch-to-batch reproducibility suitable for parenteral administration.
Pharmacologically, remimazolam acts as a positive allosteric modulator of gamma-aminobutyric acid A (GABA(A)) receptors. By binding to the benzodiazepine site at the interface of the alpha and gamma subunits, it enhances the inhibitory effects of GABA, the primary inhibitory neurotransmitter in the central nervous system. This potentiation results in increased chloride ion influx and hyperpolarization of neurons, leading to sedative and anxiolytic effects. Sedation onset typically occurs within 3 to 3.5 minutes of intravenous administration, consistent with its classification as a “soft drug” designed for rapid onset and offset.
The defining pharmacokinetic advantage of remimazolam is its rapid metabolism by tissue esterases to inactive metabolites, resulting in a short context-sensitive half-life and predictable recovery times. This metabolic pathway resembles that of other soft drugs such as remifentanil, facilitating fine-tuned control during anesthesia. Hepatic impairment can elevate plasma concentrations and prolong sedation, necessitating cautious titration in patients with severe liver dysfunction.
Safety considerations include the potential for drug dependence and abuse inherent to all benzodiazepines. Although remimazolam was approved by the FDA in July 2020 under the brand name Byfavo, it has not yet been scheduled under the U.S. Controlled Substances Act at the time of approval. Clinical use should therefore incorporate standard benzodiazepine precautions, especially in individuals with a history of substance misuse.
For active pharmaceutical ingredient (API) procurement, sourcing remimazolam requires stringent quality controls to ensure chemical purity and consistent ester bond integrity, given that metabolic fragility underpins its clinical profile. Manufacturers and suppliers must adhere to established pharmacopeial standards and regulatory guidelines to guarantee batch-to-batch reproducibility suitable for parenteral administration.
Identification & chemistry
| Generic name | Remimazolam |
|---|---|
| Molecule type | Small molecule |
| CAS | 308242-62-8 |
| UNII | 7V4A8U16MB |
| DrugBank ID | DB12404 |
Pharmacology
| Summary | Remimazolam is an ultra short-acting benzodiazepine that enhances the inhibitory neurotransmission mediated by GABA(A) receptors through positive allosteric modulation at the benzodiazepine binding site. By potentiating GABA-induced chloride ion influx, it produces sedation suitable for short-duration procedures. Its pharmacodynamic profile allows rapid onset of action with modulation of central nervous system inhibition. |
|---|---|
| Mechanism of action | 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. |
| Pharmacodynamics | 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| GABA(A) Receptor | Humans | positive allosteric modulator |
| GABA(A) Receptor Benzodiazepine Binding Site | Humans | ligand |
ADME / PK
| Absorption | The C<sub>max</sub> and AUC<sub>0-inf</sub> 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 T<sub>max</sub> of the inactive CNS7054 metabolite is approximately 20-30 minutes and its AUC<sub>0-inf</sub> 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. |
| Protein binding | Remimazolam is >91% protein-bound in plasma, primarily to serum albumin. |
| Metabolism | Remimazolam does not appear to undergo biotransformation via hepatic cytochrome P450 enzymes, nor does it induce or inhibit these enzymes. Its primary route of metabolism is hydrolysis via hepatic carboxylesterase-1 (CES1) to yield the inactive CNS7054 metabolite, which then undergoes glucuronidation and hydroxylation prior to elimination. CNS7054 possesses a 300-fold lesser affinity for GABA(A) receptors as compared to the parent drug. |
| Route of elimination | 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. |
| Volume of distribution | The volume of distribution is approximately 0.76 - 0.98 L/kg. |
| Clearance | The clearance of remimazolam is approximately 24 - 75 L/h and is independent of body weight. |
Formulation & handling
- Remimazolam is formulated as a lyophilized powder for intravenous injection, requiring reconstitution prior to administration.
- As a small molecule 1,4-benzodiazepine with low water solubility, careful formulation strategies are needed to ensure aqueous stability and solubility.
- Patients should avoid alcohol due to potentiation of sedative effects, which is relevant for clinical use and patient counseling.
Regulatory status
| Lifecycle | The API is currently protected by multiple patents in the United States expiring between 2027 and 2031. It is marketed in both the EU and US, with patent expirations indicating a mid to late lifecycle stage in the US market. |
|---|
| Markets | EU, US |
|---|
Supply Chain
| Supply chain summary | Remimazolam is manufactured by a limited number of originator companies with branded products marketed in both the US and EU. Several key patents protecting the product are set to expire between 2027 and 2031, indicating potential for generic competition either imminent or within the next few years. This patent landscape suggests evolving opportunities for sourcing and supply chain diversification post-patent expiry. |
|---|
Safety
| 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. |
|---|
High Level Warnings:
- Remimazolam may cause significant central nervous system and respiratory depression upon overdose
- Exposure risk includes ataxia and hypotension consistent with benzodiazepine adverse effects
- Flumazenil can antagonize sedative effects but does not replace comprehensive supportive measures
Remimazolam is a type of Barbiturates
Barbiturates are a category of pharmaceutical active pharmaceutical ingredients (APIs) that have sedative, hypnotic, and anticonvulsant properties. They belong to the class of drugs called depressants, which slow down the central nervous system (CNS) activity. Barbiturates have been widely used in the medical field for their ability to induce sleep, reduce anxiety, and control seizures.
The mechanism of action of barbiturates involves enhancing the effects of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) in the brain. GABA inhibits the transmission of signals between nerve cells, leading to relaxation and sedation. Barbiturates bind to specific GABA receptors, increasing the inhibitory effects of GABA and resulting in a calming effect on the CNS.
In the past, barbiturates were commonly prescribed for insomnia, anxiety disorders, and epilepsy. However, their use has decreased significantly due to the emergence of safer and more effective alternatives with fewer side effects. Nonetheless, barbiturates are still utilized in certain medical situations, such as anesthesia induction, emergency seizure control, and in some cases of refractory epilepsy.
Despite their therapeutic benefits, barbiturates carry potential risks and side effects. They can cause drowsiness, impaired coordination, and dependence when used for extended periods. Overdose of barbiturates can be life-threatening, leading to respiratory depression and coma.
In conclusion, barbiturates are a class of API widely known for their sedative, hypnotic, and anticonvulsant properties. While their use has diminished over time, they remain important in specific medical contexts. Proper caution and medical supervision are crucial when using barbiturates to ensure safety and efficacy.
