A comprehensive review of remimazolam for sedation

Benzodiazepines are one of the most commonly used medications in the field of anesthesia. They offer excellent anxiolytic and amnestic properties ideal for the perioperative period when patient anxiety is understandably heightened. Remimazolam has presented a favorable alternative to some of the com...

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Main Authors: Nazir Noor, Rhorer Legendre, Alexandra Cloutet, Ahish Chitneni, Giustino Varrassi, Alan D. Kaye
Format: Article
Language:English
Published: Open Medical Publishing 2021-06-01
Series:Health Psychology Research
Online Access:https://doi.org/10.52965/001c.24514
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author Nazir Noor
Rhorer Legendre
Alexandra Cloutet
Ahish Chitneni
Giustino Varrassi
Alan D. Kaye
author_facet Nazir Noor
Rhorer Legendre
Alexandra Cloutet
Ahish Chitneni
Giustino Varrassi
Alan D. Kaye
author_sort Nazir Noor
collection DOAJ
description Benzodiazepines are one of the most commonly used medications in the field of anesthesia. They offer excellent anxiolytic and amnestic properties ideal for the perioperative period when patient anxiety is understandably heightened. Remimazolam has presented a favorable alternative to some of the common intravenous anesthetic agents used given its fast onset of action, high safety profile, and reasonably short duration of action. The drugs within the four classes of benzodiazepines, 2-keto-benzodiazepines, 3-hydroxy-benzodiazepines, triazolo-benzodiazepines, and 7-nitro-benzodiazepines provide varying degrees of anxiolysis, sedation, and amnesia. This is provided by the benzodiazepine molecule binding and causing a conformational change to the chloride ion channel to cause hyperpolarization and thus inhibition of the central nervous system. Each type of benzodiazepine has a preferred role within the realm of medicine. For instance, diazepam is used for the treatment of seizures and anxiety. Midazolam’s anxiolytic and anterograde amnestic properties are taking advantage of during the perioperative period. Lorazepam is beneficial for anxiety and status epilepticus. Remimazolam, currently in phase II and III clinical trials, has demonstrated a very short during of action and low context-sensitive half-time, allowing for its rapid removal even during a prolonged infusion. Much of its properties may be credited to being a soft drug, meaning it is a metabolically active drug that is rapidly inactivated in the body. This provides anesthesiologists and other practitioners administering it with a more predictable sedative. These properties have the potential to push it towards becoming the drug of choice for premedication during the perioperative period and sedation in the ICU. Furthermore, remimazolam does not seem to rely on any specific organ to be metabolized. The drug's ester moiety makes it a substrate for non-specific tissue esterase enzymes, meaning its metabolism and elimination are not impaired in patients with hepatic and/or renal disease. Its addictive potential closely resembles that of its parent compound, midazolam. Reports of its adverse reactions include headache and somnolence after an involuntary movement during infusion. Benzodiazepines are a great adjunct to anesthetic care. Remimazolam’s safety profile, pharmacokinetics, pharmacodynamics, and potential practical use make it quite favorable in this regard. It has the potential to equip anesthesiologists and other medical practitioners with a more predictable medication that has a good safety profile. However, further large clinical trials will provide us with a better understanding of the advantages and disadvantages of remimazolam.
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spelling doaj-art-9f537f070e01423983e8f30b5c7ad7702025-02-11T20:30:39ZengOpen Medical PublishingHealth Psychology Research2420-81242021-06-0191A comprehensive review of remimazolam for sedationNazir NoorRhorer LegendreAlexandra CloutetAhish ChitneniGiustino VarrassiAlan D. KayeBenzodiazepines are one of the most commonly used medications in the field of anesthesia. They offer excellent anxiolytic and amnestic properties ideal for the perioperative period when patient anxiety is understandably heightened. Remimazolam has presented a favorable alternative to some of the common intravenous anesthetic agents used given its fast onset of action, high safety profile, and reasonably short duration of action. The drugs within the four classes of benzodiazepines, 2-keto-benzodiazepines, 3-hydroxy-benzodiazepines, triazolo-benzodiazepines, and 7-nitro-benzodiazepines provide varying degrees of anxiolysis, sedation, and amnesia. This is provided by the benzodiazepine molecule binding and causing a conformational change to the chloride ion channel to cause hyperpolarization and thus inhibition of the central nervous system. Each type of benzodiazepine has a preferred role within the realm of medicine. For instance, diazepam is used for the treatment of seizures and anxiety. Midazolam’s anxiolytic and anterograde amnestic properties are taking advantage of during the perioperative period. Lorazepam is beneficial for anxiety and status epilepticus. Remimazolam, currently in phase II and III clinical trials, has demonstrated a very short during of action and low context-sensitive half-time, allowing for its rapid removal even during a prolonged infusion. Much of its properties may be credited to being a soft drug, meaning it is a metabolically active drug that is rapidly inactivated in the body. This provides anesthesiologists and other practitioners administering it with a more predictable sedative. These properties have the potential to push it towards becoming the drug of choice for premedication during the perioperative period and sedation in the ICU. Furthermore, remimazolam does not seem to rely on any specific organ to be metabolized. The drug's ester moiety makes it a substrate for non-specific tissue esterase enzymes, meaning its metabolism and elimination are not impaired in patients with hepatic and/or renal disease. Its addictive potential closely resembles that of its parent compound, midazolam. Reports of its adverse reactions include headache and somnolence after an involuntary movement during infusion. Benzodiazepines are a great adjunct to anesthetic care. Remimazolam’s safety profile, pharmacokinetics, pharmacodynamics, and potential practical use make it quite favorable in this regard. It has the potential to equip anesthesiologists and other medical practitioners with a more predictable medication that has a good safety profile. However, further large clinical trials will provide us with a better understanding of the advantages and disadvantages of remimazolam.https://doi.org/10.52965/001c.24514
spellingShingle Nazir Noor
Rhorer Legendre
Alexandra Cloutet
Ahish Chitneni
Giustino Varrassi
Alan D. Kaye
A comprehensive review of remimazolam for sedation
Health Psychology Research
title A comprehensive review of remimazolam for sedation
title_full A comprehensive review of remimazolam for sedation
title_fullStr A comprehensive review of remimazolam for sedation
title_full_unstemmed A comprehensive review of remimazolam for sedation
title_short A comprehensive review of remimazolam for sedation
title_sort comprehensive review of remimazolam for sedation
url https://doi.org/10.52965/001c.24514
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