Literature DB >> 34746482

A comprehensive review of remimazolam for sedation.

Nazir Noor1, Rhorer Legendre2, Alexandra Cloutet2, Ahish Chitneni3, Giustino Varrassi4, Alan D Kaye2.   

Abstract

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.

Entities:  

Keywords:  benzodiazepine; remimazolam; sedation

Year:  2021        PMID: 34746482      PMCID: PMC8567764          DOI: 10.52965/001c.24514

Source DB:  PubMed          Journal:  Health Psychol Res        ISSN: 2420-8124


  46 in total

1.  A placebo- and midazolam-controlled phase I single ascending-dose study evaluating the safety, pharmacokinetics, and pharmacodynamics of remimazolam (CNS 7056): Part II. Population pharmacokinetic and pharmacodynamic modeling and simulation.

Authors:  Hugh R Wiltshire; Gavin J Kilpatrick; Gary S Tilbrook; Keith M Borkett
Journal:  Anesth Analg       Date:  2012-01-16       Impact factor: 5.108

2.  Safety, pharmacokinetic and pharmacodynamic properties of single ascending dose and continuous infusion of remimazolam besylate in healthy Chinese volunteers.

Authors:  Xiao-Yan Sheng; Yan Liang; Xue-Yuan Yang; Li-E Li; Xia Ye; Xia Zhao; Yi-Min Cui
Journal:  Eur J Clin Pharmacol       Date:  2019-12-23       Impact factor: 2.953

Review 3.  Reports of death with use of propofol (Diprivan) for nonprocedural (long-term) sedation and literature review.

Authors:  Diane K Wysowski; Martin L Pollock
Journal:  Anesthesiology       Date:  2006-11       Impact factor: 7.892

Review 4.  Soft drugs in anesthesia: remifentanil as prototype to modern anesthetic drug development.

Authors:  Nathaniel M Birgenheier; Ami R Stuart; Talmage D Egan
Journal:  Curr Opin Anaesthesiol       Date:  2020-08       Impact factor: 2.706

5.  Inhaled Remimazolam Potentiates Inhaled Remifentanil in Rodents.

Authors:  Tatjana Bevans; Cassandra Deering-Rice; Chris Stockmann; Joseph Rower; Derek Sakata; Christopher Reilly
Journal:  Anesth Analg       Date:  2017-05       Impact factor: 5.108

Review 6.  Classics in chemical neuroscience: diazepam (valium).

Authors:  Nicholas E Calcaterra; James C Barrow
Journal:  ACS Chem Neurosci       Date:  2014-02-27       Impact factor: 4.418

7.  Effect of peripheral benzodiazepine receptor ligands on lipopolysaccharide-induced tumor necrosis factor activity in thioglycolate-treated mice.

Authors:  T Matsumoto; M Ogata; K Koga; A Shigematsu
Journal:  Antimicrob Agents Chemother       Date:  1994-04       Impact factor: 5.191

8.  Opioids and the management of chronic severe pain in the elderly: consensus statement of an International Expert Panel with focus on the six clinically most often used World Health Organization Step III opioids (buprenorphine, fentanyl, hydromorphone, methadone, morphine, oxycodone).

Authors:  Joseph Pergolizzi; Rainer H Böger; Keith Budd; Albert Dahan; Serdar Erdine; Guy Hans; Hans-Georg Kress; Richard Langford; Rudolf Likar; Robert B Raffa; Paola Sacerdote
Journal:  Pain Pract       Date:  2008-05-23       Impact factor: 3.183

9.  Pharmacokinetics and pharmacodynamics of intranasal remimazolam-a randomized controlled clinical trial.

Authors:  Marija Pesic; Frank Schippers; Rob Saunders; Lyn Webster; Martin Donsbach; Thomas Stoehr
Journal:  Eur J Clin Pharmacol       Date:  2020-09-04       Impact factor: 2.953

10.  Remimazolam Has Low Oral Bioavailability and No Potential for Misuse in Drug-Facilitated Sexual Assaults, with or Without Alcohol: Results from Two Randomised Clinical Trials.

Authors:  Marija Pesic; Thomas Stöhr; Joachim Ossig; Keith Borkett; Martin Donsbach; Van-Anh Dao; Lynn Webster; Frank Schippers
Journal:  Drugs R D       Date:  2020-09
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  3 in total

1.  The Median Effective Dose and Bispectral Index of Remimazolam Tosilate for Anesthesia Induction in Elderly Patients: An Up-and-Down Sequential Allocation Trial.

Authors:  Miao Liu; Yuan Sun; Lingxue Zhou; Kunpeng Feng; Tianlong Wang; Xuexin Feng
Journal:  Clin Interv Aging       Date:  2022-05-20       Impact factor: 3.829

2.  Efficacy and Safety of Remimazolam Besylate versus Dexmedetomidine for Sedation in Non-Intubated Older Patients with Agitated Delirium After Orthopedic Surgery: A Randomized Controlled Trial.

Authors:  Yang Deng; Zhijun Qin; Qianyun Wu; Linsong Liu; Xi Yang; Xuan Ju; Ying Zhang; Lei Liu
Journal:  Drug Des Devel Ther       Date:  2022-08-01       Impact factor: 4.319

3.  Remimazolam in a Pediatric Patient With a Suspected Family History of Malignant Hyperthermia.

Authors:  Holly Petkus; Brittany L Willer; Joseph D Tobias
Journal:  J Med Cases       Date:  2022-08-19
  3 in total

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