Remimazolam

BYFAVO is a benzodiazepine. BYFAVO binds to brain benzodiazepine sites (gamma amino butyric acid type A [GABA A ] receptors), while its carboxylic acid metabolite (CNS7054) has a 300 times lower affinity for the receptor.

• BYFAVO ® is indicated for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less. BYFAVO (remimazolam) for injection is a benzodiazepine indicated for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less.

• BYFAVO is contraindicated in patients with a history of severe hypersensitivity reaction to dextran 40 or products containing dextran 40 [see Warnings and Precautions (5.3) ]. Hypersensitivity to dextran 40.contraindicated

Individualize and titrate BYFAVO dosing to desired clinical effect. ( 2.2 ) Adult Patients : Administer an initial dose intravenously as a 5 mg push injection over a 1-minute time period. ( 2.2 ) If necessary, administer supplemental doses of 2.5 mg intravenously over a 15-second time period. At least 2 minutes must elapse prior to the administration of any supplemental dose. ( 2.2 ) ASA III-IV Patients (at the discretion of the physician) : Based on the general condition of the patient, administer 2.5 mg to 5 mg over 1-minute time period. ( 2.2 ) If necessary, administer supplemental doses of 1.25 mg to 2.5 mg intravenously over a 15-second time period. At least 2 minutes must elapse prior to the administration of any supplemental dose. ( 2.2 ) 2.1 Important Dosage and Administration Instructions BYFAVO can depress respiration. Continuously monitor patients for early signs of hypoventilation, airway obstruction, and apnea using capnography, pulse oximetry, and clinical assessment. Only personnel trained in the administration of procedural sedation, and not involved in the conduct of the diagnostic or therapeutic procedure, should administer BYFAVO. Administering personnel must be trained in the detection and management of airway obstruction, hypoventilation, and apnea, including the maintenance of a patent airway, supportive ventilation, and cardiovascular resuscitation. Supplemental oxygen, resuscitative drugs, and age- and size-appropriate equipment for bag/valve/mask assisted ventilation must be immediately available during administration of BYFAVO.

Hypersensitivity Reactions : Hypersensitivity reactions including anaphylaxis may occur. ( 5.3 ) Neonatal Sedation and Withdrawal Syndrome : Receiving benzodiazepines during pregnancy can result in neonatal sedation and/or neonatal withdrawal. ( 5.4 , 8.1 ) Pediatric Neurotoxicity : In developing animals, exposures greater than 3 hours cause neurotoxicity. Weigh benefits against potential risks when considering elective procedures in children under 3 years old. ( 5.5 ) 5.1 Personnel and Equipment for Monitoring and Resuscitation Clinically notable hypoxia, bradycardia, and hypotension were observed in Phase 3 studies of BYFAVO. Continuously monitor vital signs during sedation and through the recovery period. Only personnel trained in the administration of procedural sedation, and not involved in the conduct of the diagnostic or therapeutic procedure, should administer BYFAVO. Administering personnel must be trained in the detection and management of airway obstruction, hypoventilation, and apnea, including the maintenance of a patent airway, supportive ventilation, and cardiovascular resuscitation. Resuscitative drugs, and age- and size-appropriate equipment for bag/valve/mask assisted ventilation must be immediately available during administration of BYFAVO [see Dosage and Administration (2.1) ] . Consider the potential for worsened cardiorespiratory depression prior to using BYFAVO concomitantly with other drugs that have the same potential (e.g., opioid analgesics or other sedative-hypnotics) [see Drug Interactions (7.1) ].

The following serious adverse reactions are discussed in greater detail in other sections: Neonatal Sedation and Withdrawal Syndrome [see Warnings and Precautions (5.4) , Use in Specific Populations (8.1) ] The most common adverse reactions (>10%) in patients receiving BYFAVO for procedural sedation are hypotension, hypertension, diastolic hypertension, systolic hypertension, hypoxia, and diastolic hypotension. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Acacia Pharma at 1-877-357-9237 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of BYFAVO was evaluated in three prospective, randomized, double-blind, multicenter, parallel group clinical studies in 630 patients undergoing colonoscopy (two studies) or bronchoscopy (one study). Colonoscopy Study 1 and the bronchoscopy study evaluated American Society of Anesthesiologists (ASA) physical status I to III patients, and Colonoscopy Study 2 evaluated ASA III and IV patients. All three studies evaluated the safety of BYFAVO compared to placebo with midazolam rescue and an open-label midazolam treatment arm. Patients were administered a total dose ranging from 5 to 30 mg of BYFAVO.

Lactation : A lactating woman may pump and discard breast milk for 5 hours after treatment with BYFAVO. ( 8.2 ) Pediatric Use : BYFAVO should not be used in patients less than 18 years of age. ( 8.4 ) Geriatric Use : Sedating drugs, such as BYFAVO, may cause confusion and over-sedation in the elderly; elderly patients generally should be observed closely. ( 8.5 ) Severe Hepatic Impairment : In patients with severe hepatic impairment the dose of BYFAVO should be carefully titrated to effect. Depending on the overall status of the patient, reduced doses might be indicated. ( 8.6 , 12.3 ) 8.1 Pregnancy Risk Summary Neonates born to mothers using benzodiazepines late in pregnancy have been reported to experience symptoms of sedation and/or neonatal withdrawal [see Warnings and Precautions (5.4) , Clinical Considerations ]. Available data from published observational studies of pregnant women exposed to benzodiazepines do not report a clear association with benzodiazepines and major birth defects (see Data ). In animal studies, reduced fetal weights but no evidence of malformations or embryofetal lethality were noted in a study in which pregnant rabbits were treated intravenously with 4 times the maximum recommended human dose (MRHD) of 30 mg during organogenesis.

Metabolism

BYFAVO has a terminal elimination half-life from plasma of 37 to 53 minutes. Mean distribution half-life (t 1/2α ) is between 0.5 and 2 minutes.

Clinical Presentation Overdosage of benzodiazepines is characterized by central nervous system depression ranging from drowsiness to coma. In mild to moderate cases, symptoms can include drowsiness, confusion, dysarthria, lethargy, hypnotic state, diminished reflexes, ataxia, and hypotonia. Rarely, paradoxical or disinhibitory reactions (including agitation, irritability, impulsivity, violent behavior, confusion, restlessness, excitement, and talkativeness) may occur. In severe overdosage cases, patients may develop respiratory depression and coma. Overdosage of benzodiazepines in combination with other CNS depressants (including alcohol and opioids) may be fatal [see Warnings and Precautions (5.2) ] . Markedly abnormal (lowered or elevated) blood pressure, heart rate, or respiratory rate raise the concern that additional drugs and/or alcohol are involved in the overdosage. Management of Overdosage In managing benzodiazepine overdosage, employ general supportive measures, including intravenous fluids and airway management.

• Jul 2, 2020NDANDA212295Acacia

1. 1Anaphylactic Shock2122%
2. 2Vascular Access Site Occlusion1111%
3. 3Anaphylactic Reaction99.4%
4. 4Hypotension99.4%
5. 5Off Label Use88.3%
6. 6Blood Pressure Decreased66.3%
7. 7Oxygen Saturation Decreased66.3%
8. 8Cardiac Arrest55.2%
9. 9Erythema55.2%
10. 10Hypersensitivity55.2%
11. 11Tachycardia55.2%
12. 12Bronchospasm44.2%
13. 13Drug Ineffective44.2%
14. 14Drug Interaction33.1%
15. 15Flushing33.1%

The 10 most recently updated of 278 ClinicalTrials.gov registrations naming Remimazolam as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• RemImazolam Besylate for ICU-sedation in Patients With Mechanical Ventilation After Oral and Maxillofacial Surgery
  Suspended · Phase 4 · Interventional · 117 enrolled · Nanfang Hospital, Southern Medical University
  NCT05606315updated 2026-06-10
• A Trial of Remimazolam for Intraoperative Sedation in Pediatric and Adolescent Patients
  Completed · Phase 2 · Phase 3 · Interventional · 249 enrolled · Jiangsu HengRui Medicine Co., Ltd.
  NCT07036419updated 2026-06-04
• Response Surface Modeling of Remimazolam and Sevoflurane
  Recruiting · Interventional · 80 enrolled · Pusan National University Yangsan Hospital
  NCT07620782updated 2026-06-02
• Deep Sedation vs. General Anesthesia for Pulsed Field Ablation in Atrial Fibrillation
  Not yet recruiting · Interventional · 80 enrolled · Second Affiliated Hospital of Nanchang University
  NCT07621432updated 2026-06-02
• The Effect of Remimazolam Versus Propofol on Postoperative Extubation Time
  Recruiting · Phase 4 · Interventional · 82 enrolled · Xuyu Zhang
  NCT07611344updated 2026-05-28
• Sedation During Endoscopy Using Remimazolam: Efficacy in a Novel Exploration
  Active not recruiting · Phase 3 · Interventional · 100 enrolled · Massachusetts General Hospital
  NCT07269808updated 2026-05-22
• Remimazolam-Propofol Combination Sedation for Gastrointestinal Endoscopy: A Prospective Observational Study
  Completed · Observational · 29 enrolled · University of Medicine and Pharmacy "Victor Babes" Timisoara
  NCT07604480updated 2026-05-22
• Tolerability of Remimazolam Versus Midazolam in EUS
  Recruiting · Observational · 126 enrolled · Azienda Socio Sanitaria Territoriale di Lecco
  NCT07600073updated 2026-05-20
• Effects of Remimazolam on Neurocognitive Function in Patients Undergoing Cardiovascular Surgery
  Not yet recruiting · Observational · 210 enrolled · Chinese Academy of Medical Sciences, Fuwai Hospital
  NCT07598019updated 2026-05-20
• Effect of Remimazolam Sedation on Outcomes of Mechanically Ventilated Patients in the ICU
  Recruiting · Phase 3 · Interventional · 80 enrolled · Southeast University, China
  NCT07596589updated 2026-05-19

Frequently asked questions

How does Remimazolam work?

BYFAVO is a benzodiazepine. BYFAVO binds to brain benzodiazepine sites (gamma amino butyric acid type A [GABA A ] receptors), while its carboxylic acid metabolite (CNS7054) has a 300 times lower affinity for the receptor.

What is Remimazolam used for?

According to FDA labeling, Remimazolam carries indications including: BYFAVO ® is indicated for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less. BYFAVO (remimazolam) for injection is a benzodiazepine indicated for the induction and maintenance of procedural sedation in adults undergoing procedures lasting 30 minutes or less.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Remimazolam?

Remimazolam is classified as Benzodiazepine derivatives, GABA A Modulators, Decreased Central Nervous System GABA Activity.

What are the brand names for Remimazolam?

Remimazolam is marketed under brand names including Byfavo.

What are the contraindications for Remimazolam?

Remimazolam labeling lists contraindications including: BYFAVO is contraindicated in patients with a history of severe hypersensitivity reaction to dextran 40 or products containing dextran 40 [see Warnings and Precautions (5.3) ]. Hypersensitivity to dextran 40.. Always consult the full prescribing information and a clinician.