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تعداد آیتم قابل مشاهده باقیمانده : 2 مورد

Remimazolam: Drug information

Remimazolam: Drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Remimazolam: Patient drug information"

For abbreviations, symbols, and age group definitions show table
ALERT: US Boxed Warning
Personnel and equipment for monitoring and resuscitation

Only personnel trained in the administration of procedural sedation, and not involved in the conduct of the diagnostic or therapeutic procedure, should administer remimazolam. 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. Remimazolam has been associated with hypoxia, bradycardia, and hypotension. Continuously monitor vital signs during sedation and during the recovery period. Resuscitative drugs, and age- and size-appropriate equipment for bag/valve/mask assisted ventilation must be immediately available during administration of remimazolam.

Risks from concomitant use with opioid analgesics and other sedative-hypnotics

Concomitant use of benzodiazepines, including remimazolam, and opioid analgesics may result in profound sedation, respiratory depression, coma, and death. The sedative effect of intravenous remimazolam can be accentuated by concomitantly administered CNS depressant medications, including other benzodiazepines and propofol. Continuously monitor patients for respiratory depression and depth of sedation.

Brand Names: US
  • Byfavo
Pharmacologic Category
  • Benzodiazepine
Dosing: Adult
Sedation

Sedation:

Note: Individualize dosing and titrate to desired clinical effect; subsequent doses should be titrated on the basis of clinical judgement and assessment of the depth of sedation; if maintenance of procedural sedation is inadequate, consider alternative medications.

Induction of procedural sedation:

Healthy adults: IV: 5 mg over 1 minute.

American Society of Anesthesiologists physical status III or IV patients: IV: 2.5 to 5 mg over 1 minute based on general condition of patient.

Maintenance of procedural sedation:

Healthy adults: IV: 2.5 mg over 15 seconds as needed; at least 2 minutes must elapse prior to administration of any supplemental dose.

American Society of Anesthesiologists physical status III or IV patients: IV: 1.25 to 2.5 mg over 15 seconds as needed; at least 2 minutes must elapse prior to administration of any supplemental dose.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling; however, pharmacokinetics were not altered in patients with mild to severe renal impairment.

Dosing: Liver Impairment: Adult

Mild to moderate impairment: There are no dosage adjustments provided in the manufacturer’s labeling.

Severe impairment: There are no specific dosage adjustments provided in the manufacturer’s labeling; use caution and carefully titrate to effect; lower frequency of supplemental doses may be needed.

Dosing: Older Adult

Refer to adult dosing; use caution and administer supplemental doses slowly.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%:

Cardiovascular: Bradycardia (4% to 11%), decreased diastolic blood pressure (8% to 14%), hypertension (20% to 28%), hypotension (33% to 39%; increased diastolic blood pressure 10% to 25%), systolic hypertension (5% to 22%)

Respiratory: Hypoxia (22%), tachypnea (14%)

1% to 10%:

Cardiovascular: Tachycardia (8%)

Gastrointestinal: Nausea (4%)

Nervous system: Headache (3%)

Miscellaneous: Fever (4%)

Contraindications

Severe hypersensitivity to dextran 40 or products containing dextran 40.

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity: Hypersensitivity reactions, including rash, urticaria, pruritus, and anaphylaxis, may occur due to the presence of dextran.

Disease-related concerns:

• Hepatic impairment: Use caution in patients with severe hepatic impairment; carefully titrate to effect; lower frequency of supplemental doses may be needed.

• Respiratory disease: Reduce dose or avoid use in patients with respiratory disease, including chronic obstructive pulmonary disease or sleep apnea. Benzodiazepines may cause significant respiratory depression.

Concurrent drug therapy issues:

• Concomitant use with opioids: [US Boxed Warning]: Concomitant use of benzodiazepines, including remimazolam, and opioid analgesics may result in profound sedation, respiratory depression, coma, and death; sedative effect may be accentuated by concomitantly administered CNS depressant medications, including other benzodiazepines and propofol. These respiratory effects are more likely to occur in patients with obstructive sleep apnea, the elderly, and the American Society of Anesthesiologists physical status III or IV patients. Continuously monitor patients for respiratory depression and depth of sedation.

Special populations:

• Elderly patients: Potential for faster onset of loss of consciousness and longer duration of action. Sedating drugs may cause confusion and over sedation in the elderly; use with caution.

• Pediatric: Neurotoxicity may occur in pediatric patients (unapproved use), particularly after repeated or prolonged exposures to anesthetic agents early in life, which may result in adverse cognitive or behavioral effects; weigh benefits against risks of anesthesia prior to elective procedures.

Other warnings/precautions:

• Personnel and equipment for monitoring and resuscitation: [US Boxed Warning]: Only personnel trained in the administration of procedural sedation should administer remimazolam and 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. Remimazolam has been associated with hypoxia, bradycardia, and hypotension; continuously monitor vital signs during sedation and during the recovery period. Resuscitative drugs and age- and size-appropriate equipment for bag/valve/mask assisted ventilation must be immediately available during administration.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous [preservative free]:

Byfavo: 20 mg (1 ea) [contains dextran 40, lactose monohydrate]

Generic Equivalent Available: US

No

Pricing: US

Solution (reconstituted) (Byfavo Intravenous)

20 mg (per each): $52.58

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Controlled Substance

C-IV

Administration: Adult

IV: Administer IV induction dose over 1 minute and maintenance dose over 15 seconds. Only persons trained in the administration of procedural sedation, and not involved in the conduct of the diagnostic or therapeutic procedure, should administer remimazolam.

Use: Labeled Indications

Sedation: Induction and maintenance of procedural sedation in adults undergoing procedures lasting ≤30 minutes.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Acrivastine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Alcohol (Ethyl): CNS Depressants may increase CNS depressant effects of Alcohol (Ethyl). Risk C: Monitor

Alizapride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Amisulpride (Oral): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

ARIPiprazole Lauroxil: May increase CNS depressant effects of Benzodiazepines. ARIPiprazole Lauroxil may increase hypotensive effects of Benzodiazepines. Specifically, the risk of orthostatic hypotension may be increased. Risk C: Monitor

ARIPiprazole: May increase CNS depressant effects of Benzodiazepines. ARIPiprazole may increase hypotensive effects of Benzodiazepines. Specifically, orthostatic hypotension may be increased. Risk C: Monitor

Articaine: May increase CNS depressant effects of CNS Depressants. Management: Consider reducing the dose of articaine if possible when used in patients who are also receiving CNS depressants. Monitor for excessive CNS depressant effects with any combined use. Risk D: Consider Therapy Modification

Azelastine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Benperidol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Beta-Acetyldigoxin: Benzodiazepines may increase serum concentration of Beta-Acetyldigoxin. Risk C: Monitor

Blonanserin: CNS Depressants may increase CNS depressant effects of Blonanserin. Management: Use caution if coadministering blonanserin and CNS depressants; dose reduction of the other CNS depressant may be required. Strong CNS depressants should not be coadministered with blonanserin. Risk D: Consider Therapy Modification

Brexanolone: CNS Depressants may increase CNS depressant effects of Brexanolone. Risk C: Monitor

Brimonidine (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Bromopride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Bromperidol: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Buclizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Buprenorphine: CNS Depressants may increase CNS depressant effects of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Risk D: Consider Therapy Modification

BusPIRone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Cannabinoid-Containing Products: CNS Depressants may increase CNS depressant effects of Cannabinoid-Containing Products. Risk C: Monitor

Certoparin: May increase serum concentration of Benzodiazepines. Risk C: Monitor

Cetirizine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk D: Consider Therapy Modification

Chloral Hydrate/Chloral Betaine: CNS Depressants may increase CNS depressant effects of Chloral Hydrate/Chloral Betaine. Management: Consider alternatives to the use of chloral hydrate or chloral betaine and additional CNS depressants. If combined, consider a dose reduction of either agent and monitor closely for enhanced CNS depressive effects. Risk D: Consider Therapy Modification

Chlormethiazole: May increase CNS depressant effects of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Risk D: Consider Therapy Modification

Chlorphenesin Carbamate: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

CloZAPine: Benzodiazepines may increase adverse/toxic effects of CloZAPine. Management: Consider decreasing the dose of (or possibly discontinuing) benzodiazepines prior to initiating clozapine. Monitor for respiratory depression, hypotension, and other toxicities if these agents are combined. Risk D: Consider Therapy Modification

CNS Depressants: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

Corticosteroids (Orally Inhaled): Benzodiazepines may increase adverse/toxic effects of Corticosteroids (Orally Inhaled). Specifically, the risk of pneumonia may be increased. Risk C: Monitor

Dantrolene: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Daridorexant: May increase CNS depressant effects of CNS Depressants. Management: Dose reduction of daridorexant and/or any other CNS depressant may be necessary. Use of daridorexant with alcohol is not recommended, and the use of daridorexant with any other drug to treat insomnia is not recommended. Risk D: Consider Therapy Modification

DexmedeTOMIDine: CNS Depressants may increase CNS depressant effects of DexmedeTOMIDine. Management: Monitor for increased CNS depression during coadministration of dexmedetomidine and CNS depressants, and consider dose reductions of either agent to avoid excessive CNS depression. Risk D: Consider Therapy Modification

Difelikefalin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Difenoxin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Dihydralazine: CNS Depressants may increase hypotensive effects of Dihydralazine. Risk C: Monitor

Dimethindene (Topical): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Dothiepin: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Doxylamine: CNS Depressants may increase CNS depressant effects of Doxylamine. Risk C: Monitor

DroPERidol: May increase CNS depressant effects of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Risk D: Consider Therapy Modification

Emedastine (Systemic): May increase CNS depressant effects of CNS Depressants. Management: Consider avoiding this combination if possible. If required, monitor for excessive sedation or CNS depression, limit the dose and duration of combination therapy, and consider CNS depressant dose reductions. Risk C: Monitor

Entacapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Esketamine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Flunarizine: CNS Depressants may increase CNS depressant effects of Flunarizine. Risk X: Avoid

Flunitrazepam: CNS Depressants may increase CNS depressant effects of Flunitrazepam. Management: Reduce the dose of CNS depressants when combined with flunitrazepam and monitor patients for evidence of CNS depression (eg, sedation, respiratory depression). Use non-CNS depressant alternatives when available. Risk D: Consider Therapy Modification

HydrOXYzine: May increase CNS depressant effects of CNS Depressants. Management: Consider a decrease in the CNS depressant dose, as appropriate, when used together with hydroxyzine. Increase monitoring of signs/symptoms of CNS depression in any patient receiving hydroxyzine together with another CNS depressant. Risk D: Consider Therapy Modification

Ilaprazole: May increase serum concentration of Benzodiazepines. Risk C: Monitor

Ixabepilone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Kava Kava: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ketotifen (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Kratom: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Lemborexant: May increase CNS depressant effects of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Risk D: Consider Therapy Modification

Levocetirizine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Lisuride: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Lofepramine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Lofexidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Loxapine: CNS Depressants may increase CNS depressant effects of Loxapine. Management: Consider reducing the dose of CNS depressants administered concomitantly with loxapine due to an increased risk of respiratory depression, sedation, hypotension, and syncope. Risk D: Consider Therapy Modification

Magnesium Sulfate: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Melatonin: May increase sedative effects of Benzodiazepines. Risk C: Monitor

Melitracen [INT]: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Mequitazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Metergoline: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Methadone: Benzodiazepines may increase CNS depressant effects of Methadone. Management: Clinicians should generally avoid concurrent use of methadone and benzodiazepines when possible; any combined use should be undertaken with extra caution. Risk D: Consider Therapy Modification

Methotrimeprazine: CNS Depressants may increase CNS depressant effects of Methotrimeprazine. Methotrimeprazine may increase CNS depressant effects of CNS Depressants. Management: Reduce the usual dose of CNS depressants by 50% if starting methotrimeprazine until the dose of methotrimeprazine is stable. Monitor patient closely for evidence of CNS depression. Risk D: Consider Therapy Modification

Methoxyflurane: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Metoclopramide: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

MetyroSINE: CNS Depressants may increase sedative effects of MetyroSINE. Risk C: Monitor

Minocycline (Systemic): May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Moxonidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Nabilone: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Nalfurafine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Noscapine: CNS Depressants may increase adverse/toxic effects of Noscapine. Risk X: Avoid

OLANZapine: Benzodiazepines may increase adverse/toxic effects of OLANZapine. Management: Monitor closely for hypotension, respiratory or central nervous system depression, and bradycardia if olanzapine is combined with benzodiazepines. Use of parenteral benzodiazepines with IM olanzapine is not recommended. Risk C: Monitor

Olopatadine (Nasal): May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Opicapone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Opioid Agonists: CNS Depressants may increase CNS depressant effects of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification

Opipramol: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Orphenadrine: CNS Depressants may increase CNS depressant effects of Orphenadrine. Risk X: Avoid

Oxomemazine: May increase CNS depressant effects of CNS Depressants. Risk X: Avoid

Oxybate Salt Products: Benzodiazepines may increase CNS depressant effects of Oxybate Salt Products. Risk X: Avoid

OxyCODONE: CNS Depressants may increase CNS depressant effects of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Risk D: Consider Therapy Modification

Paliperidone: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Paraldehyde: CNS Depressants may increase CNS depressant effects of Paraldehyde. Risk X: Avoid

Perampanel: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Periciazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Pipamperone: May increase adverse/toxic effects of CNS Depressants. Risk C: Monitor

Piribedil: CNS Depressants may increase CNS depressant effects of Piribedil. Risk C: Monitor

Pizotifen: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Pramipexole: CNS Depressants may increase sedative effects of Pramipexole. Risk C: Monitor

Procarbazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Rilmenidine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Ropeginterferon Alfa-2b: CNS Depressants may increase adverse/toxic effects of Ropeginterferon Alfa-2b. Specifically, the risk of neuropsychiatric adverse effects may be increased. Management: Avoid coadministration of ropeginterferon alfa-2b and other CNS depressants. If this combination cannot be avoided, monitor patients for neuropsychiatric adverse effects (eg, depression, suicidal ideation, aggression, mania). Risk D: Consider Therapy Modification

ROPINIRole: CNS Depressants may increase sedative effects of ROPINIRole. Risk C: Monitor

Rotigotine: CNS Depressants may increase sedative effects of Rotigotine. Risk C: Monitor

Suvorexant: CNS Depressants may increase CNS depressant effects of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Risk D: Consider Therapy Modification

Teduglutide: May increase serum concentration of Benzodiazepines. Risk C: Monitor

Thalidomide: CNS Depressants may increase CNS depressant effects of Thalidomide. Risk X: Avoid

Theophylline Derivatives: May decrease therapeutic effects of Benzodiazepines. Risk C: Monitor

Trimeprazine: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Valerian: May increase CNS depressant effects of CNS Depressants. Risk C: Monitor

Yohimbine: May decrease therapeutic effects of Antianxiety Agents. Risk C: Monitor

Zolpidem: CNS Depressants may increase CNS depressant effects of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Risk D: Consider Therapy Modification

Zuranolone: May increase CNS depressant effects of CNS Depressants. Management: Consider alternatives to the use of zuranolone with other CNS depressants or alcohol. If combined, consider a zuranolone dose reduction and monitor patients closely for increased CNS depressant effects. Risk D: Consider Therapy Modification

Pregnancy Considerations

Benzodiazepines cross the placenta.

In utero exposure to benzodiazepines has the potential to cause harm to the fetus. Teratogenic effects have been observed in some studies; however, a clear association has not been reported and additional data are needed (Bellantuono 2013; Chuang 2024; Freeman 2018; Grigoriadis 2019; Tinker 2019; Wu 2024). Exposure to a benzodiazepine late in pregnancy may cause neonatal sedation (hypotonia, lethargy, respiratory depression) and/or symptoms of neonatal withdrawal (feeding difficulties, hyperreflexia, inconsolable crying, irritability, restlessness, tremors). Monitor newborns exposed to remimazolam in utero for adverse events. Data related to long-term effects on neurodevelopment following maternal use of benzodiazepines are inconclusive (Andrade 2024; Radojčić 2017; Sundbakk 2024; Wang 2022).

Based on animal data, repeated or prolonged use of general anesthetic and sedation medications that block N-methyl-D-aspartate receptors and/or potentiate GABA activity may affect brain development.

The American College of Obstetricians and Gynecologists recommends that pregnant patients should not be denied medically necessary surgery regardless of trimester. If the procedure is elective, it should be delayed until after delivery (ACOG 2019).

Breastfeeding Considerations

It is not known if remimazolam is present in breast milk.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Lactating patients may express and discard milk for 5 hours after administration to decrease potential exposure to an infant via breast milk. Monitor breastfed infants for sedation, respiratory depression, and feeding problems.

The Academy of Breastfeeding Medicine recommends postponing elective surgery until milk supply and breastfeeding are established. Milk should be expressed ahead of surgery when possible. In general, when the child is healthy and full term, breastfeeding may resume, or milk may be expressed once the mother is awake and in recovery. For children who are at risk for apnea, hypotension, or hypotonia, milk may be saved for later use when the child is at lower risk (ABM [Reece-Stremtan 2017]).

Monitoring Parameters

Monitor vital signs continuously (during sedation and through the recovery period), especially for signs of respiratory depression, hypotension, hypoventilation, airway obstruction, apnea, and oxygen desaturation; cardiorespiratory complications (especially in elderly and hepatic impairment patients).

Mechanism of Action

Short-acting benzodiazepine (Griffin 2013). Binds to brain benzodiazepine sites (GABA-A receptors) while its carboxylic acid metabolite (CNS7054) has a 300 times lower affinity for the receptor. Remimazolam does not show a clear selectivity between subtypes of the GABA-A receptor

Pharmacokinetics (Adult Data Unless Noted)

Duration:

Classified as a short-acting benzodiazepine; classification based on benzodiazepines with half-life of 1 to 12 hours (Griffin 2013).

Indication-specific durations:

Sedation: Time to full alertness: 11 to 14 minutes after last dose.

Distribution: Vd: 0.76 to 0.98 L/kg.

Protein binding: >91%; primarily to albumin.

Metabolism: Via conversion to primary inactive metabolite CNS7054 by tissue carboxylesterases (primarily type 1A), which is then subject to hydroxylation and glucuronidation.

Half-life elimination: 37 to 53 minutes.

Time to peak: Sedation: 3 to 3.5 minutes (single dose); 11 to 14 minutes (multiple dose).

Excretion: Urine (0.003% [unchanged]; 50% to 60% [inactive metabolite]).

Pharmacokinetics: Additional Considerations (Adult Data Unless Noted)

Renal impairment: In patients with renal impairment, AUC and Cmax was not significantly different from normal to severe renal impairment.

Hepatic impairment: In patients with moderate to severe impairment, Cmax was reduced by 10% and 20%, half-life is prolonged by 60 and 105 minutes, and volume of distribution increased by 33% and 41%, respectively, compared to healthy patients.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (BG) Bulgaria: Byfavo;
  • (CN) China: Rui ma;
  • (CZ) Czech Republic: Byfavo;
  • (EE) Estonia: Byfavo;
  • (FI) Finland: Byfavo;
  • (GB) United Kingdom: Byfavo;
  • (HU) Hungary: Byfavo;
  • (LV) Latvia: Byfavo;
  • (NL) Netherlands: Byfavo;
  • (NO) Norway: Byfavo;
  • (PR) Puerto Rico: Byfavo;
  • (RO) Romania: Byfavo;
  • (SK) Slovakia: Byfavo;
  • (TW) Taiwan: Byfavo
  1. American College of Obstetricians and Gynecologists (ACOG). ACOG Committee Opinion No. 775: Nonobstetric surgery during pregnancy. Obstet Gynecol. 2019;133(4):e285-e286. doi:10.1097/AOG.0000000000003174 [PubMed 30913200]
  2. Andrade C, Varadharajan N, Bascarane S, Menon V. Gestational exposure to benzodiazepines or z-hypnotics and neurodevelopmental disorders in offspring: systematic review and meta-analysis. Acta Psychiatr Scand. 2024;150(2):65-77. doi:10.1111/acps.13696 [PubMed 38751163]
  3. Bach V, Carl P, Ravlo O, et al. A randomized comparison between midazolam and thiopental for elective cesarean section anesthesia: III. Placental transfer and elimination in neonates. Anesth Analg. 1989;68(3):238-242. [PubMed 2919760]
  4. Bellantuono C, Tofani S, Di Sciascio G, Santone G. Benzodiazepine exposure in pregnancy and risk of major malformations: a critical overview. Gen Hosp Psychiatry. 2013;35(1):3-8. doi:10.1016/j.genhosppsych.2012.09.003 [PubMed 23044244]
  5. Byfavo (remimazolam) [prescribing information]. Indianapolis, IN: Acacia Pharma Inc; January 2023.
  6. Chuang HM, Meng LC, Lin CW, et al. Concomitant use of antidepressants and benzodiazepines during pregnancy and associated risk of congenital malformations: a population-based cohort study in Taiwan. Lancet Psychiatry. 2024;11(8):601-610. doi:10.1016/S2215-0366(24)00176-7 [PubMed 38968942]
  7. Freeman MP, Góez-Mogollón L, McInerney KA, et al. Obstetrical and neonatal outcomes after benzodiazepine exposure during pregnancy: results from a prospective registry of women with psychiatric disorders. Gen Hosp Psychiatry. 2018;53:73-79. doi:10.1016/j.genhosppsych.2018.05.010 [PubMed 29958100]
  8. Griffin CE 3rd, Kaye AM, Bueno FR, Kaye AD. Benzodiazepine pharmacology and central nervous system-mediated effects. Ochsner J. 2013;13(2):214-223. [PubMed 23789008]
  9. Grigoriadis S, Graves L, Peer M, et al. Benzodiazepine use during pregnancy alone or in combination with an antidepressant and congenital malformations: systematic review and meta-analysis. J Clin Psychiatry. 2019;80(4):18r12412. doi:10.4088/JCP.18r12412 [PubMed 31294935]
  10. Radojčić MR, El Marroun H, Miljković B, et al. Prenatal exposure to anxiolytic and hypnotic medication in relation to behavioral problems in childhood: a population-based cohort study. Neurotoxicol Teratol. 2017;61:58-65. doi:10.1016/j.ntt.2017.02.005 [PubMed 28259732]
  11. Reece-Stremtan S, Campos M, Kokajko L; Academy of Breastfeeding Medicine. ABM Clinical Protocol #15: analgesia and anesthesia for the breastfeeding mother, revised 2017. Breastfeed Med. 2017;12(9):500-506. doi:10.1089/bfm.2017.29054.srt [PubMed 29624435]
  12. Sundbakk LM, Wood M, Gran JM, Nordeng H. Prenatal exposure to benzodiazepine and z-hypnotics and fifth-grade scholastic skills - emulating target trials using data from the Norwegian Mother, Father and Child Cohort Study. Am J Epidemiol. 2024:kwae159. doi:10.1093/aje/kwae159 [PubMed 38944758]
  13. Tinker SC, Reefhuis J, Bitsko RH, et al; National Birth Defects Prevention Study. Use of benzodiazepine medications during pregnancy and potential risk for birth defects, National Birth Defects Prevention Study, 1997-2011. Birth Defects Res. 2019;111(10):613-620. doi:10.1002/bdr2.1497 [PubMed 30891943]
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Topic 128915 Version 106.0