Procedural sedation, Induction and maintenance

Benzodiazepine
Remimazolam is a benzodiazepine that 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."

1.Distribution: Vd: 0.76 to 0.98 L/kg.
2.Protein binding: >91%; primarily to albumin.
3.Metabolism: Via conversion to primary inactive metabolite CNS7054 by tissue carboxylesterases (primarily type 1A), which is then subject to hydroxylation and glucuronidation.
4.Half-life elimination: 37 to 53 minutes.
5.Excretion: Urine (0.003% [unchanged]; 50% to 60% [inactive metabolite]).

Severe hypersensitivity reaction to dextran 40 or products containing dextran 40 .

Induction of procedural sedation:
1.Healthy adults: IV: 5 mg over 1 minute.
2.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:
1.Healthy adults: IV: 2.5 mg over 15 seconds as needed; at least 2 minutes must elapse prior to administration of any supplemental dose.
2.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.

1.Mild to moderate impairment: There are no dosage adjustments provided in the manufacturer's labeling.
2.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.