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Midazolam

Generic Name
Midazolam
Brand Names
Buccolam, Busulfex, Nayzilam, Seizalam
Drug Type
Small Molecule
Chemical Formula
C18H13ClFN3
CAS Number
59467-70-8
Unique Ingredient Identifier
R60L0SM5BC

Overview

Midazolam is a short-acting hypnotic-sedative drug with anxiolytic, muscle relaxant, anticonvulsant, sedative, hypnotic, and amnesic properties. It belongs to a class of drugs called benzodiazepines. This drug is unique from others in this class due to its rapid onset of effects and short duration of action. Midazolam is available by oral, rectal, intranasal, intramuscular (IM), and intravenous (IV) routes and has been used in various biomedical applications, including dentistry, cardiac surgery, and endoscopic procedures as pre-anesthetic medication, and as an adjunct to local anesthesia. This drug was initially approved by the US FDA in 1985, and has been approved for various indications since. In late 2018, the intramuscular preparation was approved by the FDA for the treatment of status epilepticus in adults. In May 2019, the nasal spray of midazolam was approved for the acute treatment of distinctive intermittent, stereotypic seizure episodes in patients 12 years of age and older. Midazolam is considered a schedule IV drug in the United States due to the low potential for abuse and low risk of dependence.

Background

Midazolam is a short-acting hypnotic-sedative drug with anxiolytic, muscle relaxant, anticonvulsant, sedative, hypnotic, and amnesic properties. It belongs to a class of drugs called benzodiazepines. This drug is unique from others in this class due to its rapid onset of effects and short duration of action. Midazolam is available by oral, rectal, intranasal, intramuscular (IM), and intravenous (IV) routes and has been used in various biomedical applications, including dentistry, cardiac surgery, and endoscopic procedures as pre-anesthetic medication, and as an adjunct to local anesthesia. This drug was initially approved by the US FDA in 1985, and has been approved for various indications since. In late 2018, the intramuscular preparation was approved by the FDA for the treatment of status epilepticus in adults. In May 2019, the nasal spray of midazolam was approved for the acute treatment of distinctive intermittent, stereotypic seizure episodes in patients 12 years of age and older. Midazolam is considered a schedule IV drug in the United States due to the low potential for abuse and low risk of dependence.

Indication

Midazolam has different indications depending on its formulation by the FDA. Nasal For the nasal spray formulation, midazolam is indicated for the acute treatment of intermittent, stereotypic episodes of frequent seizure activity (i.e., seizure clusters, acute repetitive seizures) that are distinct from a patient’s usual seizure pattern in patients with epilepsy 12 years of age and older. Intravenous For the intravenous injection formulation, midazolam is indicated as an agent for sedation/anxiolysis/amnesia and prior to or during diagnostic, therapeutic or endoscopic procedures, such as bronchoscopy, gastroscopy, cystoscopy, coronary angiography, cardiac catheterization, oncology procedures, radiologic procedures, suture of lacerations and other procedures either alone or in combination with other CNS depressants. The sedative, anxiolytic and amnestic use of midazolam can also be employed pre-operatively. It can also be indicated for induction of general anesthesia, before administration of other anesthetic agents or as a component of intravenous supplementation of nitrous oxide and oxygen for a balanced anesthesia. A relatively narrower dose range of midazolam and a shorter period of induction can be achieved if midazolam is combined with narcotic premedication. Finally, midazolam can be indicated as a continous intravenous infusion for sedation of intubated and mechanically ventilated patients as a component of anesthesia or during treatment in a critical care setting. Intramuscular For the intramusuclar injection formulation, midazolam is indicated for preoperative sedation/anxiolysis/amnesia or for treatment of status epilepticus in adults. Oral Midazolam syrup is indicated for use in pediatric patients for sedation, anxiolysis and amnesia prior to diagnostic, therapeutic or endoscopic procedures or before induction of anesthesia. It is only approved in monitored settings only and not for chronic or home use. In Europe, a buccal formulation of midazolam is also approved for the treatment of prolonged, acute, convulsive seizures in infants, toddlers, children and adolescents (from 3 months to < 18 years). For infants between 3-6 months of age treatment should be in a hospital setting where monitoring is possible and resuscitation equipment is available.

Associated Conditions

  • Epileptic seizure
  • Status Epilepticus

Research Report

Published: Jun 5, 2025

Midazolam: A Comprehensive Pharmacological and Clinical Review

I. Introduction to Midazolam

A. Overview, Chemical Properties, and Brand Names

Midazolam is a potent, short-acting benzodiazepine characterized by a rapid onset of action. It is extensively utilized in clinical practice for managing seizures, inducing and maintaining anesthesia, and alleviating anxiety, particularly in procedural settings.[1] As a small molecule drug, it is identified by DrugBank ID DB00683 and CAS Number 59467-70-8.[1]

Chemically, midazolam is 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a]benzodiazepine. A notable characteristic of its formulation is its pH-dependent solubility. In acidic solutions, such as those used for parenteral preparations, midazolam exists as an equilibrium mixture of its closed-ring form and an open-ring structure. The open-ring form contributes to its water solubility, which is advantageous for formulation. However, at physiological pH (approximately 7.4), the equilibrium shifts significantly towards the lipophilic, pharmacologically active closed-ring form, facilitating its rapid passage across the blood-brain barrier and subsequent central nervous system (CNS) effects.[2] The presence of an imidazole ring in its structure is crucial for this pH-dependent characteristic, as well as for its stability in aqueous solutions and its rapid metabolic degradation.[3] This unique chemical behavior—water solubility for administration and lipophilicity for action—is a cornerstone of its rapid onset and clinical versatility, distinguishing it from many other benzodiazepines and underpinning its widespread application in acute medical situations.[2]

Midazolam is marketed under various brand names globally, including Versed®, Seizalam®, Nayzilam®, and Buccolam®.[1]

Table 1: Midazolam - Key Identifiers and Properties

Continue reading the full research report

Clinical Trials

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Title
Posted
Study ID
Phase
Status
Sponsor
2025/04/18
Phase 4
Not yet recruiting
First Affiliated Hospital of Wannan Medical College
2025/04/09
Phase 1
Completed
2025/04/08
Phase 1
Recruiting
2025/04/08
Phase 1
Completed
2025/03/20
Phase 4
Completed
Hanoi Medical University
2025/03/17
Not Applicable
ENROLLING_BY_INVITATION
2025/03/17
Phase 3
Not yet recruiting
2025/03/10
Phase 1
Completed
2025/02/19
Phase 2
Not yet recruiting
Asklepieion Voulas General Hospital
2025/02/12
Phase 1
Completed
Ahon Pharmaceutical Co., Ltd.

FDA Drug Approvals

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Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Athenex Pharmaceutical Division, LLC.
70860-600
INTRAVENOUS, INTRAMUSCULAR
2 mg in 2 mL
3/4/2024
Henry Schein, Inc.
0404-9914
INTRAVENOUS, INTRAMUSCULAR
5 mg in 1 mL
1/13/2022
Wockhardt USA LLC.
64679-763
INTRAMUSCULAR, INTRAVENOUS
5 mg in 1 mL
12/5/2017
Cantrell Drug Company
52533-001
INTRAVENOUS
1 mg in 1 mL
5/1/2014
Hikma Pharmaceuticals USA Inc.
0143-9380
INTRAVENOUS
1 mg in 1 mL
1/19/2023
Cantrell Drug Company
52533-157
INTRAVENOUS
0.5 mg in 1 mL
1/12/2015
Hikma Pharmaceuticals USA Inc.
0641-6218
INTRAMUSCULAR, INTRAVENOUS
5 mg in 1 mL
3/29/2024
Hospira, Inc.
0409-2305
INTRAMUSCULAR, INTRAVENOUS
1 mg in 1 mL
1/3/2023
Major Pharmaceuticals
0904-7114
ORAL
2 mg in 1 mL
10/28/2021
Bryant Ranch Prepack
72162-1109
ORAL
2 mg in 1 mL
10/25/2023

EMA Drug Approvals

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Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

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Approval Number
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Approval Date
No HSA approvals found for this drug.

NMPA Drug Approvals

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Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
Midazolam Injection
国药准字H20227065
化学药品
注射剂
5/19/2022
Midazolam Injection
国药准字H20243613
化学药品
注射剂
4/24/2024
Midazolam Injection
国药准字H20243615
化学药品
注射剂
4/24/2024
Midazolam Injection
国药准字H20067040
化学药品
注射剂
5/7/2021
Midazolam Injection
国药准字H20067041
化学药品
注射剂
5/7/2021
Midazolam Injection
国药准字H19990027
化学药品
注射剂
7/14/2020
Midazolam Injection
国药准字H10980025
化学药品
注射剂
7/14/2020
Midazolam Injection
国药准字H20031071
化学药品
注射剂
7/14/2020
Midazolam Injection
国药准字H20223202
化学药品
注射剂
4/8/2022
Midazolam Injection
国药准字H20143222
化学药品
注射剂
7/14/2020

PPB Drug Approvals

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Company
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Registration Date
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