Midazolam

Benzodiazepine — NERVOUS SYSTEM

Key facts

Midazolam is an ofp drug in the Benzodiazepine class catalogued in DrugCentral. It was first approved by the FDA in 1985. DrugCentral lists 13 molecular targets, including GABRG2|GABRB3|GABRA5, GABRG2|GABRA5|GABRB2 and GABRA1|GABRG2|GABRB2. Recorded indications include Anxiety, Conscious sedation, Feeling agitated and General anesthesia.

• Approval status: ofp (first approved 1985 by the FDA).
• Drug class: Benzodiazepine.
• Molecular targets: GABRG2|GABRB3|GABRA5, GABRG2|GABRA5|GABRB2, GABRA1|GABRG2|GABRB2 and Tspo (13 listed in DrugCentral).
• Indications: Anxiety, Conscious sedation, Feeling agitated, General anesthesia and Induce Anterograde Amnesia and others.
• ATC code: N05CD08 (Benzodiazepine derivatives).
• Molecular formula: C18H13ClFN3; molecular weight 325.77 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (11)

• Anxiety
• Conscious sedation
• Feeling agitated
• General anesthesia
• Induce Anterograde Amnesia
• Local anesthesia
• Preoperative Anxiety
• Sedation
• Sedation as Adjunct to Anesthesia
• Sedation in Intubated Patients
• Status epilepticus

Off-label uses (2)

• Cocaine-Associated Acute Ischemic Heart Disease
• Insomnia

Contraindications (10)

• Angle-closure glaucoma
• Chronic heart failure
• Chronic obstructive lung disease
• Cirrhosis of liver
• Coma
• End stage renal disease
• Hemodynamic instability
• Peripheral Vasoconstriction
• Pregnancy, function
• Shock

Mechanism & targets

• Established pharmacologic class: Benzodiazepine

Molecular targets (13)

Target	Gene	Action	Activity
GABA-A receptor alpha-5/beta-3/gamma-2	GABRG2|GABRB3|GABRA5	positive allosteric modulator	Ki 9.12
GABA A receptor alpha-5/beta-2/gamma-2	GABRG2|GABRA5|GABRB2	positive allosteric modulator	Ki 9.12
GABA-A receptor alpha-1/beta-2/gamma-2	GABRA1|GABRG2|GABRB2	positive allosteric modulator	Ki 8.74
Translocator protein	Tspo	unknown	Ki 8.70
GABA-A receptor; anion channel	Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre	unknown	Ki 8.70
GABA A receptor alpha-3/beta-2/gamma-2	GABRG2|GABRA3|GABRB2	positive allosteric modulator	Ki 8.44
GABA A receptor alpha-5/beta-3/gamma-3	GABRB3|GABRA5|GABRG3	positive allosteric modulator	Ki 8.26
GABA A receptor alpha-5/beta-2/gamma-3	GABRA5|GABRB2|GABRG3	positive allosteric modulator	Ki 8.26
GABA-A receptor alpha-1/beta-2/gamma-3	GABRA1|GABRB2|GABRG3	positive allosteric modulator	Ki 7.75
GABA A receptor alpha-3/beta-2/gamma-3	GABRA3|GABRB2|GABRG3	positive allosteric modulator	Ki 7.61
Cytochrome P450 3A4	CYP3A4	unknown	Km 6.00
Thyrotropin-releasing hormone receptor	Trhr	antagonist	Ki 5.49
Multidrug resistance protein 1	ABCB1	unknown	Km 4.35

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2020-09-25	PMDA	—	TAKEDA PHARMACEUTICAL COMPANY LIMITED	Yes
2011-09-04	EMA	—	Laboratorios Lesvi S.L.
1985-12-20	FDA	—	—	Yes

ATC classification

ATC code	Therapeutic hierarchy
N05CD08	NERVOUS SYSTEM › PSYCHOLEPTICS › HYPNOTICS AND SEDATIVES › Benzodiazepine derivatives

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Status epilepticus	943.6
Drug ineffective	790.6
Hypotension	722.4
Multiple-drug resistance	692.3
Cardiac arrest	672.9
Drug ineffective for unapproved indication	643.5
Serotonin syndrome	530.4
Propofol infusion syndrome	478.8
Anaphylactic reaction	424.0
Drug interaction	412.0
Seizure	411.7
Respiratory failure	377.8

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Midazolam is on its molecule page.

• Molecular formula: C₁₈H₁₃ClFN₃
• Molecular weight: 325.77 g/mol
• CAS number: 59467-70-8
• InChIKey: DDLIGBOFAVUZHB-UHFFFAOYSA-N
• PubChem CID: 4192

CC1=NC=C2CN=C(C3=CC(Cl)=CC=C3N12)C1=C(F)C=CC=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Midazolam used for?

DrugCentral lists the following indications for Midazolam: Anxiety, Conscious sedation, Feeling agitated, General anesthesia, Induce Anterograde Amnesia, Local anesthesia, Preoperative Anxiety and Sedation and others.

How does Midazolam work?

Its molecular targets in DrugCentral include GABRG2|GABRB3|GABRA5 (positive allosteric modulator), GABRG2|GABRA5|GABRB2 (positive allosteric modulator), GABRA1|GABRG2|GABRB2 (positive allosteric modulator) and Tspo.

When was Midazolam first approved?

Midazolam was first approved by the FDA in 1985.

What drug class does Midazolam belong to?

Midazolam is in the Benzodiazepine class.

What is the chemical formula of Midazolam?

Midazolam has the molecular formula C18H13ClFN3 and a molecular weight of 325.77 g/mol.

Sources

• DrugCentral drug card 1802 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200420 — compound record and bioactivity
• PubChem CID 4192 — chemical identifiers
• DrugBank DB00683 — drug record
• FDA UNII R60L0SM5BC — substance identity
• DailyMed: FDA labels for Midazolam — current prescribing information (label search)
• UniProt P08684 (CYP3A4) — target protein
• UniProt P08183 (ABCB1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.