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Midazolam hydrochloride

Midazolam hydrochloride structure

CAS No:
59467-96-8
Formula:
C18H13ClFN3.ClH
Chemical Name:
Midazolam hydrochloride
Synonyms:
4H-Imidazo[1,5-a][1,4]benzodiazepine,8-chloro-6-(2-fluorophenyl)-1-methyl-,hydrochloride (1:1);4H-Imidazo[1,5-a][1,4]benzodiazepine,8-chloro-6-(2-fluorophenyl)-1-methyl-,monohydrochloride;Midazolam hydrochloride;Versed;Hypnovel;Rocam;Ro 21-3981/003;Syrpalta
Categories:
Active Pharmaceutical Ingredients > Nervous System Drugs

Description

Midazolam hydrochloride is the hydrochloride salt of midazolam. It has a role as an anticonvulsant, an antineoplastic agent, an anxiolytic drug, an apoptosis inducer, a central nervous system depressant, a GABAA receptor agonist, a general anaesthetic, a muscle relaxant and a sedative. It is an imidazobenzodiazepine and a hydrochloride. It contains a midazolam.|Versed is a DEA Schedule IV controlled substance. Substances in the DEA Schedule IV have a low potential for abuse relative to substances in Schedule III.|Midazolam Hydrochloride is the hydrochloride salt of a short-acting benzodiazepine derivative with an imidazole structure and anxiolytic, amnestic, hypnotic, anticonvulsant and sedative properties. Midazolam binds to the benzodiazepine receptor at the gamma-aminobutyric acid (GABA) receptor-chloride ionophore complex in the central nervous system (CNS), resulting in increases in the opening of chloride channels, membrane hyperpolarization, and the inhibitory effect of GABA. This agent may also interfere with the reuptake of GABA, thereby causing accumulation of GABA in the synaptic cleft.|A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.

Midazolam hydrochloride Basic Attributes

Molecular Weight：

362.23

Exact Mass：

361.05500

EC Number：

261-776-6

UNII：

W7TTW573JJ

DEA Code Number：

2884

NSC Number：

751451

DSSTox ID：

DTXSID8047846

NCI Thesaurus Code：

C654

HScode：

2933910000

Characteristics

PSA：

30.2

XLogP3：

4.56180

Boiling Point：

496.9ºC at 760 mmHg

Storage Conditions：

2-8°C

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

3249

RTECS Number：

NI2922250

Precautionary statement(s)：

P201, P202, P260, P261, P263, P264, P270, P271, P281, P301+P312, P304+P340, P308+P313, P312, P330, P403+P233, P405, P501

Hazard Statements：

H302

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P260, P261, P263, P264, P270, P271, P281, P301+P312, P304+P340, P308+P313, P312, P330, P403+P233, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

Drug Indication：

Epileptic seizures

MeSH：

Ultrashort-acting anesthetics that are used for induction. Loss of consciousness is rapid and induction is pleasant, but there is no muscle relaxation and reflexes frequently are not reduced adequately. Repeated administration results in accumulation and prolongs the recovery time. Since these agents have little if any analgesic activity, they are seldom used alone except in brief minor procedures. (From AMA Drug Evaluations Annual, 1994, p174) (See all compounds classified as Anesthetics, Intravenous.)|Agents that alleviate ANXIETY, tension, and ANXIETY DISORDERS, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions. ADRENERGIC BETA-ANTAGONISTS are commonly used in the symptomatic treatment of anxiety but are not included here. (See all compounds classified as Anti-Anxiety Agents.)|Agents that are administered in association with anesthetics to increase effectiveness, improve delivery, or decrease required dosage. (See all compounds classified as Adjuvants, Anesthesia.)|Substances that do not act as agonists or antagonists but do affect the GAMMA-AMINOBUTYRIC ACID receptor-ionophore complex. GABA-A receptors (RECEPTORS, GABA-A) appear to have at least three allosteric sites at which modulators act: a site at which BENZODIAZEPINES act by increasing the opening frequency of GAMMA-AMINOBUTYRIC ACID-activated chloride channels; a site at which BARBITURATES act to prolong the duration of channel opening; and a site at which some steroids may act. GENERAL ANESTHETICS probably act at least partly by potentiating GABAergic responses, but they are not included here. (See all compounds classified as GABA Modulators.)|Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. (See all compounds classified as Hypnotics and Sedatives.)

MeSH Entry Terms：

Dormicum

DEA Controlled Substances：

Midazolam|Versed|2884|Schedule IV - Substances in the DEA Schedule IV have a low potential for abuse relative to substances in Schedule III.|No

Midazolam hydrochloride Use and Manufacturing

Uses

Anti-Spasmodic

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human drugs -> Rare disease (orphan)|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:362.2
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:1
Exact Mass:361.0548810
Monoisotopic Mass:361.0548810
Topological Polar Surface Area:30.2
Heavy Atom Count:24
Complexity:471
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes