Name: | Midazolam |
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PubChem Compound ID: | 11359390 |
Description: | 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. |
Molecular formula: | C18H13ClFN3 |
Molecular weight: | 328.745 g/mol |
Name: | Midazolam |
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Name (isomeric): | DB00683 |
Drug Type: | small molecule |
Description: | 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. |
Synonyms: |
Dea No. 2884; Midazolamum [INN-Latin]; Midazolam Hcl; Midazolam Base
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Brand: | Dormicum, Versed |
Category: | Anesthetics, Intravenous, Adjuvants, Anesthesia, Anti-anxiety Agents, GABA Modulators, Hypnotics and Sedatives |
CAS number: | 59467-70-8 |
Indication: | For use as a sedative perioperatively. |
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Pharmacology: |
Midazolam is a short-acting benzodiazepine central nervous system (CNS) depressant. Pharmacodynamic properties of midazolam and its metabolites, which are similar to those of other benzodiazepines, include sedative, anxiolytic, amnesic and hypnotic activities. Benzodiazepine pharmacologic effects appear to result from reversible interactions with t...
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Mechanism of Action: |
It is thought that the actions of benzodiazepines such as midazolam are mediated through the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is one of the major inhibitory neurotransmitters in the brain. Benzodiazepines increase the activity of GABA, thereby producing a calming effect, relaxing skeletal muscles, and inducing sleep...
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Absorption: | Rapidly absorbed after oral administration (absolute bioavailability of the midazolam syrup in pediatric patients is about 36%, and intramuscular is greater than 90%). |
Protein binding: | 97% |
Biotransformation: | Midazolam is primarily metabolized in the liver and gut by human cytochrome P450 IIIA4 (CYP3A4) to its pharmacologic active metabolite, (alpha)-hydroxymidazolam, and 4-hydroxymidazolam. |
Route of elimination: | Midazolam is primarily metabolized in the liver and gut by human cytochrome P450 IIIA4 (CYP3A4) to its pharmacologic active metabolite, α-hydroxymidazolam, followed by glucuronidation of the α–hydroxyl metabolite which is present in unconjugated and conjugated forms in human plasma. The α- hydroxymidazolam glucuronide is then excreted in urine. No significant amount of parent drug or metabolites is extractable from urine before beta-glucuronidase and sulfatase deconjugation, indicating that the urinary metabolites are excreted mainly as conjugates. |
Half Life: | 2.2-6.8 hours |
Clearance: | 9.3 to 11 mL/min/kg [pediatric patients (6 months to <16 years old)] |
Toxicity: | LD50=825 mg/kg (Orally in rats). Signs of overdose include sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma, and deleterious effects on vital signs. |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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