About: Midazolam     Goto   Sponge   Distinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type
http://linked.open...gbank/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. [PubChem] Midazolam is a schedule IV drug in the United States. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/6135616 # Isojarvi JI, Tokola RA: Benzodiazepines in the treatment of epilepsy in people with intellectual disability. J Intellect Disabil Res. 1998 Dec;42 Suppl 1:80-92. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10030438 # Garratt JC, Gent JP, Feely M, Haigh JR: Can benzodiazepines be classified by characterising their anticonvulsant tolerance-inducing potential? Eur J Pharmacol. 1988 Jan 5;145(1):75-80. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/2894998 # Tokunaga S, Takeda Y, Shinomiya K, Hirase M, Kamei C: Effects of some H1-antagonists on the sleep-wake cycle in sleep-disturbed rats. J Pharmacol Sci. 2007 Feb;103(2):201-6. Epub 2007 Feb 8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17287588 # Vermeeren A: Residual effects of hypnotics: epidemiology and clinical implications. CNS Drugs. 2004;18(5):297-328. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15089115 # FDA label (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • illicit (en)
http://linked.open...drugbank/halfLife
  • Intravenous, healthy adults = 1.8 to 6.4 hours (mean of 3 hours) (en)
http://linked.open...ugbank/indication
  • The midazolam injection is indicated for preoperative sedation/anziolysis/amnesia. It is also an agent for sedation/anziolysis/amnesia prior to or during diagnostic, therapeutic, or endoscopic procedures. Midazolam can also be given intravenously for induction of general anaesthesia. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Midazolam (en)
adms:identifier
http://linked.open...mechanismOfAction
  • 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. Benzodiazepines bind to the benzodiazepine site on GABA-A receptors, which potentiates the effects of GABA by increasing the frequency of chloride channel opening. (en)
http://linked.open...drugbank/packager
http://linked.open...outeOfElimination
  • 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. The amount of midazolam excreted unchanged in the urine when given intravenously is less than 0.5%. 45% to 57% of the dose was excreted in the urine as 1-hydroxymethyl midazolam conjugate. (en)
http://linked.open.../drugbank/synonym
  • Midazolam (en)
  • Dormicum (en)
  • Buccolam (en)
  • Midazolamum (en)
http://linked.open...drugbank/toxicity
  • LD<sub>50</sub>=825 mg/kg (Orally in rats). Signs of overdose include sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma, and deleterious effects on vital signs. (en)
http://linked.open...umeOfDistribution
  • * 1.24 to 2.02 L/kg [pediatric patients (6 months to <16 years) receiving 0.15 mg/kg IV midazolam,] * 1 to 3.1 L/kg [intravenously administered, healthy adults] Female gender, old age, and obesity may increase the volume of distribution. Midazolam may also cross the placenta and has been detected in human milk and cerebrospinal fluid. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Grapefruit juice slows the product's absorption and significantly increases its bioavailability. (en)
http://linked.open...nk/proteinBinding
  • 97% protein bound. (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...ynthesisReference
  • Madhup K. Dhaon, "Process for the preparation of midazolam." U.S. Patent US6262260, issued August, 1979. (en)
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...l/drug/hasATCCode
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