Midazolam drug data and news

Midazolam drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Midazolam
Brand Names/Synonyms CHEMBANK1834; Dea No. 2884; Dormicum; Midazolam; Midazolam Base; Midazolam Hcl; Midazolamum [Inn-Latin]; Versed
Indication For use in pediatric patients for sedation, anxiolysis, and amnesia prior to diagnostic, therapeutic, or endoscopic procedures or before induction of anesthesia.
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Description Not Available
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 the (gamma)-amino butyric acid (GABA) benzodiazepine receptor in the CNS, the major inhibitory neurotransmitter in the central nervous system. The action of midazolam is readily reversed by the benzodiazepine receptor antagonist, flumazenil.
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. Benzodiazepines act as agonists at the benzodiazepine receptors, which form a component of the benzodiazepine-GABA receptor-chloride ionophore complex. Most anxiolytics appear to act through at least one component of this complex to enhance the inhibitory action of GABA.
Midazolam News
(When available)

Health Tip: Drugs to Avoid While Breast-Feeding  Feb 16, 2006
...says. Anti-anxiety drugs: Alprazolam, Diazepam, Lorazepam, Midazolam, Perphenazine, Prazepam, Quazepam, Temazepam. Antidepressant ... - Forbes

Postoperative Upper Airway Obstruction After Recovery of the Train ...  Feb 21, 2006
Spirometry was performed by a series of 3 repetitive spirometric maneuvers: the first before induction (under midazolam premedication), the second after ... - Anesthesia & Analgesia (subscription),

A Comparison of Dexmedetomidine Versus Conventional Therapy for ...  Feb 21, 2006
...patients having CEA under regional anesthesia and compared hemodynamic control using DEX versus a conventional sedation technique using midazolam and fentanyl ... - Anesthesia & Analgesia (subscription),

Nurse on trial over 29 deaths  Feb 7, 2006
Letter is alleged to have used a mixture of the sedative midazolam, the anesthetic etomidate and the muscle relaxant lysthenon to kill the patients. ... - CNN International

German nurse charged with murder of patients  Feb 7, 2006
Police say Letter used a mixture of the sedative midazolam, the anesthetic etomidate and the muscle relaxant lysthenon to kill the patients. ... - Mail & Guardian Online,

I don't remember how many patients I killed, says nurse  Feb 7, 2006
He is alleged to have used a mixture of the sedative midazolam, the anaesthetic etomidate and the muscle relaxant suxamethonium chloride to kill the patients. ... - Scotsman,

A&E nurse 'poisoned 18 patients' so he could enjoy trying to save ...  Feb 14, 2006
Smith said. This contained traces of vecuronium and midazolam, muscle relaxants used in surgery and lethal injections. Mr Austin ... - Telegraph.co.uk,

Roche to Focus Resources on Availability of Invirase, Now ...  Feb 6, 2006
Invirase/ritonavir should not be administered concurrently with terfenadine, cisapride, astemizole, pimozide, triazolam, midazolam or ergot derivatives. ... - DG News

A Strange Place to Find a Cable Tie  Feb 14, 2006
After IV sedation with midazolam, anesthesia was induced with propofol, fentanyl, and rocuronium; the trachea was intubated with a number 8.0 endotracheal tube ... - Anesthesia & Analgesia (subscription),

Coroner slams mental health unit over death  Feb 13, 2006
However, Mr Barnes said the administering of the drugs midazolam, diazepam and thioridazine or Melleril over a 30-hour period, as well as the failure of staff ... - Brisbane Courier Mail,

Boehringer Ingelheim Announces 48-week Results from Aptivus(R) ...  Feb 9, 2006
...propafenone, quinidine, astemizole, terfenadine, dihydroergotamine, ergonovine, ergotamine, methylergonovine, cisapride, pimozide, midazolam, or triazolam, due ... - PR Newswire (press release),

Nurse trial over 29 dead  Feb 6, 2006
Police said Letter used a mixture of the sedative midazolam, the anaesthetic etomidate and the muscle relaxant lysthenon to bump off patients during a 17-month ... - The Sun,

Dosage Forms LIQUID; SOLUTION
Drug_Category Anesthetics, Intravenous; Anti-anxiety Agents; Hypnotics and Sedatives; Adjuvants, Anesthesia; GABA Modulators; ATC:N05CD08
Absorption Rapidly absorbed after oral administration (absolute bioavailability of the midazolam syrup in pediatric patients is about 36%, and intramuscular is greater than 90%).
Interactions Interactions for Midazolam:

Drug Interactions:    Inhibitors of CYP3A4 Isozymes: Caution is advised when midazolam is administered concomitantly with drugs that are known to inhibit the cytochrome P450 3A4 enzyme system (ie, some drugs in the drug classes of azole antimycotics, protease inhibitors, calcium channel antagonists, and macrolide antibiotics). Drugs such as erythromycin, diltiazem, verapamil, ketoconazole, fluconazole and itraconazole were shown to significantly increase the C max and AUC of orally administered midazolam. These drug interactions may result in increased and prolonged sedation due to a decrease in plasma clearance of midazolam. Although not studied, the potent cytochrome P450 3A4 inhibitors ritonavir and nelfinavir may cause intense and prolonged sedation and respiratory depression due to a decrease in plasma clearance of midazolam. Caution is advised when VERSED Syrup is used concomitantly with these drugs. Dose adjustments should be considered and possible prolongation and intensity of effect should be anticipated.

Inducers of CYP3A4 Isozymes:   Cytochrome P450 inducers, such as rifampin, carbamazepine, and phenytoin, induce metabolism and caused a markedly decreased C max and AUC of oral midazolam in adult studies. Although clinical studies have not been performed, phenobarbital is expected to have the same effect. Caution is advised when administering VERSED Syrup to patients receiving these medications and if necessary dose adjustments should be considered.

CNS Depressants:   One case was reported of inadequate sedation with chloral hydrate and later with oral midazolam due to a possible interaction with methylphenidate administered chronically in a 2-year-old boy with a history of William's syndrome. The difficulty in achieving adequate sedation may have been the result of decreased absorption of the sedatives due to both the gastrointestinal effects and stimulant effects of methylphenidate.

The sedative effect of VERSED Syrup is accentuated by any concomitantly administered medication which depresses the central nervous system, particularly narcotics (eg, morphine, meperidine and fentanyl), propofol, ketamine, nitrous oxide, secobarbital and droperidol. Consequently, the dose of VERSED Syrup should be adjusted according to the type and amount of concomitant medications administered and the desired clinical response.

No significant adverse interactions with common premedications (such as atropine, scopolamine, glycopyrrolate, diazepam, hydroxyzine, and other muscle relaxants) or local anesthetics have been observed.

Toxicity Oral, rat LD50: 825 mg/kg. Signs of overdose include sedation, somnolence, confusion, impaired coordination, diminished reflexes, coma, and deleterious effects on vital signs.
Organisms Affected Humans and other mammals
Chemical IUPAC Name Not Available
Chemical Formula C18H13ClFN3
Molecular Weight 325.767 g/mol
Smiles String CC1=NC=C2N1C3=C(C=C(C=C3)Cl)C(=NC2)C4=CC=CC=C4F
Melting Point 159 °C
Water Solubility 40.0 mg/ml
State Solid (white crystalline powder)
LogP/Hphobicity 3.868
Isoelectric Point Not Available
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.
Half Life 2.2-6.8 hours
Protein Binding [%] 97%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Midazolam.html
http://www.rxlist.com/cgi/generic2/versedsyr.htm
Drug Type Approved Drug
Accession No APRD00680
CAS Registry Number 59467-70-8
KEGG Compound ID C07524
PubChem ID SID:183492
PharmGKB ID PA450496
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2240286

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