Dormicum - General Information: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] Dormicum is a schedule IV drug in the United States.
Pharmacology:Dormicum 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.
Dormicum for patients
To assure safe and effective use of VERSED Syrup, the following information and instructions should be communicated to the patient when appropriate: 1. Inform your physician about any alcohol consumption and medicine you are now taking, especially blood pressure medication and antibiotics, including drugs you buy without a prescription. Alcohol has an increased effect when consumed with benzodiazepines; therefore, caution should be exercised regarding simultaneous ingestion of alcohol during benzodiazepine treatment, 2. Inform your physician if you are pregnant or are planning to become pregnant, 3. Inform your physician if you are nursing, 4. Patients should be informed of the pharmacological effects of VERSED Syrup, such as sedation and amnesia, which in some patients may be profound. The decision as to when patients who have received VERSED Syrup, particularly on an outpatient basis, may again engage in activities requiring complete mental alertness, operate hazardous machinery or drive a motor vehicle must be individualized, 5. VERSED Syrup should not be taken in conjunction with grapefruit juice, and 6. For pediatric patients, particular care should be taken to assure safe ambulation.
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.
Midazolam is contraindicated in patients with a known hypersensitivity to the drug. Benzodiazepines are contraindicated in patients with acute narrow-angle glaucoma. Benzodiazepines may be used in patients with open-angle glaucoma only if they are receiving appropriate therapy. Measurements of intraocular pressure in patients without eye disease show a moderate lowering following induction with Midazolam; patients with glaucoma have not been studied.
Midazolam is not intended for intrathecal or epidural administration due to the presence of the preservative benzyl alcohol in the dosage form.
Additional information about DormicumDormicum Indication: For use in pediatric patients for sedation, anxiolysis, and amnesia prior to diagnostic, therapeutic, or endoscopic procedures or before induction of anesthesia.
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.
Drug Interactions: Amprenavir Amprenavir increases the effect and toxicity of benzodiazepine
Fosamprenavir Amprenavir increases the effect and toxicity of benzodiazepine
Aprepitant Aprepitant increases the effect and toxicity of benzodiazepine
Atazanavir Atazanavir increases the effect and toxicity of benzodiazepine
Carbamazepine Carbamazepine reduces the effect of the benzodiazepine
Cimetidine Cimetidine increases the effect of benzodiazepine
Clozapine Increased risk of toxicity
Fluconazole Fluconazole increases the effect of benzodiazepine
Kava Kava increases the effect of benzodiazepine
Omeprazole Omeprazole increases the effect of benzodiazepine
Quinupristin This combination presents an increased risk of toxicity
Rifampin Rifampin increases the effect of benzodiazepine
St. John's Wort St. John's Wort could reduce the benzodiazepine effect
Telithromycin Telithromycin increases the effect/toxicity of the benzodiazepine
Voriconazole The imidazole increases the effect of benzodiazepine
Itraconazole The imidazole increases the effect of benzodiazepine
Ketoconazole The imidazole increases the effect of benzodiazepine
Clarithromycin The macrolide increases the effect of benzodiazepine
Erythromycin The macrolide increases the effect of benzodiazepine
Josamycin The macrolide increases the effect of benzodiazepine
Verapamil The calcium channel blocker increases the effect and toxicity of benzodiazepine
Diltiazem The calcium channel blocker increases the effect and toxicity of benzodiazepine
Delavirdine The antiviral agent increases the effect and toxicity of benzodiazepine
Docetaxel The agent increases the serum levels and toxicity of docetaxel
Efavirenz The antiviral agent increases the effect and toxicity of benzodiazepine
Indinavir The protease inhibitor increases the effect of benzodiazepine
Nelfinavir The protease inhibitor increases the effect of benzodiazepine
Ritonavir The protease inhibitor increases the effect of benzodiazepine
Saquinavir The protease inhibitor increases the effect of benzodiazepine
Ethotoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Fosphenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Mephenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Phenytoin Possible increased levels of the hydantoin, decrease of benzodiazepine
Food Interactions: Not Available
Generic Name: Midazolam
Synonyms: Dea No. 2884; Midazolam Base; Midazolam Hcl; Midazolamum [Inn-Latin]
Drug Category: Anesthetics, Intravenous; Anti-anxiety Agents; Hypnotics and Sedatives; Adjuvants, Anesthesia; GABA Modulators
Drug Type: Small Molecule; Illicit; Approved
Other Brand Names containing Midazolam: Dormicum; Versed;
Absorption: Rapidly absorbed after oral administration (absolute bioavailability of the midazolam syrup in pediatric patients is about 36%, and intramuscular is greater than 90%).
Toxicity (Overdose): 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.
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.
Half Life: 2.2-6.8 hours
Dosage Forms of Dormicum: Solution Intravenous
Chemical IUPAC Name: 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine
Chemical Formula: C18H13ClFN3
Midazolam on Wikipedia: http://en.wikipedia.org/wiki/Midazolam
Organisms Affected: Humans and other mammals
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