Midazolam

Midazolam (marketed under brand names Versed®, Hypnovel®, Dormicum® and Dormonid®, pronounced mɪˈdæzəlæm ) is a drug which is a benzodiazepine derivative. It has powerful anxiolytic, amnestic, hypnotic, anticonvulsant, skeletal muscle relaxant and sedative properties. It is considered a fast-acting benzodiazepine, with a short elimination half-life. It is therefore a very useful drug to use for short minor procedures such as dental extraction.

Midazolam was first synthesized in 1976 by Fryer and Walser.

Interactions
Midazolam is metabolized almost completely by cytochrome P450-3A4. Vmax in microsomes is reported as 850 pmol/min/mg microsomal protein. Km is reported as 3.7 uMol. Metabolism in the gut wall is reported as nearly equal to metabolism in liver by CYP3A4. Therefore, midazolam will interact with other 3A4 substrates and inhibitors. Grapefruit juice reduces intestinal 3A4 and results in less gut wall metabolism and higher plasma concentrations, which could result in overdose.

Contraindications
Hypersensitivity, acute narrow angle glaucoma, shock, hypotension, head injury, and drug or alcohol use. Some may be relative contraindications.

Overdose
Symptoms of midazolam overdose include:
 * Somnolence (difficulty staying awake)
 * Mental confusion
 * Hypotension
 * Impaired motor functions
 * Impaired reflexes
 * Impaired coordination
 * Impaired balance
 * Dizziness
 * Coma

In animal models, the oral LD50 of midazolam is 825 mg/kg.

Midazolam overdose is considered a medical emergency and generally requires the immediate attention of medical personnel. The antidote for an overdose of midazolam (or any other benzodiazepine) is flumazenil (Anexate®).

Legal status
Midazolam is a Schedule IV drug under the Convention on Psychotropic Substances.

Popular Culture
Prolonged after-effects of midazolam dosing after dental surgery inspired Duran Duran vocalist Simon Le Bon to entitle the group's 1997 album Medazzaland, likely in reference to psychotropic effects he experienced.