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Lorazepam is metabolized in the liver by conjugation into inactive lorazepam-glucuronide. This metabolism does not involve liver oxidation, so is relatively unaffected by reduced liver function. Lorazepam-glucuronide is more water-soluble than its precursor, so gets more widely distributed in the body, leading to a longer half-life than lorazepam.
Typical Oral Dosage Formulations (mg) Approx. Equivalent Oral Dose to 10 mg Diazepam [b] (mg) Peak Onset of Action (hours) Elimination Half-life of Active Metabolite (hours) Primary Therapeutic Use Adinazolam: Deracyn: Research chemical: 1–2: 3: anxiolytic, antidepressant: Alprazolam
Ativan (Lorazepam) is commonly prescribed for the treatment of anxiety. It possesses many of the desirable effects of other benzodiazepines with amnesic properties. It is an effective sedative with a medium length half-life and is useful for appointments that are longer than two hours.
Benzodiazepines with a half-life of less than 24 hours include alprazolam, bromazepam, brotizolam, flunitrazepam, loprazolam, lorazepam, lormetazepam, midazolam, nitrazepam, oxazepam, and temazepam. [111] The resultant equivalent dose is then gradually reduced.
Commonly prescribed benzodiazepines in the U.S. are Valium (diazepam) and Ativan (lorazepam), which are used for muscle relaxation and to control anxiety and seizures.
Rebound insomnia, however, is more common upon discontinuation of intermediate-acting benzodiazepines than longer-acting benzodiazepines. Examples are alprazolam, estazolam, flunitrazepam, clonazepam, lormetazepam, lorazepam, nitrazepam, and temazepam. Long-acting compounds have a half-life of 40–250 hours.
The most significant difference in side effects of loprazolam and diazepam is it is less prone to day time sedation as the half-life of loprazolam is considered to be intermediate whereas diazepam has a very long half-life. The side effects of loprazolam are the following: drowsiness; paradoxical increase in aggression; lightheadedness; confusion
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