Delorazepam
Delorazepam Uses, Dosage, Side Effects, Food Interaction and all others data.
Delorazepam is a benzodiazepine which, like other drugs in its class, possesses anxiolytic, skeletal muscle relaxant, hypnotic and anticonvulsant properties. It may have adverse effects such as drowsiness, and cognitive impairments such as short term memory impairment.
Delorazepam is an active metabolite of the benzodiazepine known as cloxazolam. It is a long acting benzodiazepine which makes it superior in this sense to lorazepam which is short acting. Lorazepam is also a major active metabolite of delorazepam.
In addition to be long acting, delorazepam is relatively potent, with 1 mg of delorazepam being the equivalent of 10 mg diazepam. It has been approved for marketing in Italy.
| Trade Name | Delorazepam |
| Generic | Delorazepam |
| Delorazepam Other Names | Chlordesmethyldiazepam, Clordesmetildiazepam, Delorazepam, Delorazepamum |
| Type | |
| Formula | C15H10Cl2N2O |
| Weight | Average: 305.159 Monoisotopic: 304.017018366 |
| Protein binding | >90% protein bound. |
| Groups | Experimental, Illicit |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Delorazepam is a benzodiazepine used to manage severe anxiety disorders and insomnia.
Mainly used as an anti-anxiety agent. Studies have found delorazepam to be more effective in the first 4 weeks of use than antidepressants; however, after 4 weeks, antidepressants showed superior anti-anxiety effects. Anti-anxiety effects also appear to be weaker in elderly patients.
Effectiveness has also been observed in the treatment of alcohol withdrawal. Delorazapam was reported to be a manageable drug in that it did not exhibit severe side effects and did not require further therapies to control symptoms of withdrawal.
Delorazepam is also used to associated treatment for these conditions: Anxiety, Epilepsies, Insomnia, Sleep Disorder, Somatic Symptom Disorders, Preparation for Medical Procedure, Perioperative management therapy
Toxicity
Older patients metabolize delorazepam slower than younger patients and thus suffer from more adverse effects.
Volume of Distribution
140 L/kg apparent volume of distribution in 11 patients with normal renal function; 47 L/kg in 11 patients with renal failure and on regular hemodialysis.
In another study, apparent volume of distribution was 65 L/kg in 8 patients with liver disease and 118.4 L/kg in 12 healthy controls.
Elimination Route
77-87% oral bioavailability, with a relatively slow absorption rate. Reaches peak plasma levels within 1-2 hours of administration. Food may slow absorption, however other pharmacokinetic variables remain unchanged. After multiple doses delorazepam accumulates, although accumulation is slower in younger patients.
Half Life
Very long elimination half life of 80-115 hours, varying with age. Elimination is slower as age increases. [1] Liver disease also impacts elimination half life, with impairment resulting in half lives up to 395 hours.
Clearance
Still detectable 72 hours after dosing in healthy patients. Patients with liver disease experienced a reduction in clearance from 0.13 to 0.25 ng/mLh.
Elimination Route
Renally eliminated.
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