Delorazepam
Encyclopedia
Delorazepam also known as chlordesmethyldiazepam is a drug which is a benzodiazepine
and a derivative of desmethyldiazepam. It is marketed in Italy, where it is available under the trade name EN and Dadumir. Delorazepam (chlordesmethyldiazepam) is also an active metabolite
of the benzodiazepine drug cloxazolam
. Adverse effects may include hangover
type effects, drowsiness, behavioural impairments and short-term memory impairments. Similar to other benzodiazepines delorazepam has anxiolytic
, skeletal muscle relaxant, hypnotic
and anticonvulsant
properties.
because of its long elimination half-life; showing superiority over the short-acting drug lorazepam
. In comparison with the antidepressant
drugs, paroxetine
and imipramine
, delorazepam was found to be more effective in the short-term but after 4 weeks the antidepressants showed superior anti-anxiety effects.
Delorazepam is also used as a premedication
for dental phobia for its anxiolytic properties.
Delorazepam has also demonstrated effectiveness in treating alcohol withdrawal.
of delorazepam is lorazepam
and represents about 15 - 24 percent of the parent drug (delorazepam). The pharmacokinetics
of delorazepam are not altered if it is taken with food, except for some slowing of absorption. The potency of delorazepam is 1 mg delorazepam equals 10 mg diazepam.
on haemodialysis have a slow elimination rate and a reduced volume of distribution of the drug. Liver disease has a profound effect on the elimination rate of delorazepam, resulting in the half-life almost doubling to 395 hours, where as healthy patients showed an elimination half-life of 204 hours on average. Caution is recommended when using delorazepam in in patients with liver disease.
Benzodiazepine
A benzodiazepine is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring...
and a derivative of desmethyldiazepam. It is marketed in Italy, where it is available under the trade name EN and Dadumir. Delorazepam (chlordesmethyldiazepam) is also an active metabolite
Active metabolite
- Prodrugs :Sometimes drugs are formulated deliberately so they will break down inside the body to form the active drug, these are called prodrugs. The reason for this may be because the drug is more stable during manufacture and storage as the prodrug form, or because the prodrug is better...
of the benzodiazepine drug cloxazolam
Cloxazolam
Cloxazolam Cloxazolam Cloxazolam (marketed under brand name Sepazon, Olcadil (Brazil, Portugal and Spain), Akton (Belgium), Lubalix (Switzerland) is a drug which is a benzodiazepine derivative. Cloxazolam is metabolised into the active metabolite chlordesmethyldiazepam (delorazepam)...
. Adverse effects may include hangover
Hangover
A hangover describes the sum of unpleasant physiological effects following heavy consumption of alcoholic beverages. The most commonly reported characteristics of a hangover include headache, nausea, sensitivity to light and noise, lethargy, dysphoria, diarrhea and thirst, typically after the...
type effects, drowsiness, behavioural impairments and short-term memory impairments. Similar to other benzodiazepines delorazepam has anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
, skeletal muscle relaxant, hypnotic
Hypnotic
Hypnotic drugs are a class of psychoactives whose primary function is to induce sleep and to be used in the treatment of insomnia and in surgical anesthesia...
and anticonvulsant
Anticonvulsant
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers, and in the treatment of neuropathic pain. The goal of an...
properties.
Indications
Delorazepam is mainly used as an anxiolyticAnxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
because of its long elimination half-life; showing superiority over the short-acting drug lorazepam
Lorazepam
Lorazepam is a high-potency short-to-intermediate-acting 3-hydroxy benzodiazepine drug that has all five intrinsic benzodiazepine effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant, antiemetic and muscle relaxant...
. In comparison with the antidepressant
Antidepressant
An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...
drugs, paroxetine
Paroxetine
Paroxetine is an SSRI antidepressant. Marketing of the drug began in 1992 by the pharmaceutical company SmithKline Beecham, now GlaxoSmithKline...
and imipramine
Imipramine
Imipramine , also known as melipramine, is an antidepressant medication, a tricyclic antidepressant of the dibenzazepine group...
, delorazepam was found to be more effective in the short-term but after 4 weeks the antidepressants showed superior anti-anxiety effects.
Delorazepam is also used as a premedication
Premedication
Premedication refer to a drug treatment given to a patient before a medical procedure. These drugs are typically sedative or analgesic....
for dental phobia for its anxiolytic properties.
Delorazepam has also demonstrated effectiveness in treating alcohol withdrawal.
Availability
Delorazepam is available in tablet and liquid drop formulations. The liquid drop formulation is absorbed more quickly and has improved bioavailibility.Pharmacology
Delorazepam is well absorbed after administration, reaching peak plasma levels within 1 – 2 hours. It has a very long elimination half-life and can still be detected 72 hours after dosing. Bioavailability is about 77 percent. Peak plasma levels occur at just over one hour after administration. Significant accumulation occurs of delorazepam due to its slow metabolism; the elderly metabolise delorazepam and its active metabolite slower than younger individuals. The elderly also have a poorer response to the therapeutic effects and a higher rate of adverse effects. The elimination half-life of delorazepam is 80–115 hours. The active metaboliteActive metabolite
- Prodrugs :Sometimes drugs are formulated deliberately so they will break down inside the body to form the active drug, these are called prodrugs. The reason for this may be because the drug is more stable during manufacture and storage as the prodrug form, or because the prodrug is better...
of delorazepam is lorazepam
Lorazepam
Lorazepam is a high-potency short-to-intermediate-acting 3-hydroxy benzodiazepine drug that has all five intrinsic benzodiazepine effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant, antiemetic and muscle relaxant...
and represents about 15 - 24 percent of the parent drug (delorazepam). The pharmacokinetics
Pharmacokinetics
Pharmacokinetics, sometimes abbreviated as PK, is a branch of pharmacology dedicated to the determination of the fate of substances administered externally to a living organism...
of delorazepam are not altered if it is taken with food, except for some slowing of absorption. The potency of delorazepam is 1 mg delorazepam equals 10 mg diazepam.
Special cautions
People with renal failureRenal failure
Renal failure or kidney failure describes a medical condition in which the kidneys fail to adequately filter toxins and waste products from the blood...
on haemodialysis have a slow elimination rate and a reduced volume of distribution of the drug. Liver disease has a profound effect on the elimination rate of delorazepam, resulting in the half-life almost doubling to 395 hours, where as healthy patients showed an elimination half-life of 204 hours on average. Caution is recommended when using delorazepam in in patients with liver disease.