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Effects of long-term benzodiazepine use may include disinhibition, impaired concentration and memory, depression, [19] [20] as well as sexual dysfunction. [6] [21] The long-term effects of benzodiazepines may differ from the adverse effects seen after acute administration of benzodiazepines. [22]
Long-acting benzodiazepines with long-acting active metabolites, such as diazepam and chlordiazepoxide, are often prescribed for benzodiazepine or alcohol withdrawal as well as for anxiety if constant dose levels are required throughout the day. Shorter-acting benzodiazepines are often preferred for insomnia due to their lesser hangover effect.
Chlordiazepoxide is a long-acting benzodiazepine drug. The half-life of chlordiazepoxide is from 5 to 30 hours but has an active benzodiazepine metabolite, nordiazepam, which has a half-life of 36 to 200 hours. [31]
Benzodiazepines bind to the GABA A receptor inducing a conformational change leading to an increased affinity to GABA. The allosteric binding site is situated in a "pocket" created by the alpha and gamma subunits. The pharmacological effects on benzodiazepines vary based on which alpha subunit of the GABA A receptor the benzodiazepine binds to.
Urine (43–65% after 24 hours) Its high degree of lipophilicity (fat solubility) allows it to be detected in the urine for up to 18 months. [ 5 ] [ 57 ] Less than 1% of the unchanged drug is excreted via the kidneys in the urine, in which 20–70% is excreted as conjugated or unconjugated metabolites, whereas 5–6% is excreted in feces.
The benzodiazepines midazolam and temazepam were the two most common benzodiazepines utilized for date rape. [25] Benzodiazepines can be detected in urine through the use of drug tests administered by medical officials or sold at pharmacies and performed at home. Most tests will detect benzodiazepines for a maximum of 72 hours after it was taken.
A number of studies have drawn an association between long-term benzodiazepine use and neuro-degenerative disease, particularly Alzheimer's disease. [150] It has been determined that long-term use of benzodiazepines is associated with increased dementia risk, even after controlling for protopathic bias. [13]
Oxazepam has the potential for misuse, defined as taking the drug to achieve a high, or continuing to take the drug in the long term against medical advice. [39] Benzodiazepines, including diazepam, oxazepam, nitrazepam, and flunitrazepam, accounted for the largest volume of forged drug prescriptions in Sweden from 1982 to 1986.