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The tables below contain a sample list of benzodiazepines and benzodiazepine analogs that are commonly prescribed, with their basic pharmacological characteristics, such as half-life and equivalent doses to other benzodiazepines, also listed, along with their trade names and primary uses.
Desmethyldiazepam has a half-life of 36–200 hours, and flurazepam, with the main active metabolite of desalkylflurazepam, with a half-life of 40–250 hours. These long-acting metabolites are partial agonists. [6] [152] Short-acting compounds have a median half-life of 1–12 hours.
An equianalgesic chart can be a useful tool, but the user must take care to correct for all relevant variables such as route of administration, cross tolerance, half-life and the bioavailability of a drug. [5] For example, the narcotic levorphanol is 4–8 times stronger than morphine, but also has a much longer half-life. Simply switching the ...
Flurazepam is a "classical" benzodiazepine; some other classical benzodiazepines include diazepam, clonazepam, oxazepam, lorazepam, nitrazepam, bromazepam, and clorazepate. [15] Flurazepam generates an active metabolite, N-desalkylflurazepam, with a very long elimination half-life. [3]
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] The half-life of chlordiazepoxide increases significantly in the elderly, which may result in prolonged action as well as accumulation of the drug during repeated administration.
Benzodiazepine like compounds are acting as positive allosteric modulators to the gamma-aminobutyric acid GABA A receptor. GABA is the main inhibitor of neurotransmitters in the brain and modulates the activity of many neurons. Benzodiazepines bind to the GABA A receptor inducing a conformational change leading to an increased affinity to GABA.
Diazepam, sold under the brand name Valium among others, is a medicine of the benzodiazepine family that acts as an anxiolytic. [15] It is used to treat a range of conditions, including anxiety, seizures, alcohol withdrawal syndrome, muscle spasms, insomnia, and restless legs syndrome. [15]
Nordazepam is a partial agonist at the GABA A receptor, which makes it less potent than other benzodiazepines, particularly in its amnesic and muscle-relaxing effects. [6] Its elimination half life is between 36 and 200 hours, with wide variation among individuals; factors such as age and sex are known to impact it. [2]