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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.
Many of the pharmacologically active "classical" benzodiazepine drugs contain the 5-phenyl-1H-benzo[e] [1,4]diazepin-2(3H)-one substructure (see figure to the right). [192] Benzodiazepines have been found to mimic protein reverse turns structurally, which enable them with their biological activity in many cases.
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 ...
This is likely the result of the medication's long half-life, which continues to affect the user after waking up. [58] [59] [60] While benzodiazepines induce sleep, they tend to reduce the quality of sleep by suppressing or disrupting REM sleep. [61] After regular use, rebound insomnia may occur when discontinuing clonazepam. [62]
[6] [33] Diazepam is the most commonly used benzodiazepine for "tapering" benzodiazepine dependence due to the drug's comparatively long half-life, allowing for more efficient dose reduction. Benzodiazepines have a relatively low toxicity in overdose. [20] Diazepam has several uses, including:
Benzodiazepines require special precautions if used in the elderly, during pregnancy, in children, in alcoholics, or in other drug-dependent individuals and individuals with comorbid psychiatric disorders. [18] Triazolam belongs to the Pregnancy Category X of the FDA. [19] [1] It is known to have the potential to cause birth defects.
Midazolam is a short-acting benzodiazepine in adults with an elimination half-life of 1.5–2.5 hours. [13] In the elderly, as well as young children and adolescents, the elimination half-life is longer. [44] [66] Midazolam is metabolised into an active metabolite alpha-hydroxymidazolam.
Nordazepam is among the longest lasting (longest half-life) benzodiazepines, and its occurrence as a metabolite is responsible for most cumulative side-effects of its myriad of pro-drugs when they are used repeatedly at moderate-high doses; the nordazepam metabolite oxazepam is also active (and is a more potent, full BZD-site agonist), which ...