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Diazepam is highly plasma protein-bound, with 96–99% of the absorbed drug being protein-bound. The distribution half-life of diazepam is two to 13 minutes. [19] Diazepam is highly lipid-soluble and is widely distributed throughout the body after administration.
Drug Name Common Trade Names [a] Year Approved Typical Oral Dosage Formulations (mg) Approx. Equivalent Oral Dose to 10 mg Diazepam [b] (mg) Peak Onset of Action (hours) Elimination Half-life of Active Metabolite (hours) Primary Therapeutic Use Adinazolam: Deracyn: Research chemical: 1–2: 3: anxiolytic, antidepressant: Alprazolam
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.
In clinical practice, this means that it takes 4 to 5 times the half-life for a drug's serum concentration to reach steady state after regular dosing is started, stopped, or the dose changed. So, for example, digoxin has a half-life (or t 1 / 2 ) of 24–36 h; this means that a change in the dose will take the best part of a week to ...
Disposal of expired stock must be witnessed by a designated inspector (either a local drug-enforcement police officer or official from health authority). [218] [219] Benzodiazepine use ranges from occasional binges on large doses, to chronic and compulsive drug use of high doses. [220] Benzodiazepines are commonly used recreationally by poly ...
Clorazepate is a long-acting benzodiazepine drug. [10] Clorazepate produces the active metabolite desmethyl-diazepam, which is a partial agonist of the GABA A receptor and has a half life of 20–179 hours; a small amount of desmethyldiazepam is further metabolised into oxazepam.
Denzel Washington revealed to Esquire magazine as part of a recent cover story that he is 10 years sober. He cut off alcohol at 60 years old after a 15-year drinking pattern that started in the ...
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 ...