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The elimination half-life is how long it takes for half of the drug to be eliminated by the body. "Time to peak" refers to when maximum levels of the drug in the blood occur after a given dose. "Time to peak" refers to when maximum levels of the drug in the blood occur after a given dose.
A benzodiazepine can be placed into one of three groups by its elimination half-life, or time it takes for the body to eliminate half of the dose. [195] Some benzodiazepines have long-acting active metabolites, such as diazepam and chlordiazepoxide, which are metabolised into desmethyldiazepam. Desmethyldiazepam has a half-life of 36–200 ...
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
This explains why one lorazepam dose, despite its shorter serum half-life, has more prolonged peak effects than an equivalent diazepam dose. [99] Lorazepam is rapidly conjugated at its 3-hydroxy group into lorazepam glucuronide which is then excreted in the urine. Lorazepam glucuronide has no demonstrable CNS activity in animals.
Benzodiazepines with a half-life of less than 24 hours include alprazolam, bromazepam, brotizolam, flunitrazepam, loprazolam, lorazepam, lormetazepam, midazolam, nitrazepam, oxazepam, and temazepam. [111] The resultant equivalent dose is then gradually reduced.
A short elimination half-life and a rapid onset of action are characteristics which increase the abuse potential of a benzodiazepines. [18] The following table provides the elimination half-life, approximate equivalent doses, speed of onset of action, and duration of behavioural effects. [32] [33]
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 ...
In Italy, the gold standard for treatment of high-dose benzodiazepine dependency is 8–10 days of low-dose, slowly infused flumazenil. [26] One addiction treatment centre in Italy has used flumazenil to treat over 300 patients who were dependent on high doses of benzodiazepines (up to 70 times higher than conventionally prescribed) with ...