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Benzodiazepine drugs in sleep disorders
Published in Adam Doble, Ian L Martin, David Nutt, Calming the Brain: Benzodiazepines and related drugs from laboratory to clinic, 2020
Adam Doble, Ian L Martin, David Nutt
The first of the shorter half-life benzodiazepine hypnotics to be introduced were temazepam and triazolam, rapidly followed by others such as loprazolam, lormetazepam and brotizolam (Table 8.3). Although they all have half-lives that are sufficiently short to prevent accumulation on repeated dosing, those with half-lives (T1/2) of more than 5 hours can cause some hangover the next day. This drawback has to be considered against the possibility that very short half-life drugs, such as triazolam, are so rapidly cleared from the brain that there is a greater risk of rebound insomnia. Rebound insomnia is a state of worsened sleep which commonly follows discontinuation of a longish period of repeated or regular hypnotic use (see below and Figure 8.3).
Saturation Analysis: Radioimmunoassay and Other Ligand Assays
Published in Joseph Chamberlain, The Analysis of Drugs in Biological Fluids, 2018
Hunt developed the radioreceptor for benzodiazepines to provide a useful general method for active benzodiazepines and used it to evaluate the pharmacokinetics of diazepam, nitrazepam, clobazam, and loprazolam in humans. For loprazolam, the results were compared with a specific chromatographic method of similar sensitivity, both to obtain a single dose profile (Figure 8.7) and a multiple dose profile (Figure 8.8). During the absorption phase, both techniques give closely similar serum concentrations with a peak of 8 to 9 ng ml−1 between 2 and 3 h after a 2-mg oral dose. At later times, after about 5 h, as presumably active metabolites appear, the radioreceptor method gives higher concentrations than the chromatographic method. This difference is maintained on multiple dosing over 8 days. The results indicate that the presence of metabolites active in the receptor assay can make an important contribution to the overall pharmacokinetic profile. Jochemsen et al.1251 carried out a similar comparison of the radioreceptor assay for nitrazepam and triazolam with a gas chromatographic method and reported good correlation.
Hypnotics
Published in Ann Richards, Nursing & Health Survival Guide, 2014
Drugs to aid sleeping.Only used for short periods when absolutely necessary.May be habit forming.Benzodiazepines (BZs), e.g. nitrazepam, flurazepam, temazepam, loprazolam.Newer drugs that are not BZs but do act as BZ receptor include zaleplon, zolpidem and zopiclone. Have a short duration of action but dependence has been reported.
Adaptation of a deprescription intervention to the medication management of older people living in long-term care facilities
Published in Expert Opinion on Drug Safety, 2019
Gregorio Sanz-Tamargo, Sergio García-Cases, Andrés Navarro, Blanca Lumbreras
The intervention was considered satisfactory if it resulted in one of the following three outcomes: a) complete withdrawal of the drug, b) dose reduction or interval extension, or c) exchange for another drug with a better safety profile, for example, the collective data for the benzodiazepine group, where we recommended a change to lorazepam when other alternatives were not possible [23]. Benzodiazepines are metabolized at the liver level and most use the cytochrome P450 system through oxidation, which becomes less efficient with age and tends to leave active metabolites. In elderly patients it is preferable to avoid this metabolic route and choose benzodiazepines that are metabolized by conjugation (lormetazepam, lorazepam, loprazolam and oxazepam), which does not suffer significant alterations with age.