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Pharmacokinetic determinants of clinical activity
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
Desalkylflurazepam is an example of an active metabolite that is eliminated from the body very slowly. As described above, this metabolite is produced in high quantities after administration of both flurazepam and quazepam and is probably responsible for a considerable part of the biological activity of these two hypnotic benzodiazepines. This metabolite persists in the body well after the parent benzodiazepines have been eliminated, due to its higher plasma elimination half-life (Table 7.3; Kaplan et al, 1973; Greenblatt et al, 1981b; Zampaglione et al, 1985). Accumulation of desalkylflurazepam has been detected after chronic dosing of both these hypnotics (Kaplan et al, 1973; Chung et al, 1984). Another example of an accumulating metabolite is desmethyldiazepam (see above).
Medications That May Be Useful in the Management of Patients with Chronic Intractable Pain
Published in Michael S. Margoles, Richard Weiner, Chronic PAIN, 2019
Benzodiazepines generally decrease sleep latency and decrease the number of awakenings and the time spent in stage 0 (awake stage). Flurazepam, quazepam, and temazepam decrease stage 1 (descending drowsiness). Stage 2 (unequivocal sleep) is increased by all benzodiazepines, and most benzodiazepines shorten stages 3 and 4 (slow wave sleep). Temazepam has prolonged stage 3 and shortened stage 4 in neurotic patients or patients with depression. All but flurazepam prolong REM latency. REM sleep is usually shortened, but with temazepam or low-dose flurazepam, this may not be the case. The result of benzodiazepine administration is an increase in total sleep time (Facts and Comparisons, 1996).
Drug profiles: generic names A-Z
Published in Jerome Z. Litt, Neil H. Shear, Litt's Drug Eruption & Reaction Manual, 2017
Clinically important, potentially hazardous interactions with: benzodiazepines, chlordiazepoxide, cilostazol, clonazepam, clopidogrel, clorazepate, diazepam, digoxin, flurazepam, lorazepam, midazolam, oxazepam, posaconazole, quazepam, rifampin, rilpivirine, St John’s wort, temazepam, tipranavir, voriconazole
Do Placebos Primarily Affect Subjective as Opposed to Objective Measures? A Meta-Analysis of Placebo Responses in Insomnia RCTs
Published in Behavioral Sleep Medicine, 2023
Alexandria Muench, Joshua Giller, Knashawn H. Morales, Elizabeth Culnan, Waliuddin Khader, Ted J. Kaptchuk, William V. McCall, Michael L. Perlis
The keywords utilized included insomnia, treatment, randomized controlled trial (RCT), clinical trial, medication class, and medication name (i.e., BZRAs: flurazepam, quazepam, estazolam, temazepam, triazolam, clonazepam, lorazepam, alprazolam, diazepam, chlordiazepoxide, zolpidem, zaleplon, and eszopiclone; DORAs: suvorexant, almorexant, and lemborexant; MELAs: ramelteon; SADs: amitriptyline, doxepin, trazodone, and mirtazapine). The queries elicited 329 articles, where 17 met inclusion criteria. Please note that the reason multiple queries were conducted was because many of the drug classes include a variety of medications and it was our preference to identify RCTs by each specific medication. For example, “Clinical Trial” + “Insomnia” + “Flurazepam” vs. “Clinical Trial” + “Insomnia” + “Temazepam,” etc.
Evaluating lemborexant for the treatment of insomnia
Published in Expert Opinion on Pharmacotherapy, 2021
Benzodiazepines act by binding to a site on the GABA-A receptor and increasing the effect of the neurotransmitter GABA when it binds to this receptor [21]. This decreases neural activity and can have broad effects on central nervous system function including myorelaxation, anxiolysis, anticonvulsant effects, and sedation. Although many benzodiazepines are available and have shown efficacy in clinical trials, particularly for improving sleep duration [4,21], they are generally only indicated for short-term treatment [22,23] because of a paucity of data on long-term treatment. However, they are relatively contraindicated with opioids [22,23] and data are lacking on the risk–benefit ratio of longer term use. Additionally, there is a risk of dependence and withdrawal symptoms associated with these medications, particularly with higher doses, longer duration, older age, alcohol dependence, and use of the high-potency, short-acting options [24]. Adverse events associated with benzodiazepines can include daytime sedation, cognitive impairment, and motor impairment [25]. Although many benzodiazepines have been approved by the United States Food and Drug Administration (FDA) for treatment of insomnia (the short-acting temazepam, triazolam, and estazolam, and the longer-acting flurazepam and quazepam), the AASM clinical practice guidelines recommend only temazepam for treatment of both sleep onset and sleep maintenance insomnia, and triazolam for sleep onset insomnia [19] because they are short-acting and therefore have a lower likelihood of next day residual effects [26]. In the current United States market, the benzodiazepines are not among the agents most commonly prescribed for insomnia [27].
Incremental health care resource use and costs among adult patients with depression and treated for insomnia with zolpidem, trazodone, or benzodiazepines
Published in Current Medical Research and Opinion, 2022
Emerson M. Wickwire, Diana T. Amari, Timothy R. Juday, Feride Frech, Deval Gor, Manoj Malhotra
D + TI patients were required to have at least 1 prescription fill for a medication of interest with an FDA-approved indication for insomnia treatment or trazodone ≤100 mg or at least 1 off-label insomnia treatment claim coupled with at least 1 physician-assigned ICD-9/ICD-10 insomnia diagnosis code within 12 months prior to first insomnia medication claim. Medications of interest included zolpidem immediate-release (IR), zolpidem extended-release (ER), trazodone, and benzodiazepines (as a class). Some benzodiazepines have an FDA-approved indication for insomnia (estazolam, flurazepam, temazepam, triazolam, quazepam) while others do not (clonazepam, lorazepam, alprazolam); patients prescribed benzodiazepines without an insomnia indication were required to also have an insomnia diagnosis code. Trazodone ≤100 mg daily was the threshold identified for use in insomnia management (≥150 mg/day is the recommended dosage for treatment of depression). Patients were excluded for the following: 1. the presence of a prescription drug claim for a fill of any insomnia medication of interest within the 12-month period before the index date; 2. claims for a single insomnia treatment with ≤5 days’ supply; and 3. an index prescription for benzodiazepines and an anxiety diagnosis during the 12-month baseline period. Patients on polypharmacy with at least two of the study medications of interest used concurrently during the study period were not excluded from the sample, as they represented <4% of the total population (data not shown). Patients with claims for two or more insomnia medications of interest on the index date were assigned to a treatment group based on the following hierarchy: zolpidem ER, zolpidem IR, trazodone, benzodiazepines.