Can oral formulation increase the risk of lormetazepam abuse?

Costa, Enrico; Sterzi, Enrico; Tedeschi, Federico; Casari, Rebecca; Marini, Paola; Lugoboni, Fabio

doi:10.1007/s11739-020-02538-2

Cited by 5 publications

(5 citation statements)

References 9 publications

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“…However, the same studies reported a low incidence of abuse with lormetazepam tablets; for example, in the largest cohort, only 13 of the 1112 patients with benzodiazepine dependence (1.2%) were using lormetazepam tablets ( Faccini et al , 2019 ). Various authors have speculated on the reasons for the high rate of abuse with lormetazepam oral solution, suggesting that this is related to the drip rate, excipients, α 1 -receptor selectivity or a combination of these factors, but the exact reason is not clear ( Faccini et al , 2019 ; Horowski, 2020 ; Costa et al , 2021 ). Until there is more clarity about the exact cause of any relationship between lormetazepam oral solution and the risk of abuse, and the extent to which any relationship may be related to the formulation or patient characteristics, clinicians would be advised to preferentially prescribe the tablet formulation.…”

Section: Methodsmentioning

confidence: 99%

The role of benzodiazepines in common conditions: a narrative review focusing on lormetazepam

Pallanti

2024

International Clinical Psychopharmacology

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This review aimed to examine the place of benzodiazepines, specifically lormetazepam, in the treatment of insomnia, including during pregnancy or in patients with psychodermatoses. PubMed was searched for the term “lormetazepam” in association with MeSH terms encompassing anxiety, insomnia/sleep disorders, pregnancy/gestation, and psychodermatoses/skin disorders. English-language articles up to 31 July 2022 were identified. Ad hoc searches for relevant literature were performed at later stages of review development. Multiple randomized, placebo-controlled studies have demonstrated that lormetazepam dose-dependently increases total sleep time, decreases wakefulness over a dosing range of 0.5–2.0 mg, and improves subjective assessments of sleep quality. Lormetazepam is as effective as other benzodiazepines in improving sleep duration and quality, but is better tolerated than the long-acting agents with minimal next-day effects. Benzodiazepines can be used as short-term monotherapy at the lowest effective dose during the second or third trimesters of pregnancy; lormetazepam is also a reasonable choice due to its limited transplacental passage. Insomnia associated with skin disorders or pregnancy can be managed by effective symptom control (especially itching), sleep hygiene, treatment of anxiety/depression, and a short course of hypnotics.

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Section: Methodsmentioning

confidence: 99%

The role of benzodiazepines in common conditions: a narrative review focusing on lormetazepam

Pallanti

2024

International Clinical Psychopharmacology

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“…CNS side effects, such as excitement and violence, have also been described (Faccini et al, 2019). A very high dependence potential of lormetazepam with drop formulation has recently increased concerns regarding its use (Costa et al, 2021).…”

Section: Lormetazepammentioning

confidence: 99%

Pharmacotherapeutic management of insomnia and effects on sleep processes, neural plasticity, and brain systems modulating stress: A narrative review

Palagini

Bianchini

2022

Front. Neurosci.

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IntroductionInsomnia is a stress-related sleep disorder, may favor a state of allostatic overload impairing brain neuroplasticity, stress immune and endocrine pathways, and may contribute to mental and physical disorders. In this framework, assessing and targeting insomnia is of importance.AimSince maladaptive neuroplasticity and allostatic overload are hypothesized to be related to GABAergic alterations, compounds targeting GABA may play a key role. Accordingly, the aim of this review was to discuss the effect of GABAA receptor agonists, short-medium acting hypnotic benzodiazepines and the so called Z-drugs, at a molecular level.MethodLiterature searches were done according to PRISMA guidelines. Several combinations of terms were used such as “hypnotic benzodiazepines” or “brotizolam,” or “lormetazepam” or “temazepam” or “triazolam” or “zolpidem” or “zopiclone” or “zaleplon” or “eszopiclone” and “insomnia” and “effects on sleep” and “effect on brain plasticity” and “effect on stress system”. Given the complexity and heterogeneity of existing literature, we ended up with a narrative review.ResultsAmong short-medium acting compounds, triazolam has been the most studied and may regulate the stress system at central and peripheral levels. Among Z-drugs eszopiclone may regulate the stress system. Some compounds may produce more “physiological” sleep such as brotizolam, triazolam, and eszopiclone and probably may not impair sleep processes and related neural plasticity. In particular, triazolam, eszopiclone, and zaleplon studied in vivo in animal models did not alter neuroplasticity.ConclusionCurrent models of insomnia may lead us to revise the way in which we use hypnotic compounds in clinical practice. Specifically, compounds should target sleep processes, the stress system, and sustain neural plasticity. In this framework, among the short/medium acting hypnotic benzodiazepines, triazolam has been the most studied compound while among the Z-drugs eszopiclone has demonstrated interesting effects. Both offer potential new insight for treating insomnia.

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“…In our case history, 99% of the abusers that were hospitalized for addiction to lormetazepam were addicted to its soluble formula, unlike all other molecules for which tablets were prevalent 2 . This phenomenon is still unclear, but it's so evident in Italy that other countries should beware of introducing such a formula 4 . In Italy, lormetazepam has also shown to be the most abused intravenous drug for heroin addicts 5 .…”

Section: Istvan and Colleagues Hint At The Similarities Between The Regulation Policies Of Flunitrazepam To Drawmentioning

confidence: 99%

Zolpidem: a masked hero. A reply to ZORRO study

Lugoboni¹,

Casari²,

Fusina

et al. 2021

Preprint

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The use of zolpidem has been driven by the still-widespread false belief among doctors that, since zolpidem is chemically not a benzodiazepine, it cannot lead to addiction and tolerance. We would like to contribute to better highlight certain characteristics of zolpidem and its potential as a substance of abuse due to the fact that our operating unit, which is entirely dedicated to medication abuse, has described among the most numerous cases of addiction to high doses of benzodiazepines and related hypnotics. - Zolpidem was in fourth place among the 29 molecules present on the Italian market; - We believe it’s now time to drop the term “Z-drugs”: zolpidem, zopiclone e zaneplon all have different chemical structures, they bind to different receptors and have completely different abuse potentials3. In our case history, both zopiclon and zaneplon were virtually absent, albeit being commonly used in Italy; - Istvan & colleagues highlight the fact that addiciton and abuse are prevalent in samples suffering from mental illness. In our case history this hasn’t been confirmed: about half of our patients had no history of psychiatric illnesses, nor a history of addiction to illicit substances or alcohol; - Lastly, regarding zolpidem’s hazardousness, we would like to report the fact that the drug was significantly preferred by addicts with a positive ADHD test result. In conclusion, the 2000s saw solid confirmation of the effectiveness of partial agonists in the treatment of some common addictions, such as buprenorphine, varenicline, cytisine. This didn’t happen for BZs

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Can oral formulation increase the risk of lormetazepam abuse?

Cited by 5 publications

References 9 publications

The role of benzodiazepines in common conditions: a narrative review focusing on lormetazepam

The role of benzodiazepines in common conditions: a narrative review focusing on lormetazepam

Pharmacotherapeutic management of insomnia and effects on sleep processes, neural plasticity, and brain systems modulating stress: A narrative review

Zolpidem: a masked hero. A reply to ZORRO study

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