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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
The rate at which maximal plasma levels are obtained is also an important determinant of utility, especially for hypnotics. As a class, benzodiazepines are in general well and rapidly absorbed from the gastrointestinal tract. Their absolute bioavailability is generally high, although certain drugs, such as temazepam, undergo extensive first-pass metabolism in the liver. Inasmuch as the latter are transformed into bioactive metabolites, this does not significantly affect either the extent or rate of arrival of pharmacologically active material in the circulation. Since one of the goals of benzodiazepine treatment of insomnia is to induce sleep in patients who have difficulty falling asleep, it is important that hypnotic benzodiazepines enter the CNS rapidly after systemic absorption so that sleep induction occurs within an acceptable delay of around 30 minutes. Most recent hypnotics have a half-life (T1/2) of absorption of an hour or less (Table 7.2). Certain earlier hypnotics, such as nitrazepam or lormetazepam, do not fulfil this criterion, necessitating the use of high doses to obtain rapid sleep induction. The consequence of this is that the individual is exposed to ‘unnecessary’ drug which enters the brain after sleep induction has occurred. The elimination of this superfluous benzodiazepine will take time, and this material can contribute to benzodiazepine hangover the next day.
Marvin the Paranoid Android and Alice in Wonderland
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Pierluigi Simonato, Attilio Negri, Marco Solmi, Rita Santacroce
Alice’s case also underlined how a multiple intoxication scenario produces difficulties in the assessment and the treatment of these patients. At arrival, Alice was taking a SSRI, a mood stabilizer, three neuroleptics, and two benzodiazepines as prescribed by her psychiatrist. In addition to this, she developed severe dependence on lormetazepam, but she was still reporting anxiety, low mood, and a sense of ‘instability’; at the end of the recovery, the medical staff recommended a psychopharmacological medication with an SNRI (venlafaxine), a mood stabilizer (valproic acid), and an atypical antipsychotic drug (quetiapine), which is a well-known drug used for alcohol and stimulant dependence, in order to stabilize the most critical psychopathological areas.
Classifications
Published in Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani, Pharmacology in 7 Days for Medical Students, 2018
Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani
Sedative/hypnoticsFlurazepamNitrazepamTriazolamLormetazepam
What are the pharmacotherapeutic options for adjustment disorder?
Published in Expert Opinion on Pharmacotherapy, 2022
Initial medication trials focused on agents typically used to treat depression and anxiety disorders. The first trial in adjustment disorder examined the effects of multiple agents [8]. In a 4-week trial (n = 85), De Leo compared an antidepressant with noradrenergic and serotonergic effects (viloxazine) to a benzodiazepine with GABAergic effects (lormetazepam), a neutraceutical with serotonergic effects (S-adenosylmethionine), and placebo. Psychoanalytic psychotherapy was also included as a comparator arm. None of the interventions had significant effects compared to placebo. There were also a number of methodological flaws, including lack of clear diagnostic criteria for inclusion, lack of standardized outcome measures, lack of double-blind study design, and lack of adequate reporting of adverse events.
Designer benzodiazepines versus prescription benzodiazepines: can structural relation predict the next step?
Published in Critical Reviews in Toxicology, 2021
Raneem E. Moustafa, Fuad Tarbah, Huda Sulaiman Saeed, Suleiman I. Sharif
Each of those two drugs produces three unique classic benzodiazepines with relatively long half-lives that will be discussed in detail in the next section. Diclazepam, for example, gets metabolized to lorazepam, lormetazepam, and delorazepam (three well known classic benzodiazepines), having elimination half-lives that are relatively long-reaching 78 h for delorazepam, 12 h for lorazepam, and 13 h for lormetazepam. This imposes an issue that has been shown by a study on diclazepam organ distribution that its metabolites get redistributed in the same manner as their parent drug which may cause toxicity and overdose-like problems due to their accumulation in addition to the parent drug (diclazepam) which already has a long half-life. This leads to long-lasting sedative effects most likely when applying high or repeated doses (Lehmann et al. 2019).
Does high-dose benzodiazepine abuse really produce liver toxicity? Results from a series of 201 benzodiazepine monoabusers
Published in Expert Opinion on Drug Safety, 2018
Fabio Lugoboni, Antonio Mirijello, Laura Morbioli, Elena Arzenton, Roberto Leone, Marco Faccini, Rebecca Casari, Salvatore De Cosmo, Antonio Gasbarrini, Giovanni Addolorato
More than half of our HDU patients was lormetazepam addicted, indicating that lormetazepam represents the most addictive BZD among 26 available in Italy, as previously reported [7]. However, lormetazepam is prohibited in some Countries (i.e. USA) and this could limit the generalizability of our results.