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Structures of benzodiazepine recognition site ligands
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 imidazopyridines, zolpidem and alpidem (Figure 5.10), exhibit high affinity for the benzo-diazepine receptor. Zolpidem is a hypnotic drug with rapid onset and short duration of action; it also displays anticonvulsant, myorelaxant and anticonflict activities (Arbilla et al, 1985; Deporteere et al, 1986; Nicholson and Pascoe, 1986; Benavides et al, 1988), although at higher doses than those required for sedation.
Drugs Affecting the Central Nervous System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: The use of Zolpidem should be avoided in pregnant women because the pregnancy experience in humans has shown the risk of low birth weights, preterm birth, and cesarean birth associated with the use of this drug.
Sedative and Hypnotic Drugs
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Arup Kumar Misra, Pramod Kumar Sharma
Zolpidem belongs to imidazopyridine family. Zolpidem has an agonist effect on α1subunit of benzodiazepine receptor site on GABAA receptors and thus have similar pharmacological actions. Zolpidem after absorption undergoes significant hepatic metabolism providing only 70% bioavailability (Swainston and Keating, 2005). The peak plasma concentration of the drug is reached within 1–3 h. Hepatic CYP3A4 enzymes rapidly metabolized zolpidem to inactive metabolites by oxidation and hydroxylation. In normal individuals, half-life of the drug is 2 h but depending on the age, sex, and clinical conditions, there may be some variation in the elimination half-life (Swainston and Keating, 2005). The elimination half-life may be significantly high in women, cirrhotic patients, renal failure patients, and elderly, thus requiring adjustment of dosage. Different dosage forms are available for the patient with insomnia like the sublingual and oral spray dosage forms. Zolpidem reduces onset to fall asleep and overall maintains the total time of sleep in patients of insomnia (Swainston and Keating, 2005). Zolpidem may exhibit mild rebound insomnia on the first night after stopping the drug but the benefit may last for approximately 1 week. Zolpidem is given in the therapeutic range of 5–10 mg for the short-term treatment of insomnia. Zolpidem exhibits less tolerance and physical dependence. Sedation on next morning, anterograde amnesia, and delayed reaction time may be observed if zolpidem is administered late-night (Atkin et al., 2018).
Dieckol is a natural positive allosteric modulator of GABAA-benzodiazepine receptors and enhances inhibitory synaptic activity in cultured neurons
Published in Nutritional Neuroscience, 2021
Sangoh Kwon, Jong Hoon Jung, Suengmok Cho, Kwang-Deog Moon, Jaekwang Lee
To treat sleep disorders in clinics, zolpidem is a medication primarily used for the short term treatment of sleeping problems. It works by increasing GABA effects in the central nervous system by binding to GABAA receptors at the same location as benzodiazepines as positive allosteric modulator. Zolpidem has higher affinity with α1-subunit compared with the α2- and α3- subunits, and no appreciable affinity for α5 subunit-containing receptors [27,28]. And also diazepam (DZP) is known as a positive modulator of GABAA receptor with a high affinity with a benzodiazepine (BZD) site of GABAA receptor containing α1 subunit while other subunits has low affinity with a BZD site [29]. In current study, we tested dieckol and α1 subunit-containing GABAARs to see a relevant efficacy on BZD sites. However, phlorotannins contains several bioactive molecules such as Eckstolonol, Triphlorethol A, Eckol, Fucodiphlorethol G, including dieckol, which have a characteristic to bind with GABAA-BDZ receptors and what causes hypnotic effect of PS is still under investigation. For more accurate mechanism of sleep induction by PS supplements, more investigation is required because sleep effect of PSs could be mediated by single molecule or combination of molecules. Although we demonstrated the direct function of dieckol on GABAA-BZD receptors for the first time. However, its effect on sleep behavior is needed to be tested in the future study.
An analysis of the effects of using Zolpidem and an innovative multimodal interdisciplinary team approach in prolonged disorders of consciousness (PDOC)
Published in Brain Injury, 2019
Mark Delargy, Rebecca O’Connor, Alison McCann, Irene Galligan, Heather Cronin, Dee Gray, Caoimhe O’Toole
Zolpidem is a widely prescribed sedative, belonging to the group of drugs known as imidazopiridines. It is a highly selective non-benzodiazepine gamma-aminobutyric acid (GABA) agonist acting on the omega-1 site of the GABA-A receptor, and has a short half-life of 3 hours(13). Singh, McDonald, Dawson, Lewis, Pringle, Smith, Pentland (2008) (14) explained that following a brain injury, the brain attempts to reduce the amount of metabolism taking place in an effort to protect damaged neurons. This effect is mediated by GABA and may spread to other un-effected areas of the brain. Zolpidem may work to reverse this dormancy effect(14). Zolpidem was administered using the same dosage and methods as outlined by Whyte and Meyers (2009). (3) Zolpidem 10 mg was administered in liquid form via the feeding tube followed by a flush of water (90 mls). In contrast to the approach of Whyte and Meyers (2009), (3) who instructed the research observer to interact freely with the patients involved, the team in this current case report carried out eight structured interdisciplinary multi-sensory hierarchical protocols over an eight week period. Each weekly session took place within 30–60 min of Zolpidem administration (see Appendix 1)
Making sleep easier: pharmacological interventions for insomnia
Published in Expert Opinion on Pharmacotherapy, 2018
Lukas Frase, Christoph Nissen, Dieter Riemann, Kai Spiegelhalder
As sleep regulation and perception is changing drastically throughout the lifespan, differing recommendations could be hypothesized following a review of the available literature: For ID in children and adolescents, BZ, HBRA, and antihistamines are advised against, melatonin might be useful in children with sleep onset problems and sedating antidepressants and antipsychotics should be restricted to patients suffering from comorbid psychiatric diseases. During pregnancy, BZ and HBRA could be used in very severe cases of ID and zolpidem should be considered first, if treatment is needed. Limited data exists on trazodone or mirtazapine during pregnancy while antihistamines, antipsychotics, and melatonin should be avoided. In the elderly, BZ and HBRA are advised against without consideration of duration in patients aged 65 years or older. Melatonin and ramelteon might be more efficacious in older patients and suvorexant displays promising results. Antihistamines, antipsychotics and antidepressant medication should be used carefully due to anticholinergic side effects. The only antidepressant, which has been positively evaluated in patients older than 65 years, is doxepin in doses from 3 to 6 mg per day.