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Drugs Affecting the Central Nervous System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: The use of Estazolam during the in 1st and 3rd Trimesters should be avoided because the pregnancy experience in humans, and the reproduction studies in animals, have shown an increased risk of congenital abnormalities, neonatal flaccidity and withdrawal symptoms.
Medication effects on sleep
Published in S.R. Pandi-Perumal, Meera Narasimhan, Milton Kramer, Sleep and Psychosomatic Medicine, 2017
Benzodiazepines are rapid eye movement (REM) sleep–suppressant medications, and withdrawal often results in episodes of increased REM sleep (REM rebound). REM sleep is known to play a role in learning and memory consolidation. For short-acting agents such as triazolam (Halcion), this rebound occurs during the same night in which the medication was taken, and has been associated with daytime memory impairment, particularly at higher dosages.14 Temazepam (Restoril) and estazolam (Prosom) have halflives that are compatible with an 8-hour night of sleep. Temazepam, because of its slower onset of action, is less efficacious as a sleep-inducing agent than other drugs used as hypnotics in this class. All benzodiazepines can result in respiratory depression in patients with pulmonary disease and tend to lose sleep-inducing efficacy with prolonged use.15 Chronic hypnotic (particularly benzodiazepine) use has been associated with the development of mood disorders (depression) and hypnotic-dependent disorders of sleep.16 Therefore, the underlying reasons and the diseases resulting in chronic insomnia should be addressed.
Hospice, Cancer Pain Management, and Symptom Control
Published in Mark V. Boswell, B. Eliot Cole, Weiner's Pain Management, 2005
Samira Kanaan Beckwith, Charles Wellman
Anxiety, depression, fear, sleeplessness, and restlessness may all lower a patient’s pain tolerance (Emanuel et al., 1999; Hanks, 1984). Benzodiazepines, although not thought of as analgesics, have a limited role in the management of cancer pain. Most hospice patients sleep fairly well; but as some of them near the end of their lives, they may have disturbing dreams and recurrent nightmares interfering with the restful quality of their sleep for which benzodiazepines may prove helpful. Additionally, when pain interferes with the normal sleep pattern such that little or no stage four delta-wave sleep occurs, the addition of a short-acting sedative hypnotic agent (estazolam, triazolam, or zolpidem) may be beneficial. It appears that without the deepest stage of sleep, muscles do not completely relax, and muscular pain may spontaneously develop, causing the patient widespread discomfort. By improving deep stage four sleep, this diffuse muscular ache that many patients with cancer experience, which is also a consequence of their debilitation and malnutrition, can be lessened. When patients are morbidly anxious about their condition, the addition of a benzodiazepine medication may significantly allay their anxiety. For this indication, the long half-life benzodiazepine medications are preferable to the short half-life medications, which are more likely to produce wide swings in blood levels and consequent rebound anxiety.
Lilium davidii extract alleviates p‑chlorophenylalanine‑induced insomnia in rats through modification of the hypothalamic-related neurotransmitters, melatonin and homeostasis of the hypothalamic-pituitary-adrenal axis
Published in Pharmaceutical Biology, 2020
Yanpo Si, Lili Wang, Jinxu Lan, Hanwei Li, Tao Guo, Xiaohui Chen, Chunhong Dong, Zhen Ouyang, Sui-qing Chen
As shown in Figure 3(A–C), compared with the Control group, PCPA administration significantly increased serum levels of CRH (11.24 ± 3.16 ng/mL), ACTH (565.87 ± 103.44 pg/mL) and CORT (44.28 ± 8.73 ng/mL) (p < 0.05 or 0.01). In addition, oral administration of LD extract over 7 days produced a significant (p < 0.05 or 0.01) decrease in CRH (LD-L, 8.76 ± 0.78 ng/mL; LD-M, 7.78 ± 1.78 ng/mL; LD-H, 7.45 ± 1.25 ng/mL) and CORT (LD-L, 33.3 ± 5.09 ng/mL; LD-M, 26.13 ± 2.99 ng/mL; LD-H, 30.50 ± 4.71 ng/mL) levels at all tested doses, and a significant decrease in the ACTH level at high (433.02 ± 105.89 pg/mL) and middle (369.37 ± 69.34 pg/mL) doses. These beneficial effects were comparable with that of 0.5 mg/kg Estazolam, which is a benzodiazepine drug that binds the benzodiazepine receptor and enhances GABA effects.
Traditional Chinese medicine: perspectives on and treatment of menopausal symptoms
Published in Climacteric, 2018
A systematic review19 consisting of six randomized, controlled studies with a total of 510 patients comparing the efficacy and safety of JiaWeiSuanZaoRen soup and sleeping pills in the treatment of menopausal insomnia showed that JiaWeiSuanZaoRen soup showed comparable effects to diazepam and alprazolam tablets, whereas JiaWeiSuanZaoRen soup treatment showed better efficacy than estazolam (p < 0.05). Additionally, JiaWeiSuanZaoRen soup improved the quality of sleep, as indicated by the Pittsburgh Sleep Quality Index, when compared with alprazolam (p < 0.05). More adverse events were reported in the group receiving sleeping pills than in the JiaWeiSuanZaoRen soup group (p < 0.05, χ2 = 4.9246). In addition, a randomized, double-blind, placebo-controlled, small-sample study20 found that the sleep quality index was improved significantly after menopausal women (n = 18) received acupuncture therapy, and polysomnography indicated that the duration of deep sleep increased after treatment.
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].