Search Results (8)

Adolescence is a critical developmental stage for the initiation of substance use worldwide, which is one of the main risk-taking behaviors that may impact adolescents’ physical and mental well-being. The aims of this study were to (1) assess the prevalence of the co-use of tranquilizers, sedatives, and sleeping pills with alcohol (TSSp&AC) by gender in the Spanish adolescent population in 2018 and (2) identify the variables associated with TSSp&AC. An observational cross-sectional study following STROBE guidelines was conducted. We analyzed data from 38,010 adolescents aged 14 to 18 years old (18,579 males and 19,431 females) who participated in ESTUDES (Survey on Drug Use in Secondary Education in Spain) 2018. Female adolescents reported a higher prevalence of TSSp&AC than males (p < 0.001). The factors associated with female co-use were being 16–18 years of age (OR 1.65); the consumption of tobacco (OR 1.73), cocaine (OR 1.84), other illicit psychoactive drugs (OR 1.89); and novel illicit psychoactive drugs (OR 1.74); no perceived health risk from the consumption of TSSps (OR 2.45); and the perceived availability of TSSps (OR 2.23) and alcohol (OR 2.09). There are several factors associated with TSSp&AC in Spanish female adolescents with potential implications for healthcare providers. Full article

2-Benzoxazolone, as well as its derivatives, are valuable structural fragments of a number of important biologically active substances. 2-Benzoxazolone derivatives are promising as antitumor, antimicrobial, antiretroviral, anticonvulsant, tranquilizing, and insecticidal agents. 2-Benzoxazolone is usually produced by the condensation of o-aminophenol with urea, phosgene, and other carbonic acid derivatives. There are also methods for the synthesis of 2-benzoxazolone from salicylamide with trichloroisocyanuric acid as a chlorinating agent, from hydroxybenzoic acid using ammonium azide and the Vilsmeier complex. The disadvantages of these methods are the high cost of the initial reagents, the need to use aggressive and toxic reagents (phosgene, ammonium azide), and the complexity of the hardware design for the reactors. We have developed the highly efficient oxidative cyclocarbonylation of 2-aminophenol to oxazolidin-2-one using FeCl₃*6H₂O and Fe(acac)₃ as catalysts under relatively mild conditions (100–120 °C) in the presence of CCl₄ and water. We assume that in situ-formed carbon dioxide is involved in a cyclization reaction with o-aminophenol to form the target 2-benzoxazole. The reaction takes 2–10 h to give 2-benzoxazolone a high yield. Full article

Thrombocytopenia is one of the most common complications of cancer therapy. Until now, there are still no satisfactory medications to treat chemotherapy and radiation-induced thrombocytopenia (CIT and RIT, respectively). Caulis Polygoni Multiflori (CPM), one of the most commonly used Chinese herbs, has been well documented to nourish blood for tranquilizing the mind and treating anemia, suggesting its beneficial effect on hematopoiesis. However, it is unknown whether CPM can accelerate megakaryopoiesis and thrombopoiesis. Here, we employ a UHPLC Q–Exactive HF-X mass spectrometer (UHPLC QE HF-X MS) to identify 11 ingredients in CPM. Then, in vitro experiments showed that CPM significantly increased megakaryocyte (MK) differentiation and maturation but did not affect apoptosis and lactate dehydrogenase (LDH) release of K562 and Meg-01 cells. More importantly, animal experiments verified that CPM treatment markedly accelerated platelet recovery, megakaryopoiesis and thrombopoiesis in RIT mice without hepatic and renal toxicities in vivo. Finally, RNA-sequencing (RNA-seq) and western blot were used to determine that CPM increased the expression of proteins related to PI3K/Akt and MEK/ERK (MAPK) signaling pathways. On the contrary, blocking PI3K/Akt and MEK/ERK signaling pathways with their specific inhibitors suppressed MK differentiation induced by CPM. In conclusion, for the first time, our study demonstrates that CPM may be a promised thrombopoietic agent and provide an experimental basis for expanding clinical use. Full article

As tranquilizers, benzodiazepines have a wide range of clinical uses. Recently, there has been a significant rise in the number of novel psychoactive substances, including designer benzodiazepines. Flubromazolam(8-bromo-6-(2-fluorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazeZpine) is a triazolo-analogue of flubromazepam. The most common effects noted by recreational users include heavy hypnosis and sedation, long-lasting amnesia, and rapid development of tolerance. Other effects included anxiolysis, muscle-relaxing effects, euphoria, loss of control, and severe withdrawals. Clonazolam, or 6-(2-chlorophenyl)-1-methyl-8-nitro-4H-[1,2,4]triazolo[4,3-α]-[1,4]-benzodiazepine, is a triazolo-analog of clonazepam. It is reported to be over twice as potent as alprazolam. Deschloroetizolam (2-Ethyl-9-methyl-4-phenyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine) is part of the thienodiazepine drug class, which, like benzodiazepines, stimulates GABA-A receptors. Meclonazepam ((3S)-5-(2-chlorophenyl)-3-methyl-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one) is a designer benzodiazepine with additional anti-parasitic effects. Although it has proven to be an efficacious therapy for schistosomiasis, its sedative side effects have prevented it from being marketed as a therapeutic agent. The use of DBZs has been a subject of multiple recent clinical studies, likely related to increasing presence and availability on the internet drug market and lack of regulation. Many studies have aimed to identify the prevalence of DBZs and their effects on those using them. This review discussed these designer benzodiazepines and the dangers and adverse effects that the clinician should know. Full article

(1) Background: the variety of autism spectrum disorder makes the definition of guidelines for dental care a challenging task. The aim of this review was to evaluate the literature concerning the use of conscious sedation for dental treatments in pediatric autistic patients. (2) Methods: we searched MEDLINE/PubMed, EMBASE, Cochrane databases in order to identify pertinent studies. The search strategy was based on these areas of interest: autistic spectrum disorder, pediatric patients, dentistry, tranquilizing agents, and conscious sedation. (3) Results: the search yielded 177 non-duplicated articles, of which 24 articles were retrieved for full text review, and 2 were found to address our review aim. The first paper was a retrospective study that included 83 autistic patients sedated either with an oral premedication combined with nitrous oxide/oxygen inhalation or with nitrous oxide/oxygen inhalation alone; the second article was a prospective trial on the effectiveness of 0.3 mg/kg of oral diazepam with 0.5 mg/kg of oral midazolam in 13 sedated uncooperative autistic patients. (4) Conclusions: this review highlights the insufficiency of studies that can provide concrete indications for the dental treatment in conscious sedation of pediatric patients with autism. New studies are needed to better define the appropriate drugs, dosages, sedation level and evaluate patient cooperation. Full article

Background: Neurotic disturbances, anxiety, neurosis-like disorders, and stress situations are widespread. Benzodiazepine tranquillizers have been found to be among the most effective antianxiety drugs. The pharmacological action of benzodiazepines is due to their interaction with the supra-molecular membrane GABA-a-benzodiazepine receptor complex, linked to the Cl-ionophore. Benzodiazepines enhance GABA-ergic transmission and this has led to a study of the role of GABA in anxiety. The search for anxiolytics and anticonvulsive agents has involved glutamate-ergic, 5HT-ergic substances and neuropeptides. However, each of these well-known anxiolytics, anticonvulsants and cognition enhancers (nootropics) has repeatedly been reported to have many adverse side effects, therefore there is an urgent need to search for new drugs able to restore damaged cognitive functions without causing significant adverse reactions. Objective: Considering the relevance of epilepsy diffusion in the world, we have addressed our attention to the discovery of new drugs in this field Thus our aim is the synthesis and study of new compounds with antiepileptic (anticonvulsant) and not only, activity. Methods: For the synthesis of compounds classical organic methods were used and developed. For the evaluation of biological activity some anticonvulsant and psychotropic methods were used. Results: As a result of multistep reactions 26 new, five-membered heterocyclic systems were obtained. PASS prediction of anticonvulsant activity was performed for the whole set of the designed molecules and probability to be active Pa values were ranging from 0.275 to 0.43. The studied compounds exhibit protection against pentylenetetrazole (PTZ) seizures, anti-thiosemicarbazides effect as well as some psychotropic effect. The biological assays evidenced that some of the studied compounds showed a high anticonvulsant activity by antagonism with pentylenetetrazole. The toxicity of compounds is low and they do not induce muscle relaxation in the studied doses. According to the study of psychotropic activity it was found that the selected compounds have an activating behavior and anxiolytic effects on the models of “open field” and “elevated plus maze” (EPM). The data obtained indicate the anxiolytic (anti-anxiety) activity of the derivatives of pyrimidines, especially pronounced in compounds 6n, 6b, and 7c. The studied compounds increase the latent time of first immobilization on the model of “forced swimming” (FST) and exhibit some antidepressant effect similarly to diazepam. Docking studies revealed that compound 6k bound tightly in the active site of GABA_A receptor with a value of the scoring function that estimates free energy of binding (ΔG) at −7.95 kcal/mol, while compound 6n showed the best docking score and seems to be dual inhibitor of SERT transporter as well as 5-HT_1A receptor. Conclusions: Тhe selected compounds have an anticonvulsant, activating behavior and anxiolytic effects, at the same time exhibit some antidepressant effect. Full article

The aims of this study were: (a) to estimate time trends in the prevalence of the co-use of cannabis and other cannabis-based products (CBP) with the misuse of tranquilizers, sedatives, and sleeping pills (TSSp) between 2009 and 2015; and (b) to identify the factors associated with the probability of the co-use of CBP with TSSp misuse during this period among Spanish younger adults (15–34 years old). We analyzed data collected from the Spanish National Surveys on Alcohol and Other Drugs (EDADES) in 2009, 2011, 2013, and 2015. CBP co-use with TSSp misuse were the dependent variables. We also analyzed sociodemographic features, self-perceived health status, lifestyle habits, perceived health risk of consumption, and perceived availability of substance using logistic regression models. The prevalence of CBP co-use with TSSp misuse has decreased in Spain. The factors associated with co-use were a lack of education (OR 2.34), alcohol (OR 7.2), tobacco (OR 6.3) and other illicit psychoactive drug (OR 6.5) consumption, perceived non-health risk for the consumption of CBP and TSSp (OR 3.27), and perceived availability of CBP (OR 2.96). Our study identified several factors that appear to affect CBP and TSSp co-use in younger adults, with potential implications for healthcare providers. Full article

Many vegetable extracts, essential oils, and their main constituents are active on the Central Nervous System (CNS). In fact, they have been used as sedatives, hypnotics, or tranquilizers for their activity in treating CNS disorders. In this research, we studied the possible activities of Lavandula angustifolia (LA) essential oil and of its main constituent, linalool, as anti-stress compounds on anxiety and social interaction and their in vitro effects on proteins (pERK and PKA) involved in the transmission of the signal. An acute intraperitoneal injection of linalool (100 mg/kg) and of LA essential oil (200 mg/kg) reduced motor activity without any anxiolytic effect, but significantly increased social interaction. Stressed mice, after being exposed to a social defeat encounter, showed heightened anxiety and social avoidance. Acute administration of LA essential oil blocked stress-induced anxiety, while linalool showed no effects. However, both compounds were capable of reversing social aversion, acting as antidepressant agents. Our results showed that linalool inhibits pERK and PKA expression in the SH-SY5Y cell, but no effect was detected with the LA essential oil. Therefore, the LA essential oil and linalool may be considered as useful alternative tools to the available traditional treatments for social stress-induced mental illnesses. Full article