Search results for "Sedative"
showing 10 items of 62 documents
Search for New Antihistaminic Compounds by Molecular Connectivity
1999
In this paper it is demonstrated that by adequate selection of topological descriptors we can make possible the prediction of different pharmacological properties, such as plasmatic concentration or sedative effect, within a group of antihistaminic drugs. Moreover, also demonstrated is the usefulness of molecular connectivity in the search of new active compounds. Examples of such compounds are 4-(l-buthylpenthyl)pyridine, N-(3-bromopropyl)-phtalimide and N-(3-chlorpropyl)-piperidin hydrochloride. All of them show antihistaminic activity values more than 30% higher than that of terfenadine, which is used as the reference drug.
Inhaled isoflurane via the anaesthetic conserving device versus propofol for sedation of invasively ventilated patients in intensive care units in Ge…
2021
Summary Background Previous studies indicate that isoflurane could be useful for the sedation of patients in the intensive care unit (ICU), but prospective studies evaluating isoflurane's efficacy have been small. The aim of this study was to test whether the sedation with isoflurane was non-inferior to sedation with propofol. Methods This phase 3, randomised, controlled, open-label non-inferiority trial evaluated the efficacy and safety of up to 54 h of isoflurane compared with propofol in adults (aged ≥18 years) who were invasively ventilated in ICUs in Germany (21 sites) and Slovenia (three sites). Patients were randomly assigned (1:1) to isoflurane inhalation via the Sedaconda anaesthet…
Assessment and treatment of the withdrawal syndrome in paediatric intensive care units
2020
Background: Sedoanalgesia secondary iatrogenic withdrawal syndrome (IWS) in paediatric intensive units is frequent and its assessment is complex. Therapies are heterogeneous, and there is currently no gold standard method for diagnosis. In addition, the assessment scales validated in children are scarce. This paper aims to identify and describe both the paediatric diagnostic and assessment tools for the IWS and the treatments for the IWS in critically ill paediatric patients. Methods: A systematic review was conducted according to the PRISMA guidelines. This review included descriptive and observational studies published since 2000 that analyzed paediatric scales for the evaluation of the i…
Continuous Theta-Burst Stimulation Intensity Dependently Facilitates Motor-Evoked Potentials Following Focal Electrical Stimulation of the Rat Motor …
2020
Although theta-burst stimulation (TBS) is known to differentially modify motor cortical excitability according to stimulus conditions in humans, whether similar effects can be seen in animals, in particular rats, remains to be defined. Given the importance of experimental rat models for humans, this study explored this stimulation paradigm in rats. Specifically, this study aimed to explore corticospinal excitability after TBS in anesthetized animals to confirm its comparability with human results. Both inhibition-facilitation configurations using paired electrical stimulation protocols and the effects of the TBS paradigm on motor-evoked potentials (MEPs) in rat descending motor pathways wer…
GABAA-receptor Subtypes: Clinical Efficacy and Selectivity of Benzodiazepine Site Ligands
1997
The main inhibitory neurotransmitter receptor of the brain, the gamma-aminobutyric acid type A receptor (GABA[A]), mediates the actions of several classes of clinically important drugs, such as benzodiazepines, barbiturates and general anaesthetics. This review summarizes the current knowledge on how classical benzodiazepines and novel nonbenzodiazepine compounds act on the benzodiazepine site of GABA(A) receptors and on their clinical pharmacology related to anxiolytic, sedative, hypnotic and cognitive effects or side-effects. Partial agonism, receptor subtype selectivity and novel binding sites are discussed as possible strategies to develop new drugs with fewer adverse effects than are s…
Separating efficacy and sedative effects of guanfacine extended release in children and adolescents with ADHD from four randomized, controlled, phase…
2016
IntroductionGuanfacine extended release (GXR) is a non-stimulant treatment for attention-deficit/hyperactivity disorder (ADHD).ObjectiveTo separate efficacy and sedative treatment-emergent adverse events (TEAEs) associated with GXR in four randomized, controlled trials in children (6–12 years) and adolescents (13–17 years) with ADHD.MethodsSPD503-301 (n = 345) and SPD503-304 (n = 324) were 8 and 9 week studies of fixed-dose GXR (≤ 4 mg/day). SPD503-312 (n = 314; adolescents only) and SPD503-316 (n = 338) were 10–13 week studies of dose-optimized GXR (1–7 mg/day).ResultsIn fixed-dose studies, pooled incidences of sedative TEAEs with GXR were highest at week 1 (GXR, 13.9–18.7%; placebo, 8.7%)…
Sedation in allergic rhinitis is caused by the condition and not by antihistamine treatment
1996
Sedation is regarded as a common side-effect of most H1-antihistamines. This view must be accepted, yet can hardly be assessed under treatment of allergic disorders. Since central sedative potency is hard to evaluate, different methods of measurement have been introduced in the four phases of clinical investigation. While tests of high complexity in early trials can detect true central effects, they seem to have the disadvantage of not taking into consideration the important interactions of drugs with the disorder. Therefore, we used a visual analog scale (VAS) as an instrument to demonstrate sedative effects in five clinical studies carried out between 1989 and 1994 with a total number of …
Palliative sedation in advanced cancer patients followed at home: A retrospective analysis
2012
Abstract CONTEXT: Data regarding palliative sedation at home in dying patients are lacking. OBJECTIVES: To describe the frequency, indication, and modality of palliative sedation (PS) in patients followed at home. METHODS: A retrospective analysis of home care cancer patients was performed. Patients who received PS before dying were selected and information about epidemiologic characteristics, indications, duration, drugs, and outcomes was collected. RESULTS: Of 370 medical charts of patients who died at home, 49 patients received PS before dying. PS was proposed by the team, relatives, or both in 63.3%, 4.1%, and 32.6% of cases, respectively. Delirium alone or in combination with other sym…
Palliative sedation in patients with advanced cancer followed at home: A systematic review
2011
Abstract Context Patients with advanced cancer who are near the end of life may experience intolerable suffering refractory to targeted palliative therapies. Palliative sedation (PS) is considered to be an effective treatment modality for these refractory symptoms when aggressive efforts fail to provide relief. Objectives The aim of this study was to systematically review articles regarding PS performed at home in patients with intractable symptoms. Methods Literature databases searched included MedLine, PubMed, and EMBASE. The text words and MeSH/EMTREE terms "home care" and "sedation" were used for electronic database searches. Results Six articles met the inclusion criteria for research …
Prediction of properties of chiral compounds by molecular topology
1998
Abstract A common assumption in chemistry is that chiral behavior is associated with 3-D geometry. However, chiral information is related to symmetry, which allows the topological handling of chiral atoms by weighted graphs and the calculation of new descriptors that give a weight to the corresponding entry in the main diagonal of the topological matrix. In this study, it is demonstrated that, operating in this way, chiral topological indices are obtained that can differentiate the pharmacological activity between pairs of enantiomers. The 50% inhibitory concentration (IC50) values of the D2 dopamine receptor and the σ receptor for a group of 3-hydroxy phenyl piperidines are specifically pr…