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Drug Side Effect Frequency Mining over a Large Twitter Dataset Using Apache Spark
Published in Saravanan Krishnan, Ramesh Kesavan, B. Surendiran, G. S. Mahalakshmi, Handbook of Artificial Intelligence in Biomedical Engineering, 2021
Dennis Hsu, Melody Moh, Teng-Sheng Moh, Diane Moh
Based on the results from the pipeline, a domain expert provided some analysis and insight on the different drug side effects and their frequency. The following drugs are discussed based on information from Medscape (WebMD LLC, 2019) and Medline Plus (Medline Plus, 2017). It is not surprising that the Xanax, a benzodiazepine utilized for anxiety, causes drowsiness as a side effect. Its rapid action on the GABA receptors in the limbic system and reticular formation also explains how the dopamine surge in response contributes to addictive behavior, abnormal highs, and withdrawal symptoms. Overdoses of benzodiazepines, especially in the elderly, or use in combination with alcohol or other central nervous system depressants, can cause anterograde amnesia and loss of consciousness.
Sedation, analgesia and patient observation in interventional radiology
Published in William H. Bush, Karl N. Krecke, Bernard F. King, Michael A. Bettmann, Radiology Life Support (Rad-LS), 2017
Jeffrey E. Quam, Michael A. Bettmann
The primary mode of action of the benzodiazepines is through facilitation of the gamma-aminobutyric acid (GABA) system in the CNS. This system is the largest and most powerful inhibitory system in the brain. Benzodiazepine-binding sites are found throughout the CNS, but are most numerous in the cerebral cortex and least numerous in the spinal cord. Benzodiazepines do not act directly at GABA-receptor sites, but instead enhance the binding of GABA to its receptors.4 This enhances the GABA-mediated conductance of chloride through the cell membrane.5 Through direct GABA potentiation, benzodiazepines enhance the degree of general CNS inhibition.
Enzyme Kinetics and Drugs as Enzyme Inhibitors
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
As in other cases, allosteric drugs may be classified as covalent (see below) or noncovalent. To the latter belong the benzodiazepines, the non-benzodiazepine Z-drugs (zopiclone, zolpidem, etc.) or barbiturate drugs, targeting the ionotropic GABA receptor and acting as positive allosteric modulator molecules that increase the activity of the GABAA receptor protein in the central nervous system (e.g., Henschel et al., 2008). Cinacalcet is a positive G-protein-coupled receptor (GPCR) modulator that enhances Ca2+ activation of calcium-sensing receptor (Brown, 2010) and is employed to treat hyperparathyroidism; the cellular mechanisms for allosteric modulation of calcium-sensing receptors has been discussed by Cavanaugh et al. (2012). Maraviroc is a negative modulator of the GPCR chemokine receptor CCR5 and used for the treatment of HIV-type 1 (Conn et al., 2009, and literature cited therein). Metabotropic glutamate receptors (mGluRs, several different groups) involved in the modulation of synaptic transmission and neuronal excitability are members of the GPCR superfamily; mGluRs are drug targets of positive allosteric modulators for treating neurological and psychiatric disorders (Alzheimer’s, anxiety, schizophrenia, etc.) as reviewed by Niswender and Conn (2010), Wood et al. (2011), or Herman et al. (2012). A recent example are allosteric BCR-ABL tyrosine kinase fusion protein inhibitors in Philadelphia chromosome-positive acute lymphoblastic leukemia, developed to overcome resistance towards drugs like imatinib and others (Hantschel, 2012). For covalent allosteric inhibitors see the next section.
Evaluating drugged driving: Effects of exemplar pain and anxiety medications
Published in Traffic Injury Prevention, 2018
Timothy L. Brown, Gary Milavetz, Gary Gaffney, Andrew Spurgin
Benzodiazepines, such as alprazolam, become pharmacologically active by modulating effects of the powerful neuroinhibitory neurotransmitter gaba-aminobutyric acid (GABA). Benzodiazapines enhance GABA-receptor sensitivity and responsiveness, thus adding to the inhibitory effects of the most widespread inhibitory neurotransmitter system in the CNS. There are 4 major receptor subtypes in the CNS (α, γ, β, δ) and there are receptor subunits within these subtypes. Pharmacological actions of benzodiazepines, predominately through the α receptors, induce sedation, anxiolysis, amnesia, myorelaxation, motor impairment, and anticonvulsant activity, The neuromoduating inhibitory effects of the benzodiazepine receptors, as well as the widespread neuroanatomical locations of GABA, suggest neurophysiological mechanisms of action by which alprazolam could affect the cognitive and motor actions involved in driving a motor vehicle. Hypothesized psychological and physiological components of driving include alertness; sensory–perceptual processing, reaction time and psychological processing; memory; executive functioning; and motor coordination. Benzodiazepines could be implicated in any of those levels of cognitive and psychomotor processing. Alprazolam clearly produces powerful CNS effects, including drowsiness, impaired concentration, impaired executive functioning, as well as possible effects peripherally, including loss of motor coordination.