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Gepirone
Gepirone, sold under the brand name Exxua, is a medication used for the treatment of major depressive disorder. It is taken orally. Side effects of gepirone include dizziness, nausea, insomnia, abdominal pain, and dyspepsia (indigestion). Gepirone acts as a partial agonist of the serotonin 5-HT1A receptor. An active metabolite of gepirone, 1-(2-pyrimidinyl)piperazine, is an α2-adrenergic receptor antagonist. Gepirone is a member of the azapirone group of compounds. Gepirone was synthesized by Bristol-Myers Squibb in 1986 and was developed and marketed by Fabre-Kramer Pharmaceuticals. It was approved for the treatment of major depressive disorder in the United States in September 2023. This came after the drug had been rejected by the Food and Drug Administration (FDA) three times over two decades due to insufficient evidence of effectiveness. Medical uses Gepirone is indicated for the treatment of major depressive disorder (MDD) in adults. Of 15 clinical trials of gepi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fabre-Kramer Pharmaceuticals
Fabre-Kramer Pharmaceuticals is a pharmaceutical company that specializes in the development of psychotropic drugs. Products in their current development pipeline include gepirone and FKB01MD for major depression, gepirone and FKW00GA for social anxiety disorder, gepirone for hypoactive sexual desire disorder, FKF02SC for schizophrenia, and FKK01PD for Parkinson's disease. The company has also conducted clinical studies on a gepirone extended release formulation for major depression. In 2007, Fabre-Kramer Pharmaceuticals along with GlaxoSmithKline (GSK) received a 'not approvable' letter from the US Food and Drug Administration, for a gepirone extended release drug, an antidepressant Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathi ... treatment for adults. References External ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azapirone
Azapirones are a class of drugs used as anxiolytics, antidepressants, and antipsychotics. They are commonly used as Augmentation (psychiatry), add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs). List of azapirones The azapirones include the following agents: ; Anxiolytics * Alnespirone (S-20,499) * Binospirone (MDL-73,005) * BMY-7,378 (CAS number: ) * Buspirone (Buspar) * Enilospirone (CERM-3,726) * Eptapirone (F-11,440) * Gepirone (Exxua) * Ipsapirone (TVX-Q-7,821) * MJ-7378 (CAS number: ) * Revospirone (BAY-VQ-7,813) * Tandospirone (Sediel) * Zalospirone (WY-47,846) ; Antipsychotics * Perospirone (Lullan) * Tiospirone (BMY-13,859) * Umespirone (KC-9,172) ; others *SNAP-8719 (CAS number: )CID:14086451 Medical uses Azapirones have shown benefit in general anxiety and augmenting SSRIs in social anxiety and depression. Evidence is not clear for panic disorder and functional gastrointestinal disorders. Tandospirone has also been used to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1A Receptor
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarization and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene. Distribution The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, Septum pellucidum, septum, amygdala, and Raphe nuclei, raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. Function Neur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-2 Adrenergic Receptor
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi alpha subunit, Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-adrenergic, α2A-, α2B-adrenergic, α2B-, and α2C-adrenergic, α2C-adrenergic. Some species other than humans express a fourth α2D-adrenergic receptor as well. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central nervous system, central and peripheral nervous systems. Cellular localization The Alpha-2A adrenergic receptor, α2A adrenergic receptor is localised in the following central nervous system (CNS) structures: * Brainstem (especially the locus coeruleus as presynaptic & somatodendritic autoreceptor ) * Midbrain * Hypothalamus * Olfactory system * Hippocampus * Spinal cord * Cerebral cortex * Cerebellum * Septum Whereas the Alpha-2B adrenergic receptor, α2B adren ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
1-(2-pyrimidinyl)piperazine
1-(2-Pyrimidinyl)piperazine (1-PP, 1-PmP) is a chemical compound and piperazine derivative. It is known to act as an antagonist of the α2-adrenergic receptor (Ki = 7.3–40 nM) and, to a much lesser extent, as a partial agonist of the 5-HT1A receptor (Ki = 414 nM; Emax = 54%). It has negligible affinity for the dopamine D2, D3, and D4 receptors (Ki > 10,000 nM) and does not appear to have significant affinity for the α1-adrenergic receptors. Its crystal structure has been determined. Derivatives A number of pyrimidinylpiperazine derivatives are drugs, including: * Buspirone anxiolytic * Dasatinib anticancer agent * Eptapirone anxiolytic * Gepirone anxiolytic * Ipsapirone anxiolytic * Piribedil antiparkinsonian agent * Revospirone anxiolytic * Tandospirone anxiolytic * Tirilazad neuroprotective agent * Umespirone anxiolytic * Zalospirone anxiolytic The anxiolytics are also classified as azapirones due to the azaspirodecanedione moiety in their stru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Extended-release
Modified-release dosage is a mechanism that (in contrast to immediate-release dosage) delivers a drug with a delay after its administration (delayed-release dosage) or for a prolonged period of time (extended-release R, XR, XLdosage) or to a specific target in the body (targeted-release dosage).Pharmaceutics: Drug Delivery and Targeting p. 7-13 Sustained-release dosage forms are s designed to release (liberate) a drug at a predetermined rate in order to maintain a constant drug concentrat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hamilton Depression Rating Scale
The Hamilton Rating Scale for Depression (HRSD), also called the Hamilton Depression Rating Scale (HDRS), sometimes also abbreviated as HAM-D, is a multiple-item questionnaire used to provide an indication of depression, and as a guide to evaluate recovery. Max Hamilton originally published the scale in 1960 and revised it in 1966, 1967, 1969, and 1980. The questionnaire is designed for adults and is used to rate the severity of their depression by probing mood, feelings of guilt, suicide ideation, insomnia, agitation or retardation, anxiety, weight loss, and somatic symptoms. The HRSD has been criticized for use in clinical practice as it places more emphasis on insomnia than on feelings of hopelessness, self-destructive thoughts, suicidal cognitions and actions. An antidepressant may show statistical efficacy even when thoughts of suicide increase but sleep is improved, or for that matter, an antidepressant that as a side effect increases sexual and gastrointestinal symptom r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Effect Size
In statistics, an effect size is a value measuring the strength of the relationship between two variables in a population, or a sample-based estimate of that quantity. It can refer to the value of a statistic calculated from a sample of data, the value of one parameter for a hypothetical population, or to the equation that operationalizes how statistics or parameters lead to the effect size value. Examples of effect sizes include the correlation between two variables, the regression coefficient in a regression, the mean difference, or the risk of a particular event (such as a heart attack) happening. Effect sizes are a complement tool for statistical hypothesis testing, and play an important role in power analyses to assess the sample size required for new experiments. Effect size are fundamental in meta-analyses which aim to provide the combined effect size based on data from multiple studies. The cluster of data-analysis methods concerning effect sizes is referred to as estima ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Placebo Group
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small pilot studies, and subsequently conduct progressively larger scale comparative studies. Clinical trials can vary in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Statistical Significance
In statistical hypothesis testing, a result has statistical significance when a result at least as "extreme" would be very infrequent if the null hypothesis were true. More precisely, a study's defined significance level, denoted by \alpha, is the probability of the study rejecting the null hypothesis, given that the null hypothesis is true; and the p-value, ''p''-value of a result, ''p'', is the probability of obtaining a result at least as extreme, given that the null hypothesis is true. The result is said to be ''statistically significant'', by the standards of the study, when p \le \alpha. The significance level for a study is chosen before data collection, and is typically set to 5% or much lower—depending on the field of study. In any experiment or Observational study, observation that involves drawing a Sampling (statistics), sample from a Statistical population, population, there is always the possibility that an observed effect would have occurred due to sampling error al ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methodology
In its most common sense, methodology is the study of research methods. However, the term can also refer to the methods themselves or to the philosophical discussion of associated background assumptions. A method is a structured procedure for bringing about a certain goal, like acquiring knowledge or verifying knowledge claims. This normally involves various steps, like choosing a Sample (statistics), sample, Data collection, collecting data from this sample, and interpreting the data. The study of methods concerns a detailed description and analysis of these processes. It includes evaluative aspects by comparing different methods. This way, it is assessed what advantages and disadvantages they have and for what research goals they may be used. These descriptions and evaluations depend on philosophical background assumptions. Examples are how to conceptualize the studied phenomena and what constitutes evidence for or against them. When understood in the widest sense, methodology al ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
