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MIN-202
Seltorexant, also known by its developmental code names MIN-202 and JNJ-42847922, is an orexin receptor antagonist, orexin antagonist medication which is under development for the treatment of depression (mood), depression and insomnia. It is a binding selectivity, selective receptor antagonist, antagonist of the orexin receptor, orexin hypocretin (orexin) receptor 2, OX2 receptor (2-SORA). The medication is taken oral administration, by mouth. As of February 2022, seltorexant is in Phases of clinical research#Phase III, phase 3 clinical trials for treatment of major depressive disorder (MDD) and Phases of clinical research#Phase II, phase 2 trials for treatment of insomnia. It was also under investigation for the treatment of sleep apnea, but no recent development has been reported for this indication. Seltorexant is under development by Minerva Neurosciences and Johnson & Johnson's Janssen Pharmaceuticals. Seltorexant is being explored at doses of 5 to 80mg. In the early clinica ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Orexin Antagonist
An orexin receptor antagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptor antagonist of one or both of the orexin receptors, OX1 and OX2. Medical applications include treatment of sleep disorders such as insomnia. Examples Marketed * Daridorexant (nemorexant; Quviviq) – dual OX1 and OX2 antagonist – approved for insomnia in January 2022, formerly under development for sleep apnea – half-life 8 hours * Lemborexant (Dayvigo) – dual OX1 and OX2 antagonist – approved for insomnia in December 2019 and released June 1 2020, under development for circadian rhythm sleep disorders, chronic obstructive pulmonary disease, and sleep apnea – half-life 17–55 hours * Suvorexant (Belsomra) – dual OX1 and OX2 antagonist – approved for insomnia in August 2014, under development for delirium – half-life 12 hours Under development * Seltorexant (MIN-202, JNJ-42847922, JNJ-922) – selective OX2 antagonist – under development for m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Orexin Receptor
The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that binds the neuropeptide orexin. There are two variants, OX1 and OX2, each encoded by a different gene (, ). Both orexin receptors exhibit a similar pharmacology – the 2 orexin peptides, orexin-A and orexin-B, bind to both receptors and, in each case, agonist binding results in an increase in intracellular calcium levels. However, orexin-B shows a 5- to 10-fold selectivity for orexin receptor type 2, whilst orexin-A is equipotent at both receptors. Several orexin receptor antagonists are in development for potential use in sleep disorders. The first of these, suvorexant, has been on the market in the United States since 2015. There were two orexin agonists under development . Ligands Several drugs acting on the orexin system are under development, either orexin agonists for the treatment of conditions such as narcolepsy, or orexin antagonists for insomnia. In Augus ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Orexin Receptor Antagonist
An orexin receptor antagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptor antagonist of one or both of the orexin receptors, OX1 and OX2. Medical applications include treatment of sleep disorders such as insomnia. Examples Marketed * Daridorexant (nemorexant; Quviviq) – dual OX1 and OX2 antagonist – approved for insomnia in January 2022, formerly under development for sleep apnea – half-life 8 hours * Lemborexant (Dayvigo) – dual OX1 and OX2 antagonist – approved for insomnia in December 2019 and released June 1 2020, under development for circadian rhythm sleep disorders, chronic obstructive pulmonary disease, and sleep apnea – half-life 17–55 hours * Suvorexant (Belsomra) – dual OX1 and OX2 antagonist – approved for insomnia in August 2014, under development for delirium – half-life 12 hours Under development * Seltorexant (MIN-202, JNJ-42847922, JNJ-922) – selective OX2 antagonist – under development fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sleep Onset
Sleep onset is the transition from wakefulness into sleep. Sleep onset usually transmits into non-rapid eye movement sleep (NREM sleep) but under certain circumstances (e.g. narcolepsy) it is possible to transit from wakefulness directly into rapid eye movement sleep (REM sleep). History During the 1920s an obscure disorder that caused encephalitis and attacked the part of the brain that regulates sleep influenced Europe and North America. Although the virus that caused this disorder was never identified, the psychiatrist and neurologist Constantin von Economo decided to study this disease and identified a key component in the sleep-wake regulation. He identified the pathways that regulated wakefulness and sleep onset by studying the parts of the brain that were affected by the disease and the consequences it had on the circadian rhythm. He stated that the pathways that regulated sleep onset are located between the brain stem and the basal forebrain. His discoveries were not a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Total Sleep Time
Sleep is a sedentary state of mind and body. It is characterized by altered consciousness, relatively inhibited sensory activity, reduced muscle activity and reduced interactions with surroundings. It is distinguished from wakefulness by a decreased ability to react to stimuli, but more reactive than a coma or disorders of consciousness, with sleep displaying different, active brain patterns. Sleep occurs in repeating periods, in which the body alternates between two distinct modes: REM sleep and non-REM sleep. Although REM stands for "rapid eye movement", this mode of sleep has many other aspects, including virtual paralysis of the body. Dreams are a succession of images, ideas, emotions, and sensations that usually occur involuntarily in the mind during certain stages of sleep. During sleep, most of the body's systems are in an anabolic state, helping to restore the immune, nervous, skeletal, and muscular systems; these are vital processes that maintain mood, memory, and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Wake After Sleep Onset
Middle-of-the-night insomnia (MOTN) is characterized by having difficulty returning to sleep after waking up during the night or very early in the morning. This kind of insomnia (sleeplessness) is different from initial or sleep-onset insomnia, which consists of having difficulty falling asleep at the beginning of sleep. The disrupted sleep patterns caused by middle-of-the-night insomnia make many sufferers of the condition complain of fatigue the following day. Excessive daytime sleepiness is reported nearly two times higher by individuals with nocturnal awakenings than by people who sleep through the night. Sleep research conducted in the 1990s showed that such waking up during the night may be a natural sleep pattern, rather than a form of insomnia. If interrupted sleep (called "biphasic sleeping" or "bimodal sleep") is perceived as normal and not referred to as "insomnia", less distress is caused and a return to sleep usually occurs after about one hour. Causes * Pain * Pregn ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sleep Efficiency
Sleep efficiency (SE) is the ratio between the time a person spends asleep, and the total time dedicated to sleep (i.e. both sleeping and attempting to fall asleep or fall back asleep). It is given as a percentage. SE of 80% or more is considered normal/healthy with most young healthy adults displaying SE above 90%. SE can be determined with a polysomnograph and is an important parameter of a sleep study. Sleep efficiency is often described as the ratio between time spent asleep ("total sleep time (TST)"), and time spent "in bed" ("time in bed (TIB)"), however, TIB does not encompass "non-sleep-related activities" performed in bed (e.g. reading, watching television, etc.) as the phrase may seem to suggest. Clinical significance Apparently long sleep duration may in fact be a sign of low sleep efficiency. SE is significantly reduced in insomnia; SE is therefore an important clinical parameter in clinical investigations of insomnia. SE declines with age and low SE is common in th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug Safety
Term Given By Tushar Sharma (UPES Batch 2025) Pharmacovigilance (PV, or PhV), also known as drug safety, is the pharmaceutical science relating to the "collection, detection, assessment, monitoring, and prevention" of adverse effects with pharmaceutical products. The etymological roots for the word "pharmacovigilance" are: (Greek for drug) and (Latin for to keep watch). As such, pharmacovigilance heavily focuses on adverse drug reactions (ADR), which are defined as any response to a drug which is noxious and unintended, including lack of efficacy (the condition that this definition only applies with the doses normally used for the prophylaxis, diagnosis or therapy of disease, or for the modification of physiological disorder function was excluded with the latest amendment of the applicable legislation). Medication errors such as overdose, and misuse and abuse of a drug as well as drug exposure during pregnancy and breastfeeding, are also of interest, even without an adve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tolerability
Tolerability refers to the degree to which overt adverse effects of a drug can be tolerated by a patient. Tolerability of a particular drug can be discussed in a general sense, or it can be a quantifiable measurement as part of a clinical study. Usually, it is measured by the rate of "dropouts", or patients that forfeit participation in a study due to extreme adverse effects. Tolerability, however, is often relative to the severity of the medical condition a drug is designed to treat. For instance, cancer patients may tolerate significant pain or discomfort during a chemotherapeutic study with the hope of prolonging survival or finding a cure, whereas patients experiencing a benign condition, such as a headache, are less likely to. As an example, tricyclic antidepressants (TCAs) are very poorly tolerated and often produce severe side effects including sedation Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as 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 willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...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 increase sexual and gastrointestinal symptom r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Somnolence
Somnolence (alternatively sleepiness or drowsiness) is a state of strong desire for sleep, or sleeping for unusually long periods (compare hypersomnia). It has distinct meanings and causes. It can refer to the usual state preceding falling asleep, the condition of being in a drowsy state due to circadian rhythm disorders, or a symptom of other health problems. It can be accompanied by lethargy, weakness and lack of mental agility. Somnolence is often viewed as a symptom rather than a disorder by itself. However, the concept of somnolence recurring at certain times for certain reasons constitutes various disorders, such as excessive daytime sleepiness, shift work sleep disorder, and others; and there are medical codes for somnolence as viewed as a disorder. Sleepiness can be dangerous when performing tasks that require constant concentration, such as driving a vehicle. When a person is sufficiently fatigued, microsleeps may be experienced. In individuals deprived of sleep, somnol ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
