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Tasimelteon
Tasimelteon, sold under the brand name Hetlioz, is a medication approved by the U.S. Food and Drug Administration (FDA) in January 2014, for the treatment of non-24-hour sleep–wake disorder (also called non-24, N24 and N24HSWD). In June 2014, the European Medicines Agency (EMA) accepted an EU filing application for tasimelteon and in July 2015, the drug was approved in the European Union for the treatment of non-24-hour sleep-wake rhythm disorder in totally blind adults, but not in the case of non-24 in sighted people. The most common side effects include headache, somnolence, nausea (feeling sick) and dizziness. Medical uses In the United States, tasimelteon capsules are indicated for the treatment of non-24-hour sleep–wake disorder (Non-24) in adults and for the treatment of nighttime sleep disturbances in Smith-Magenis Syndrome (SMS) in people sixteen years of age and older. Tasimelteon oral suspension is indicated for the treatment of nighttime sleep disturbances in S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Non-24-hour Sleep–wake Disorder
Non-24-hour sleep–wake disorder (non-24, N24SWD, or N24) is one of several chronic circadian rhythm sleep disorders (CRSDs). It is defined as a "chronic steady pattern comprising ..daily delays in sleep onset and wake times in an individual living in a society". Symptoms result when the non-entrained ( free-running) endogenous circadian rhythm drifts out of alignment with the light–dark cycle in nature. Although this sleep disorder is more common in blind people, affecting up to 70% of the totally blind, it can also affect sighted people. Non-24 may also be comorbid with bipolar disorder, depression, and traumatic brain injury. The American Academy of Sleep Medicine (AASM) has provided CRSD guidelines since 2007 with the latest update released in 2015. People with non-24 experience daily shifts in the circadian rhythm such as peak time of alertness, body temperature minimum, metabolism and hormone secretion. These shifts do not align with the natural light–dark cycle. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Discovery And Development Of Melatonin Receptor Agonists
Melatonin receptor agonists are analogues of melatonin that bind to and activate the melatonin receptor. Agonists of the melatonin receptor have a number of therapeutic applications including treatment of sleep disorders and depression. The discovery and development of melatonin receptor agonists was motivated by the need for more potent analogues than melatonin, with better pharmacokinetics and longer half-lives. Melatonin receptor agonists were developed with the melatonin structure as a model. The melatonin receptors are G protein-coupled receptors and are expressed in various tissues of the body. There are two subtypes of the receptor in humans, melatonin receptor 1 (MT1) and melatonin receptor 2 (MT2). Melatonin and melatonin receptor agonists, on market or in clinical trials, all bind to and activate both receptor types. The binding of the agonists to the receptors has been investigated since 1986, yet is still not fully understood. When melatonin receptor agonists bind t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Melatonin (medication)
Melatonin is a naturally occurring hormone produced in the brain that is also used as a dietary supplement and medication. As a hormone, melatonin is released by the pineal gland and is involved in sleep–wake cycles. As a supplement, it is often used for the short-term treatment of disrupted sleep patterns such as from jet lag or shift work, and is typically taken orally. There is evidence of its benefit for insomnia, but the evidence is not strong. A 2017 review found that sleep onset occurred six minutes faster with use on average, but found no change in total time asleep. Side effects from melatonin supplements are minimal at low doses for short durations (the studies reported that side effects occurred about equally for both melatonin and placebo). Side effects of melatonin are rare but may occur in 1 to 10 patients out of 1,000. They may include somnolence, headaches, nausea, diarrhea, abnormal dreams, irritability, restlessness, insomnia, anxiety, migraine, leth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ramelteon
Ramelteon, sold under the brand name Rozerem among others, is a melatonin agonist medication which is used in the treatment of insomnia. It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset. It reduces the time taken to fall asleep, but the degree of clinical benefit is small. The medication is approved for long-term use. Ramelteon is taken oral administration, by mouth. Side effects of ramelteon include somnolence, dizziness, fatigue (medical), fatigue, nausea, exacerbated insomnia, and changes in hormone levels. Ramelteon is an structural analog, analogue of melatonin (medication), melatonin and is a binding selectivity, selective agonist of the melatonin receptor, melatonin MT1 receptor, MT1 and MT2 receptor, MT2 receptors. The elimination half-life, half-life and duration of action, duration of ramelteon are much longer than those of melatonin. Ramelteon is not a benzodiazepine or Z-drug and does not interact with GABA r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYP1A2
Cytochrome P450 1A2 (abbreviated CYP1A2), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the human body. In humans, the CYP1A2 enzyme is encoded by the ''CYP1A2'' gene. Function CYP1A2 is a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. CYP1A2 localizes to the endoplasmic reticulum and its expression is induced by some polycyclic aromatic hydrocarbons (PAHs), some of which are found in cigarette smoke. The enzyme's endogenous substrate is unknown; however, it is able to metabolize some PAHs to carcinogenic intermediates. Other xenobiotic substrates for this enzyme include caffeine, aflatoxin B1, and paracetamol (acetaminophen). The transcript from this gene contains four Alu sequences flanked by direct repeats in the 3' untranslated region. CYP1A2 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Orphan Drug
An orphan drug is a medication, pharmaceutical agent that is developed to treat certain rare medical conditions. An orphan drug would not be profitable to produce without government assistance, due to the small population of patients affected by the conditions. The conditions that orphan drugs are used to treat are referred to as orphan diseases. The assignment of orphan status to a disease and to drugs developed to treat it is a matter of public policy that depends on the legislation (if there is any) of the country. Designation of a drug as an orphan drug has yielded medical breakthroughs that might not otherwise have been achieved, due to the economics of drug medical research, research and development. Examples of this can be that in the U.S. and the EU, it is easier to gain marketing approval for an orphan drug. There may be other financial incentives, such as an extended period of exclusivity, during which the producer has sole rights to market the drug. All are intended to en ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzofurans
Benzofuran is the heterocyclic compound consisting of fused benzene and furan rings. This colourless liquid is a component of coal tar. Benzofuran is the structural nucleus (parent compound) of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. Production Benzofuran is extracted from coal tar. It is also obtained by dehydrogenation of 2-ethylphenol. Laboratory methods Benzofurans can be prepared by various methods in the laboratory. Notable examples include: *''O''-alkylation of salicylaldehyde with chloroacetic acid followed by dehydration reaction, dehydration (cyclication) of the resulting ether and decarboxylation. *Perkin rearrangement, where a coumarin is reacted with a hydroxide: : *Diels–Alder reaction of Nitroalkene, nitro vinyl furans with various dienophiles: : *Isomerization, Cycloisomerization of alkyne Arene substitution pattern, ortho-substituted phenols: : Related compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sedatives
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are central nervous system (CNS) depressants and interact with brain activity, causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter gamma-aminobutyric acid (GABA). Most sedatives produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or relieve anxiety, whereas the term ''hypnotic'' describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness), they are often referred to collectively as ''sedative–hypnotic'' drugs. Terminology There is some overlap between the terms "sedative" and "hypnotic". Advances in pharmacol ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Advocacy Group
Advocacy groups, also known as lobby groups, interest groups, special interest groups, pressure groups, or public associations, use various forms of advocacy or lobbying to influence public opinion and ultimately public policy. They play an important role in the development of political and social systems. Motives for action may be based on Politics, political, Economy, economic, religious, morality, moral, commerce, commercial or common good-based positions. Groups Methods used by advocacy groups, use varied methods to try to achieve their aims, including lobbying, media campaigns, consciousness raising, awareness raising publicity stunts, Opinion poll, polls, research, and policy briefings. Some groups are supported or backed by powerful business or political interests and exert considerable influence on the political process, while others have few or no such resources. Some have developed into important social, and political institutions or social movements. Some powerful advo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Public Citizen
Public Citizen is an American non-profit, Progressivism in the United States, progressive consumer rights advocacy group, and think tank based in Washington, D.C. It was founded in 1971 by the American activist and lawyer Ralph Nader. Lobbying efforts Public Citizen advocates before all three branches of the United States federal government. Its five divisions include Congress Watch; Energy; Global Trade Watch; the Health Research Group; and Public Citizen Litigation Group, a nationally prominent public interest law firm founded by Alan Morrison and known for its Supreme Court and appellate practice. Among other issues, Public Citizen has been a public voice on Prescription drug prices in the United States, drug pricing. For example, they advocated for Gilead Sciences to test GS-441524, a cheaper alternative to remdesivir. History In 1968, Nader recruited seven volunteer law students, dubbed "Nader's Raiders" by the Washington press corps, to evaluate the efficacy and operation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
