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Z-drugs
Nonbenzodiazepines (), sometimes referred to colloquially as Z-drugs (as many of their names begin with the letter "z"), are a class of psychoactive drugs that are very benzodiazepine-like in nature. They are used in the treatment of sleep problems, and for their anxiolytic effects. Nonbenzodiazepine pharmacodynamics are almost entirely the same as benzodiazepine drugs and therefore exhibit similar benefits, side-effects, and risks. However, nonbenzodiazepines have dissimilar or entirely different chemical structures and are therefore unrelated to benzodiazepines on a molecular level. Classes Currently, the major chemical classes of nonbenzodiazepines are: Imidazopyridines * Alpidem * Necopidem * Saripidem * Zolpidem (Ambien, Ambien CR, Intermezzo, Zolpimist, Edluar, Ivadal, Sanval, Stilnox, etc.) Pyrazolopyrimidines * Divaplon * Fasiplon * Indiplon * Lorediplon * Ocinaplon * Panadiplon * Taniplon * Zaleplon (Sonata, Starnoc, Andante) Cyclopyrrolones * Eszopiclone (Lunesta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzodiazepine
Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, insomnia, and seizures. The first benzodiazepine, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955 and was made available in 1960 by Hoffmann–La Roche, who soon followed with diazepam (Valium) in 1963. By 1977, benzodiazepines were the most prescribed medications globally; the introduction of selective serotonin reuptake inhibitors (SSRIs), among other factors, decreased rates of prescription, but they remain frequently used worldwide. Benzodiazepines are depressants that enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor, resulting in sedative, hypnotic ( sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant properties. High doses o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zolpidem
Zolpidem, sold under the brand name Ambien, among others, is a medication primarily used for the short-term treatment of sleeping problems. Guidelines recommend that it be used only after cognitive behavioral therapy for insomnia and behavioral changes, such as sleep hygiene, have been tried. It decreases the time to sleep onset by about fifteen minutes and at larger doses helps people stay asleep longer. It is taken by mouth and is available in conventional tablets, sublingual tablets, or oral spray. Common side effects include daytime sleepiness, headache, nausea, and diarrhea. More severe side effects include memory problems and hallucinations. The previously recommended dose was decreased in 2013, by the US Food and Drug Administration (FDA), to the immediate-release 10mg for men, and 5mg for women, in an attempt to reduce next-day somnolence. Newer extended-release formulations include the 6.25mg for women, and 12.5mg or 6.25mg for men, which also cause next-day somnolenc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Insomnia
Insomnia, also known as sleeplessness, is a sleep disorder in which people have trouble sleeping. They may have difficulty falling asleep, or staying asleep as long as desired. Insomnia is typically followed by daytime sleepiness, low energy, irritability, and a depressed mood. It may result in an increased risk of motor vehicle collisions, as well as problems focusing and learning. Insomnia can be short term, lasting for days or weeks, or long term, lasting more than a month. The concept of the word insomnia has two possibilities: insomnia disorder and insomnia symptoms, and many abstracts of randomized controlled trials and systematic reviews often underreport on which of these two possibilities the word insomnia refers to. Insomnia can occur independently or as a result of another problem. Conditions that can result in insomnia include psychological stress, chronic pain, heart failure, hyperthyroidism, heartburn, restless leg syndrome, menopause, certain medications, and d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zopiclone
Zopiclone, sold under the brand name Imovane among others, is a nonbenzodiazepine used to treat insomnia, difficulty sleeping. Zopiclone is molecularly distinct from benzodiazepine drugs and is classed as a cyclopyrrolone. However, zopiclone increases the normal transmission of the neurotransmitter gamma-aminobutyric acid (GABA) in the central nervous system, via modulating GABAA receptor, GABAA receptors similarly to the way benzodiazepine drugs do. Zopiclone is a sedative. It works by causing a depression or tranquilization of the central nervous system. After prolonged use, the body can become accustomed to the effects of zopiclone. When the dose is then reduced or the drug is abruptly stopped, withdrawal symptoms may result. These can include a range of symptoms similar to those of benzodiazepine withdrawal. Although withdrawal symptoms from therapeutic doses of zopiclone and its isomers (i.e., eszopiclone) do not typically present with convulsions and are therefore not cons ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zaleplon
Zaleplon, sold under the brand names Sonata among others, is a sedative-hypnotic, used to treat insomnia. It is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class. It is manufactured by King Pharmaceuticals and Gedeon Richter Plc. It has been discontinued in Canada but can be manufactured if a prescription is brought to a compounding pharmacy. It was prescribed rarely in the United Kingdom, with zopiclone being the preferred Z-drug by the National Health Service (NHS) and is now unavailable. Medical uses Zaleplon is slightly effective in insomnia, primarily characterized by difficulty falling asleep. Zaleplon significantly reduces the time required to fall asleep by improving sleep latency and may therefore facilitate sleep induction rather than sleep maintenance. Due to its ultrashort elimination half-life, zaleplon may not be effective in reducing premature awakenings; however, it may be administered to alleviate middle-of-the-night awakenings. However, zaleplo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Panadiplon
Panadiplon (U-78875) is an anxiolytic drug with a novel chemical structure that is not closely related to other drugs of this type. It has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and relatively little sedative or amnestic effect, and so is classified as a nonbenzodiazepine anxiolytic. Panadiplon acts as a high-affinity GABAA receptor partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ..., but despite showing a useful effects profile of a potent anxiolytic with little sedative effects, panadiplon was discontinued from clinical development for use in humans after showing evidence of liver damage in both animals and human trials. Panadiplon however continues to be used in animal research, mainly as a s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gedocarnil
Gedocarnil (INN) is an anxiolytic of the β-carboline class related to abecarnil. It is registered as an anxiolytic under the WHO's ATC classification system; however, there are no trade names associated with it and it does not appear to have ever been marketed. See also * Nonbenzodiazepine Nonbenzodiazepines (), sometimes referred to colloquially as Z-drugs (as many of their names begin with the letter "z"), are a class of psychoactive drugs that are very benzodiazepine-like in nature. They are used in the treatment of sleep proble ... References Anxiolytics Beta-Carbolines Chloroarenes Carboxylate esters Ethers Phenol ethers GABAA receptor positive allosteric modulators {{Anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abecarnil
Abecarnil (ZK-112,119) is an anxiolytic drug from the β-Carboline family. It is one of a relatively recently developed class of medicines known as the nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures. It is a partial agonist acting selectively at the benzodiazepine site of the GABAA receptor. Abecarnil was originally developed as an anti-anxiety drug, but has not as yet been commercially developed for use in humans, instead so far mainly being used for research into the development of other new sedative and anxiolytic drugs. Investigations are continuing into its actions and it looks likely to be developed for use both in the treatment of anxiety, and as a less addictive substitute drug for the treatment of benzodiazepine and alcohol addiction. Abecarnil may also have fewer problems of tolerance and withdrawal problems compared to nonselective full agonist benzodiazepine acting drugs. Abecarnil is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
β-Carboline
β-Carboline (9''H''- pyrido ,4-''b'' ndole) represents the basic chemical structure for more than one hundred alkaloids and synthetic compounds. The effects of these substances depend on their respective substituent. Natural β-carbolines primarily influence brain functions but can also exhibit antioxidant effects. Synthetically designed β-carboline derivatives have recently been shown to have neuroprotective, cognitive enhancing and anti-cancer properties. Pharmacology The pharmacological effects of specific β-carbolines are dependent on their substituents. For example, the natural β-carboline harmine has substituents on position 7 and 1. Thereby, it acts as a selective inhibitor of the DYRK1A protein kinase, a molecule necessary for neurodevelopment. It also exhibits various antidepressant-like effects in rats by interacting with serotonin receptor 2A. Furthermore, it increases levels of the brain-derived neurotrophic factor (BDNF) in rat hippocampus. A decreased BDNF le ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Suriclone
Suriclone (Suril) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Other cyclopyrrolone drugs include zopiclone and pagoclone. Suriclone has a very similar pharmacological profile to the benzodiazepine family of drugs including sedative and anxiolytic properties but with less amnestic effects, and its chemical structure A chemical structure determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target molecule or other solid. Molecular geometry refers to the spatial arrangement of at ... is quite different from that of the benzodiazepine drugs. The mechanism of action by which suriclone produces its sedative and anxiolytic effects is by modulating GABAA receptors, although suriclone is more subtype-selective than most benzodiazepines. References {{GABAAR PAMs Carbamates Chloroarenes Cyclopyrrolones GABAA receptor positive allosteric modulators Naphthyridines Pip ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Suproclone
Suproclone is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs, developed by the French pharmaceutical company Rhône-Poulenc. Other cyclopyrrolone drugs include zopiclone, pagoclone and suriclone. Suproclone is very similar in structure to the related drug suriclone Suriclone (Suril) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Other cyclopyrrolone drugs include zopiclone and pagoclone. Suriclone has a very similar pharmacological profile to the benzodiazepine family of drugs inc ..., but little information has been published about it specifically. However it can be expected that the mechanism of action by which suproclone produces its sedative and anxiolytic effects is by modulating benzodiazepine receptors (resulting in an increased response to endogenous GABA), in a similar manner to other drugs of this class. References Carbamates Chloroarenes Cyclopyrrolones GABAA receptor positive allosteric modulators Lactams ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pazinaclone
Pazinaclone (DN-2327) is a sedative and anxiolytic drug in the cyclopyrrolone family of drugs. Some other cyclopyrrolone drugs include zopiclone and eszopiclone. Pazinaclone has a very similar pharmacological profile to the benzodiazepines including sedative and anxiolytic properties, but with less amnestic effects, and at low doses it is a relatively selective anxiolytic, with sedative effects only appearing at higher doses. Pazinaclone produces its sedative and anxiolytic effects by acting as a partial agonist at GABAA benzodiazepine receptors, although pazinaclone is more subtype-selective than most benzodiazepines. Synthesis Reaction of 2-amino-7-chloro-1,8-naphthyridine with phthalic anhydride leads to the corresponding phthalimide. Selective reduction of one of the imide carbonyl groups in essence converts that to an aldehyde. Condensation with ''tert''-butyl(triphenylphosphoranylidene)acetate gives the Wittig product. The carboxylic acid is then treated with diethyl cy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
