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Triazolobenzodiazepine
upChemical structure of alprazolam, a common triazolobenzodiazepine Triazolobenzodiazepines (TBZD) are a class of benzodiazepine (BZD) derivative pharmaceutical drugs. Chemically, they differ from other benzodiazepines by having an additional triazole ring fused to the diazepine ring. The triazole and diazepine rings share a nitrogen atom. Examples include: * Adinazolam * Alprazolam * Bromazolam * Clonazolam * Estazolam * Flualprazolam * Flubromazolam * Flunitrazolam * Nitrazolam * Pyrazolam * Triazolam Triazolam, sold under the brand name Halcion among others, is a central nervous system (CNS) depressant tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepine (BZD) derivatives. It possesses pharmacological properti ... * Zapizolam Synthesis Synthesis of 1-methyltriazolobenzodiazepines (alprazolam type) is possible by heating 1,4-benzodiazepin-2- thiones with hydrazine and acetic acid in ''n''-butanol under reflux.Hester JB, Duchamp DJ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alprazolam Structure
Alprazolam, sold under the brand name Xanax among others, is a fast-acting, potent tranquilizer of moderate duration within the triazolobenzodiazepine group of chemicals called benzodiazepines. Alprazolam is most commonly prescribed in the management of anxiety disorders, especially panic disorder and generalized anxiety disorder (GAD). Other uses include the treatment of Chemotherapy-induced nausea and vomiting, chemotherapy-induced nausea, together with other treatments. GAD improvement occurs generally within a week. Alprazolam is generally taken oral administration, orally. Common side effects include sleepiness, Depression (mood), depression, Reduced affect display, suppressed emotions, mild to severe Ataxia, decreases in motor skills, Hiccup, hiccups, dulling or declining of cognition, decreased alertness, xerostomia, dry mouth (mildly), Bradycardia, decreased heart rate, CNS depression, suppression of central nervous system activity, impairment of judgment (usually in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alprazolam
Alprazolam, sold under the brand name Xanax among others, is a fast-acting, potent tranquilizer of moderate duration within the triazolobenzodiazepine group of chemicals called benzodiazepines. Alprazolam is most commonly prescribed in the management of anxiety disorders, especially panic disorder and generalized anxiety disorder (GAD). Other uses include the treatment of chemotherapy-induced nausea, together with other treatments. GAD improvement occurs generally within a week. Alprazolam is generally taken orally. Common side effects include sleepiness, depression, suppressed emotions, mild to severe decreases in motor skills, hiccups, dulling or declining of cognition, decreased alertness, dry mouth (mildly), decreased heart rate, suppression of central nervous system activity, impairment of judgment (usually in higher than therapeutic doses), marginal to severe decreases in memory formation, decreased ability to process new information, as well as partial ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adinazolam
Adinazolam (marketed under the brand name Deracyn) is a tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It possesses anxiolytic, anticonvulsant, sedative, and antidepressant properties. Adinazolam was developed by Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed. Adinazolam was never FDA approved and never made available to the public market; however, it has been sold as a designer drug. Chemical Information Reactivity Adinazolam contains multiple reactive parts in its structure. The first is the dimethylamine which is mildly basic with a pKa of 6.30 making over 5% of the compound protonated under physiological pH. The tertiary amine could also be important in protein binding with the ability to form hydrogen bridges and is also likely a target for metabolism via demethylation. The dimethylamine is also labile for oxidative decomposition res ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Flualprazolam
Flualprazolam is a tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It was first synthesised in 1976, but was never marketed. It can be seen as the triazolo version of fludiazepam. It has subsequently been sold as a designer drug, first being definitively identified as such in Sweden in 2018. It can be described as the 2'-fluoro derivative of alprazolam or the fluoro instead of chloro analogue of triazolam, and has similar sedative and anxiolytic effects. Legal status Flualprazolam is banned in Sweden and illegal in the UK. In December 2019, the World Health Organization recommended flualprazolam for international scheduling as a Schedule IV medication under the Convention on Psychotropic Substances. In the United States, Oregon and Virginia have placed Flualprazolam into Schedule I. On December 23, 2022, the DEA announced it had begun consideration on the matter of placing Flualprazolam under temporary Sc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Triazolam
Triazolam, sold under the brand name Halcion among others, is a central nervous system (CNS) depressant tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepine (BZD) derivatives. It possesses pharmacological properties similar to those of other benzodiazepines, but it is generally only used as a sedative to treat severe insomnia. In addition to the hypnotic properties, triazolam's amnesic, anxiolytic, sedative, anticonvulsant, and muscle relaxant properties are pronounced as well. Triazolam was initially patented in 1970 and went on sale in the United States in 1982. In 2017, it was the 289th most commonly prescribed medication in the United States, with more than one million prescriptions. Medical uses Triazolam is usually used for short-term treatment of acute insomnia and circadian rhythm sleep disorders, including jet lag. It is an ideal benzodiazepine for this use because of its fast onset of action and short half-life. It puts a person to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrazolam
Nitrazolam is a triazolobenzodiazepine (TBZD) , which are benzodiazepine (BZD) derivatives, that has been sold online as a designer drug. It is closely related to clonazolam or flunitrazolam, only differing by the removal of a chlorine or fluorine group respectively at the benzene ring. A study in mice indicated that nitrazolam can be several times more potent than diazepam as an antagonist of electroshock-induced tonic-extensor convulsions but less potent than diazepam at preventing the righting reflex. Nitrazolam has been used as an example compound to demonstrate the microscale synthesis of reference materials utilizing polymer‐supported reagents. Legal status United Kingdom In the UK, nitrazolam has been classified as a Class C drug by the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs. See also * Adinazolam * Alprazolam (licensed) * Flubromazolam * Nifoxipam * Nitemazepam * Pyrazolam * Triazolam ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Flunitrazolam
Flunitrazolam (FNTZ, Flunazolam) is a triazolobenzodiazepine (TBZD), which are benzodiazepine (BZD) derivatives, that has been sold online as a designer drug, and is a potent hypnotic and sedative drug similar to related compounds such as flunitrazepam, clonazolam and flubromazolam. It was first definitively identified and reported to the EMCDDA Early Warning System, by an analytical laboratory in Germany in October 2016, and had not been described in the scientific or patent literature before this. It is the triazole analogue of Flunitrazepam (Rohypnol). The addition of the triazole ring to the scaffold increases potency significantly, this is evident as flunitrazolam is reported anecdotally to be active in the microgram In the metric system, a microgram or microgramme is a unit of mass equal to one millionth () of a gram. The unit symbol is μg according to the International System of Units (SI); the recommended symbol in the United States and United Kingdom wh ... level. It ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Flubromazolam
Flubromazolam (JYI-73) is a triazolobenzodiazepine (TBZD), which are benzodiazepine (BZD) derivatives. Flubromazolam is reputed to be highly potent, and concerns have been raised that clonazolam and flubromazolam in particular may pose comparatively higher risks than other designer benzodiazepines, due to their ability to produce strong sedation and amnesia at oral doses of as little as 0.5 mg. Life-threatening adverse reactions have been observed at doses of only 3 mg of flubromazolam. Legal status Sweden Flubromazolam has been classified as an illegal substance in Sweden after seizures by customs and police, as well as indications from the EMCDDA of wider use as a recreational drug. Switzerland Flubromazolam is illegal in Switzerland as of December 2015. United Kingdom In the UK, flubromazolam has been classified as a Class C drug by the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs. Australia ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Estazolam
Estazolam, sold under the brand name Prosom among others, is a tranquilizer medication of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. Estazolam is an intermediate-acting oral benzodiazepine. It is used for short-term treatment of insomnia. It was patented in 1968 and came into medical use in 1975. Medical uses Estazolam is prescribed for the short-term treatment of certain sleep disorders. It is an effective hypnotic drug showing efficacy in increasing the time spent asleep as well as reducing awakenings during the night. Combination with non-pharmacological options for sleep management results in long-term improvements in sleep quality after discontinuation of short-term estazolam therapy. Estazolam is also sometimes used as a preoperative sleep aid. It was found to be superior to triazolam in side effect profile in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clonazolam
Clonazolam (also known as clonitrazolam) is a drug of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. Although little research has been done about its effects and metabolism, it is sold online as a designer drug. The synthesis of clonazolam was first reported in 1971 and the drug was described as the most active compound in the series tested. Depending on dose consumed, clonazolam may pose comparatively higher risk than other designer benzodiazepines due to its ability to produce strong sedation and amnesia at doses as small as 0.5 mg. Legality United Kingdom In the UK, clonazolam has been classified as a Class C drug by the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs. United States It is a Schedule I controlled substance in the United States and is not FDA approved for human consumption. Virginia state law has declared all of the following related me ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bromazolam
Bromazolam (XLI-268) is a triazolobenzodiazepine (TBZD) which was first synthesised in 1976, but was never marketed. It has subsequently been sold as a designer drug, first being definitively identified by the EMCDDA in Sweden in 2016. It is the bromo instead of chloro analogue of alprazolam and has similar sedative and anxiolytic effects to it and other benzodiazepines. Bromazolam is a non subtype selective agonist at the benzodiazepine site of GABAA receptors, with a binding affinity of 2.81 nM at the α1 subtype, 0.69 nM at α2 and 0.62 nM at α5. The "common" dosage range for users of bromazolam was reported to be 1–2 mg, suggesting its potency is similar to alprazolam. Adverse effects Because bromazolam is relatively new, epidemiological research regarding the individual's health effects as well as the effects on the public health are quite scarce. Most of the knowledge about the effects are known from case studies and individual reports. The typi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzodiazepine
Benzodiazepines (BZD, BDZ, BZs), colloquially known as "benzos", are a class of central nervous system (CNS) depressant, 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 Roche, Hoffmann–La Roche, which followed with the development of diazepam (Valium) three years later, 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, gamma-aminobutyric acid (GABA) at the GABAA receptor, GABAA receptor, resulting ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
