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Pyrazolam
Pyrazolam (SH-I-04) is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s. It has since been "rediscovered" and sold as a designer drug since 2012. Pyrazolam has structural similarities to alprazolam and bromazepam. Unlike other benzodiazepines, pyrazolam does not appear to undergo metabolism, instead being excreted unchanged in the urine. It is most selective for the α2 and α3 subtypes of the GABAA receptor, GABAA receptor. Legal Status United Kingdom In the UK, pyrazolam has been classified as a Drugs controlled by the UK Misuse of Drugs Act, Class C drug by section 5 of the May 2017 amendment to Misuse of Drugs Act 1971, The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs. See also * List of benzodiazepine designer drugs References {{GABAAR PAMs Triazolobenzodiazepines GABAA receptor positive allosteric modulators Designer drugs 2-Pyridyl compo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Benzodiazepine Designer Drugs
The below tables contain a sample list of benzodiazepines and benzodiazepine analogs that are commonly prescribed, with their basic pharmacological characteristics, such as half-life and equivalent doses to other benzodiazepines, also listed, along with their trade names and primary uses. The elimination half-life is how long it takes for half of the drug to be eliminated by the body. "Time to peak" refers to when maximum levels of the drug in the blood occur after a given dose. Benzodiazepines generally share the same pharmacological properties, such as anxiolytic, sedative, hypnotic, skeletal muscle relaxant, amnesic, and anticonvulsant effects. Variation in potency of certain effects may exist amongst individual benzodiazepines. Some benzodiazepines produce active metabolites. Active metabolites are produced when a person's body metabolizes the drug into compounds that share a similar pharmacological profile to the parent compound and thus are relevant when calculating how long ... [...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] |
GABAA Receptor
The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor on the postsynaptic cell is selectively permeable to chloride ions (Cl−) and, to a lesser extent, bicarbonate ions (HCO3−). Depending on the membrane potential and the ionic concentration difference, this can result in ionic fluxes across the pore. If the membrane potential is higher than the equilibrium potential (also known as the reversal potential) for chloride ions, when the receptor is activated Cl− will flow into the cell. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring at the postsynaptic cell. The reversal potential of the GABAA-mediated inhibitory postsynaptic potential (IPSP) in normal solution is −70 mV, contrasting the GABAB IPSP (-100 mV). T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor Positive Allosteric Modulators
In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open its chloride channel to allow chloride ions into the neuron, making the cell hyperpolarized and less likely to fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid (GABA) neurotransmitter molecule: they affect the receptor by binding at a different site on the protein. This is called allosteric modulation. In psychopharmacology, GABAA receptor PAMs used as drugs have mainly sedative and anxiolytic effects. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Triazolobenzodiazepines
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 fused triazole ring. 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 properties ... * 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, Chidester CG (1971): "A synthetic approach to new 1,4-benzodiazepine derivatives." Tetr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Misuse Of Drugs Act 1971
The Misuse of Drugs Act 1971 is an Act of the Parliament of the United Kingdom. It represents action in line with treaty commitments under the Single Convention on Narcotic Drugs, the Convention on Psychotropic Substances, and the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances. Offences under the Act include: * Possession of a controlled drug unlawfully * Possession of a controlled drug with intent to supply it * Supplying or offering to supply a controlled drug (even where no charge is made for the drug) * Allowing premises you occupy or manage to be used unlawfully for the purpose of producing or supplying controlled drugs It is often presented as little more than a list of prohibited drugs and of penalties linked to their possession and supply. In practice, however, the act establishes the Home Secretary as a key player in a drug licensing system. Therefore, for example, various opiates are available legally as prescription-o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drugs Controlled By The UK Misuse Of Drugs Act
These drugs are known in the UK as ''controlled drugs'', because this is the term by which the act itself refers to them. In more general terms, however, many of these drugs are also controlled by the Medicines Act 1968, there are many other drugs which are controlled by the Medicines Act but not by the Misuse of Drugs Act 1971, Misuse of Drugs Act, and some other drugs (alcohol (drug), alcohol, for example) are controlled by other laws. The Misuse of Drugs Act sets out three separate categories, Class A, Class B, and Class C. Class A drugs represent those deemed most dangerous, and so carry the harshest punishments. Class C represents those thought to have the least capacity for harm, and so the Act demands more lenient punishment. In reality the potential harm has little bearing on the class, which has led to dissatisfaction with drug laws. Being found drug possession, in possession of a drug on this list is dealt with less seriously than would be if it were deemed that there ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bromazepam
Bromazepam, sold under many brand names, is a benzodiazepine. It is mainly an anti-anxiety agent with similar side effects to diazepam (Valium). In addition to being used to treat anxiety or panic states, bromazepam may be used as a premedicant prior to minor surgery. Bromazepam typically comes in doses of 3 mg and 6 mg tablets. It was patented in 1961 by Roche and approved for medical use in 1974. Medical uses Treatment of severe anxiety. Despite certain side effects and the emergence of alternative products (e.g. pregabalin), benzodiazepine medication remains an effective way of reducing problematic symptoms, and is typically deemed effective by patients and medical professionals. Similarly to other intermediate-acting depressants, it may be used as hypnotic medication or in order to mitigate withdrawal effects of alcohol consumption. Pharmacology Bromazepam is a "classical" benzodiazepine; other classical benzodiazepines include: diazepam, clonazepam, oxazepam, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sublingual Administration
Sublingual (abbreviated SL), from the Latin for "under the tongue", refers to the pharmacological route of administration by which substances diffuse into the blood through tissues under the tongue. The sublingual glands receive their primary blood supply from the sublingual and submental arteries, which are branches of the lingual artery and facial artery, respectively. These arteries are both branches of the external carotid artery. The sublingual vein drains into the lingual vein, which then flows into the internal jugular system. The sublingual glands receive their parasympathetic input via the chorda tympani nerve, which is a branch of the facial nerve via the submandibular ganglion. The nerve functions in a secretomotor capacity. The chorda tympani branches from the motor branch of the facial nerve in the middle ear cavity, which then exits the middle ear through the petrotympanic fissure. The chorda tympani then travels with the lingual nerve to synapse at the submand ... [...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 medium duration in the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It is most commonly used in management of anxiety disorders, specifically panic disorder or 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 by mouth. Common side effects include sleepiness, depression, headaches, feeling tired, dry mouth, and memory problems. Some of the sedation and tiredness may improve within a few days. Withdrawal or rebound symptoms may occur if use is suddenly decreased; gradually decreasing the dose over weeks or months may be required. Alprazolam increases all-cause mortality. Alprazolam, like other benzodiazepines, acts through the GABAA receptor. Alprazolam was inve ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drug
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
