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Diazepam , first marketed as Valium, is a medicine of the benzodiazepine family that typically produces a calming effect. It is commonly used to treat a range of conditions, including anxiety, seizures, alcohol withdrawal syndrome, benzodiazepine withdrawal syndrome, muscle spasms, trouble sleeping, and restless legs syndrome. It may also be used to cause memory loss during certain medical procedures. It can be taken by mouth, inserted into the rectum, injected into muscle, injected into a vein or used as a nasal spray. When given into a vein, effects begin in one to five minutes and last up to an hour. By mouth, effects begin after 15 to 60 minutes.
Common side effects include sleepiness and trouble with coordination. Serious side effects are rare.They include suicide, decreased breathing, and an increased risk of seizures if used too frequently in those with epilepsy. Occasionally, excitement or agitation may occur. Long term use can result in tolerance, dependence, and withdrawal symptoms on dose reduction. Abrupt stopping after long-term use can be potentially dangerous. After stopping, cognitive problems may persist for six months or longer. It is not recommended during pregnancy or breastfeeding. Its mechanism of action is by increasing the effect of the neurotransmitter gamma-aminobutyric acid (GABA).
Diazepam was patented in 1959 by Hoffmann-La Roche. It has been one of the most frequently prescribed medications in the world since its launch in 1963. In the United States it was the highest selling medication between 1968 and 1982, selling more than two billion tablets in 1978 alone. In 2017, it was the 135th most commonly prescribed medication in the United States, with more than five million prescriptions. In 1985 the patent ended, and there are more than 500 brands available on the market. It is on the World Health Organization’s List of Essential Medicines
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Diazepam is a benzodiazepine derivative with anti-anxiety, sedative, hypnotic and anticonvulsant properties. Diazepam potentiates the inhibitory activities of gamma-aminobutyric acid (GABA) by binding to the GABA receptor, located in the limbic system and the hypothalamus. This increases the frequency of chloride channel opening, allowing the flow of chloride ions into the neuron and ultimately leading to membrane hyperpolarization and a decrease in neuronal excitability.
NCI Thesaurus (NCIt)
Diazepam, also known as valium or diastat, belongs to the class of organic compounds known as 1, 4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1, 4-azepine. Diazepam is a drug which is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. Diazepam exists as a solid and is considered to be practically insoluble (in water) and relatively neutral. Diazepam has been detected in multiple biofluids, such as urine and blood. Within the cell, diazepam is primarily located in the cytoplasm and membrane (predicted from logP). Diazepam can be converted into fludiazepam. Outside of the human body, diazepam can be found in common wheat and potato. This makes diazepam a potential biomarker for the consumption of these food products. Diazepam is a potentially toxic compound.