
Pyrazolam
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Pyrazolam | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Chemical Nomenclature | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Common names | Xanax, Alprazolam, Ksalol | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Substitutive name | Alprazolam | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Systematic name | 8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Class Membership | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Psychoactive class | Depressant | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Chemical class | Benzodiazepine | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Routes of Administration | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Interactions | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Pyrazolam is a benzodiazepine derivative originally developed by a team lead by Leo Sternbach at Hoffman-La Roche in the 1970s,[1] and subsequently "rediscovered" and sold as a research chemical starting in 2012.[2] It is mainly an anxiolytic, but it has also shown muscle relaxant and hypnotic effects at high doses.
Chemistry
stuff and things
Pharmacology
Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site on the GABAA receptor and modulating the function of the GABA receptor, the most prolific inhibitory receptor within the brain. The GABA chemical and receptor system mediates inhibitory (or calming effects) of alprazolam on the nervous system.
Pyrazolam has structural similarities to alprazolam[3] and bromazepam. Unlike other benzodiazepines pyrazolam does not appear to undergo metabolism, instead being excreted unchanged in the urine, no metabolites have been found in the urine of volunteers [4][5] and has anxiolytic activity 12x stronger than diazepam while causing little ataxia and sedation when used in its anxiolytic dose range. It is most selective for the α2 and α3 receptor subtypes.[6] It is excreted by the body unchanged thus not interacting with liver enzymes like other benzodiazepines[7] meaning that its use in people with reduced liver function may be safer.
Subjective effects
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely if ever occur all at once but heavier dosages will increase the chances and are more likely to induce a full range of effects.
Physical Effects
The physical effects of Pyrazolam can be broken down into 3 components all of which progressively intensify proportional to dosage. These are described below and generally include:
- Sedation - In terms of energy level alterations, Pyrazolam is considerably less edating than other substances of the same class unless it is taken at heavy dosages.
- Dizziness
- Motor control loss
Cognitive Effects
The cognitive effects of Pyrazolam can be broken down into 5 components all of which progressively intensify proportional to dosage. The general head space of Pyrazolam is described by many as one of intense sedation and decreased inhibition. It contains a large number of typical depressant cognitive effects.
The most prominent of these cognitive effects generally include:
- Amnesia
- Anxiety suppression
- Thought deceleration
- Disinhibition
- Information processing suppression
- Compulsive redosing
Toxicity and Harm Potential
Lethal Dosage
The lethal dosage of Pyrazolam has not been established, however like many benzodiazepines it has a large therapeutic index and margin of safety. Complications may arise when administered in excess. Intentional overdoses have been reported.
As with all GABAergic drugs, overdose can be lethal when mixed with other depressants including alcohol or opioids.
Tolerance and Addiction Potential
Tolerance will develop to the sedative-hypnotic effects within a couple of days of repeated administration. Abrupt discontinuation of Pyrazolam, following regular dosing over several days, can result in a withdrawal phase which includes rebound symptoms such as increased anxiety and insomnia. It is possible to gradually reduce the dose over the course of several days, which will lengthen the duration of the withdrawal period, but reduce the perceived intensity.
Thienodiazepine discontinuation is notoriously difficult; it is potentially life threatening for individuals using regularly to discontinue use without tapering their dose over a period of weeks. There is an increased risk of seizure following discontinuation of Deschloroetizolam. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.
Legal Issues
Deschloroetizolam is currently a grey area compound within all parts of the world. This means that it is not known to be specifically illegal within any country but that people may still be charged for its possession under certain circumstances such as under analogue laws and with intent to sell or consume.
See Also
- Specific Substances
- Entactogens
- Alcohol
- Benzodiazepines
- Depressants
- Preparation:Benzodiazepine solution
References
- ↑ 1.0 1.1 Reissig, C. J., Harrison, J. A., Carter, L. P., Griffiths, R. R. (2015). "Inhaled vs. oral alprazolam: subjective, behavioral and cognitive effects, and modestly increased abuse potential". Psychopharmacology. doi:10.1007/s00213-014-3721-0.