Pyrazolam
Pyrazolam is a research chemical depressant of the triazolobenzodiazepine class. Originally developed at Hoffmann-La Roche in the 1970s, it emerged on the research chemical market around 20121. Pyrazolam is distinguished from other benzodiazepines by its predominantly anxiolytic profile, producing comparatively less sedation and euphoria at common doses. It is structurally related to alprazolam and bromazepam and is notably reported to pass through the body unmetabolized1.
Contents
Dosage & Duration
Dosage
Duration
Subjective Effects
Effects vary widely by individual, dose, and context.
Physical
The physical effects of pyrazolam can be broken down into several components which progressively intensify proportional to dosage.
Cognitive
The general head space of pyrazolam is described by many as one of mild sedation and proportionlly intense anxiety suppression. It contains a large number of typical depressant cognitive effects.
Reagent Testing
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Pharmacology
Pharmacodynamics
Pyrazolam acts as a positive allosteric modulator at the GABAA receptor via the benzodiazepine binding site, enhancing the inhibitory signaling of GABA.12 It is most selective for the α2 and α3 subtypes of the GABAA receptor, which is consistent with its predominantly anxiolytic profile. The anticonvulsant properties observed with benzodiazepines as a class may be partly attributable to interaction with voltage-dependent sodium channels rather than the benzodiazepine site itself.3
Pharmacokinetics
Pyrazolam does not appear to undergo metabolism and is instead excreted unchanged in the urine. As a result, it does not interact with liver enzymes, which may make it comparatively safer for individuals with reduced hepatic function.
Dangerous
Highest riskThese combinations are considered extremely harmful and should always be avoided. Reactions to these drugs taken in combination are highly unpredictable and have a potential to cause death.
Unsafe
AvoidThere is considerable risk of physical harm when taking these combinations, they should be avoided where possible.
Caution
Use cautionThese combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.
Tolerance
Benzodiazepines
Harm Potential
Addiction & Dependence
Psychological
HighPyrazolam is described as extremely psychologically addictive, with compulsive redosing commonly reported as a cognitive effect. However, its comparatively limited sedative and euphoric effects relative to other benzodiazepines may somewhat reduce recreational appeal and abuse potential.
Physical
Extremely HighPhysical dependence develops with regular use. Withdrawal following a few weeks or longer of steady dosing can be potentially life-threatening, with symptoms including hypertension and seizures4; abrupt discontinuation after extended use may result in death. Gradual tapering over weeks is strongly recommended.4
Seizure Risk
While benzodiazepines have anticonvulsant properties during use4, abrupt discontinuation after regular use can cause potentially fatal seizures.45 Paradoxical seizure reactions during use are rare in the general population, with an incidence rate below 1%, occurring more frequently in epileptics and high-dosage regimes.
History & Culture
Pyrazolam was originally developed during the 1970s by a research team led by Leo Sternbach at Hoffman-La Roche6, the pharmaceutical company responsible for discovering many clinically significant benzodiazepines. Despite its initial synthesis during this prolific…
Trip Reports
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Legality
By Country
References
Source Pages
Citations
- Bjoern Moosmann, Melanie Hutter, Laura M. Huppertz, Sascha Ferlaino, Lisa Redlingshöfer, & Volker Auwärter. (2013). Characterization of the designer benzodiazepine pyrazolam and its detectability in human serum and urine. Forensic Toxicology, 31, 263–271. https://doi.org/10.1007/s11419-013-0187-4123456
- Alshaimaa A. Elgarf, David C. B. Siebert, Felix Steudle, & et al.. (2018). Different Benzodiazepines Bind with Distinct Binding Modes to GABAA Receptors. ACS Chemical Biology, 13(8), 2033–2039. https://doi.org/10.1021/acschembio.8b001441
- M. J. McLean, & R. L. Macdonald. (1988). Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. Journal of Pharmacology and Experimental Therapeutics, 244(2), 789–795. https://pubmed.ncbi.nlm.nih.gov/2450203/123
- Angela C. Regina, Srinivasa B. Gokarakonda, & Fibi N. Attia. (2024). Withdrawal Syndromes. StatPearls Publishing. https://www.ncbi.nlm.nih.gov/books/NBK459239/1
- (n.d.). Preparation of triazolo benzodiazepines and novel compounds. https://patents.google.com/patent/US3954728A/en1
- (June 2015). Designer benzodiazepines: A new challenge. World Psychiatry, 14(2), 248. https://doi.org/10.1002/wps.202361
- (n.d.). Verordnung zur Änderung der Anlage des Neue-psychoaktive-Stoffe-Gesetzes und von Anlagen des Betäubungsmittelgesetzes, BGBl. I 2019 S. 1083. https://www.buzer.de/gesetz/13500/index.htm1
- (n.d.). The Misuse of Drugs Act 1971 (Amendment) Order 2017 (S.I. 2017/634). https://www.legislation.gov.uk/uksi/2017/634/article/5/made1
Further Reading
Automated synthesisInformation aggregated and synthesized using an autonomous workflow built by Josie Kins.
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