Pyrazolam

There is a high incidence of death due to respiratory depression when benzodiazepines are combined with depressants such as opiates, alcohol or other GABAergic substances.

Pyrazolam
The skeletal formula of Pyrazolam.
Chemical Nomenclature
Common names	Pyrazolam
Systematic name	8-bromo-1-methyl-6-(pyridin-2-yl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
Class Membership
Psychoactive class	Depressant
Chemical class	Benzodiazepine
Routes of Administration
Oral Dosage WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. Threshold 0.25 mg Light 0.25 - 0.75 mg Common 1 - 3 mg Strong 3 - 6 mg Heavy 7 mg+ Duration Total 2 - 6 hours Onset 15 - 90 minutes Peak 1 - 2 hours Offset 2 - 6 hours Afterglow 2 - 4 hours

Summary sheet: Pyrazolam

Pyrazolam is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s and subsequently "rediscovered" and sold as a research chemical starting in 2012. It is mainly an anxiolytic, but has also shown muscle relaxant and hypnotic effects at high doses.

Chemistry

Pyrazolam is a drug of the benzodiazepine class. Benzodiazepine drugs contain a benzene ring fused to a diazepine ring, which is a seven membered ring with the two nitrogen constituents located at R₁ and R₄. Bromine is bound to this bicyclic structure at R₇. Additionally, at R₆ the bicylic core is substitued with a 2-pyridine ring. Pyrazolam also contains a 1-methylated triazole ring fused to and incorporating R₁ and R₂ of its diazepine ring. Pyrazolam belongs to a class of benzodiazepines containing this fused triazole ring, called triazolobenzodiazepines, distinguished by the suffix "-zolam".

Pharmacology

Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors. As this site is the most prolific inhibitory receptor within the brain, its modulation results in the sedating (or calming effects) of pyrazolam on the nervous system.

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. No metabolites have been found in the urine of volunteers. It 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. It is excreted by the body unchanged thus not interacting with liver enzymes like other benzodiazepines, 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 several components which progressively intensify proportional to dosage.

These are described below and generally include:

• Sedation - In terms of energy level alterations, pyrazolam is considerably less sedating than other substances of the same class unless it is taken at heavy doses.
• Dizziness
• Motor control loss
• Muscle relaxation
• Respiratory depression

Cognitive effects

The cognitive effects of pyrazolam can be broken down into several components which progressively intensify proportional to dosage. 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.

The most prominent of these cognitive effects generally include:

• Amnesia
• Anxiety suppression
• Thought deceleration
• Disinhibition
• Information processing suppression
• Compulsive redosing
• Delusions of sobriety - This is the false belief that one is perfectly sober despite obvious evidence to the contrary such as severe cognitive impairment and an inability to fully communicate with others.

Paradoxical effects

Paradoxical reactions to benzodiazepines such as increased seizures (in epileptics), aggression, increased anxiety, violent behavior, loss of impulse control, irritability and suicidal behavior sometimes occur (although they are rare in the general population, with an incidence rate below 1%).

These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.

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.

Benzodiazepine 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 pyrazolam. Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

• Depressants (1,4-Butanediol, 2-methyl-2-butanol, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances also potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - It is dangerous to combine benzodiazepines with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of benzodiazepines, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of benzodiazepines will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only dosing a certain amount of benzodiazepines per hour. This combination can also potentially result in severe dehydration if hydration is not monitored.

Legal issues

Pyrazolam 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 people may still be charged for its possession under certain circumstances such as under analogue laws and with intent to sell or consume.

Preparation methods

Preparation methods for this compound within our preparation index include:

• Volumetric liquid dosing

See also

• Responsible use
• Pyrazolam (Wikipedia)
• Entactogens
• Alcohol
• Benzodiazepines
• Depressants
• Volumetric liquid dosing