Talk:Phenazepam

Phenazepam 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. The benzyl ring of phenazepam is substituted at R7 with a bromine group. Like most benzodiazepines, phenazepam has a phenyl ring in R₅ which is substituted by chlorine in the R_2' group. Phenazepam also contains an oxygen group double bonded to R2 of its diazepine ring to form a ketone. This oxygen substitution at R₂ is shared with other benzodiazepine drugs with the suffix -azepam.

Like other benzodiazepines, phenazepam (7-bromo-5-(2-chlorophenyl)-1,3-dihydro-1,4-benzodiazepin-2-one) is composed of a benzene ring fused to a seven-membered 1,4-diazepine ring. A 2-chlorophenyl ring is attached at the 5-position and a bromine is attached at the 7-position. Phenazepam has a molecular formula of C15H10BrClN2O and a molecular weight of 349.6 g/mol.^[4]

While the toxicity of phenazepam is relatively low in relation to dosage, it still carries the addiction, overdose, and withdrawal risks associated with benzodiazepines. Additionally, the drug is potent at one-tenth of the normal dose of diazepam. Higher doses of phenazepam are sometimes prescribed for severe anxiety or epileptic seizures.^[5]

Phenazepam is an agonist of the gamma-aminobutyric acid-A (GABAA) receptor and produces CNS depression. In plus-maze and conflict tests in male rats, very low doses of phenazepam showed an anxiolytic effect. Phenazepam in conventional doses acts as a potent tranquilizer. Phenazepam has been shown to fully substitute for pentobarbital in adult rats trained to discriminate pentobarbital vs saline. In the antagonism tests, the discriminative effects of phenazepam were fully antagonized by the selective benzodiazepine antagonist flumazenil. Phenazepam has a half-life of up to 60 hours and onset of effects is approximately 2-3 hours following oral administration; due to this, there is a potential for users to re-dose prior to the observation of its effects. 3-Hydroxyphenazepam, a metabolite of phenazepam, is also a GABAA receptor agonist. This pharmacokinetic data suggests that phenazepam would have a high overdose potential.^[6]

Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

• Erowid Experience Vaults: Phenazepam

Phenazepam likely has a low toxicity relative to dose.^[15] However, it is potentially lethal when mixed with depressants like alcohol or opioids.

It is strongly recommended that one use harm reduction practices, such as volumetric dosing, when using this substance to ensure the administration of the intended dose.

Tolerance and addiction potential

Benzodiazepines are known to be extremely physically and psychologically addictive.^{[citation needed]}

Tolerance will develop to the sedative-hypnotic effects within a couple of days of continuous use.^[16] After cessation, the tolerance returns to baseline in 7-14 days. Withdrawal symptoms or rebound symptoms may occur after ceasing one's usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction.^[17][18]

Overdose

Benzodiazepine overdose may occur with extremely high doses or, more commonly, when it is taken with other depressants. This risk is especially present with other GABAergic depressants, such as barbiturates and alcohol, since they work in a similar fashion but bind to distinct sites on the GABA_A receptor, resulting in significant cross-potentiation.^{[citation needed]}

Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly. Symptoms may include severe slurred speech, confusion, delusions, respiratory depression, and non-responsiveness. The user might seem like they are sleepwalking. The user is also more susceptible to consume more of the same or another substance due to their impaired judgement, which is typically not seen with other substances during overdose.

Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Care is primarily supportive in nature, although overdoses are sometimes treated with flumazenil, a GABA_A antagonist^[19] or additional procedures such as adrenaline injections if other substances are involved.^{[citation needed]}

Discontinuation and withdrawal

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 high blood pressure, seizures, and death.^[20] Substances which lower the seizure threshold such as tramadol should be avoided during withdrawal.^{[citation needed]} Abrupt discontinuation also causes rebound stimulation which presents as anxiety, insomnia and restlessness.^{[citation needed]}

If one wishes to discontinue after a period of regular use, it is safest to reduce the dose each day by a very small amount for a couple of weeks until close to abstinence. If using a short half-life benzodiazepine such as alprazolam or etizolam, a longer acting variety such as diazepam or clonazepam can be substituted. Symptoms may still be present, but their severity will be reduced significantly.

For more information on tapering from benzodiazepines in a controlled manner, please see this guide. Small quantities of alcohol can also help to reduce the symptoms, but otherwise cannot be used as an effective tapering agent.

The duration and severity of withdrawal symptoms depend on a number of factors including the half-life of the substance used, tolerance and the duration of abuse. Major symptoms will usually start within just a few days after discontinuation and persist for around a week for shorter lasting benzodiazepines. Benzodiazepines with longer half-lives will exhibit withdrawal symptoms with a slow onset and extended duration.^{[citation needed]}

Dangerous interactions

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.

• Depressants (1,4-Butanediol, 2M2B, alcohol, benzodiazepines, barbiturates, GHB/GBL, methaqualone, opioids) - This combination potentiates the muscle relaxation, amnesia, sedation, and respiratory depression caused by one another. At higher doses, it can lead to a sudden, unexpected loss of consciousness along with a dangerous amount of depressed respiration. There is also an increased risk of suffocating on one's vomit while unconscious. If nausea or vomiting occurs before a loss of consciousness, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can unpredictably potentiate the amnesia, sedation, motor control loss and delusions that can be caused by each other. It may also result in a sudden loss of consciousness accompanied by a dangerous degree of respiratory depression. If nausea or vomiting occurs before consciousness is lost, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states. This combination can also potentially result in severe dehydration if one's fluid intake is not closely monitored. If choosing to combine these substances, one should strictly limit themselves to a pre-set schedule of dosing only a certain amount per hour until a maximum threshold has been reached.

• Russia: Phenazepam is only available through a prescription, and since 22.03.2021 is listed in the Section II of the nomenclature of potent and toxic substances that are not precursors to narcotic drugs and psychotropic substances, making it a controlled substance.^[21]

• Responsible use
• Volumetric dosing
• Benzodiazepines

• Phenazepam (Wikipedia)
• Phenazepam (Isomer Design)