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WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.
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Nitrazepam was first synthesized in 1965 by the pharmaceutical company Hoffmann-La Roche. It is used for the short-term treatment of severe insomnia in some countries. Its potency by weight is approximately similar to diazepam.
Users should note that the sudden discontinuation of benzodiazepines can be potentially dangerous or life-threatening for individuals using regularly for extended periods of time, sometimes resulting in seizures or death.[3] It is highly recommended to taper one's dose by gradually lowering the amount taken each day for a prolonged period of time instead of stopping abruptly.[4]
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Nitrazepam was developed by Hoffmann-La Roche and entered the commercial market in the mid-1960s under the name Mogadon. It has since been marketed under various brand names around the world.
While less infamous than some of its counterparts, misuse and recreational use of nitrazepam has been reported. It has been implicated in several cases of drug-facilitated crimes, including sexual assaults and robberies. The compound can also be lethal when combined with other depressants, such as alcohol or opioids.
Chemistry
Nitrazepam belongs to the class of nitro-benzodiazepines. Benzodiazepines share a common chemical structure, and they generally consist of a benzene ring fused to a seven-membered diazepine ring.
In the structure of nitrazepam, the benzodiazepine ring is substituted at R7 with a nitro (NO2) group. At the R5 position, it has a phenyl ring. The benzodiazepine ring is also bonded at R1 to a carboxamide group (C=O)NH2). [5]
Nitrazepam differs from certain other benzodiazepines like diazepam due to the presence of the nitro group instead of a carbonyl group at the 7th position in the diazepine ring. The presence of the nitro group in the chemical structure of nitrazepam is thought to be partly responsible for its hypnotic effect.
Pharmacology
Benzodiazepines like nitrazepam produce their effects by binding to the benzodiazepine receptor site and enhancing the efficiency and effects of the neurotransmitter gamma-aminobutyric acid (GABA) by acting on its receptors. As this site is the most abundant inhibitory receptor set within the brain, its modulation results in the sedating effects of nitrazepam on the nervous system.[5]
The muscle-relaxing properties of nitrazepam are believed to result from its influence on supraspinal motor centers in the brain.
Nitrazepam is also known to cause anterograde amnesia in sufficient doses, which means individuals are unable to remember certain events they experienced while under the influence of the drug
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.
Alcohol:[5] The concomitant use of Nitrazepam with alcohol can potentiate sleepiness and slow your breathing, potentially leading to life-threatening side-effects. This combination should be avoided.
Opioids:[5] The combination of Nitrazepam with opioids can cause serious side effects including respiratory distress, coma, and death. These effects are more likely when these drugs are used in high doses or in combination with other substances that cause drowsiness.
Antidepressants:[5] Combining Nitrazepam with certain antidepressants can cause excessive sedation, confusion, and coordination problems. This is more common in elderly, ill, or debilitated individuals.
Antipsychotics:[5] Combining Nitrazepam with antipsychotic medications can cause excessive sedation, confusion, and coordination problems.
Barbiturates:[5] Co-use of Nitrazepam and barbiturates can result in increased sedation, severe respiratory depression, coma, and even death.
Other Benzodiazepines:[5] Co-use of Nitrazepam and other benzodiazepines can lead to excessive sedation, respiratory depression, and death.
Subjective effects
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 PsychonautWikicontributors. 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 ☠.
Physical effects
Sedation - Nitrazepam can induce significant sedation, leading to an overwhelmingly lethargic state. Higher doses may cause users to feel as though they have been deprived of sleep for an extended period, potentially resulting in a forced state of unconsciousness.
Perception of bodily heaviness - Nitrazepam can cause a sensation of heaviness in the body, which may lead to difficulty moving or complete lethargy at high doses.
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 (though 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.
Cognitive effects
The cognitive effects of Nitrazepam can be broken down into several components which progressively intensify proportional to dosage. It contains a large number of typical depressant cognitive effects.
The most prominent of these cognitive effects generally include:
Amnesia - Nitrazepam can induce a significant level of amnesia.
Emotion suppression - While this compound primarily suppresses anxiety, it also has the ability to dampen other emotions in a manner that is distinct, though less intensive, than that of antipsychotics.
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. It most commonly occurs at heavy dosages.
Confusion - At heavy doses, nitrazepam can induce confusion. This effect is due to the drug's ability to suppress basic cognitive functions such as comprehension, memory, and reasoning skills.
Motivation suppression - Due to nitrazepam's pronounced sedative effect and the resultant lethargy, activities that require physical movement or high amounts of effort may become challenging while under the influence of this compound, especially at higher doses.
Language suppression - Nitrazepam can induce slurred speech and difficulty in articulating words clearly or coherently.
Dream potentiation - Although many report that benzodiazepines like nitrazepam result in states of dreamless sleep, the opposite effect has also been noted, particularly during withdrawal from GABAergic substances (with alcohol being a notable example). The cause for these differences remains unclear at this point in time.
After effects
Rebound anxiety - Rebound anxiety is a commonly observed effect with anxiety relieving substances like benzodiazepines. It typically corresponds to the total duration spent under the substance's influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction.
Residual sleepiness - While benzodiazepines can be used as an effective sleep-inducing aid, their effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours.
↑Mandrioli, R., Mercolini, L., Raggi, M. A. (October 2008). "Benzodiazepine metabolism: an analytical perspective". Current Drug Metabolism. 9 (8): 827–844. doi:10.2174/138920008786049258. ISSN1389-2002.
↑Lann, M. A., Molina, D. K. (June 2009). "A fatal case of benzodiazepine withdrawal". The American Journal of Forensic Medicine and Pathology. 30 (2): 177–179. doi:10.1097/PAF.0b013e3181875aa0. ISSN1533-404X.
