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The cognitive effects of flunitrazepam can be broken down into several components which progressively intensify proportional to dosage. The general head space of flunitrazepam is described by many as one of intense sedation, relaxation, anxiety suppression and decreased inhibition similar to [[Temazepam]] and [[Diazepam]]. It contains a large number of typical [[Psychoactive class::depressant]] cognitive effects.
The cognitive effects of flunitrazepam can be broken down into several components which progressively intensify proportional to dosage. The general head space of flunitrazepam is described by many as one of intense sedation, relaxation, anxiety suppression and decreased inhibition similar to [[Diazepam]] and [[Temazepam]]. It contains a large number of typical [[Psychoactive class::depressant]] cognitive effects.
The most prominent of these cognitive effects generally include:
The most prominent of these cognitive effects generally include:
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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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Flunitrazepam (trade name Rohypnol) was first synthesized in 1972 by Hoffmann-La Roche and is an intermediate-acting hypnotic of the benzodiazepine chemical class. It possesses anxiolytic, anticonvulsant, sedative, hypnotic, depressant and amnestic properties.[3] It is used for the short term treatment of insomnia and as a preoperative sedative in some countries, these were also the indications in which it was originally studied. Flunitrazepam is approximately 10 times more potent by weight than Diazepam.
It's worth noting 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.[4] 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.[5]
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Flunitrazepam was discovered at Roche as part of the benzodiazepine work led by Leo Sternbach and it was first marketed in 1974. It first entered the commerical market in Europe in 1975 as Rohypnol and In the 1980's it began to be available in other countries. [6]
In 1998, due to the abuse of the drug for date rape and recreation, Roche modified their 1mg tablets to make them less soluble, and add a blue dye for easier detection in drinks. [7]
Chemistry
Flunitrazepam 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.
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.[8] As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of Flunitrazepam on the nervous system.
The anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.[9]
Flunitrazepam is known to induce anterograde amnesia in sufficient doses (individuals are unable to remember certain events that they experienced while under the influence of the drug). This effect could be particularly dangerous, if flunitrazepam is used to aid in the commission of sexual assault, because victims may be unable to clearly recall the assault, the assailant, or the events surrounding the assault. [10]
80% of the flunitrazepam that is taken orally is absorbed but the bioavailability in suppository form is closer to 50%. [11]
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 - In terms of energy level alterations, flunitrazepam has the potential to be extremely sedating and often results in an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit down and generally feel as if they are constantly on the verge of passing out instead of engaging in physical activities. This sense of sleep deprivation increases proportional to dosage and eventually becomes powerful enough to force a person into complete unconsciousness.
Perception of bodily heaviness - Flunitrazepam is known to cause feelings of heaviness in the body. This effect can range from motor impairment and difficulty moving at lower doses to complete lethargy or inability to stand up or move 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 (although they are rare in the general population, with an incidence rate below 1%).[12][13]
These paradoxical effects occur with greater frequency in recreational abusers, individuals with mental disorders, children, and patients on high-dosage regimes.[14][15]
Cognitive effects
The cognitive effects of flunitrazepam can be broken down into several components which progressively intensify proportional to dosage. The general head space of flunitrazepam is described by many as one of intense sedation, relaxation, anxiety suppression and decreased inhibition similar to Diazepam and Temazepam. It contains a large number of typical depressant cognitive effects.
The most prominent of these cognitive effects generally include:
Emotion suppression - Although this compound primarily suppresses anxiety, it also dulls other emotions in a manner which is distinct but 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, flunitrazepam can cause confusion. This effect is a result of the drug suppressing basic cognitive functions at heavy doses, such as comprehension, memory, and reasoning skills.
Motivation suppression - Due to flunitrazepam's heavy sedation and lethargy, doing any type of activity that requires moving, or high amounts of effort may be difficult to do on this compound, especially at higher doses.
Language suppression - Flunitrazepam is known to cause slurred speech and difficulty communicating words in a clear fashion.
Dream potentiation - While most people report that benzodiazepines like flunitrazepam tend to result in states of dreamless sleep, the opposite effect has also been reported, and seems to be particularly prevalent when a user is experiencing withdrawal from GABAergic substances (with alcohol being one notable example). The cause for these differences remain 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.
Flunitrazepam likely has a low toxicity relative to dose.[17] However, it is [[Toxicity::potentially lethal when mixed with depressants like alcohol or opioids]].
The oral LD50 (lethal dose in 50% of the population) of flunitrazepam is 1200 mg/kg in mice and 415 mg/kg in rats.
[18]
Tolerance and addiction potential
Flunitrazepam is extremely physically and psychologically addictive.
Tolerance will develop to the sedative-hypnotic effects within a couple of days of continuous use. After cessation, the tolerance returns to baseline in 7 - 14 days. However, in certain cases, this may take significantly longer in a manner which is proportional to the duration and intensity of one's long-term usage.
Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing and may necessitate a gradual dose reduction. For more information on tapering from benzodiazepines in a controlled manner, please see this guide.
Benzodiazepine discontinuation is notoriously difficult; it is potentially life-threatening for individuals regularly using to discontinue use without tapering their dose over a period of weeks. There is an increased risk of hypertension, seizures, and death.[19] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.
Flunitrazepam presents cross-tolerance with [[Cross-tolerance::all benzodiazepines]], meaning that after its consumption, all benzodiazepines will have a reduced effect.
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 small 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.
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.
Overdose
Benzodiazepine overdose may occur when a benzodiazepine is taken in large quantities or concurrently with other depressants. This is particularly dangerous with other GABAergic depressants such as barbiturates and alcohol since they work similarly, but bind to distinct allosteric sites on the GABAA receptor. Thus their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABAA receptor while barbiturates increase the duration in which they are open, meaning when both are consumed, the ion pore will open more frequently and stay open longer[20]. Benzodiazepine overdose is a medical emergency that may lead to a coma, permanent brain injury or death if not treated promptly and appropriately.
Symptoms of a benzodiazepine overdose may include severe thought deceleration, slurred speech, confusion, delusions, respiratory depression, coma or death. Benzodiazepine overdoses may be treated effectively in a hospital environment, with generally favorable outcomes. Benzodiazepine overdoses are sometimes treated with flumazenil, a GABAA antagonist[21]. However, care is primarily supportive in nature.
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International: Flunitrazepam is a Schedule III drug under the international Convention on Psychotropic Substances of 1971. [citation needed]
Canada: Flunitrazepam is a Schedule I controlled substance and is available by prescription only. [citation needed]
Germany: Since November 2011, flunitrazepam is controlled under Anlage 3 of the BtMG and requires a special prescription. [citation needed]
United Kingdom: Flunitrazepam is a Class C, Schedule 4 controlled drug under the Misuse of Drugs Regulations 2001.[22][citation needed]
United States: Flunitrazepam is a Schedule IV drug under the Controlled Substances Act in the U.S but is not medically used. [citation needed]
Preparation methods
Volumetric liquid dosing - If one's benzodiazepines are in powder form, they are unlikely to weigh out accurately without the most expensive of scales due to their extreme potency. To avoid this, one can dissolve the benzodiazepine volumetrically into a solution and dose it accurately based upon the methodological instructions linked within this tutorial here.
↑Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/2450203
