Flunitrazepam

Flunitrazepam was discovered at Roche as part of the benzodiazepine work led by Leo Sternbach. It was first marketed in 1974 and entered the commerical market in Europe in 1975 under the name Rohypnol. In the 1980's it began to be available in other countries. ^[5]

It may be better known as the date-rape drug Rohypnol (with the street name “roofie”). In 1998, due to the abuse of the drug and recreation, Roche modified their 1 mg tablets to make them less soluble and added a blue dye for easier detection in drinks. ^[6]

In studies in Sweden, flunitrazepam was the second most common drug used in suicides, being found in about 16% of cases. In a retrospective Swedish study of 1587 deaths, in 159 cases benzodiazepines were found. In suicides when benzodiazepines were implicated, the benzodiazepines flunitrazepam and nitrazepam were occurring in significantly higher concentrations, compared to natural deaths. ^[5]

Flunitrazepam is classed as a nitro-benzodiazepine. It is the fluorinated N-methyl derivative of nitrazepam. Other nitro-benzodiazepines include nitrazepam (the parent compound), nimetazepam (methylamino derivative) and clonazepam (2ʹ-chlorinated derivative).^[7]

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. ^[5]

80% of the flunitrazepam that is taken orally is absorbed but the bioavailability in suppository form is closer to 50%. ^[5]

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 ☠.

The general head space of flunitrazepam is described as one of intense sedation, sleepiness, relaxation, anxiety suppression, memory suppression and decreased inhibition similar to the headspace of higher doses of diazepam and temazepam.

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: Flunitrazepam

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.

Flunitrazepam likely has a low toxicity relative to dose.^[2] However, it is potentially lethal when mixed with depressants like alcohol or opioids.

It is strongly recommended that one use harm reduction practices when using this drug.

Lethal dosage

The oral LD₅₀ (lethal dose in 50% of the population) of flunitrazepam is 1200 mg/kg in mice and 415 mg/kg in rats.

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.^[3] Drugs which lower the seizure threshold such as tramadol should be avoided during withdrawal.

Flunitrazepam presents cross-tolerance with 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.

• 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 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.

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 GABA_A receptor. Thus their effects potentiate one another. Benzodiazepines increase the frequency in which the chlorine ion pore opens on the GABA_A 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^[15]. 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 GABA_A antagonist^[16]. However, care is primarily supportive in nature.

• International: Flunitrazepam is a Schedule III drug under the international Convention on Psychotropic Substances of 1971.^{[citation needed]}
• Australia: Flunitrazepam is a Schedule 8 (S8) or controlled drug.^{[citation needed]}
• Austria: Flunitrazepam is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).^{[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]}
• Switzerland: Flunitrazepam is listed as a controlled narcotic substance, but it is also sparesly prescribed as a sleep aid in major cases. Flunitrazolam tablets only come in 1mg dosage and are dyed green and blue which colors one's mouth notably when ingested in a dissolved beverage.^[17]
• United Kingdom: Flunitrazepam is a Class C, Schedule 4 controlled drug under the Misuse of Drugs Regulations 2001.^{[18][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]}

• Responsible use
  • Volumetric liquid dosing
• Psychoactive substance index
• Flunitrazolam
• Temazepam
• Benzodiazepines
• Depressants

• Flunitrazepam (Wikipedia)
• Flunitrazepam (Erowid Vault)
• Flunitrazepam (Isomer Design)
• Flunitrazepam (DrugBank)