Rohypnol: Uses, Adverse Effects, Risks, Interactions, Pharmacology and History

It is a powerful sedative that acts as a central nervous system depressant. It is significantly stronger than other common sedatives like Valium.

Rohypnol, also known as flunitrazepam, among other names, is an intermediate-acting benzodiazepine that is used in some countries in short-term treatment to treat severe insomnia and as a premedication in surgical procedures and initially to induce anesthesia.

As with other hypnotics, rohypnol should be used strictly short-term only or by those with chronic insomnia occasionally. Rohypnol has been referred to as a date rape drug, although its incidence is very rare in reported rape cases.

It can also release growth hormones that increase the user’s muscles, which may make it popular with those looking for a quick physical boost.

What does rohypnol look like?

Rohypnol is a small white tablet that is tasteless and odorless when mixed into a drink.

How is it taken?

Rohypnol is usually taken by mouth in pill form, but it can also be crushed and snorted.

Who uses it?

Rohypnol is predominantly abused among teens and young adults, usually in raves and nightclubs.

What are the effects of rohypnol?

The drug affects the central nervous system and creates a feeling of drugged or drunk. Rohypnol often leaves people in a semi-unconscious state or coma.

In some cases, sexual predators may add rohypnol in powder or liquid form to the victim’s drink. When the drug is added to alcohol, it slows down the victim’s senses and bodily coordination.

The effects of rohypnol can last from eight to 26 hours, during which time the user has little or no memory of what happened while under the influence of the drug.

What are the risks of rohypnol?

It can cause blackouts, disorientation, and can inhibit the ability to speak or move. It can also produce “anterograde amnesia,” which means that victims under the influence of drugs may not remember the events they experienced.

If mixed with alcohol or other depressants, it can be fatal.

Is rohypnol addictive?

Rohypnol is addictive and produces physical and psychological dependence, causing withdrawal seizures among addicts.

Drugs similar to rohypnol

Clonazepam, marketed in the US as Klonopin, and alprazolam, marketed as Xanax, are two similar drugs that are abused and have replaced Rohypnol in certain parts of the country.

Rohypnol uses

Although this drug is illegal in the US, rohypnol is legal in many other countries. Perhaps the most concerning problem surrounding rohypnol is its use as a date rape drug. This drug is tasteless and odorless, so the individual does not even know that they have been drugged.

As rohypnol is a benzodiazepine, and this type of substances can provide anxiolytic, muscle relaxant and sedative-hypnotic effects. It is often used for the purpose of treating insomnia, as the above effects can help a person relax and fall asleep.

In countries where the drug is still used, it is used for the treatment of insomnia and, in some countries, also to start anesthesia; these were also the indications in which it was originally studied.

Of course, these types of effects can also be very attractive to many recreational users.

Misuse of this form of drug often leads to drug problems such as substance abuse or even addiction. Although benzodiazepines such as Valium or Xanax are commonly prescribed in the US, rohypnol is considered especially dangerous.

Rohypnol is not approved for medical use or manufactured in the United States and is not legally available. However, rohypnol can be legally prescribed in more than 60 countries and is widely available in Mexico, Colombia, and Europe.

Adverse effects to rohypnol

The adverse effects of rohypnol include dependence, both physical and psychological; decreased quality of sleep causing drowsiness; and an overdose, resulting in excessive sedation, impaired balance and speech, respiratory depression or coma, and possibly death.

Because of the latter, rohypnol is commonly used in suicide. When used during pregnancy, it can cause hypotonia.

Dependence

Rohypnol as with other benzodiazepines can lead to drug dependence and benzodiazepine withdrawal syndrome. Discontinuation may lead to withdrawal symptoms when the medicine is stopped.

Abrupt withdrawal can lead to a benzodiazepine withdrawal syndrome characterized by seizures, psychosis, insomnia, and anxiety.

Rebound insomnia, worse than basal insomnia, generally occurs after discontinuation of rohypnol even after short-term evening single-dose therapy.

Depth of sleep

Rohypnol produces a decrease in delta wave activity. However, the effect of benzodiazepines on delta waves cannot be mediated by benzodiazepine receptors.

Delta activity is an indicator of the depth of sleep within non-REM sleep; increased delta sleep levels reflect a better quality of sleep. Therefore, rohypnol and other benzodiazepines cause a deterioration in the quality of sleep.

Cyproheptadine may be superior to benzodiazepines in the treatment of insomnia, as it improves the quality of sleep according to electroencephalography (EEG) studies.

Paradoxical effects

Rohypnol can cause a paradoxical reaction in some individuals and cause symptoms such as anxiety, aggressiveness, agitation, confusion, disinhibition, loss of impulse control, talkativeness, violent behavior, and even seizures.

Paradoxical adverse effects can even lead to criminal behavior.

Hypotonia

Benzodiazepines, such as rohypnol, are lipophilic and rapidly penetrate membranes and therefore rapidly pass to the placenta with significant drug absorption.

The use of benzodiazepines, including rohypnol in late pregnancy, especially at high doses, can lead to hypotonia, also known as floppy baby syndrome.

Other

Rohypnol affects cognitive functions. This can appear as poor concentration, confusion, and anterograde amnesia. It can be described as a hangover effect that can persist into the next day.

It also affects psychomotor functions similar to other benzodiazepines and hypnotic drugs that are not benzodiazepines; falls and hip fractures were frequently reported.

The combination with alcohol increases these deficiencies. Partial, but incomplete tolerance develops to these deficiencies.

Other adverse effects include:

  • Difficulty speaking
  • Gastrointestinal disturbances, lasting 12 or more hours.
  • He retched.
  • Respiratory depression in higher doses.

Special precautions

Benzodiazepines require special caution when used in the elderly, during pregnancy, in children, in people who are dependent on alcohol or drugs, and in people with comorbid psychiatric disorders.

Impaired driving skills with consequent increased risk of traffic accidents is probably the most important adverse effect.

This side effect is not unique to rohypnol, but it also occurs with other hypnotic drugs.

Rohypnol appears to have a particularly high risk of traffic accidents compared to other hypnotics. Drivers should be very careful after taking rohypnol.

Interactions

The use of rohypnol in combination with alcoholic beverages synergizes adverse effects and can lead to toxicity and death.

Rohypnol overdose

Rohypnol is a drug that is frequently involved in drug intoxication, including overdose. Rohypnol overdose can cause excessive sedation or impaired balance or speech.

This can progress to severe overdose of respiratory depression or coma and possibly death. The risk of overdose is increased if rohypnol is taken in combination with central nervous system (CNS) depressants such as ethanol (alcohol) and opioids.

Rohypnol overdose responds to the benzodiazepine receptor antagonist flumazenil, which can be used as a treatment.

Detection

As of 2016, blood tests can identify rohypnol at concentrations as low as 4 ng / ml; the elimination half-life of the drug is 11 to 25 hours.

For urine samples, metabolites can be identified 60 hours to 28 days, depending on the dose and the analytical method used.

Hair and saliva can also be tested; hair is useful when a long time has passed since ingestion, and saliva for drug tests in the workplace.

Rohypnol can be measured in blood or plasma to confirm a diagnosis of poisoning in hospitalized patients, provide evidence in an impaired driving arrest, or assist in a medicolegal death investigation.

Rohypnol concentrations in blood or plasma are generally in a range of 5-20 μg / L in people receiving the drug therapeutically as a nocturnal hypnotic, 10-50 μg / L in those arrested for impaired conduction, and 100-1000 μg / L in victims of acute fatal overdose.

Urine is often the preferred specimen for routine drug abuse control purposes. The presence of 7-aminorohypnol, a pharmacologically active metabolite and an in vitro degradation product, is helpful in confirming the ingestion of rohypnol.

In postmortem samples, the parent drug may have completely degraded over time to 7-aminorohypnol. Other metabolites include desmethylrohypnol and 3-hydroxydesmethylrohypnol.

Pharmacology

The main pharmacological effects of rohypnol are the enhancement of gamma-aminobutyric acid (GABA) at various gamma-aminobutyric acid receptors.

While 80% of rohypnol taken orally is absorbed, the bioavailability in the form of suppositories is closer to 50%.

Rohypnol has a long half-life of 18-26 hours, which means that the effects of rohypnol after nocturnal administration persist through the following day.

Rohypnol is lipophilic and is metabolized by the liver through oxidative pathways. The CYP3A4 enzyme is the major enzyme in its phase 1 metabolism in human liver microsomes.

Chemistry

Rohypnol is classified 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 (2′-chlorinated derivative).

History

The history of rohypnol is deeply intertwined with the history of benzodiazepines. Benzodiazepines were originally first developed in the 1950s.

Rohypnol was discovered in the laboratories of the Swiss pharmaceutical company Hoffman-La Roche as part of the benzodiazepine work led by Leo Sternbach .

Sternbach led a team of researchers that helped him create and introduce many benzodiazepines. Rohypnol was first introduced by Hoffman-La Roche in 1975. The patent application was filed in 1962 and it was marketed for the first time.

Doctors wanted a safer alternative to barbiturates, which had a high risk of respiratory depression. During the 1970s, benzodiazepines became popular with both physicians and patients.

However, in the 1980s, medical providers began to voice their concerns about abuse and dependency. Medical providers and legislators began to create restrictions on the use of benzodiazepines during this time.

Due to abuse of the rape and recreation drug, in 1998 the Swiss pharmaceutical company Hoffman-La Roche modified the formulation to give lower doses, make it less soluble, and add a blue dye for easier detection in beverages.

It was never marketed in the US, and by 2016 it had been withdrawn from markets in Spain, France, Germany, and the UK.

Society and culture

People can use substances for different purposes. It could be that they have been prescribed something for a medical condition, are looking for the euphoric effects of some substance, or maybe they are trying to feel better with something.

Whatever the case, there are numerous substances that can be used for all of the above, and there are also some that people can use on their own or use on others for malicious reasons.

The physical effects of rohypnol on a person can range from minor to severe, to addiction and dependence.

Recreational and illegal uses

Recreational use

A 1989 journal of Clinical Pharmacology reports that benzodiazepines accounted for 52% of prescription counterfeits, suggesting that benzodiazepines were a major class of prescription drug abuse.

Nitrazepam accounts for 13% of counterfeit prescriptions. Rohypnol and other sedative-hypnotic drugs are frequently detected in people suspected of driving under the influence of drugs.

Other benzodiazepines and non-benzodiazepines (anxiolytic or hypnotic) such as zolpidem and zopiclone (as well as cyclopyrrolones, imidazopyridines, and pyrazolopyrimidines) are also found in large numbers of drug-suspect drivers.

Many drivers have blood levels that far exceed the therapeutic dose range, suggesting a high degree of abuse potential for benzodiazepines and similar medications.

Of course, there is also the potential for physical dependence and addiction. If an individual continues to use this medication over time, they may either dispose of it when they are no longer taking it or engage in risky behavior in seeking it. In this situation, they should seek professional help to get out of it.

There is also the possibility of overdose, which could include symptoms such as decreased heart rate, severe sedation, loss of consciousness, and respiratory suppression that could lead to death.

Suicide

In studies carried out in Sweden, rohypnol was the second most used drug in suicides, being found in around 16% of cases. In a retrospective Swedish study of 1,587 deaths, benzodiazepines were found in 159 cases.

In suicides when benzodiazepines were implicated, the benzodiazepines rohypnol and nitrazepam were occurring at significantly higher concentrations, compared to natural deaths.

In 4 of the 159 cases, where benzodiazepines were found, benzodiazepines alone were the only cause of death. It was concluded that rohypnol and nitrazepam could be more toxic than other benzodiazepines.

Drug-facilitated sexual assault

Rohypnol is known to induce anterograde amnesia in sufficient doses; people cannot remember certain events they experienced while under the influence of the drug, complicating investigations.

When used in this way, it is usually introduced into someone’s drink so that sexual assault can take place. It can cause drowsiness and sedation to incapacitate an individual for this to happen, and it can also cause amnesia so that the victim does not even remember the assault.

This effect could be particularly dangerous if rohypnol is used to aid in the commission of a sexual assault; Victims may be unable to clearly recall the assault, the assailant, or the events surrounding the assault.

There are also several other effects of rohypnol that can happen to an individual, including judgment and reaction time, aggression, confusion, and excitability.

With regard to physical effects, it can cause loss of motor coordination, respiratory depression, headaches, weakness, and difficulty speaking.

Due to the frequency with which rohypnol was used for this purpose, steps were taken to help prevent it.

One of them was that the pill was reformulated from a white tablet to an oblong green tablet that stains liquids blue as it used to be colorless when placed in beverages. Although, generic brands may not have this protection in place.

While the use of rohypnol in sexual assault has been prominent in the media, as of 2015 it appears to be quite rare, and the use of alcohol and other benzodiazepine drugs in rape appears to be a major but unreported problem.

Drug-facilitated robbery

In the UK, the use of rohypnol and other ‘date rape’ drugs have also been linked to stealing from sedated victims.

An activist quoted by a British newspaper estimated that up to 2,000 individuals are robbed each year after being dried off with powerful sedatives, making drug-assisted robbery a more frequently reported problem than drug-assisted rape.

Regional use

Rohypnol is a Schedule III drug under the 1971 International Convention on Psychotropic Substances.

In Australia, as of 2013 the drug was authorized for the prescription of severe cases of insomnia, but it was restricted as a Schedule 8 drug. In France, as of 2016, rohypnol was not marketed.

In Germany, as of 2016, rohypnol is an Anlage III Betäubungsmittel (controlled substance that can be marketed and prescribed by doctors under specific provisions).

In Germany it is available in a special prescription for narcotic drugs such as Rohypnol (English name) in 1 mg presentations and various generic preparations (November 2016).

In Ireland, rohypnol is a Schedule 3 controlled substance with strict restrictions. In Mexico, the drug with the name Rohypnol is approved for medical use.

In Japan, rohypnol is marketed by the Japanese pharmaceutical company Chugai under the English trade name Rohypnol and is indicated for the treatment of insomnia and for pre-anesthetic medication.

In Norway, on January 1, 2003, rohypnol was raised one notch in the controlled drug program, and on August 1, 2004, the manufacturer Roche completely removed the drug under the name Rohypnol from the market.

In South Africa, this drug is classified as a Schedule 6 drug. It is available by prescription and is restricted to 1 mg doses. Travelers from South Africa to the United States are limited to a 30-day supply.

The drug must be declared to United States Customs upon arrival. If a valid prescription cannot be produced, the drug may be subject to search and seizure by Customs, and the traveler may face criminal charges or deportation.

In Sweden, rohypnol is available from Mylan. It is listed as Schedule II (Annex II) under the Narcotics Control Act (1968).

In the UK, rohypnol is not licensed for medical use and is a Schedule 3 and Class C controlled drug

In the United States, the drug has not been approved by the Food and Drug Administration and is considered to be an illegal drug; As of 2016, it is Annex IV, Title 21 of the United States Code, paragraph 841 and Title 21 of the United States Code, paragraph 952.

It establishes penalties for the importation and distribution of up to 20 years in prison and a fine; possession is punishable by three years and a fine.

Names

Rohypnol is marketed under many trademarks in countries where it is legal. It also has many street names, including “roofie” and “ruffie.”