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Flunitrazepam

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Flunitrazepam chemical structure
Flunitrazepam

6-(2-fluorophenyl)-2-methyl-9-nitro-
2,5-diazabicyclo[5.4.0]undeca-
5,8,10,12-tetraen-3-one

IUPAC name
CAS number
1622-62-4
ATC code
N05CD03
PubChem
3380
DrugBank
none
Chemical formula C16H12FN3O3
Molecular weight 313.3
Bioavailability  ?
Metabolism Hepatic
Elimination half-life 18-26 hours
Excretion Renal
Pregnancy category  ?
Legal status Schedule III(US)
Routes of administration Oral


Flunitrazepam (formerly marketed under the trade name Rohypnol in the United States) is a drug which is a benzodiazepine derivative. It has powerful sedative, anxiolytic, and skeletal muscle relaxant properties.

Contents

History

Flunitrazepam was first synthesized in the early 1970s by Roche and was used in hospitals when deep sedation was needed. It first entered the commercial market in Europe in 1975, and in the 1980s it began to be available in other countries.

It originally came in 1 mg, 2 mg, and 5 mg sizes, but due to its potency and potential for abuse, the higher doses were taken off the market and it is now only available in 1 mg.

Pharmacology

Like other benzodiazepines, flunitrazepam's pharmacological effects include sedation, muscle relaxation, reduction in anxiety, and prevention of convulsions. However, flunitrazepam's sedative effects are approximately 7 to 10 times more potent than diazepam. The effects of flunitrazepam appear approximately 15 to 20 minutes after oral administration, and last for approximately four to six hours. Some residual effects can persist up to 12 hours or more after administration.

Medical Uses

Flunitrazepam has not been approved by the Food and Drug Administration for medical use in the United States. It is available only by private prescription in the United Kingdom[1](though Rohypnol was discontinued in 2004) and prescription in Australia is restricted.[2][3] It is used primarily for the treatment of severe insomnia that has not responded to other treatments.

Illegal Uses

Use as a date rape drug

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 is particularly dangerous when flunitrazepam is used to aid in the commission of sexual assault; victims may not be able to clearly recall the assault, the assailant, or the events surrounding the assault.

It is difficult to estimate just how many flunitrazepam-facilitated rapes have occurred in the United States. Very often, biological samples are taken from the victim at a time when the effects of the drug have already passed and only residual amounts remain in the body fluids. These residual amounts are difficult, and sometimes impossible, to detect using standard screening assays available in the United States. If flunitrazepam exposure is to be detected at all, urine samples need to be collected within 72 hours and subjected to sensitive analytical tests. The problem is compounded by the onset of amnesia after ingestion of the drug, which causes the victim to be uncertain about the facts surrounding the rape. This uncertainty may lead to critical delays or even reluctance to report the rape and provide appropriate biological samples for testing. If a person suspects that he or she is the victim of a flunitrazepam-facilitated rape, he or she should get laboratory testing for flunitrazepam as soon as possible.

It must be noted that an inability to remember events, including sexual encounters, is not conclusive evidence of having consumed a drugged drink: Drunkenness itself causes blackouts, sleepiness, and a reduction in inhibitions. Only a timely screening for flunitrazepam can demonstrate its use.

Use for theft

In the United Kingdom, the use of flunitrazepam and other "date rape" drugs is becoming widespread as a means of sedating victims and stealing from them. It is estimated that up to 2000 men and women are robbed each year after being spiked with powerful sedatives [1], making drug-assisted robbery a more common problem than drug-assisted rape.

In December 2004, Selina Hakki was found guilty of using flunitrazepam to drug wealthy men and rob them of their clothes and accessories in the UK.

Use as a recreational drug

Although flunitrazepam has become widely known in USA for its use as a date-rape drug, it is used more frequently as a recreational drug. It is used by high school and college students, rave party attendees, and heroin and cocaine users (who call a dose of flunitrazepam a "roofie") for recreational purposes, including:

  • To produce profound intoxication (Kurt Cobain overdosed on a mixture of flunitrazepam and champagne several weeks before his death)
  • To boost the high produced by heroin, or ease the anxiety and/or sleeplessness of withdrawal
  • To counteract the side effects of stimulants (e.g. insomnia, paranoia, jitteriness)
  • To "soften" the so-called "crash" which follows heavy usage of stimulants, such as cocaine or methamphetamine
  • To improve sex drive and appetite.

Flunitrazepam is usually consumed orally, and is often combined with alcohol. It is also occasionally insufflated (i.e. tablets are crushed into powder and snorted). In some European contries, there was an alcohol solution of flunitrazepam(Darkene), abused by injection with very strong effects.

Used for robberies

Robbers may use flunitrazepam before a robbery as it makes you calm and emotionless so you can perform the robbery without getting nervous. Flunitrazepam is also known to induce anterograde amnesia making police interrogations more difficult.

Side effects

Flunitrazepam is considered to be one of the most addictive of the benzodiazepines, along with clonazepam, midazolam, temazepam, lorazepam and alprazolam. Its use causes several notable side effects, including:

Long-term use of flunitrazepam can result in psychological and physical dependence and the appearance of withdrawal symptoms when the drug is discontinued. Flunitrazepam impairs cognitive and psychomotor functions, affecting reaction time and driving skill. The use of this drug in combination with alcohol potentiates these side effects, and can lead to toxicity.

Legal Status

Flunitrazepam is a Schedule III drug under the Convention on Psychotropic Substances[2]. Flunitrazepam has never been approved for medical use in the United States, and it was placed into Schedule IV of the Controlled Substances Act in 1984, and was later moved to Schedule III.

According to FDA Associate Director for Domestic and International Drug Control Nicholas Reuter[3]:

Flunitrazepam was "temporarily controlled in Schedule IV pursuant to a treaty obligation under the 1971 Convention on Psychotropic Substances. At the time flunitrazepam was placed temporarily in Schedule IV . . . there was no evidence of abuse or trafficking of the drug in the United States."

Rohypnol is currently under consideration to be moved to a Schedule I substance, and is considered as such in the States of Florida, Idaho, Minnesota, New Hampshire, New Mexico, North Dakota, Oklahoma, and Pennsylvania.

21 U.S.C. § 841 and 21 U.S.C. § 952 provide for very stiff prison terms for possession of flunitrazepam, including life in prison if death or serious bodily or emotional injury results from the use of flunitrazepam.

See also

References

Footnotes

  1. ^ "UK Rohypnol: The date rape drug", BBC News Online, Thursday, May 20, 1999. URL accessed on 2006-03-13.
  2. ^ (13 August 2004). Authorisation to Supply or Prescribe Drugs of Addiction: Flunitrazepam. Statutory Medical Notifications. Department of Health, Government of Western Australia. URL accessed on 2006-03-13.
  3. ^ (August 2000). Guidelines for the Prescribing of Flunitrazepam. (PDF) Pharmaceutical Services Branch. New South Wales Health. URL accessed on 2006-03-13.

External links


Benzodiazepines edit

{Adinazolam} {Alprazolam} {Bromazepam} {Brotizolam} {Camazepam} {Chlordiazepoxide} {Cinolazepam} {Clobazam} {Clonazepam} {Clorazepate} {Clotiazepam} {Cloxazolam} {Diazepam} {Doxefazepam} {Estazolam} {Ethyl loflazepate} {Etizolam} {Fludiazepam} {Flunitrazepam} {Flurazepam} {Gidazepam} {Halazepam} {Ketazolam} {Loprazolam} {Lorazepam} {Lormetazepam} {Medazepam} {Midazolam} {Nimetazepam} {Nitrazepam} {Nordazepam} {Oxazepam} {Pinazepam} {Prazepam} {Quazepam} {Temazepam} {Tofisopam} {Triazolam}

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