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Alexandra Glen

21321729
PHAR2220: Human Pharmacology
Self-Directed Learning Assignment
Rohypnol: Pharmacological properties to user misuse and criminal abuse
Word Count: 1608

A rising prevalence in anxiety disorders necessitates the production of anxiolytics,


particularly with sedative or hypnotic properties (Schechter, 1998). The creation of
benzodiazepines, a group of central nervous system depressants with anxiolytic properties (a
notable example of which is Diazepam, or its more common name Valium), marked the start
of an effective drug class for treating psychological disorders such as depression and anxiety
(Saum & Inciardi, 1997; Schwartz & Weaver, 1998). Rohypnol (chemical name:
flunitrazepam), a typical sedative-hypnotic benzodiazepine, is manufactured by the HoffmanLa Roche Company for indications such as insomnia and pre-operative anaesthesia (Britt &
McCance-Katz, 2005; Saum & Inciardi, 1997; Schwartz & Weaver, 1998). Produced and
marketed in European countries, South America, and even Australia, this potent drug, while
not sanctioned in the U.S., has become readily available through smuggling for recreational
and even more sinister purposes (Labianca, 1998; Saum & Inciardi, 1997; Schwartz &
Weaver, 1998). Gaining popularity as a Club Drug, its spreading use as a cheap way to
potentiate the effects of other drugs has evolved as a way to cover its other damaging
purpose; to render victims helpless to defend themselves from a sexual assault they may not
even remember (Gahlinger, 2004; Saum & Inciardi, 1997; Schechter, 1998).
In the movie The Hangover (2009), starring some drunk and then hung-over actors, 3
friends attempt to piece together a night out in order to find their missing friend, this attempt
made harder by the fact they cannot remember anything. They realise they have been
roofied, using the accidental and un-consensual ingestion of a possibly toxic dose of
Rohypnol as a light-hearted and comedic way to further complicate the plot of finding the
missing bachelor. The effects of this drug become clear: with the main, and perhaps overimplicated symptoms being amnesia following a black-out. These effects following taking
Rohypnol, whether intentionally or unintentionally, have been well documented throughout
their history, particularly following their introduction into the U.S., where they are not
sanctioned by the FDA, making their entire use there illicit (Britt & McCance-Katz, 2005;
Labianca, 1998). Initially manufactured for the purpose of treating legitimate physiological
issues, Rohypnol has been implicated in recreational use due to its relaxing and euphoric
effects; causing a rapid and long-lasting reduction in anxiety and an increase in enjoyment
and effectiveness of other drugs (Britt & McCance-Katz, 2005; Druid, Holmgren & Ahlner,
2001; Schechter, 1998). With the effects starting within half an hour, and lasting up to 24
hours depending on dose, street users of this drug can inexpensively enjoy themselves more

in the convenient form of a bubble-wrapped pill (Gahlinger, 2004; Saum & Inciardi, 1997;
Schwartz & Weaver, 1998).
However, not only can they be adulterated or misrepresented, dose non-withstanding,
possibly leading to dangerous outcomes, in large doses Rohypnol can have highly toxic
effects (Gahlinger, 2004). At doses larger than milligrams, they can produce amnesia, loss
of muscular and visual control, cognitive impairment, decreased body temperature and
eventually, a loss of consciousness/blackouts (Britt & McCance-Katz, 2005; Gahlinger, 2004;
Saum & Inciardi, 1997). While not usually fatal taken on their own, taken with other CNS
depressants, typically alcohol, the mortality rate of the overdose can increase due to a marked
reduction in activity of the respiratory reflex centre (Labianca, 1998; Saum & Inciardi, 1997;
Schwartz & Weaver, 1998). Immediate concerns of treating physicians should be maintaining
cardio-respiratory activity, followed by monitoring of most body systems (Gahlinger, 2004).
However, problems can arise due to probable adulteration of the substance taken, which
should, in most cases, be treated as a relatively unknown substance. If it is specifically known
that pure Rohypnol was ingested, within 60 minutes activated charcoal can be used to
decontaminate the gastro-intestinal tract by absorbing the drug, and after that time frame has
passed, the specific antidote, flumazenil (a benzodiazepine antagonist) can be used to reverse
Rohypnols effects (Britt & McCance-Katz, 2005; Gahlinger, 2004; Schwartz & Weaver,
1998).
As a benzodiazepine, Rohypnol functions as a GABA receptor agonist. GABA, an
inhibitory neurotransmitter, causes chloride channels to open, hyperpolarising neurons and
decreasing the excitatory properties of said neuron (Britt & McCance-Katz, 2005; Labianca,
1998). By increasing affinity of GABA for the receptors it binds, it results in a net reduction
of nervous system excitation, causing sedation and a decrease in anxiety levels (Britt &
McCance-Katz, 2005; Labianca, 1998). Its amnesic effects arise from its ability to change the
peptide formation of specific neurons in the brain, a positive effect for clinical use, but a
negative for dealing with criminal use (Labianca, 1998; Saum & Inciardi, 1997). While its
effects may be long-lasting, Rohypnol is metabolised by the liver, producing 7aminoflunitrazepam as its predominant metabolite, via reduction (Gahlinger, 2004; Labianca,
1998; Schwartz & Weaver, 1998). Rohypnol, due to the aqueous properties of its metabolites
that contain carboxylate groups, a polar substituent, is excreted via the kidneys (Labianca,
1998).
Physical dependence can readily occur when taking Rohypnol over a significant
period of time, with unpleasant withdrawal symptoms including headache, muscle pain, and
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even seizures (Britt & McCance-Katz, 2005). A possible explanation for the existence of this
dependence from an individual point of view may be its relatively low cost, convenient
administration route (generally oral, although can be crushed and snorted), and the fact it is
readily smuggled into the U.S, and legal in other parts of the world (Britt & McCance-Katz,
2005; Gahlinger, 2004; Schwartz & Weaver, 1998). When orally administrated, roughly 80%
is absorbed from the gastro-intestinal system, leading to an overall bioavailability of 50%
(Mattila & Larni, 1980). A half-life of around 20 hours, combined with long last clinical
effects peaking around 1 hour after administration, may contribute to dependence as positive
effects that last this long are similar to alcohol, a widely used substance many people are
dependent on, only cheaper and longer enjoyed (Gahlinger, 2004; Mattila & Larni, 1980;
Saum & Inciardi, 1997).
Rohypnol, while perhaps legal elsewhere in the world, has been classified as a
Schedule 1 drug by the DEA in the U.S., resulting in the penalties for carrying, use or
distribution to be similar to those of possession of cocaine and heroin (Saum & Inciardi,
1997). This is due to the concerning use of it, predominantly due to its amnesic
characteristics, to intoxicate and sexually assault victims, who probably would not even be
aware they had ingested it (Britt & McCance-Katz, 2005; Saum & Inciardi, 1997). Odourless,
colourless and tasteless when dissolved in liquid, it is all too easy to slip it into the drink of
someone who is distracted (Britt & McCance-Katz, 2005). While Rohypnol and its
metabolite 7-aminoflunitrazepam are detectable by gas chromatography and mass
spectrometry testing, due to the fact a victim may not remember the assault for a while, the
time period in which they can be detected may have passed (Gahlinger, 2004; Schwartz &
Weaver, 1998). For this reason, its manufacturers are attempting to add a dye to the pill, so
that a drink laced with Rohypnol will be readily identifiable, to reduce the number of assaults
mediated by this drug (Britt & McCance-Katz, 2005).
This drug, due to its apparent ease of access regardless of laws and regulations
currently in place, appears to need stricter distribution, or at least some way to control its
spread through this population of club-goers in search for a cheap way to become intoxicated,
or worse (Gahlinger, 2004). Hoffman-La Roche also have been rumoured to consider
discontinuing production of the 2mg dose (Schwartz & Weaver, 1998). Its rapid effects,
extreme potency (an estimated 7 times more potent than Valium), and resulting memory loss
are a problem that needs addressing, even posing the question if such a powerful drug is
needed considering its toxic potential (Saum & Inciardi, 1997). Sold over-the-counter in
some countries, predominantly for insomnia relief, it could very well become an epidemic.
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The pharmacology of this drug; biotransformation into its active metabolite facilitated by
liver enzymes, high affinity for its target, and ability to erase all memory of its very ingestion,
makes it an effective, but highly dangerous drug in the wrong hands (Labianca, 1998). In its
context of frequent co-ingestion with alcohol, another CNS depressant, it is easy to see how a
fatal overdose can easily occur, particularly in uneducated individuals, or those who are
unaware they have even consumed it (Labianca, 1998). Efforts to warn people about its
effects, while well intentioned, also run the risk of alerting more people about their malicious
properties and how they can then commit crimes using Rohypnol, with its amnesic properties,
that they very well may never get caught for (Saum & Inciardi, 1997).
In conclusion, while useful in its clinical indications as a night-time sedativehypnotic, and an amnesic to reduce unpleasant memories after a surgical procedure,
Rohypnol is incredibly effective (Mattila & Larni, 1980). With ideal pharmacological
properties including rapid and long lasting effects, a reasonable bioavailability, and low risk
of kidney accumulation in relatively healthy patients, it seems to make sense to continue its
use, perhaps with the suggestion of a prescription being required rather than over the counter
sales (Gahlinger, 2004; Mattila & Larni, 1980; Saum & Inciardi, 1997). However, its
additional use as a recreational drug that can easily lead to death when combined with
alcohol, which appears to be a prevalent occurrence, thought should be taken to control its
access to its abusing population (Britt & McCance-Katz, 2005). Its criminal potential as a
way to subdue victims in an assault, and then effectively erase their memory is a worrying
scenario, which unfortunately can occur quite easily. This issue of public safety needs to be
effectively dealt with, and may even outweigh the associated benefits of this drug.

References
Britt GC, & McCance-Katz EF (2005). A brief overview of the clinical
pharmacology of
club drugs. Substance use & misuse 40: 1189-1201.
Druid H, Holmgren P, & Ahlner J (2001). Flunitrazepam: an evaluation of
use, abuse and
toxicity. Forensic Science International 122: 136-141.
Gahlinger PM (2004). Club drugs: MDMA, gamma-hydroxybutyrate (GHB),
Rohypnol,
and ketamine. American family physician 69: 2619-2626.
Labianca DA (1998). Rohypnol: Profile of the" date-rape drug". Journal of
chemical
education 75: 719.
Mattila MAK, & Larni HM (1980). Flunitrazepam: A Review of its
Pharmacological
Properties and Therapeutic Use. Drugs 20: 353-374.
Saum CA, & Inciardi JA (1997). Rohypnol misuse in the United States.
Substance Use &
Misuse 32: 723-731.
Schechter MD (1998). Rohypnol (Roofies) control of drug discrimination:
effect of
coadministered ethanol or flumenazil. Pharmacology Biochemistry
and Behavior
59: 19-25.
Schwartz RH, & Weaver AB (1998). Rohypnol, the date rape drug. Clinical
pediatrics 37:
321.

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