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