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Greetings! Thank you for subscribing to the MEDTOX Journal. We hope that you find this newsletter interesting and educational. In addition to this month's mystery drug article, this issue focuses on the newest designer drug Dragonfly, the latest research on the changes in the brain regarding long-term amphetamine abuse, and an article that chronicles a scientist who is known and loved. You may forward a copy to others by clicking this box.
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What Could Be Wrong With a Little Dragonfly?
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 | Dr. Oz Explains DragonFLY |
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Recent reports into the MEDTOX Drug Abuse Recognition (DAR) Hotline suggest that the designer drug world is undergoing some shifts in drug preferences and manners of use. In the course of a recently held MEDTOX DAR Designer Drug webinar, approximately 800 attendees responded to the presentation with anecdotes and other stories of designer drug use in the jurisdictions they serve. As you can imagine, designer drug abuse is wide and varied. It is also quite dangerous. In this regard, leading the list of unusual and unregulated substances is a hallucinogenic phenethylamine product called Bromo-DragonFLY. Rarely mentioned in media coverage, Bromo-DragonFLY is a potent hallucinogen, a drug that is very capable of rendering a user incapacitated and in need of emergency medical attention. While its legal status in the United States is murky, a number of other countries have moved quickly to regulate or outright ban the drug. A related compound called 2 C-B-FLY is sometimes confused as Bromo-DragonFLY, and although the two drugs share hallucinogenic properties, they can produce profoundly different physical effects. Bromo-DragonFLY's name arose out of the drug's unique physical chemistry. The furanyl rings coupled with double bonds and an amphetamine arm create a strange structural arrangement that depicts the form of a dragonfly.
Bromo-benzodifuranyl-isopropylamine, aka: Bromo-DragonFLY is found on the streets as a white to pink looking powder that is snorted, smoked, or injected. The drug has allegedly been distributed in blotter paper in some western U.S. locales, in this form the drug may be mistaken as L.S.D. A typical dose of this powerful hallucinogen is purported to a very small 500 micrograms; straying much beyond that amount can quickly lead to toxic or even fatal outcomes. Once absorbed into the bloodstream, Bromo-DragonFLY powerfully stimulates serotonin receptors in the brain. The effects experienced are similar to L.S.D., but are apparently much exaggerated. For DRE and DAR trained readers, Bromo-DragonFLY users will present with classic hallucinogen symptoms. The drug's amphetamine lineage will trigger very dilated pupils and a symptomatic edginess that may cause users to become extremely confused and agitated.
Bromo-DragonFLY's nomenclature has been confused with a closely related compound, 2C-Bromo-Fly, also known as 2C-B-FLY. This drug is a more commonly abused hallucinogen, a substance that is less potent and shorter acting than DragonFLY. The use of the term "FLY" in the drug's name reflects the modified phenethylamine's chemical tail, a clipped or "hemi" variation of the full tail found with Bromo-DragonFLY. This may seem to be a trivial structural distinction, but it results in some significant differences in how both drugs work in the central nervous system. Like nearly all other modern designer drugs, neither of these substances has been studied in any scientifically acceptable way. 2C-B-Fly is arguably an analog, a very close chemical relative of 2C-B (officially recognized as 2-(4-bromo 2,5-dimethoxyphenyl)ethanamine). It is 2C-B that has received the most attention from designer drug aficionados. In the mid-70s, 2C-B was made famous by Alexander "Sasha" Shulgin a renowned research chemist and author of the book PIHKAL. The main title is an acronym for "Phenethylamines I Have Known And Loved." Shulgin's tome explains and details the experiential effects of 2C-B, as well as the procedures that need to be followed in the synthesis of the drug. Shulgin's PIHKAL is indeed a designer drug cookbook.
Schedule I of the U.S. Controlled Substances Act bans the use and possession of 2C-B. Nevertheless, it continues to circulate in communities throughout the country. For Bromo-DragonFLY and 2C-BFly, possession and sale of these drugs are putative analogs of the banned drug 2C-B; therefore, they are most likely amenable to prosecution under the Federal Analog Act. It is unclear at this point however as to whether or not either of the FLY drugs has been prosecuted using analog provisions of the law. Manufacturers of these designer drugs have danced around American law by stamping their product with advisories such as "not intended for human consumption", or by naming the products plant food, bath salts, or potpourri. Some individual state legislatures have moved to ban these drugs by adding them to state controlled substances acts.
The designer drug phenomenon continues to plague many American communities. It does not appear to be slowing down. In fact, the phenomenon might be gaining momentum. The names, identities, and legal status of these designer drug substances can be confusing and frustrating. Stay tuned to the MEDTOX DAR Journal for up-to-date news and information related to these drugs. Also check each edition for news and schedules for MEDTOX's DAR (Drug Abuse Recognition) webinar series that starts in 2012.
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Drinking and House Fires: A Recipe for Disaster
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Smoking cigarettes is a well-recognized factor in the incidence of deadly residential fires. Bedside smoking is a harbinger for disaster. But what about the role that drinking plays in these horrible events? What role does alcohol consumption play in the incidence of fatal fires? Does consumption of alcohol in the home exacerbate the risks of in-home smokers? A recent investigation in the Journal of Studies on Alcohol and Drugs provided strong evidence connecting high blood alcohol concentrations with higher rates of fatal cigarette caused residential fires[1].
To examine the role of alcohol in deadly house fires, scientists used coroners' reports of deaths caused by residential fires in the state of Victoria, Australia during the years 1998-2006. Of the 95 adults who died in the fires where blood alcohol concentrations were available for analysis, 58% tested positive for the drug. In this cohort, 94% had blood alcohol concentrations that were greater than 0.10%, a level that exceeds U.S. limits for operation of a motor vehicle. Amazingly, 31% had blood alcohol concentrations that were greater than 0.20%, over twice the legal limit. The mean blood alcohol concentration was .22%, a level that almost certainly indicates a condition of gross impairment. Digging further into the data, alcohol was three times more likely to be a factor in the death of men than in women. The likelihood that smoking was the cause of a house fire was four times greater in people with high blood alcohol concentrations than those who had not been drinking. And of critical importance was the fact that victims with elevated blood alcohol concentrations were three times less likely to have had their escape routes blocked by an obstacle. In other words, the inebriated victims were impaired by their alcohol consumption, not by obstacles that had fallen or had otherwise blocked their escape.
In summary of the data presented in the study, it is clear that alcohol consumption is a major factor in smoking related fatalities. Further, the data suggests that intoxication is a major factor in deterring a safe escape from a burning home. As a practical matter, this data suggests that practitioners should strongly admonish patients and clients about the dangers inherent in smoking and drinking in the home. Lives will likely be saved.
[1] Bruck D et al. Fire fatality and alcohol intake: Analysis of key risk factors. J Stud Alcohol & Drugs, 2011 Sept; 72:31
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Chronic Amphetamine Abuse May Result in Long-Term Changes in Brain Activity
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Recent animal studies seem to corroborate findings that rehabilitation and addiction specialists have acknowledged for years; chronic amphetamine use disrupts the emotional and cognitive processes of those who abuse it. The research in the studies cited here involved analysis of rats and rat brains that had been subjected to chronic exposure to amphetamines. This research sheds light on how the amphetamines distort and disrupt the basic processes of the brain and central nervous system[1]. Although amphetamines can increase attention, reaction times and focus in the short term, long-term use of the drugs can result in a chemical rewiring of those parts of the brain that mediate messages of memory, arousal, and emotional responses to environmental cues. The systems most affected by amphetamine use are those that manage and mediate D1 and D2 dopamine neurons located in the amygdala. Pathways and neuronal circuits leading from the amygdala to the prefrontal cortex seem to be hit hardest. In the experiments reported here, rats were separated into two groups. The experimental group received moderate doses of amphetamine every other day for 10 days. A two-week washout period followed. A control set of rats was treated with saline every other day over the same timeframe. Analysis revealed that the rats treated with amphetamine exhibited less sensitivity to inhibitory messages in the amygdala and enhanced reactions to excitatory messages. The amphetamine-treated rats also displayed desensitization at D1 and D2 receptors, making them less reactive to their own stores of dopamine. They also displayed more tolerance to a later single dose of amphetamine that followed a two-week hiatus from amphetamines. The rats were also subjected to aversive conditioning and a lever pulling exercise to determine how amphetamine affected their abilities at avoiding noxious stimuli. The amphetamine-treated rats displayed degraded learning skills and learning memory when compared to the saline treated rats. This study of rats revealed that repeated exposure to amphetamine led to disrupted connections and circuits linking the amygdala and prefrontal cortex. These alterations persisted long after discontinuation of amphetamine use. This situation caused the experimental group to forget associations between environmental cues and negative outcomes. The loss of this avoidance-memory capability prevented them from remembering the cause of something that resulted in discomfort. The fear response mechanism however was intact with the amphetamine-exposed rats. Their problems rested with their inabilities to use emotionally tied memories to guide their behaviors in response. Addiction professionals and public safety officers have frequent contact with people who abuse amphetamines. Methamphetamine is hands-down the most notorious drug of the amphetamine family. For years, the DAR Program staff has listened to stories and anecdotes from Journal readers about how methamphetamine disrupts the cognitive abilities and behaviors of those who abuse it. These stories have often involved extraordinary reports of the behaviors of amphetamine users, behaviors that for the layperson are hard to believe. But as time goes by, the evidence is mounting that the amphetamines are uniquely harmful drugs and when taken chronically at moderate doses they pose almost certain risk to the brain. And of genuine concern from the research mentioned, this damage to the brain may be such that amphetamine abusers may not be able to rationally act and respond to the harmful consequences of their drug use. This research may help explain why methamphetamine abusers are unable to properly or emotionally react to their deteriorating faces or tooth loss that plagues them.
[1] Tse MT et al. Repeated amphetamine exposure disrupts the dopaminergic modulation of amygdala-prefrontal circuitry and cognitive/emotional processing. Journal of Neuroscience 2011, Aug 3; 31:11282.
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Alexander "Sasha" Shulgin Ph.D.: An Important Figure Who Is Known and Loved
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 | Alexander "Sasha" Shulgin in Laboratory |
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Designer Drug News
Few people have had an impact on the breadth and direction of the modern designer drug movement than the noted chemist Alexander "Sasha" Shulgin Ph.D. Born in 1925 in the United States to Russian parents, the 86-year-old Dr. Shulgin represents perhaps the greatest single body of designer drug knowledge in the world today. Focusing primarily on hallucinogenic drugs, Shulgin has produced dozens of books and papers related to his fastidious research of the synthesis and physical effects of the drugs he has studied. Two of his publications have reached near mythical status amongst fans of designer drugs in general, and hallucinogenic drugs in particular. Phenylethylamines I Have known and Loved (PiHKAL) and its sequel, Tryptamines I Have Known and Loved (TiHKAL) are arguably the most precise records of hallucinogen synthesis and experimentation in the world today. It should be noted that Dr. Shulgin's wife, Ann Shulgin, co-authored these books with him. She was also a partner in many of the experiments and processes that were undertaken in the course of his research.
Dr. Shulgin is a Berkley educated scientist. A World War II U.S. Navy veteran, Shulgin directed his interests and energy to the study of pharmacology and psychiatry. A biochemist by trade, Dr. Shulgin ended up at Dow Chemical Company where he began work as a research chemist. Through the course of his work there, Dr. Shulgin began experimentation with the hallucinogenic drug, mescaline, the active ingredient found in the peyote cactus. His mescaline use occurred in the late 50s, a time that predated the relaxed drug using days of the Vietnam War era. Now interested in the potential for hallucinogens in psychotherapy, Shulgin turned his interests into research of drugs and compounds that he thought possessed pharmacological potential. He left Dow and began working in a small lab that he set up along side of his home.
Dr. Shulgin artfully established himself as a consultant to the nascent Drug Enforcement Administration (DEA); he even obtained a Schedule I license, a permit to work and experiment with powerful psychoactive compounds. His interests pivoted somewhat and caused him to focus on MDMA and related psychedelic amphetamines. This move led him to two principle classes of drugs that in his mind had infinite potential: phenylethylamines and tryptamines. By experimenting with these drugs himself, and with a select group of associates, Dr. Shulgin began a methodical process of identification and analysis. He set about to manipulating core chemical structures through a process of chemical substitution and rearrangement. By tinkering with the molecular structure of a parent drug, he was able to create a series of new drugs that while different, shared many of the same principle effects. In some cases, he creates hundreds of these chemical variants, each a psychoactive drug in its own right. His experiments were assiduously reported in his notes. These notes were then converted into text that was published in his books. His formulas for drug synthesis were also published in his books, achievements that earn them "cookbook" status.
The phenylethylamines are a diverse family of drugs that lead ultimately to substituted phenethylamines and a series of substances that have MDMA-like effects. Many of these drugs have erupted into the designer drug world. The same holds true for tryptamines, a class of drugs that was immensely popular in the 60s and 70s. The designer drug craze has pushed these substances back into the light. DMT, dimethyltryptamine, is the most commonly encountered tryptamine on the street today. Its effects are more LSD- like than they are ecstasy-like. In any event, both classes of drugs possess potent psychedelic and mind-altering effects. And like most experimental drugs, few, if any, of these substances have undergone anything close to rigorous study in humans.
There are few really big personalities that have changed the course of drug use and experimentation in the United States. Sasha Shulgin is certainly one of them.
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November 2011 Mystery Drug: Newest Member in the Campaign Against Pain
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This month's mystery drug is a recent addition to physicians' pain fighting armamentarium of narcotics. And although the drug is in its adolescents, it has already become quite effective. This month's drug is a narcotic, a synthetic analgesic that is controlled under the regulations of the Controlled Substances Act. And although the manufacturer believed the drug was best served by assigning it to Schedule III, the DEA ultimately approved the drug for placement into Schedule II.
This month's drug has some rather unique narcotic analgesic capabilities. Like morphine, hydromorphone, and oxycodone, the drug is a potent agonist of the primary mu opiate receptor. But unlike its analgesic siblings, the drug also is a very effective selective norepinephrine reuptake inhibitor (SNRI). In other words, this month's drug possesses antidepressant actions in addition to its potency as a narcotic. There is only one other narcotic analgesic today with similar powers, an older but less utilized drug called Levorphanol, also known as Levo-Dromoran.
This month's drug was recently approved for the market in an extended release format, a formula designed for use in the treatment of long-term, chronic pain. To that end, the drug appears to work well. This drug joins other well-known narcotics in this type of special pain treatment. And like those other well-known drugs, this month's drug has shown the potential for abuse and diversion. Like Oxycontin, drug abusers can crush up the extended release form of this drug and cause uncontrolled absorption of the drug into the blood stream. And like Oxycontin, there is a potential for overdose and fatal reactions when the time-release matrix of the drug has been disabled. But, Oxycontin has brand recognition on the streets. This month's drug does not even have a nom de guerre; there is no street name for it other than the brand name given to it by its maker. In fact, law enforcement agencies have yet to agree on what the set street price is for this drug. At present, diversion is at worst, sporadic.
This drug was brought to market by pharmaceutical giant Johnson and Johnson in late 2008. The original formula for instant release was available in three different doses: 50, 75 and 100 mg. In the extended release format, the drug is available in concentrations that extend up to 250 mg, with two daily doses typically needed. It is the extended release forms of the drug that attract the interests of drug abusers and dealers. But law enforcement authorities indicate that the reports of diversion of this drug are few; it has not generated the levels of abuse witnessed with Oxycontin or Vicodin.
The name of this drug is a play on its classification as a narcotic and as an opiate. The drug is a synthetic narcotic. In that sense, the drug is similar to other synthetics such as Demerol and methadone. The product's brand name is a twist on its descriptor, "new synthetic" narcotic. It is likely that this drug will continue to grow and take on greater market share in the dynamic, risky business of pain management. With its dual action as an analgesic and SNRI to consider, this medication has seemingly great potential as a long-term therapy in treating chronic pain. Its status as an SNRI will surely help many chronic pain patients who are in a constant battle with depression. The future appears bright for this drug.
Click Here for this month's mystery drug.
For those who are unable to open the link, email medtoxjournal@medtox.com for the answer.
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The Inside Dope
| This new section of the Journal will offer an interesting fact or article to spur conversation around the water-cooler.
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Thank you subscribers. We appreciate your dedicated readership. At MEDTOX we are committed to providing clients with the service and solutions you need to run successful drug testing programs. Our Journal is just one way that we show that commitment. We always encourage feedback from our Journal. Please send your thoughts to medtoxjournal@medtox.com.
MEDTOX Journal MEDTOX Scientific, Inc.
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