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NAME THAT DRUG


SUBMITTED BY MEDTOX LABORATORIES


Mystery Drug: Iconic Drug Qualifies as Godfather of Sedatives


A


significant clue can be found in the title of this month’s mystery drug essay. Tis month’s drug has been


a tour de force in the genre of sedative, anxiolytic, and muscle relaxant medicines. Te drug has been utilized in the American healthcare system for over 50 years; it is considered a front line drug for treating a variety of medical conditions. And it was serendipity that led to its discovery. Tis drug was hatched as an unexpected consequence of a commercial chemistry experiment that had gone awry. And since this drug’s approval by the FDA, there have been dozens of second, third, and fourth generation sibling drugs that have been in- troduced to market. Tis month’s drug has beaten the odds of time. It is still a relevant, standard of care therapy despite the devel- opment of newer, more powerful drugs that followed it. Tis month’s drug is a Schedule IV controlled substance. It is not a narcotic. It is not a barbiturate. It is capable of caus- ing drug dependence if it is used chroni- cally over an extended period of time. Te drug has a devoted, albeit small, population of people who use it recreationally. By now there are readers who have


seized on the early clues and have ac- curately identified this drug. For those readers who are still stumped, let us move on. As mentioned, this drug is a sedative. It has a profound effect in the alleviation of anxiety and emotional tension. It also has direct effects in reducing the effects of skeletal muscle spasm. As an anxiolytic, this drug presents special utility in treating alcoholic withdrawal. Compounded with clidinium—an anti-cholinergic smooth gut relaxant—the drug can also be used to treat irritable bowel syndrome and various other spastic conditions of the gut. An- other interesting application for this drug involves its pharmaceutical combination


56 datia focus


with amitriptyline, a widely used tricyclic antidepressant. In this formula, our mystery drug boosts the net effects of the tricyclic by reducing anxiety and boosting mood. Tis drug was propelled into the market precisely for its value as an alternative to barbituric acid and barbiturate products, the drugs of their day that were used to ease anxiety, reduce spasm, and induce sleep. Te drug’s side effects and overall safety profile were a significant improvement over the other sedative drugs of its day. Early experiments with the drug proved it to be capable of reversing most of the more onerous symptoms caused by anxiety, ten- sion, and alcohol withdrawal. Te drug also established itself as a potent anticonvulsant. Te drug achieves these effects through enhancement of central and peripheral GABA (gamma amino butyric acid) action. Te substances that were borne out of the chemical formula for this month’s drug all do the same. Trough modulation of GABA, these drugs all achieve the same net effects of stress and tension reduction, along with skeletal muscle relaxation. In higher doses, the drug can induce sleep, but its effects are less hypnotic than they are anxiolytic. Nearly all the drugs in this family have a liability for dependency and addiction if they are used indiscriminately. As mentioned, this month’s mystery


substance is an abused recreational drug, mostly in the form of a “combo” with other sedatives, or as an antagonist to powerful stimulants, such as methamphet- amine and cocaine. In the eastern United States, the drug is frequently partnered with methadone, a potent analgesic and standard therapy in the treatment of opi- ate addiction and dependency (narcotic substitution therapy). Tis month’s mystery drug exhibits a long half-life, a characteristic that adds


to its efficacy in the treatment of anxiety disorders. Because of its extended half-life, patients who take this drug may test posi- tive through urinalysis for five or more days beyond its last use. Patients treated with the drug must also be aware of the potent effects that occur when taken with alcohol. When combined with alcohol, this month’s drug can lead to exaggerated symptoms of intoxication. In the 70s and 80s, a popular recreational drug habit involved the partnering of this drug with a mixed property synthetic narcotic called Talwin (pentazocine). In those instances, the drug was utilized as a chemical sub- stitute for a drug called Doriden, a more potent sleeping pill of those times. As Doriden became scarcer on the streets, the month’s drug was inserted as a cheap and widely available stand-in; ultimately, the popularity of the Doriden and Talwin (T’s and Blues) drug combination wore off and this month’s drug retired into a quiet, unassuming pharmaceutical life. Someone under the influence of this


month’s drug will exhibit sublime symp- toms of intoxication. Te typical clinical dose ranges from 5 to 25 milligrams (4-6 hours) depending on the nature of the condition being treated. For instance, mild cases of generalized anxiety disorder may warrant a lower dose of the drug; moder- ate to moderately severe cases of alcohol withdrawal may require a substantially higher dose. Te drug is available in capsule form in both generic and brand formulas. A liquid preparation is manufactured mainly for use in treating alcoholic withdrawal. At lower doses and wider intervals of admin- istration, the signs of intoxication will be difficult to detect. When intoxication is noticeable, DAR & DRE signs will include some or all of the following: • Horizontal gaze nystagmus (present)


spring 2012


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