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BY AMY GALLUP, QUEST DIAGNOSTICS Mother’s Little Helper A


few years after the Food and Drug Administration’s (FDA) approval in the 1960s, this month’s mystery


drug quickly became one of the most commonly prescribed medications in the world. By the 1970s, two billion tablets of the mystery drug were sold in the United States alone, earning it the mark of the country’s highest selling medication from 1969–1982. Doctors preferred prescribing this drug over other psychotropic medications due to its initial calming effects, low toxicity and reduced chance of fatalities caused by overdose. Medical professionals and the general public greatly supported use of the mystery drug, and its popularity helped to launch Hoffmann-La Roche into becoming one of the largest pharmaceutical companies worldwide. During the 20th century, Hoffmann-La


Roche set out to improve on psychotropic drugs used as treatments for common psychological diseases including anxiety disorders and schizophrenia. Dr. Leo Sternbach, who was employed as a chemist for the company, discovered a compound that produced favorable antipsychotic effects. Its success in clinical applications led to the synthesis of analogs, which could potentially improve on the actions of the parent compound. Tis month’s mystery drug was the second agent developed by Sternbach and it proved to have several beneficial properties. With an increased potency, onset of action and an absence of a very biter aſtertaste, the mystery drug quickly replaced its predecessor and became the go-to psychotropic agent in the United States. Te mystery drug is commonly


prescribed for the treatment of anxiety, muscle spasms, seizures, sleep disorders and symptoms of alcohol withdrawal. Typically, this drug is administered as


56 datia focus


tablets, extended-release capsules or in liquid form and can be taken with or without food. Te circular tablets have a “V” scored in their center and the dosage usually comes in 2, 5 and 10 milligram (mg) unites. An adult dose to treat anxiety and seizures may range from 2 to 10 mg taken two to four times daily. If prescribed to treat alcohol withdrawal symptoms, then a 10 mg dose is taken three to four times for the first 24 hours and reduced to 5 mg taken three or four times daily or as needed. Aſter oral ingestion, 90% of the mystery drug is absorbed and peak plasma levels will occur from 15 minutes to 2.5 hours. Delays can be seen if administered with high-fat meals as opposed to fasting. Excretion of the mystery drug is mainly through urine which produces several significant metabolites, many of which are therapeutic drugs in their own right. Aſter a single dose, the drug and its metabolites can routinely be detected in urine within 3 days; with detection periods reaching several weeks based on dose, length of usage and differences in metabolism. Laboratory detection can be performed by an immunoassay (initial screen) followed by gas chromatography mass spectrometry (GC-MS) or liquid chromatography tandem mass spectrometry (LC-MS/MS) to confirm the presence of the drug. Due to the low potential for abuse and


its accepted use in medical applications, the mystery drug is a Schedule IV narcotic under the Controlled Substances Act. However, abuse of this drug, especially with opioids, has become increasingly common. According to SAMHSA, use of the mystery drug in combination with opioids caused a substantial increase in patients who were admited to drug treatment programs between 2000 and 2010. Additionally, abuse has also been observed in combination with stimulant


use. For instance, the mystery drug is effective against cocaine-associated chest pains and also eases withdrawal symptoms aſter a cocaine binge. Tis month’s drug works by


increasing the effects of an inhibitory neurotransmiter (GABA) that moderates the activity of nerve signals in the central nervous system. It is highly habit-forming and is only intended for short-term use. Common side effects include drowsiness, fatigue, muscle weakness and clumsiness. More extreme side-effects include cognitive and mobility impairment and both should be monitored closely, especially in older patients. Abrupt discontinuation of treatment should be avoided to prevent severe withdrawal symptoms such as tremors, abdominal and muscle cramps, vomiting, sweating and insomnia. Tese symptoms usually only occur in those who have taken the medication in excess or for extended periods of time. Terefore, a gradual decrease in dosage is recommended prior to discontinuing the use of the mystery drug. Patients taking this drug should also be advised not to drink alcohol or take other medications that depress the central nervous system. Hazardous activities that require complete mental awareness, including driving a vehicle or operating heavy machinery, should not be atempted by the user. Interestingly, common consumables such as grapefruit and grapefruit juice may cause unwanted side effects and should be avoided when taking this drug. Grapefruit juice is known to inhibit the metabolism of the mystery drug and increase its concentration in the bloodstream; therefore patients should consult their doctor before consuming. Notably, Te Rolling Stones, an English


rock band, released a renowned song entitled “Mother’s Litle Helper” that


summer 2016


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