Toxicology Corner: News on Narcotics and Naloxone

Toxicology Corner: News on Narcotics and Naloxone

POSTED IN: Fall 2016, Toxicology,

Evan Schwarz, MD, FACEP

Articles about substance abuse dominate both the mainstream media and medical literature. Generally, these focus on designer drugs such as K2, bathsalts or heroin. Lately, the focus has shifted to designer opioids and a much more potent medicinal opioid, fentanyl.

While abuse of fentanyl is not a new problem, heroin is increasingly being cut with fentanyl. Seizures of drugs containing fentanyl more than tripled between 2013 and 2014. This is occurring for multiple reasons,  fentanyl is cheap and potent, nearly 100 times more powerful than morphine. It also allows narcotics to be shipped in smaller volumes making distribution easier and is extremely easy to make (for drug dealers, at least).

There are some ominous consequences of this adulteration. Overdosing is much easier as users do not realize the potency of what they think is ‘just heroin.’ This has lead to an increase in the number of fatalities from heroin. Between 2005-2007, there were more than 1,000 deaths in the US from heroin adulterated with fentanyl. Pills have also been adulterated with fentanyl. Recently in California there were multiple deaths after fentanyl was compounded into pills and sold as oxycodone. While you might think this would cause users to be more hesitant, they see this potency as a good thing even if it carries a substantial risk of overdosing. Unfortunately, dealers also realize people overdosing from their product is actually good for business as it shows their product is incredibly potent. Fentanyl derivatives, including acetyl fentanyl and carfentanil, are also increasingly being found in heroin. Carfentanil is approximately 10,000 times as potent as morphine. It can be used to tranquilize elephants and was used by Russian authorities in 2002 when rebels took over a movie theater.

In addition, new designer opioids are causing substantial morbidity and mortality. U-47700 was developed in the 1970s as part a project to develop a non-addicting alternative to morphine.  Currently, it is available online for as little as $40 since it is sold as a research chemical. W-18, also known as “beans” or “shady 80s,” was developed as an analgesic but never marketed for therapeutic use. It is one member of a group of 32 compounds developed in Alberta in the 1980s and is the most toxic of the “w-series.” In addition to being sold as a designer drug, it has been sold in pill forms masquerading as oxycodone, which is problematic since the drug is much more potent, nearly 100 times that of fentanyl. Like many of the designer drugs, it most likely is being synthesized in labs in China and being imported into Canada and the US. It is unclear, though possible, that larger doses of naloxone will be required to reverse respiratory depression from these drugs.

Luckily, changes with naloxone should increase its availability. First and foremost, there are now two prescription products on the market. One is an injection device that is similar to an epipen that gives verbal instructions. The other is an intranasal device, which may make prescribers and users more comfortable as it is needleless. Availability is the biggest issue. Unfortunately, not all pharmacies carry naloxone. Those that do may not keep it in stock, but most of the bigger chains can get it within a day or two. Hopefully as it is prescribed more, pharmacies will begin to keep it on the shelf. Another deterrent is the cost; both products are rather expensive. Hospitals could easily make their own naloxone kit with an atomizer. While it could not be given directly to a patient due to Missouri law, hospitals with mobile pharmacies could give high-risk patients this prior to discharge. Also in August, the Governor signed into law a bill that allows pharmacists to prescribe and distribute naloxone without requiring a prescription from a physician.

Just as always, the drug landscape continues to change. This has led to the development of some very potent and dangerous opioids. Luckily, changes with naloxone will hopefully make it more available as our patients are likely to continue to need it.