Conway McLean, DPM, Journal columnist

The attention directed at the opioid epidemic has been considerable of late, a consequence of the many deaths and hospitalizations resulting from its abuse. Too often, some injury or surgical procedure necessitates a prescription for pain, treated with one of the many prescription opioids. Should the pain continue, or an addiction develop, desperate measures are sometimes taken. Another example of careless, inaccurate marketing claims leading to overuse and misuse.

When it comes to pain relief from a chronic condition, there are few options. Most frequently utilized are the non-steroidal anti-inflammatory drugs, available without a prescription for decades. Like any medication, these have their complications and side effects. And they were never meant to be used on a long term, semi-permanent basis. But they are extremely accessible, found in every gas station and pharmacy. The most frequently encountered examples in commercial products are ibuprofen and naproxen (in all their numerous iterations).

A drug developed in the 70’s received approval in 1993 as a muscle relaxant and an anti-spasmodic. The drug was titled gabapentin. Initial marketing efforts painted it as a medication with low potential for abuse. For this and other reasons, it has rapidly grown in popularity and in frequency of use (and misuse). Once touted as being both safe and effective, a growing body of evidence demonstrates the potential risks of overprescribing this ubiquitous pharmaceutical agent.

Gabapentin belongs to a class of drugs indicated for the treatment of partial-onset seizures and post-herpetic nerve pain. These drugs cross the blood-brain barrier and act to mimic the inhibitory actions of certain neurotransmitters, important signaling substances that nerves produce to send information. But numerous uses for the drug have been attempted over the years, often following recommendations from the pharmaceutical industry.

Prescriptions for the drug have risen steadily over the last decade or so, stimulated by industry promotions, recommending these off-label uses. This prescribing of a medication for a condition other than one it’s approved, i.e. “off label,” has been commonplace for years. But there is an element of risk since it means there hasn’t been extensive study of that particular use. Will it work or cause problems, complications?

In 2021, gabapentin was one of the ten most prescribed medications in the US. One study found that one in five adults with chronic pain were provided with a prescription. And the list of uses has continued to grow as well, including anxiety, alcohol use disorder, depression, sleep problems, painful neuropathy, migraines, and more. These uses have been industry driven, despite these applications of the drug being off-label and unapproved. One pharmaceutical manufacturer, Pfizer, was fined over 400 million dollars as a result of illegal marketing of these off-label uses.

Gabapentin misuse was first reported in 1997, but concern has grown since, specifically over the abuse potential. Still, the drug remains federally nonscheduled, widely available, and easily prescribed. Often, it is prescribed in combination with some other agent, typically an opioid, such as for postoperative pain. Or, for anxiety and sleep problems, it is dispensed with a benzodiazepine (e.g. valium).

Despite the lax regulations, we have learned much about these potentially dangerous combinations, with respiratory problems being a common concern. Even when used for legitimate reasons, gabapentin taken in combination with opioids increases the risk of respiratory depression and death. The reactions to the medicine can be severe when the individual has COPD. But there are many other recognized complications which don’t require the concomitant use of another drug. Some more frequently seen include unsteady gait and the falls associated, problems with concentration, mood disturbances, hyperexcitable states, depression, sore throat, and more.

When taken for recreational purposes (obviously not an intended use per the manufacturers of the pharmaceutical), overdosing is not uncommon. Symptoms of an overdose include drowsiness, rapid heartbeat, low blood pressure, dizziness, nausea/vomiting, and impaired coordination. In severe cases, coma and death can occur.

Many practitioners of modern medicine consider gabapentin a relatively benign medication and a safer alternative to many controlled substances. Unfortunately, the drug manufacturers have fostered an inappropriate sense of safety concerning its use because, as is so frequently mentioned, it’s not an opioid. Further complicating the issue is the ease of access: gabapentin is relatively inexpensive and widely available.

Still, most of the evidence for these off-label uses is limited to relatively few, low-quality studies. It boils down to the fact that every prescription medication has potential complications. This is true for gabapentin, of course. Indeed, the more dire consequences occur rarely. But you cannot expect to take ANY medication and have no potential for harmful or negative side effects. It comes with the territory: the human body is a strange, complex thing……and we’re all a little different..

EDITORS NOTE: Dr. Conway McLean is a podiatric physician now practicing foot and ankle medicine in the Upper Peninsula, having assumed the practice of Dr. Ken Tabor. McLean has lectured internationally on surgery and wound care, and is board certified in both, with a sub-specialty in foot orthotic therapy. Dr. McLean welcomes questions, comments and suggestions at drcmclean@penmed.com.