By Kathleen Doheny
WebMD Health News
In the wake of the opioid epidemic, doctors and patients are turning to other medications to ease pain.
Some experts say that may be leading to another painkiller problem–the off-label overprescribing of drugs known as the gabapentinoids. These include gabapentin (Neurontin, Gralise) and pregabalin (Lyrica).
The FDA has approved these drugs for seizures and certain pain conditions including nerve pain caused by shingles (postherpetic neuralgia), fibromyalgia and nerve pain linked with diabetes or spinal cord injuries. However, as doctors look for alternatives to the opioids, the use of the gabapentinoids has skyrocketed. In 2016, 64 million gabapentin prescriptions were dispensed, compared to 39 million in 2012. Sales of Lyrica more than doubled from 2012 to 2016.
FDA Commissioner Scott Gottlieb, MD, said in February that the agency is concerned about the possible misuse and abuse of gabapentinoids in the wake of the opioid epidemic and is tracking the issue.
WebMD asked Jeffrey Fudin, PharmD, managing editor of PainDR.com and adjunct associate professor of pharmacy practice and pain management at the Albany College of Pharmacy & Health Sciences, to elaborate on the drugs and their use and misuse.
WebMD: Can you discuss a brief history of these drugs?
Fudin: Gabapentinoids are drugs originally developed as anticonvulsants. They affect particularly neuropathic pain, because neuropathic pain is caused by damaged nerves. Think of damaged nerves as synonymous with electrical wires. Electrical wires have charges. The drugs stabilize the electroconductivity of the nerves.
WebMD: Why are gabapentinoids being prescribed more? Are doctors turning to them or are patients requesting them?
Fudin: Prescribers are shying away from opioids and/or reducing doses for many reasons. One is because they are beginning to acknowledge the very real dangers associated with opioids. Another is because of heightened awareness around necessary risk mitigation strategies, many are intimidated by opioids or they feel unqualified [to prescribe them]. Some fear regulatory scrutiny, and others are fearful of lawsuits. All of these things have contributed to prescribers looking for opioid alternatives, or to lower doses and add-on non-opioids to maximize benefits by combining one or more medications that treat pain by variable mechanisms, the combination of which is often better than any single agent. Patients also are requesting alternatives.
WebMD: Why are these drugs suddenly being abused?
Fudin: These drugs alone are not uniquely suddenly being abused. We shouldn’t lose that in this discussion. Other drugs are starting to be abused as well. People are looking to other drugs [for pain relief] as it is getting more difficult to obtain prescription opioids.
WebMD: What other medications besides the gabapentenoids are doctors prescribing if they cut down on or eliminate opioids?
Fudin: Others include anticonvulsants other than the gabapentinoids, anti-inflammatories, and certain antidepressants that have shown benefit for generalized and neuropathic pain syndromes such as duloxetine (duloxetine), milnacipran (Savella), and venlafaxine (Effexor). All three of these drugs classes are commonly used in combination with or without opioids.
WebMD: What is the danger with the gabapentinoids?
Fudin: I think generally they are pretty safe drugs if taken as prescribed. But people abuse them and take them in high doses.
Let’s say a patient is on a legitimate opioid prescription and overuses and can’t get more, or a state has a new regulation, saying cut the daily dose. So the patient says, ‘I have a gabapentinoid, I’ll take more of that.’ [Patients may have prescriptions for both.]
When you start combining high doses with these other drugs, you have problems. When you start taking drugs on top of each other it can lead to respiratory depression.
Too high of a dose [of gabapentenioids] can cause dissociative effects. For example, you can’t connect things you normally can, such as you go to pick up something and your hand doesn’t go where it needs to go. That’s just one example of disassociation.
Too much can also cause sedation. It can cause you to fall and become confused.
WebMD: Are gabapentinoids addictive?
Fudin: No. Gabapentinoids are neither physically or psychologically addicting. But, if a person takes high-doses of gabapentinoids regularly and abruptly stops them, there could be withdrawal symptoms to physical dependence, so a taper is in order. We see a similar situation with antidepressants, beta blockers, and many other drugs that should not be abruptly discontinued. It is important to note that physical dependence and addiction are not the same. Patients on opioids that are coming off of them also need to be tapered to prevent withdrawal symptoms but that is not synonymous with addiction.
WebMD: Is it Ok to drink alcohol when taking gabapentinoids?
Fudin: I tell patients to avoid alcohol when taking gabapentinoids and there is a warning in the label consistent with that recommendation. The reality is that people do [drink], so they should be aware that if this occurs it should be in the safest environment possible. If a patient is on a low dose of gabapentin and has an occasional glass of wine or one beer, that is generally okay.
WebMD: What advice would you give about the gabapentinoids?
Fudin: People need to be careful about taking high doses. I would say nothing over 3,600 milligrams a day of gabapentin. Pregabalin, nothing over 600 mg a day.