Gabapentinoids and Pain

gabapentinoids Feb 27, 2023

Gabapentinoids - you may know these by their names Lyrica, Neurontin, Gralise, among others. The drug is gabapentin. Lyrica is another generation of gabapentin. Not necessarily better, but another option.

These drugs are blessed with few side effects. Extraordinarily rare, someone might become hooked, and therefore, Lyrica is a scheduled drug. A word about scheduling. Scheduling has nothing to do with potency. It has everything to do with abuse. The FDA, and others, believes Lyrica has that potential. In clinical reality, it is almost nonexistent.


Gabapentin–a potent drug, comes in a number of different strengths. The strengths are measured in milligrams. Gabapentin is absorbed poorly, and so the drug is often administered in fairly high doses. Gastro-retentive technology, found in Gralise, improves absorption. This is a newer generation of gabapentin, and has transformed this drug to a more useful molecule. 

Gabapentin works in the central nervous system to decrease certain types of pain, particularly associated with neuropathy, and other types of "nerve" pain. It is not a traditional pain medicine. It is not an opioid. It is not felt to be habit-forming. It is a drug used in combination with other medications which we term "adjunct". It increases the potency of certain opioids, and can cause sedation. We can use the sedating effect to our advantage. In fact, this agent enhances certain stages of sleep that are beneficial to recovery, learning, memory. This drug is particularly helpful with fibromyalgia, back problems, neck problems, and neuropathies. Nerve type pains commonly respond to this drug.

Background of Gabapentin

This drug was found to be useful quite by serendipity over 20 years ago. Gabapentin was originally developed as a seizure medication. A number of pain professionals noted its ability to treat painful entities in the mid 90s. This drug is not labeled for pain, but is labeled for certain diagnoses. Definitely a front line drug in the treatment of a number of painful disease states.

Lyrica, or Pregabalin, is a Second-Generation Gabapentin 

Like it's brother, this drug has a very small potential for habit-forming characteristics. It is, however, a scheduled drug. Pregabalin is associated with very few side effects, but some people become sedated with this drug, complain of blurred vision, and weight gain. The benefits of this drug usually outweigh the side effects. This drug is used for many pain states including nerve pain, and widespread pain. The FDA has labeled this drug for a positive influence on fibromyalgia, among other painful entities. It is a front line drug for adjunct pain care, similar to gabapentin.

A word about potency. 

Potency is the strength of the drug to effect change. Change in effect, side effects, strength, or the ability to grow a mustache, potency is commonly misunderstood. People want a "strong" drug, and they think it will work better. Often, less is better. Decisions to prescribe certain medications are made in the individual's best interest, with the intent on effecting a change, and the experience of few side effects.

In treatment of Neuropathy, the gabapentin type drugs are ideal. Opioids, however, tend to be less effective.


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