The Pharmacokinetic Action of Gabapentin

Knowing the how a drug works in the body is important in evaluating the usefulness of new anticonvulsant drugs. It helps doctors and drug manufacturers understand how it can affect different parts of the body. With this, they are able to adjust the chemistry of the drug to improve its performance or remove unwanted side effects. (1)

Gabapentin is the generic version of Neurontin. It is a drug used to prevent and control seizures. The drug can be taken on its own or as an adjuvant to other anti-seizure medications. Aside from that, it can also be consumed to alleviate neuropathic pain (nerve pain) in adults.

Two of its known unverified uses include treatment for migraines and insomnia. However, although not a controlled substance, Gabapentin has also been the subject of substance abuse. Known on the streets as the “gabbies,” some have been taking advantage of this drug’s side effects to feel euphoria.

Understanding Epilepsy and Neuropathic Pains

To fully understand how Gabapentin works, you must first know and understand the diseases it aims to prevent: epilepsy and neuropathic pains.

Epilepsy is a disorder rooted in the nervous system. It causes the sufferer to become unconscious suddenly and to have violent and uncontrolled movements in the body. If we think of it in terms of electricity, epilepsy is like your body short circuiting. (2)

Now, let’s discuss neuropathic pains. This happens when the nervous system or nerves undergo an abnormally quick rate of degeneration. It is usually linked to other diseases such as herpes, shingles, or even diabetes.

As you can observe, both the diseases Gabapentin treats are problems mainly on the nervous system, giving you an idea of how this drug works.

How Is Gabapentin Processed by Your Body?

Gabapentin is handled in the same way other drugs are processed by the body. Once you take the recommended dosage of Gabapentin, it goes to the stomach where it is broken down.

Then, it is absorbed in your intestines. The blood vessels carry the absorbed Gabapentin along with the other nutrients to the liver. Now, the drug goes through a “screening process.” As it is a foreign object, the liver will do its job and block a certain amount of it.

Once transported into the brain, Gabapentin will stabilize the electrical impulses that fire within the central nervous system. Now, the way neurotransmitters send messages to the brain is now affected. (3)

Gabapentin does that by altering the amount of GABA, a “nerve-calming” agent produced by the body. At the same time, it inhibits the production of glutamate, a “nerve-exciting” agent. This neurotransmitter is said to be the reason why epileptic seizures happen.

Why Are There Side Effects?

Although quite effective in preventing epileptic seizures, it comes with a number of side effects that may range from very mild to severe. Some of them happen simply as a result of how the drug works.

Drowsiness – Knowing already what GABA and its function in your body, it makes sense to feel drowsiness as an effect. It is the reason why some have also used it to cure insomnia. What GABA does is basically calm the brain, thus the drowsiness.





Suicidal thoughts – Gabapentin is a depressant. Especially if the one who takes it already has a history of mood swings or even depression, he is prone to have suicidal thoughts when under the influence of this drug.

Gabapentin has been used for many decades now. However, more researches are still needed to verify its pharmacokinetic actions completely. There are still some uncertainties on how this drug works. Nevertheless, although not entirely understood, most doctors still prescribe it due to its effectiveness.

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