Gabapentin works by affecting certain neurotransmitters in the brain, specifically by modulating the action of the neurotransmitter gamma-aminobutyric acid (GABA), though its exact mechanism is not entirely understood. It was initially developed as a treatment for epilepsy and is structurally similar to GABA, but it doesn’t directly act on GABA receptors. Instead, it binds to a specific subunit of calcium channels in the brain (the α2δ subunit), which helps to reduce the release of excitatory neurotransmitters like glutamate.
Here’s how it’s believed to work for various conditions:
- Seizures: Gabapentin reduces excessive neural activity in the brain, which can help prevent seizures.
- Nerve Pain: By reducing the release of certain neurotransmitters, gabapentin can lessen the sensation of pain, especially in cases of nerve-related pain (neuropathy), which can be persistent and hard to treat with typical pain relievers.
- Anxiety and Mood Disorders: Gabapentin may have calming effects for some individuals, likely by influencing neurotransmitter release. While it’s not an approved anxiety treatment, some doctors prescribe it off-label for this purpose.
Gabapentin usually has a delayed onset of action, taking several days to weeks to reach therapeutic levels, and works best when taken consistently as prescribed.
Neuropathic pain is a common and potentially treatable cause of considerable lifelong morbidity. Effective pharmacological treatments are scarce, but one group of drugs that has shown promise is the antiepileptics.
Gabapentin has become popular as a first-line treatment for neuropathic pain because of its efficacy as an antineuropathic agent and relatively benign side-effect profile. However, its mechanism of action is far from clear.
Neuropathic pain is pain coming from damaged nerves. It differs from pain messages carried along healthy nerves from damaged tissue (a fall, cut, or arthritic knee). Neuropathic pain is treated by different medicines than pain from damagedtissue. Medicines like paracetamol or ibuprofen are not effective in neuropathic pain, while medicines that are sometimes used to treat depression or epilepsy can be very effective in some people with neuropathic pain. Our understanding of fibromyalgia (a condition of persistent, widespread pain and tenderness, sleep problems, and fatigue) is poor, but fibromyalgia can respond to the same medicines as neuropathic pain.
Glutamate is also involved in transmitting pain signals in the brain and nervous system. As gabapentin reduces the release of this neurotransmitter it can also be used to treat nerve pain occuring as a result of damage to or a disturbance in the function of nerves (neuropathic pain)
The way in which gabapentin works is not fully understood. It is thought to work by binding to calcium channels found on nerve cells in the brain and spinal cord. This is thought to affect the release of various neurotransmitters from these nerve cells.
Neurotransmitters are natural body chemicals that are stored in nerve cells. They are involved in transmitting messages between the nerve cells. Gabapentin is thought to reduce the release of a neurotransmitter called glutamate.
Glutamate is a neurotransmitter that acts as a natural ‘nerve-exciting’ agent. It is released when electrical signals build up in nerve cells and subsequently excites more nerve cells. It is thought to play a key role in causing epileptic seizures. Reducing the release of glutamate from the nerve cells in the brain is thought to help stabilise the electrical activity in the brain and prevent epileptic fits.
Gabapentin is used to prevent partial seizures, and partial seizures that spread to secondary generalised seizures.
Glutamate is also involved in transmitting pain signals in the brain and nervous system. As gabapentin reduces the release of this neurotransmitter it can also be used to treat nerve pain occuring as a result of damage to or a disturbance in the function of nerves (neuropathic pain). It probably works in other ways in this area as well.
How Does Gabapentin Work?
Gabapentin is a medication primarily used to treat nerve-related conditions such as neuropathic pain, seizures, and sometimes anxiety disorders.
- Gabapentin (Neurontin) is FDA approved to treat seizures and nerve pain from shingles. It has many off-label uses as well, including treatment for alcohol use disorder and anxiety.
- We don’t know exactly how gabapentin works. But we know it mimics a chemical called gamma-aminobutyric acid (GABA). This chemical quiets brain and nerve activity, which can relieve pain and cause drowsiness.
- How long gabapentin takes to work depends on what you’re treating. For example, you may start to feel the effects of gabapentin for nerve pain within a week. But it can take several weeks to experience the medication’s full effects.
Its exact mechanism of action isn’t fully understood, It’s not exactly clear how gabapentin works to treat various health conditions. But we know that gabapentin mimics a brain chemical called gamma-aminobutyric acid (GABA). GABA slows down, or quiets, brain and nerve activity. This is thought to relieve nerve pain, decrease anxiety, and prevent seizures — among other functions. Here’s what we know about how it works:
1. Structure and Function
- Gabapentin is structurally similar to the neurotransmitter gamma-aminobutyric acid (GABA), but it does not act directly on GABA receptors.
- Instead, it interacts with voltage-gated calcium channels, specifically binding to the α2δ subunit. This reduces calcium influx into nerve cells.
2. Effects on Neurotransmission
- By modulating calcium entry, gabapentin decreases the release of excitatory neurotransmitters like glutamate, substance P, and noradrenaline.
- This dampens overactive nerve signals, which can lead to reduced pain perception or seizure activity.
3. Applications
- Neuropathic Pain: Gabapentin reduces the hyperexcitability of nerve cells, which is a hallmark of chronic pain conditions.
- Seizures: It helps stabilize electrical activity in the brain, reducing the likelihood of seizure episodes.
- Off-label Uses: Gabapentin is sometimes used for conditions like anxiety disorders, migraines, and fibromyalgia.
4. Notable Characteristics
- Gabapentin does not interact with opioid receptors, making it distinct from traditional painkillers.
- It is generally well-tolerated but can cause side effects like dizziness, fatigue, and sedation, particularly at higher doses.
While mimicking GABA can have several positive effects, it can also cause side effects such as drowsiness. People who have trouble sleeping may welcome drowsiness, but it can also make it more difficult to complete daily tasks.