Gabapentin

What Does Gabapentin Do?

Gabapentin is a medication primarily utilised for the treatment of seizures, nerve pain, and restless legs syndrome. Off-label uses of this drug include treatment for anxiety disorders, bipolar disorder, and insomnia.

How Does Gabapentin Work? (the complicated stuff)

Gabapentin regulates neuron activity by targeting the alpha-2-delta subunit of voltage-controlled calcium channels situated in the brain and spinal cord. This process minimises the dissemination of certain neurotransmitters such as glutamate, affiliated with pain perception and epileptic impulses. Consequently, nerve excitability is reduced, resulting in a decrease in pain signals and seizure episodes.

Drug Type and Category of Gabapentin

Gabapentin is classified as an anticonvulsant medication, specifically a gamma-aminobutyric acid (GABA) analogue.

What dosage of Gabapentin should you be taking? ¹

General Dosage Guidelines

• Initial Dose: Typically starts at 300 mg taken orally once in the evening.
• Titration: The dose is gradually increased based on patient response and tolerance.

Partial Seizures:

• Recommended Dosage: 300 to 1200 mg taken orally three times daily.
• Maximum Daily Dosage: 3600 mg.

Postherpetic Neuralgia:

• Recommended Dosage: 300 to 600 mg taken orally three times daily.
• Maximum Daily Dosage: 1800 mg.

Neuropathic Pain:

• Recommended Dosage: 300 to 1200 mg taken orally three times daily.
• Maximum Daily Dosage: 3600 mg.

Fibromyalgia:

• Recommended Dosage: 400 to 800 mg taken orally three times daily.
• Maximum Daily Dosage: 2400 mg.

Restless Legs Syndrome (Gabapentin Enacarbil):

• Recommended Dosage: 600 mg taken orally once daily.
• Maximum Daily Dosage: 1800 mg.

Dosage adjustments are necessary for patients with renal impairment. 

For example:

• Creatinine clearance of 30-59 mL/min: 200 mg to 700 mg twice per day.
• Creatinine clearance of 15 mL/min or less: 100 mg to 300 mg once daily.

Tapering: When discontinuing gabapentin, it should be tapered over a period of at least one week to avoid withdrawal symptoms. It can be hard to come off gabapentin, and many people will still experience pain even while taking gabapentin. However, it is necessary to come off and long-term use is not recommended. 

What are the side-effects of Gabapentin?

Common Side Effects:

• Drowsiness: One of the most frequent side effects, gabapentin can cause drowsiness or sedation.
• Dizziness: Some people experience dizziness or lightheadedness, which can affect balance and coordination.
• Fatigue: Gabapentin may cause tiredness or a general sense of fatigue.
• Peripheral Edema: Swelling of the hands, feet, or legs can occur.
• Weight Gain: Increased appetite and subsequent weight gain are possible side effects.
• Coordination Problems: Difficulty with coordination or unsteadiness can be a concern, particularly in the elderly.

Less Common Side Effects:

• Dry Mouth: Gabapentin can cause a dry mouth in some people.
• Nausea and Vomiting: Gastrointestinal symptoms like nausea or vomiting may occur.
• Blurred Vision: Some individuals report visual disturbances, including blurred vision.
• Memory Problems: Difficulty with memory or cognitive function can be a side effect.
• Mood Changes: Changes in mood, including feelings of depression or anxiety, have been reported.
• Rash: Skin rashes or itching can occur, though they are less common.
• Tremors: Involuntary shaking or tremors may be experienced by some people.
• Sleep Disturbances: Gabapentin can sometimes cause sleep disturbances or vivid dreams.

Serious Side Effects:

• Severe Allergic Reactions: Rare but serious allergic reactions, including swelling of the face, throat, or tongue, can occur.
• Suicidal Thoughts: Antiepileptic drugs, including gabapentin, have been associated with an increased risk of suicidal thoughts and behaviors.
• Respiratory Depression: Although rare, high doses can lead to respiratory issues.

Drug Interactions

Common Drug Interactions

Gabapentin can interact with various medications, particularly those that affect the central nervous system (CNS). Some frequently reported interactions include:

• CNS Depressants: Increased risk of sedation and respiratory depression when combined with:
• Opioids (e.g., Norco, oxycodone)
• Benzodiazepines (e.g., Xanax, diazepam)
• Muscle relaxants (e.g., Flexeril)
• Antidepressants (e.g., Cymbalta, Zoloft)
• Antiepileptic Drugs: While gabapentin generally has a low profile of interaction with other antiepileptic medications, caution is advised when used with:
• Topiramate (pharmacodynamic interaction)
• Phenytoin and carbamazepine (some reports indicate potential interactions).
• Antacids: Certain antacids containing aluminum or magnesium may decrease gabapentin absorption if taken simultaneously.
  

Natural Alternatives to Gabapentin

Physiotherapy, osteopathy and other manual therapies are key to help patients naturally recover from nerve pain and chronic pain. Working with a therapist over several weeks or months is important and necessary as a way to naturally relieve pain without the need for drugs. Exercise therapy, lifestyle coaching and healthy living are key parts of the recovery. 

Some other natural alternatives include: 

Boswellia (Frankincense): Used in Ayurvedic medicine to treat arthritis, inflammation, and reduce brain swelling. ² Boswellia has anti-inflammatory and neuroprotective effects.

Ginkgo Biloba: The extract EGb 761 has shown benefits for neuropathic pain in animal studies, likely due to anti-inflammatory, antioxidant and neuroprotective effects. ³ It reversed diabetes-induced nerve pain in rats.

Cannabidiol (CBD): A natural 17-amino acid molecule called CBD3 specifically binds and deactivates the Cav2.2 calcium channel, which is involved in pain signaling. ⁴ A synthetic compound called CBD3063 that mimics this effect is being researched as a non-euphoric alternative to gabapentin.

Ginger Root: Ginger has potent anti-inflammatory and antioxidant properties that may help with nerve pain. ⁵ It's a rhizome of the Zingiber officinale plant.

Acupuncture: This ancient Chinese practice involves inserting thin needles into the skin at specific points. It may relieve pain by reducing inflammation and increasing natural pain-relieving chemicals. ²

Interesting facts about Gabapentin

Gabapentin is also used in veterinary medicine to treat pain, anxiety, and seizures in pets, indicating its broad applicability beyond human medicine.

Gabapentin was originally developed as an antiepileptic drug to treat seizures. It was approved by the FDA in 1993 for this use and has since been found useful for a variety of other conditions, and most commonly now used to help reduce nerve pain. 

Disclaimer

This article is generated for informational purposes only. It was created in December 2024. Medications and medical guidance can change over time. Therefore, it is essential to consult with your general practitioner or healthcare provider before making any decisions regarding medications or treatment plans. Your GP can provide personalised advice based on your specific health needs and conditions.

References:

1. https://bnf.nice.org.uk/drugs/gabapentin/
2. https://www.healthline.com/health/pain-relief/surprising-natural-pain-killers
3. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5960749/
4. https://www.kevinmd.com/2024/01/euphoria-free-pain-relief-a-gabapentin-alternative-youve-been-waiting-for.html
5. https://lyphe.com/natural-remedies-for-nerve-pain/