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What is the use of gabapentin Ointment? Understanding Compounded Topical Preparations

4 min read

Over half of gabapentin users do not achieve significant neuropathic pain relief from oral versions and often experience unwanted side effects. For these patients, compounded topical preparations, which are similar to a gabapentin ointment or cream, offer a targeted alternative for managing localized nerve pain with fewer systemic side effects.

Quick Summary

Compounded gabapentin creams or gels are used for targeted relief of localized neuropathic pain, such as postherpetic neuralgia and diabetic neuropathy, often minimizing the systemic side effects common with oral gabapentin.

Key Points

  • Compounded, not Standardized: Gabapentin is not available as a standard commercial ointment but is custom-made by compounding pharmacies, typically as a gel or cream.

  • Targeted Pain Relief: Topical gabapentin is designed for localized neuropathic pain, such as postherpetic neuralgia and diabetic neuropathy, providing relief exactly where it is needed.

  • Reduced Systemic Side Effects: A major benefit is minimizing systemic side effects like dizziness and drowsiness, which are common with the oral version, by concentrating the drug at the application site.

  • Mechanism of Action: It works locally by modulating neurotransmitters and inhibiting specific calcium channels to reduce nerve excitability and pain signaling.

  • Combination Formulations: It can be combined with other agents like lidocaine, ketoprofen, or amitriptyline in a compounded preparation for a multimodal approach to pain management.

  • Use with Caution: Proper application to intact skin is crucial, and covering the area with an occlusive dressing can increase systemic absorption and risk.

  • Limited but Promising Evidence: While large-scale clinical trials are lacking, case reports, animal studies, and current clinical use support its effectiveness, especially for patients intolerant to oral gabapentin.

In This Article

Compounded Gabapentin: A Targeted Approach to Pain

Unlike a standard, mass-produced gabapentin ointment, topical gabapentin is a custom-made medication prepared by a compounding pharmacy. It is typically formulated as a gel or cream, designed to deliver the active ingredient directly to a specific area of localized nerve pain. This targeted approach bypasses the gastrointestinal system, resulting in minimal systemic absorption and significantly fewer side effects like dizziness and fatigue that are often associated with oral gabapentin.

Primary Conditions Treated with Topical Gabapentin

Compounded gabapentin preparations are primarily used to manage localized neuropathic pain, a type of chronic pain resulting from damaged nerves. It is important to note that the FDA has not approved this specific topical use, though it is often prescribed off-label based on clinical practice and case reports.

Common conditions treated include:

  • Postherpetic Neuralgia (PHN): Persistent nerve pain that can occur after a shingles (herpes zoster) infection has cleared.
  • Diabetic Neuropathy: Nerve pain, tingling, or numbness that can develop in the extremities due to diabetes.
  • Fibromyalgia: The gel may be used to address localized areas of pain associated with this widespread chronic pain condition.
  • Chronic Localized Musculoskeletal Pain: Including conditions like arthritis, sciatica, and myofascial pain syndrome.
  • Vulvodynia: A condition of chronic vulvar pain. Case reports and small studies have shown promising results for topical gabapentin in managing symptoms.
  • Chronic Pruritus (Itching): Some studies have investigated topical gabapentin for itching associated with chronic kidney disease in dialysis patients.

How Does Topical Gabapentin Work?

When applied to the skin, gabapentin is absorbed locally to target peripheral nerves. While the precise mechanism isn't fully understood, it is believed to work by modulating the release of excitatory neurotransmitters by binding to the alpha-2-delta subunit of voltage-gated calcium channels on neurons. This action reduces the hyperexcitability of the nerves in the affected area, which helps to alleviate the burning, tingling, and hypersensitivity characteristic of nerve pain. The advantage of this topical application is that it can concentrate the therapeutic effect at the site of the pain while minimizing the drug's systemic circulation.

Oral vs. Topical Gabapentin: A Comparison

For patients considering gabapentin, understanding the differences between the oral and compounded topical versions is critical. The choice often depends on the type of pain (localized versus generalized), a patient's tolerability for systemic side effects, and the preference for a targeted treatment approach.

Feature Oral Gabapentin Compounded Topical Gabapentin
Systemic Side Effects Common: dizziness, drowsiness, ataxia, and fatigue. Rare: Low systemic absorption minimizes side effects like drowsiness.
Targeted Pain Relief Generalized: Treats pain throughout the body after systemic absorption. Localized: Delivers medication directly to the affected area.
Primary Use Neuropathic pain (e.g., PHN, diabetic neuropathy), seizures. Primarily localized neuropathic pain and chronic pruritus.
Formulation Tablets, capsules, and oral solution. Compounded creams, gels, or ointments.
FDA Approval Approved for certain conditions. Not FDA-approved; use is off-label and based on compounding pharmacy guidelines.
Drug Interactions Higher risk of interactions with other systemic medications. Lower risk of systemic interactions due to minimal absorption.
Patient Suitability For patients who can tolerate systemic side effects or need widespread relief. For patients who experience intolerable side effects from oral gabapentin or have localized pain.

Formulations and Combinations in Compounded Preparations

Because topical gabapentin is made by compounding pharmacies, the specific formulations can vary greatly. It may be created as a cream, gel, or ointment, often in concentrations ranging from 5% to 10%. To create a multimodal approach to pain management, gabapentin is frequently combined with other active ingredients. These combinations are intended to address different pain mechanisms simultaneously and are tailored to a patient’s specific needs.

Commonly combined ingredients include:

  • Lidocaine: A local anesthetic that provides immediate numbing.
  • Ketoprofen: A nonsteroidal anti-inflammatory drug (NSAID) to reduce inflammation.
  • Amitriptyline: A tricyclic antidepressant sometimes used for nerve pain.
  • Baclofen: A muscle relaxant.

Considerations for Use: What Patients Should Know

Before starting a compounded topical gabapentin product, patients must discuss the potential benefits and risks with a healthcare provider. While the systemic side effects are reduced, certain local precautions are necessary.

Application guidelines:

  • Apply the medication only to clean, intact skin as directed by the prescribing physician and compounding pharmacist.
  • Do not apply to open wounds, cuts, or irritated skin, as this can increase systemic absorption.
  • Wash your hands thoroughly before and after application to prevent accidental transfer to sensitive areas like the eyes, nose, or mouth.
  • Avoid covering the treated area with occlusive (airtight) dressings unless specifically instructed by a doctor, as this can increase systemic absorption and side effect risk.

Potential side effects:

  • The most common side effects are local skin reactions, including irritation, redness, or a burning sensation at the application site.
  • Though rare, minimal systemic absorption can occur, especially if used over large surface areas or on compromised skin. Monitor for any signs of dizziness or drowsiness.

Conclusion: Targeted Relief with Custom-Compounded Gabapentin

Compounded topical gabapentin, though not a commercially available ointment, offers a valuable and highly customized treatment option for managing localized neuropathic and chronic pain conditions. By delivering the pain-modulating effects of gabapentin directly to the affected area, it provides effective, targeted relief with a significantly reduced risk of the systemic side effects common with oral administration. Whether used alone or in a multi-ingredient formulation, it represents an important alternative for patients who have not found success with or cannot tolerate oral therapies. Due to its custom nature, it is crucial to use this medication only under the guidance of a healthcare professional and a licensed compounding pharmacy, such as Bayview Pharmacy which provides specialized compounded medications.

Frequently Asked Questions

It is used for treating localized nerve pain (neuropathic pain) from conditions such as postherpetic neuralgia, diabetic neuropathy, fibromyalgia, and chronic musculoskeletal pain. Compounding allows for customized preparations like creams or gels.

Topical gabapentin is preferred for localized pain, especially for patients who experience significant side effects from the oral version, such as dizziness or sleepiness. The topical form provides targeted relief with minimal systemic absorption.

When applied topically, the gabapentin is absorbed into the skin to affect peripheral nerves. It modulates nerve activity by blocking calcium channels and reducing the release of pain-signaling neurotransmitters at the site of application.

The most common side effects are local skin reactions, including irritation, redness, or a burning sensation. Systemic side effects are rare due to low absorption but can occur if the medication is used improperly.

No, compounded gabapentin preparations require a prescription from a healthcare provider and must be prepared by a specialty compounding pharmacy. They are not commercially available over the counter.

Apply a thin layer to clean, dry, intact skin over the affected area as directed by your healthcare provider. Avoid applying it to open wounds, cuts, or irritated skin, and wash your hands after use.

The onset of relief varies by individual and condition. Some people may experience relief shortly after application, while others may require several weeks of consistent use for maximum effect.

References

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Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.