Gabapentin Enacarbil: Uses, Dosage, and Side Effects Explained

Summary of Key Points

Gabapentin enacarbil is a prescription medication commonly used to manage conditions such as neuropathic pain, postherpetic neuralgia, restless legs syndrome, and others. It works by altering the way nerves communicate pain signals to the brain. Unlike standard gabapentin, gabapentin enacarbil is a prodrug, meaning it is specifically designed for improved absorption in the body. Always consult your healthcare provider before starting or adjusting your dosage to ensure safe and effective use.

Medication Names

US Brand Name: Horizant

Generic Name: Gabapentin enacarbil

The generic name refers to the active ingredient in the medication, which is often listed in parentheses alongside the brand name for clarity.

Pharmacologic Category

1. Anticonvulsants
2. GABA analogs

Gabapentin Enacarbil Dosage

Gabapentin enacarbil is prescribed for a variety of conditions, with the dosage carefully tailored to the specific condition being treated. It is essential to follow your healthcare provider’s instructions and consult them before making any changes to your dose. If needed, you can schedule a telemedicine appointment to discuss your treatment plan in detail.

Neuropathic Pain

Initial Dose: 600 mg once daily with food.

Maintenance Dose: 600 mg twice daily with food.

Postherpetic Neuralgia

Initial Dose: 600 mg once daily with food.

Maintenance Dose: 600 mg twice daily with food.

Gabapentin Enacarbil for Restless Legs Syndrome

Initial Dose: 600 mg once daily, taken at approximately 5 PM with food.

Fibromyalgia

Initial Dose: 600 mg once daily with food.

Maintenance Dose: 600 mg twice daily with food.

Diabetic Neuropathy

Initial Dose: 600 mg once daily with food.

Maintenance Dose: 600 mg twice daily with food.

Chronic Pain

Initial Dose: 600 mg once daily with food.

Maintenance Dose: 600 mg twice daily with food.

Anxiety Disorders

Initial Dose: 600 mg once daily with food.

Maintenance Dose: 600 mg twice daily with food.

Migraine

Initial Dose: 600 mg once daily with food.

Maintenance Dose: 600 mg twice daily with food.

Sciatica

Initial Dose: 600 mg once daily with food.

Maintenance Dose: 600 mg twice daily with food.

Dosage Forms and Strengths

Gabapentin enacarbil is available as extended-release tablets in the following strengths:

1. 300 mg
2. 600 mg

Administration Instructions

Gabapentin enacarbil should always be taken with food to enhance absorption. Swallow the tablet whole—do not crush, chew, or split it. If you miss a dose, take it as soon as you remember, unless it is close to the time of your next scheduled dose. In that case, skip the missed dose and continue with your regular dosing schedule. Avoid taking two doses at the same time to prevent potential side effects.

Contraindications

Contraindications are specific conditions or circumstances in which a medication should not be used due to potential risks. If you have any of the following conditions, avoid taking gabapentin enacarbil or consult your healthcare provider for guidance:

1. Severe kidney disease: Gabapentin enacarbil is processed by the kidneys. Impaired kidney function can lead to drug accumulation in the body, increasing the risk of toxicity or adverse effects.
2. Hypersensitivity or allergy to gabapentin: If you have experienced an allergic reaction to gabapentin or its components, taking gabapentin enacarbil could trigger a severe, potentially life-threatening allergic response.
3. Alcohol use: Gabapentin enacarbil can intensify the effects of alcohol, leading to excessive drowsiness, dizziness, or impaired coordination, which may increase the risk of falls or accidents.
4. Respiratory issues: Conditions such as chronic obstructive pulmonary disease (COPD) or sleep apnea may worsen with gabapentin enacarbil due to its potential to cause respiratory depression (slowed or shallow breathing).

Drug-to-Drug Interactions with Gabapentin Enacarbil

Gabapentin enacarbil, a prodrug of gabapentin, has the potential to interact with other medications, which may increase the risk of side effects or reduce the effectiveness of either drug. It is essential to inform your healthcare provider about all the medications you are currently taking, including over-the-counter drugs, herbal supplements, and vitamins. Below are some common medications that may interact with Gabapentin enacarbil:

Opioids: Medications such as oxycodone (OxyContin), hydrocodone (Vicodin), and morphine can amplify the sedative effects of Gabapentin enacarbil. This combination may lead to pronounced drowsiness or, in severe cases, respiratory depression. Use caution and follow your healthcare provider’s guidance when combining these medications.

Antacids: Antacids containing aluminum hydroxide or magnesium hydroxide (e.g., Maalox, Mylanta) can interfere with the absorption of Gabapentin enacarbil, potentially reducing its effectiveness. To minimize this interaction, it is recommended to take Gabapentin enacarbil at least two hours after using an antacid.

Alcohol: Consuming alcohol while taking Gabapentin enacarbil can heighten side effects such as dizziness, drowsiness, and difficulty concentrating. Avoid alcohol or limit its use to reduce the risk of these complications.

Sleep aids or sedatives: Medications like zolpidem (Ambien) and benzodiazepines, including lorazepam (Ativan) and diazepam (Valium), can intensify the sedative effects of Gabapentin enacarbil. This may result in excessive drowsiness, impaired coordination, or difficulty performing daily activities. Always consult your healthcare provider before combining these medications.

Gabapentin Enacarbil and Pregnancy

Is it safe to take Gabapentin enacarbil during pregnancy?

The safety of Gabapentin enacarbil during pregnancy is not fully established. While animal studies suggest there may be potential risks to the developing fetus, data on its use in pregnant women are limited. Gabapentin enacarbil should only be used during pregnancy if the potential benefits to the mother outweigh the potential risks to the baby. If you are pregnant or planning to become pregnant, it is crucial to discuss your treatment options with your healthcare provider to determine whether Gabapentin enacarbil is appropriate for your situation.

Gabapentin Enacarbil While Breastfeeding

Is it safe to take Gabapentin enacarbil while breastfeeding?

Gabapentin enacarbil can pass into breast milk, and its effects on nursing infants are not yet fully understood. Although some studies suggest that gabapentin levels in breast milk are relatively low, there is still a possibility of side effects in infants, such as drowsiness or feeding difficulties. If you are breastfeeding, it is important to have an open discussion with your healthcare provider about the potential risks and benefits. Your provider may recommend monitoring your baby for any signs of side effects or exploring alternative treatments if necessary.

Estimated Cost of Gabapentin Enacarbil

The cost of a 30-day supply of Gabapentin enacarbil (Horizant) without insurance can vary depending on the pharmacy and location. With a GoodRX coupon, prices typically range from $300 to $400 for 600 mg extended-release tablets. To find the most affordable option, consider comparing prices at different pharmacies or using a GoodRX coupon to reduce costs.

Possible Alternatives to Gabapentin Enacarbil

If Gabapentin enacarbil is not suitable for you, there are alternative treatments and lifestyle adjustments that may help manage your condition. Always consult your healthcare provider before making any changes to your treatment plan. Telemedicine appointments can also be a convenient way to explore your options.

Neuropathic pain: Alternatives include medications such as pregabalin (Lyrica), duloxetine (Cymbalta), or amitriptyline. Non-medication approaches, like physical therapy and adopting a healthy lifestyle with regular exercise and a balanced diet, may also provide relief.

Postherpetic neuralgia: Treatment options include lidocaine patches, capsaicin cream, or tricyclic antidepressants. Additional pain management strategies, such as acupuncture or nerve blocks, may also be effective.

Restless legs syndrome: Dopamine agonists like pramipexole (Mirapex) or ropinirole (Requip) are commonly prescribed. Lifestyle changes, such as improving sleep hygiene and reducing caffeine intake, can also help alleviate symptoms.

Epilepsy: Other anticonvulsants, such as lamotrigine (Lamictal) or levetiracetam (Keppra), may be considered. Maintaining a consistent medication schedule and avoiding triggers like sleep deprivation are essential for managing epilepsy.

Fibromyalgia: Medications like duloxetine (Cymbalta) or milnacipran (Savella) may help reduce symptoms. Incorporating regular exercise, stress management techniques, and cognitive behavioral therapy (CBT) into your routine can also be beneficial.

Diabetic neuropathy: Common treatments include pregabalin (Lyrica) or duloxetine (Cymbalta). Managing blood sugar levels through a combination of diet, exercise, and medication is critical for controlling symptoms and preventing further nerve damage.

Chronic pain: Non-opioid pain relievers, physical therapy, and mindfulness-based stress reduction (MBSR) techniques are often effective. Collaborate with your healthcare provider to develop a comprehensive pain management plan tailored to your needs.

Anxiety disorders: Treatment options may include cognitive behavioral therapy (CBT), selective serotonin reuptake inhibitors (SSRIs) like sertraline (Zoloft), or benzodiazepines. Incorporating mindfulness practices and regular physical activity into your routine can also help reduce anxiety symptoms.

Migraine: Medications such as triptans (e.g., sumatriptan, Imitrex) or beta-blockers (e.g., propranolol) may be prescribed. Identifying and avoiding migraine triggers, along with implementing lifestyle changes, can significantly improve symptom management.

Sciatica: Physical therapy, anti-inflammatory medications, and muscle relaxants are commonly used to manage sciatica symptoms. In more severe cases, corticosteroid injections or surgical intervention may be necessary.

Recent Updates on Gabapentin Enacarbil Research

Recent studies are uncovering new possibilities for Gabapentin enacarbil, a prodrug of gabapentin, in treating conditions beyond its current FDA-approved uses. For instance, ongoing research is evaluating its potential effectiveness in managing alcohol dependence and chronic cough. These emerging applications could significantly expand its role in medical treatment.

In addition, researchers are examining the long-term safety and effectiveness of Gabapentin enacarbil for addressing neuropathic pain and restless legs syndrome. This includes exploring its benefits as an extended-release formulation, which may improve patient adherence to treatment and provide more consistent symptom relief. While these findings are promising, further clinical trials are necessary to confirm these advantages and to refine treatment guidelines.

If you’re curious about these advancements or wondering how they might relate to your condition, consider discussing them with your healthcare provider. A telemedicine consultation can be a convenient way to explore whether Gabapentin enacarbil, including its extended-release options, could be an appropriate addition to your treatment plan.

James Kingsley

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