Gabapentin and its role in the treatment of epilepsy

Epilessia; Gabapentin

Gabapentin is a drug approved to prevent and control partial seizures, relieve post-herpetic neuralgia following shingles, and moderate-to-severe restless legs syndrome. The following article explores how this medicine works and Flarer’s role in managing its distribution

Gabapentin: what is it used for?

The active ingredient in this drug has an agonist action against gamma-aminobutyric acid (GABA) receptors, an inhibitory neurotransmitter involved in central nervous system function. GABA plays a vital role in central nervous system inhibition, especially in slowing down nerve activity. 

It is a prescription drug that is part of the anticonvulsant class and reduces the excitability of brain nerve cells, which play a role in seizures and the transmission of pain signals. 

Due to its role in the treatment of pain, Gabapentin also has some off-label uses (not officially recognized but regularly prescribed for its efficacy) for various common disorders, both related to particular physical conditions and mood disorders such as: anxiety, depression, bipolar disorder, post-traumatic stress disorder (PTSD), and social phobia. Other disorders that can be treated through this medication are:

  • neuropathic pain;
  • fibromyalgia;
  • hot flashes in postmenopause;
  • irritable bowel syndrome (IBS);
  • alcohol withdrawal;
  • postoperative analgesia;
  • nausea and vomiting;
  • migraine prophylaxis;
  • headache;
  • interstitial cystitis;
  • painful diabetic neuropathy;
  • generalized tonic-clonic seizures;
  • itching;
  • insomnia;
  • chronic refractory cough.

Gabapentin: the mechanism of action

Researchers are still determining the mechanism of action of Gabapentin; however, this drug freely crosses the blood-brain barrier and effectively affects gamma-aminobutyric neurotransmitters.

The hypothesis is that the drug’s active ingredient acts as an anticonvulsant and analgesic due to its binding to N-type voltage-dependent calcium channels in the central nervous system. In this way, it can decrease the activity of several neurotransmitters, such as norepinephrine, glutamate, and substance P, and amplify the activity of the neurotransmitter GABA 

Gabapentin’s elimination half-life is dose-independent and averages 5-7 hours. It takes the body two days to eliminate the drug from the system.

How is Gabapentin marketed?

Gabapentin is available in several forms: as a solution, capsules, and tablets. The drug is administered orally and has an oral bioavailability of more than 90%, independent of dose, except in the case of patients with renal insufficiency.

Usually, the effects are evident in the first week of treatment, but sometimes, it takes about a month to achieve significant improvement. 

Particular attention should be paid to avoiding sudden discontinuation of the drug as it can cause serious problems, including increased risk of seizures (if you are taking it for that reason) or failure to improve symptoms (if you are taking Gabapentin for other indications). 

Because it acts on the central nervous system, the use of Gabapentin is not recommended if you have to drive, operate heavy machinery, and do other risky activities.


Use of Gabapentin for neuropathic pain

One of the indications for Gabapentin is neuropathic pain, which a variety of conditions, including diabetes, herpes zoster, or after injury, can cause.

The U.S. Food and Drug Administration (FDA), the drug regulatory agency on U.S. soil, has approved Gabapentin to manage postherpetic neuralgia in adults. Extensive scientific literature supports the efficacy of Gabapentin in the treatment of painful diabetic neuropathy, postherpetic neuralgia, and other neuropathic pain syndromes.

Through a collection of randomized trials conducted between the second half of 1900 and 2014, in which the drug was compared with placebos, it was found that Gabapentin was helpful in relieving symptoms related to allodynia, burning pain, stabbing pain, and hyperesthesia. Side effects were mild to moderate; in most cases, Gabapentin does not cause significant side effects. Some individuals may experience drowsiness, fatigue, and dizziness, but in these cases, the side effects are generally mild and disappear within 10 days after starting treatment.

Gabapentin in psychiatry: for anxiety and depression

Although Gabapentin is traditionally used to treat seizures, it is sometimes used, like Pregabalin – another anticonvulsant drug – in psychiatry as a mood stabilizer for depression and bipolar disorder. In addition, clinical studies have found that Gabapentin can be a good alternative to benzodiazepines in the treatment of generalized anxiety disorder. For this reason, it may be beneficial as an alternative for people who respond only partially to other mood stabilizers.

However, it should be remembered that the use of Gabapentin against anxiety disorders has not yet been thoroughly studied, although there is some evidence that it improves anxiety in cancer survivors, individuals with social anxiety disorder, and in the treatment of alcohol dependence. Due to the cross-cutting nature of this drug’s effects and possible therapeutic applications, Gabapentin is still the subject of research.

Gabapentin in veterinary settings: for dogs and cats

In addition to its use in human health, Gabapentin is also a drug used in veterinary medicine. It is used off-label, in combination with other treatments, to control seizures when other drugs are ineffective or to treat neuropathic pain and anxiety in animals.

Gabapentin is mainly used in dogs, cats, and horses. It is also useful in veterinary medicine preoperatively to minimize the pain an animal experiences after surgery. It can also be used as an adjunctive treatment to manage seizures and to relieve anxiety associated with travel, veterinary visits, or other stressful situations.

Flarer and the supply of Gabapentin

Our team has built strong partnerships with certified companies to ensure we can reliably supply Gabapentin to our customers. 

Part of our service is taking full responsibility for the scouting and supply phases of this important active ingredient, which is critical in several pain management therapies. Since its inception, our company has expanded its reach, establishing solid partnerships with over 100 quality-certified companies. We have extensive knowledge that enables us to handle all phases of transportation (including non-EU) of various active pharmaceutical ingredients.

Our team is committed to finding the best solution for each client’s specific needs. To learn more about Flarer’s services, you can contact our consultants.

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