Gabapentin EU

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Gabapentin – Neuromodulation for Pain, Anxiety & Seizures

Gabapentin is a versatile GABA analogue used for neuropathic pain, epilepsy, and anxiety. It acts on calcium channels in the nervous system to reduce nerve overactivity without directly affecting GABA receptors.

  • Powerful neuropathic pain relief
  • Effective seizure control (as add-on therapy)
  • Used off-label for anxiety and insomnia
  • Low addiction risk when used responsibly

Gabapentin is a proven compound in the study of calcium channel modulation, with extensive applications in neuroscience and psychiatry research.

For research use only. Not for human consumption.

Ce produit est expédié depuis l'Europe avec un numéro de suivi.

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UGS : Gabapentin-EU Catégories : ,

Gabapentin is a synthetic analog of gamma-aminobutyric acid (GABA), originally developed as an antiepileptic drug (AED). Though structurally related to GABA, gabapentin does not bind to GABA receptors; instead, it modulates voltage-gated calcium channels by binding to the α2δ subunit. This results in decreased excitatory neurotransmitter release, making it effective in a range of neurological and psychiatric disorders.


Chemical Information

  • IUPAC Name: 1-(aminomethyl)cyclohexaneacetic acid
  • Molecular Formula: C9H17NO2
  • Poids moléculaire: 171.24 g/mol
  • CAS Number: 60142-96-3
  • Drug Class: Anticonvulsant, Neuromodulator

Pharmacodynamie

Gabapentin does not directly modulate GABA receptors but exerts its effects by binding with high affinity to the α2δ-1 and α2δ-2 subunits of voltage-gated calcium channels (VGCCs). This leads to:

  • Reduced calcium influx in neurons
  • Inhibition of excitatory neurotransmitters like glutamate and substance P
  • Modulation of pain signaling in the spinal cord

Indications

Gabapentin is approved or widely used off-label for:

  • Epilepsy (partial seizures, adjunct therapy)
  • Neuropathic pain (postherpetic neuralgia, diabetic neuropathy)
  • Generalized anxiety disorder (off-label)
  • Fibromyalgie
  • Alcohol withdrawal syndrome
  • Restless Legs Syndrome (off-label)

Dosage et administration

Typical adult dosages vary by condition:

  • Epilepsie: 900–1800 mg/day, in 3 divided doses
  • Douleur neuropathique: Start at 300 mg once daily, titrate to 1800–3600 mg/day
  • Anxiety (off-label): 300–1200 mg/day

Titration is critical to minimize side effects, and abrupt discontinuation should be avoided to prevent withdrawal symptoms or seizure rebound.


Pharmacocinétique

  • Absorption: Bioavailability is dose-dependent (60% at 300 mg, drops with higher doses)
  • Distribution: Not significantly protein-bound; crosses the blood-brain barrier
  • Métabolisme: Not metabolized by the liver
  • Excrétion: Renal elimination; unchanged
  • Half-life: ~5–7 hours

Effets secondaires

Commun :

  • Somnolence
  • Vertiges
  • Ataxia
  • Fatigue
  • Peripheral edema

Rare:

  • Mood changes
  • Suicidal ideation
  • Severe allergic reactions (DRESS syndrome)

Gabapentin may cause dependence in some individuals, especially at high doses or with long-term use. Caution is advised in individuals with a history of substance misuse.


Harm Reduction & Safety

  • Avoid combining with other CNS depressants (e.g., alcohol, benzodiazepines)
  • Renal function should be assessed regularly in chronic users
  • Tapering is necessary to avoid withdrawal symptoms
  • May impair cognitive and motor skills—caution with driving or machinery

Legal Status

  • ÉTATS-UNIS: Prescription-only, Schedule V in some states due to abuse potential
  • L'UE: Prescription-only, not scheduled
  • ROYAUME-UNI: Controlled (Class C, Schedule 3) due to rising misuse

Research and Emerging Uses

Gabapentin continues to be studied in:

  • Chronic cough
  • Migraine prophylaxis
  • Social anxiety disorder
  • PTSD-related sleep disturbances

Its role in modulating central sensitization makes it a candidate in multiple pain-related and psychiatric conditions.


Conclusion

Gabapentin is a well-established neuromodulatory agent with a broad therapeutic range. Despite its relatively benign profile, responsible use and harm reduction are essential due to potential misuse and withdrawal risks. For researchers, it offers a powerful tool for studying calcium channel modulation and neuropathic pathways.

Product and Dosage

Gabasign 300mg, Gabatop, Gabimax 400, Gabimax 600

Package Size

30 Capsules/Tablets, 50 Capsules/Tablets, 100 Capsules/Tablets, 200 Capsules/Tablets, 400 Capsules/Tablets

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