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.

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商品コード: Gabapentin-EU カテゴリー: ,

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
  • 分子量: 171.24 g/mol
  • CAS Number: 60142-96-3
  • Drug Class: Anticonvulsant, Neuromodulator

薬力学

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

適応症

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)
  • 線維筋痛症
  • Alcohol withdrawal syndrome
  • Restless Legs Syndrome (off-label)

用法・用量

Typical adult dosages vary by condition:

  • てんかん: 900–1800 mg/day, in 3 divided doses
  • 神経障害性疼痛: 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.


薬物動態学

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

副作用

よくあることだ:

  • 眠気
  • めまい
  • Ataxia
  • 疲労
  • 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

  • アメリカ: Prescription-only, Schedule V in some states due to abuse potential
  • EU: Prescription-only, not scheduled
  • 英国: 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.


結論

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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