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Chemical Name:
(S)-3-(Aminomethyl)-5-methylhexanoic acid
Molecular Weight: 159.23 g/mol
CAS Number: 148553-50-8
Class: GABA analogue / Calcium channel modulator
Mechanism:
Binds to the α2-δ subunit of voltage-gated calcium channels in the CNS, reducing excitatory neurotransmitter release (e.g., glutamate, noradrenaline)
Unlike GABA, it does not directly interact with GABA receptors but may enhance GABAergic activity over time
Neuropathic Pain:
Diabetic peripheral neuropathy (DPN)
Postherpetic neuralgia (PHN)
Fibromyalgia (FDA-approved)
Epilepsy: Adjunctive therapy for partial-onset seizures
Generalized Anxiety Disorder (GAD): Off-label use in some countries
Absorption: Rapid (~90% bioavailability), peak plasma levels in 1 hour
Metabolism: Minimal hepatic metabolism; 90% excreted unchanged in urine
Half-life: 5-6.5 hours (prolonged in renal impairment)
Starting Dose: 75 mg twice daily or 50 mg three times daily
Max Dose: 600 mg/day (divided into 2-3 doses)
Renal Adjustment: Reduce dose in patients with CrCl <60 mL/min
Common: Dizziness (21-32%), somnolence (12-22%), peripheral edema, weight gain
Serious (Rare):
Angioedema (throat swelling)
Suicidal ideation (monitor in depression/anxiety patients)
Hypersensitivity: Avoid in patients with known allergy
Pregnancy: Potential fetal risk (Category C)
Withdrawal: Taper gradually to avoid rebound seizures or insomnia
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