Mirogabalin is a derivative of gamma-amino acids that selectively binds to the α2δ subunits of voltage-gated calcium channels (VGCCs). This binding reduces calcium influx at presynaptic terminals, thereby suppressing neurotransmitter release and decreasing hyperexcitability of central nervous system (CNS) neurons.
Absorption: Rapidly absorbed; peak plasma concentration within 0.5–1.5 hours.
Distribution: Volume of distribution: 64–88 L; plasma protein binding ~25%.
Metabolism: Mainly excreted unchanged by the kidneys (61–72%). A minor portion (13–20%) undergoes metabolism via UGT isoforms.
Elimination: Half-life 2–4.9 hours. About 99% is eliminated through urine; ~1% via feces.
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Nervion is prescribed for the management of various neuropathic pain conditions, including:
Pregnancy: Use only if benefits outweigh risks. Animal studies show placental transfer.
Lactation: Excretion into breast milk observed in animals; weigh benefits of treatment vs. breastfeeding.
Common adverse reactions:
Somnolence, dizziness
Peripheral edema
Weight gain
Rare but serious effects:
CNS: Severe drowsiness, loss of consciousness
Liver: Fatigue, loss of appetite, jaundice (possible hepatic dysfunction)
Adults: Start with 5 mg twice daily. Titrate by 5 mg at weekly intervals up to 15 mg twice daily, depending on the patient’s age and symptoms.
Children & Adolescents: Safety and efficacy not established.
Hepatic Impairment: Mild–moderate impairment does not require adjustment. No data for severe cases.
Renal Impairment:
Mild: 5 mg twice daily, titrate up to 10 mg.
Moderate: 2.5 mg twice daily, titrate up to 7.5 mg twice daily.
Severe: 2.5 mg once daily, titrate up to 7.5 mg once daily.
With Medicines:
Cimetidine, Probenecid → may increase plasma levels.
Lorazepam → enhances CNS depressant effects.
Inhibitors of OAT1, OAT3, OCT2, MATE1, MATE2-K, or UGT → may raise drug exposure.
With Food: No significant effect on absorption.
With Alcohol: Avoid due to additive sedative and motor-impairing effects.
Known hypersensitivity to mirogabalin.
Caution in patients with hepatic or renal impairment.
Store below 30°C, in a dry place, protected from light and moisture.
Keep out of reach of children.
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