For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Since gabapentin enacarbil is a prodrug of gabapentin, it’s physiological effects are the same as gabapentin. Concerning PHN, gabapentin prevents allodynia and hyperalgesia.
Mode of Action:
Although the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors.
Gabapentin enacarbil does not interact with any of the major cytochrome P450 enzymes.
Most common adverse reactions are headache, dizziness, and somnolence.
Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther. 2004 Oct;311(1):324-33. Epub 2004 May 14. [PubMed:15146029 ]
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