Future Prospects for Treating Chronic Pain and Central Sensitization in Cattle
GABAPENTIN. Gabapentin (1-[aminomethyl] cyclohexane acetic acid) is a γ-aminobutyric acid (GABA) analog originally developed for the treatment of spastic disorders and epilepsy.
Studies have reported that gabapentin is also effective for the management of chronic pain of inflammatory neuropathic origin. Although the mechanism of action of gabapentin is poorly understood, it is thought to bind to the o2-δ subunit of voltage-gated calcium channels acting presynaptically to decrease the release of excitatory neurotransmitters. Efficacy of gabapentin in humans is associated with 2 pg/mL plasma drug concentrations. It has also been reported that gabapentin can interact synergistically with NSAIDs to produce antihy- peralgesic effects. We report a mean peak plasma gabapentin concentration (Cmax) of 3.40 μgZmL (range: 1.70 to 4.60 μg/ mL) at 7.20 hours (range: 6 to 10 hours) after oral gabapentin administration to calves at 15 mg/kg.67 An elimination half-life (T∕2) of 7.9 hours (range: 6.9 to 12.4 hours) was recorded. Oral administration of gabapentin at 15 mg/kg may be associated with plasma concentrations of greater than 2 μgZmL for up to 15 hours. The pharmacokinetics of gabapentin suggests that this compound may be useful in mitigating chronic neuropathic and inflammatory pain in ruminant cattle.
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