Start low, aim high. The role of doses in successful pregabalin therapy

Abstract

Pregabalin belongs to a group of anti-epileptic drugs that act on the alpha 2/delta subunit of the G protein of voltage-gated calcium channels. As a consequence of its pharmacological effect, pregabalin reduces the levels of intracellular calcium ions and enhances pre- and postsynaptic inhibition in the central nervous system, which translates directly into its clinical action. The expanding indications for pregabalin, not only in the treatment of neuropathic pain, but also in neurology and psychiatry, mean that the drug is accepted by an increasing number of patients with different pharmacokinetic characteristics. Pregabalin treatment can be started at lower doses of 25–50–75 mg at a time, and then slowly up-titrated to an effective and welltolerated dose. Doses may also need to be reduced in patients with renal insufficiency. Pregabalin dosing in elderly patients is based on an established adult regimen, but with a prolonged titration period. It is worth recalling that the recommended dose of pregabalin in the case of neuropathic pain should be 300–600 mg per day. Therefore, different doses of the drug are needed to ensure optimal efficacy and reduce the risk of side effects. Considering the pharmacokinetic profile of pregabalin, the drug should be available in various doses for individualised use. This is of particular importance due to its linear pharmacokinetics, which allows achieving doses that are effective and well-tolerated by the patient in a much more effective way than in the case of gabapentin, which in turn is a condition for compliance.