[Pregabalin--profile of efficacy and tolerability in neuropathic pain]

Drugs Today (Barc). 2009 Oct:45 Suppl C:19-27.
[Article in Portuguese]

Abstract

Pregabalin (PGB), like its predecessor gabapentin, is a structural analogue (but not functional) of the gammaaminobutyric acid (GABA). PGB has analgesic, antoconvulsivant, and ansiolytic activities. Neuropathic pain (NP) initial recommended dose is 150 mg per day. Depending on the patient response or bodily resistance to the drug the initial dose can be increased up to 300 mg per day (divided in 2-3 daily doses) during a one-week period. PGB is quickly absorbed in the digestive system with high oral biodisponibility. The drug is eliminated almost exclusively by renal excretion (98%). PGB efficacy was evaluated by several studies by means of visual analog scales (VAS) in several NP conditions such as post-herpetic neuropathy (PHN) or painful diabetic neuropathy (PDN). When compared with placebo, PGB provided significant benefit with 150 mg doses in the treatment of PHN pain. In studies developed in patients with PDN, the significant difference between placebo and treatment group only was achieved in individuals with daily doses of 300 mg/day, and the response was clearly dose-dependent. Tolerability information obtained from a number of studies has shown that the drug has a very good safety and tolerability profile. Side effects were mild to moderate and dose-dependent. Based on controlled studies, the main adverse effects observed with PGB are dizziness (23.1%), drowsiness (14.6%), and peripheral aedema (10.4%). As these side effects are dosedependent, they can be easily managed by a simple dose reduction, with no need to discontinue the therapy. Thus, according to efficacy and tolerability data, PGB is an important therapeutic option in NP treatment.

Publication types

  • English Abstract
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / administration & dosage*
  • Analgesics / adverse effects
  • Analgesics / pharmacokinetics
  • Diabetic Neuropathies / drug therapy
  • Humans
  • Neuralgia / drug therapy*
  • Neuralgia / metabolism
  • Neuralgia, Postherpetic / drug therapy
  • Pain Measurement
  • Pregabalin
  • gamma-Aminobutyric Acid / administration & dosage
  • gamma-Aminobutyric Acid / adverse effects
  • gamma-Aminobutyric Acid / analogs & derivatives*
  • gamma-Aminobutyric Acid / pharmacokinetics

Substances

  • Analgesics
  • Pregabalin
  • gamma-Aminobutyric Acid