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      Pregabalina en el tratamiento del dolor neuropático periférico Translated title: Pregabalin for the management of peripheral neuropathic pain


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          La aparición de pregabalina (PGBB), un nuevo fármaco del grupo de los neuromoduladores, con un perfil farmacocinético mejor al de sus predecesores y con indicación en dolor neuropático periférico abre nuevos horizontes en el tratamiento de estos enfermos. PGBB es un análogo del GABA aunque no se liga a su receptor ni es capaz de desarrollar acciones gabaérgicas. PGBB debe el efecto analgésico a su capacidad de ligarse a la subunidad proteica alfa-2-delta de los canales de calcio voltaje dependientes en el SNC, con una afinidad mayor a la de gabapentina. En varios modelos animales de dolor, PGBB ha demostrado eficacia antihiperalgésica y un perfil antialodínico superior a morfina y amitriptilina; se absorbe rápidamente por vía digestiva, con una biodisponibilidad del 90%, una farmacocinética altamente predecible y lineal con baja variabilidad interindividual y larga vida media, lo que permite su administración en dos dosis diarias. PGBB no se liga a las proteínas plasmáticas y se elimina inalterada por orina casi en su totalidad, por lo que presenta escasa interacción con otros fármacos. En esta revisión se evalúan los resultados de cinco estudios en neuralgia postherpética (NPH), en un total de 1.034 pacientes y otros seis en pacientes portadores de neuropatía diabética dolorosa (NDD) que incluyeron 1.628 pacientes. En todos ellos, PGBB en dosis de 150 mg.día-1 o superiores, ha demostrado eficacia frente a placebo de una forma dosis dependiente para controlar el dolor, mejorar el sueño y mejorar muchos de los parámetros de la calidad de vida de los pacientes. La dosis más eficaz demostró ser 600 mg (p < 0,001 vs. placebo) y en dosis flexible, con una dosis media de 457 mg.día-1 manifestó también alta eficacia (p = 0,002 vs. placebo). PGBB en dosis terapéuticas ha demostrado altos índices de seguridad, con efectos adversos leves, reversibles y con baja incidencia. La presencia de efectos adversos graves fue similar a la de placebo. En conclusión: PGBB demostró ser un fármaco eficaz y seguro en el tratamiento del dolor neuropático en pacientes portadores de NPH y NDD.

          Translated abstract

          The availability of pregabalin (PGBB), a new drug belonging to the group of neuromodulators with a better pharmacokinetic profile compared to its predecessors and effective for the management of peripheral neuropathic pain, opens up new horizons for the management of these patients. PGBB is a GABA analogue, although it does not bind to its receptors nor it shows gabaergic actions. Analgesic effects of PGBB are due to its binding to the proteic alpha-2-delta subunit of the voltage-dependant calcium channels at the CNS with greater affinity than gabapentin. In several animal pain models, PGBB has shown antihyperalgesic effectiveness and a better antiallodynia profile compared to morphine and amitriptilin; it is quickly absorbed when orally administered, with a 90% bioavailability, a highly predictable and linear pharmacokinetics with low interindividual variability and a long half life. Consequently, it can be administered in two daily doses. PGBB does not bind to plasma proteins and is mainly excreted unaltered in the urine, so its interaction with other drugs is rare. In this review, the results of five studies of postherpetic neuralgia (PHN) were assessed, with a total of 1,034 patients and other six studies in painful diabetic neuropathy (PDN) that included 1,628 patients. In all of them, PGBB administered in doses of at least 150 mg.day-1 was effective versus placebo in a dose-dependant way in terms of pain relief, improved sleep and improved parameters of quality of life. The most effective dose was 600 mg (p < 0.001 vs. placebo) and, with a flexible dosage, a mean dose of 457 mg.day-1 was also highly effective (p = 0.002 vs. placebo). Therapeutic doses of PGBB also showed high safety levels, with a low incidence of slight reversible adverse effects. The presence of severe adverse effects was the same as with placebo. In conclusion, PCBB was an effective and safe drug for the management of neuropathic pain in patients with PHN and DNP.

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          Most cited references 66

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          Pregabalin for the treatment of postherpetic neuralgia: a randomized, placebo-controlled trial.

          To evaluate the efficacy and safety of pregabalin in the treatment of postherpetic neuralgia (PHN). The authors conducted a multicenter, parallel-group, double-blind, placebo-controlled, 8-week, randomized clinical trial in PHN, defined as pain for 3 or more months following herpes zoster rash healing. Patients (n = 173) were randomized to treatment with pregabalin or placebo. Patients randomized to pregabalin received either 600 mg/day (creatinine clearance > 60 mL/min) or 300 mg/day (creatinine clearance 30 to 60 mL/min). The primary efficacy measure was the mean of the last seven daily pain ratings. Secondary endpoints included additional pain ratings, sleep interference, quality of life, mood, and patient and clinician ratings of global improvement. Pregabalin-treated patients had greater decreases in pain than patients treated with placebo (endpoint mean scores 3.60 vs 5.29, p = 0.0001). Pain was significantly reduced in the pregabalin-treated patients after the first full day of treatment and throughout the study, and significant improvement on the McGill Pain Questionnaire total, sensory, and affective pain scores was also found. The proportions of patients with >or=30% and >or=50% decreases in mean pain scores were greater in the pregabalin than in the placebo group (63% vs 25% and 50% vs 20%, p = 0.001). Sleep also improved in patients treated with pregabalin compared to placebo (p = 0.0001). Both patients and clinicians were more likely to report global improvement with pregabalin than placebo (p = 0.001). Given the maximal dosage studied, pregabalin had acceptable tolerability compared to placebo despite a greater incidence of side effects, which were generally mild to moderate in intensity. Treatment of PHN with pregabalin is safe, efficacious in relieving pain and sleep interference, and associated with greater global improvement than treatment with placebo.
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            Painful diabetic polyneuropathy: epidemiology, pain description, and quality of life.

            A prospective survey study was performed in patients with painful diabetic polyneuropathy (PDN) to assess the nature and scope of their pain. Pain associated with diabetic neuropathy is commonly encountered in clinical practice. Yet, little is known regarding the pain experience and impact on quality of life in persons with painful diabetic neuropathy. These 105 patients noted an average of 6/10 pain, most often described as 'burning', 'electric', 'sharp', and 'dull/ache', which, for most, is worse at night time and when tired or stressed. On average, patients reported that the pain caused substantial interference in sleep and enjoyment of life and moderate interference in recreational activities, normal work, mobility, general activity, social activities, and mood. Unexpectedly, a potential genetic predisposition to the development of painful neuropathy was suggested by the fact that a majority (56%) reported a family member with PDN. Thus, this study found that pain associated with diabetic neuropathy is a significant medical issue that has a substantial impact on the quality of life of many people with this condition.
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              Pregabalin pharmacology and its relevance to clinical practice.

              Pregabalin is a potent ligand for the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system that exhibits potent anticonvulsant, analgesic, and anxiolytic activity in a range of animal models. In addition, pregabalin has been shown to be a highly effective adjunctive therapy for partial seizures in clinical trials. Potent binding to the alpha-2-delta site reduces depolarization-induced calcium influx with a consequential modulation in excitatory neurotransmitter release. Pregabalin has no demonstrated effects on GABAergic mechanisms. Pregabalin demonstrates highly predictable and linear pharmacokinetics, a profile that makes it easy to use in clinical practice. Absorption is extensive, rapid, and proportional to dose. Time to maximal plasma concentration is approximately 1 h and steady state is achieved within 24-48 h. These characteristics reflect the observed onset of efficacy as early as day two in clinical trials. High bioavailability, a mean elimination half life (t(1/2)) of 6.3 h, and dose-proportional maximal plasma concentrations and total exposures predict a dose-response relationship in clinical practice and allow an effective starting dose of 150 mg/day in clinical practice without need for titration. Administration with food has no clinically relevant effect on the amount of pregabalin absorbed, providing for a dosing regimen uncomplicated by meals. Pregabalin does not bind to plasma proteins and is excreted virtually unchanged (<2% metabolism) by the kidneys. It is not subject to hepatic metabolism and does not induce or inhibit liver enzymes such as the cytochrome P450 system. Therefore, pregabalin is unlikely to cause, or be subject to, pharmacokinetic drug-drug interactions--an expectation that has been confirmed in clinical pharmacokinetic studies. However, dose adjustment may be necessary in patients with renal insufficiency. Thus, the pharmacological and pharmacokinetic profiles of pregabalin provide a predictable basis for its use in clinical practice.

                Author and article information

                Role: ND
                Revista de la Sociedad Española del Dolor
                Rev. Soc. Esp. Dolor
                Sociedad Española del Dolor (Madrid )
                April 2005
                : 12
                : 3
                : 169-180
                [1 ] Hospital Ramón y Cajal Spain
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