Clinical Pharmacokinetics of Pregabalin in Healthy Volunteers

Abstract

Pregabalin has shown clinical efficacy for treatment of neuropathic pain syndromes, partial seizures, and anxiety disorders. Five studies in healthy volunteers are performed to investigate single- and multiple-dose pharmacokinetics of pregabalin. Pregabalin is rapidly absorbed following oral administration, with peak plasma concentrations occurring between 0.7 and 1.3 hours. Pregabalin oral bioavailability is approximately 90% and is independent of dose and frequency of administration. Food reduces the rate of pregabalin absorption, resulting in lower and delayed maximum plasma concentrations, yet the extent of drug absorption is unaffected, suggesting that pregabalin may be administered without regard to meals. Pregabalin elimination half-life is approximately 6 hours and steady state is achieved within 1 to 2 days of repeated administration. Corrected for oral bioavailability, pregabalin plasma clearance is essentially equivalent to renal clearance, indicating that pregabalin undergoes negligible nonrenal elimination. Pregabalin demonstrates desirable, predictable pharmacokinetic properties that suggest ease of use. Because pregabalin is eliminated renally, renal function affects its pharmacokinetics.

A review on pregabalin for the treatment of painful diabetic peripheral neuropathy

“…7 This dose should be continued for at least 3 weeks, and if the person is not responding, then, other drugs or treatments should be tried. 8 Well, a large number of clinical studies have been done to support the potential of pain relieving attribute of pregabalin.…”

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“…Son análogos del ácido gammaaminobutírico, que actúan bloqueando los canales del calcio voltaje dependientes en el SNP y SNC, alterando la liberación de neurotransmisores excitadores (80). PGB logra un pico plasmático en 1 hora, sus concentraciones plasmáticas son más predecibles y tiene menos efectos secundarios que GBP (80,81).…”

“…Son análogos del ácido gammaaminobutírico, que actúan bloqueando los canales del calcio voltaje dependientes en el SNP y SNC, alterando la liberación de neurotransmisores excitadores (80). PGB logra un pico plasmático en 1 hora, sus concentraciones plasmáticas son más predecibles y tiene menos efectos secundarios que GBP (80,81). En diferentes modelos de dolor agudo postoperatorio, como la artroplastia de rodilla y la fusión espinal, PGB a una dosis de 150 mg cada 12 horas, ha demostrado una adecuada analgesia, menor consumo de opioides y una menor incidencia de dolor crónico asociado a la cirugía (82,83); también se ha visto que reduce la incidencia de dolor neuropático asociado a la cirugía en ATR (82).…”

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“…Fibromiyaljide birçok çalışma ile ağrıda azalma sağladığı gösterilmiştir [41][42][43][44] . Uyku kalitesi üzerine de etkilidir ve bu etkinin yaklaşık 26 hafta devam ettiği gösterilmiştir 45 .…”