摘要
Pregabalin [S-(+)-3-isobutylgaba]是一種1990年代新合成的抗癲癇劑，為神經傳導物質γ-aminobutyric acid (GABA)的結構衍生物，同時對依性鈣離子通道之α2δ副單位上(α2 δ subunit of voltage-gated calcium channels)有著選擇性及高親和力；並具有止痛、抗癲痛及解除焦慮等藥理作用。因此，它也被應用於治療各種不同之疾病，包括神經病變性疼痛、痛覺過度、焦慮及睡眠障礙等。臨床前置研究及臨床研究發現，Pregabalin對緩解神經病變性疼痛所引起之痛苦有著迅速且持久之作用。目前所知，Pregabalin並沒有藥物間之相互作用、劑量簡單、且有著線性的藥物動力學之劑量反應關係(Dose-response relationship)、高比例之口服生物可用率(≧90%)和良好之耐受性及安全性等優點。最常見之副作用則為眩暈、嗜睡及週邊水腫等。本文獻回顧主要就該藥物之藥理性質、最近之臨床研究報告及臨床應用等作詳細討論。
並列摘要
Pregabalin [S-(+)-3-isobutylgaba] is a novel anticonvulsant, which was synthesized in 1990 as a structural analog of the neurotransmitter γ-aminobutyric acid (GABA). It is a selective, high-affinity ligand for the α 2 δ subunit of voltage-gated calcium channels, which causes analgesic, anticonvulsant and anxiolytic activities. Therefore, it is used to treat of several disorders, including neuropathic pain, hyperalgesia, anxiety and sleep diseases. Preclinical and clinical trials were found that Pregabalin is rapid and sustained relief to treat the agony of neuropathic pain. They are also presented as no drug interactions, simple dosing, linear pharmacokinetics with a clear dose-response relationship, high oral bioavailability (≧90%), favorable tolerability and safety profile. The most common adverse events of Pregabalin are dizziness, somnolence and peripheral edema. This review discusses its pharmacological properties, recent clinical trials as well as its clinical applications.