Leiderman D B
Parke-Davis Pharmaceutical Research, Division of the Warner-Lambert Company, Ann Arbor 48105.
Epilepsia. 1994;35 Suppl 5:S74-6. doi: 10.1111/j.1528-1157.1994.tb05974.x.
Gabapentin (GBP, Neurontin), a new antiepileptic drug (AED) with a novel mechanism of action, exhibits low acute toxicity in mice, rats, and monkeys, and is not teratogenic. GBP pharmacokinetics are simple and predictable; GBP is eliminated by urinary excretion, is not protein-bound or metabolized, does not induce or inhibit hepatic enzymes, and does not interact with other AEDs. In five placebo-controlled, double-blind studies of GBP as add-on therapy, 307 patients with refractory partial seizures received placebo and 485 received GBP dosages of 600, 900, 1,200, or 1,800 mg/day for 12 weeks following a 12-week baseline. Seizure frequency, as measured by response ratio and responder rate, was improved for patients receiving GBP compared with placebo; differences were statistically significant in two of the three large, multicenter studies. Adverse events occurred in 76% of GBP-treated patients, compared with 57% of placebo-treated patients. No serious adverse events were consistently attributable to GBP therapy. Changes in clinical laboratory values were not considered clinically important. GBP represents a significant addition to the armamentarium of AEDs available for treatment of patients with epilepsy.
加巴喷丁（GBP，商品名：Neurontin）是一种具有全新作用机制的新型抗癫痫药物（AED），在小鼠、大鼠和猴子身上显示出低急性毒性，且无致畸性。GBP的药代动力学简单且可预测；GBP通过尿液排泄消除，不与蛋白质结合或代谢，不诱导或抑制肝酶，也不与其他抗癫痫药物相互作用。在五项将GBP作为附加治疗的安慰剂对照双盲研究中，307例难治性部分性癫痫患者接受了安慰剂治疗，485例患者在为期12周的基线期后，接受了每日600、900、1200或1800毫克的GBP治疗，为期12周。与安慰剂相比，接受GBP治疗的患者的癫痫发作频率（通过反应率和有效率衡量）有所改善；在三项大型多中心研究中的两项中，差异具有统计学意义。76%接受GBP治疗的患者出现了不良事件，而接受安慰剂治疗的患者这一比例为57%。没有严重不良事件一直被认为是由GBP治疗所致。临床实验室值的变化不被认为具有临床重要性。GBP是可用于治疗癫痫患者的抗癫痫药物库中的一个重要补充。
