Lucis O J
Can Med Assoc J. 1983 Jan 1;128(1):24-6.
During the 1970s two biguanide drugs, phenformin and metformin, were used to control hyperglycemia. Phenformin was phased out of the Canadian market because it carried an unacceptable risk of causing lactic acidosis, but metformin remains available. All documented cases of lactic acidosis associated with metformin administration, which are rare, have occurred abroad in patients who were taking the drug in spite of having contraindications to its use. The two drugs are metabolized differently, phenformin being deactivated and concentrated in the liver, and metformin being excreted rapidly, unchanged, by the kidneys. In properly selected diabetic patients therapeutic doses of metformin do not raise the blood levels of intermediary metabolites enough to induce ketoacidosis or lactic acidosis. The safety of the drug is supported by the clinical experience over about 56,000 patient-years in Canada.
20世纪70年代,两种双胍类药物,苯乙双胍和二甲双胍,被用于控制高血糖。苯乙双胍因具有不可接受的导致乳酸性酸中毒的风险而被逐步淘汰出加拿大市场,但二甲双胍仍可使用。所有记录在案的与二甲双胍给药相关的乳酸性酸中毒病例都很罕见,均发生在国外那些尽管有使用禁忌仍服用该药的患者身上。这两种药物的代谢方式不同,苯乙双胍在肝脏中失活并浓缩,而二甲双胍则由肾脏迅速以原形排泄。在经过适当选择的糖尿病患者中,治疗剂量的二甲双胍不会使中间代谢产物的血药浓度升高到足以诱发酮症酸中毒或乳酸性酸中毒的程度。在加拿大,约56000患者年的临床经验支持了该药的安全性。