丁二胍，又名丁雙胍，藥品名丁福明（INN：），是一種口服降血糖藥，於 1957 年被合成 Seymour L Shapiro et al Salts Of NAmylbiguanide US Patent number 2961377 Filing date Aug 5 1957 Issue date 1960，主要用於二型糖尿病的治療，與二甲雙胍、苯乙雙胍同屬於雙胍類口服降血糖藥。 化學性質 鹽酸丁二胍是白色或黃色，無味，晶體粉末，嚐起來有微酸苦味。 熔點 174 到 177C，為強鹼，可溶於水、甲醇、乙醇，不溶於氯仿和醚類 Jacker HJ New Pharmacologic Products 2 Buformin For Oral Therapy Of Diabetes Pharm Prax 1964102479Eustace George Coverly Clarke Judith Berle Pharmaceutical Society of Great Britain Dept of Pharmaceutical Sciences Isolation and identification of drugs in pharmaceuticals body fluids and postmortem material Volume 1 Pharmaceutical Press 1974 p226。 分配係數 log P 辛醇 水 120E00；水溶性在 25C 為 746E05 毫克 升。蒸汽壓於 25C 為 164E04 毫米汞柱 估計值。 作用機理 鹽酸丁二胍能夠延遲腸胃途徑的糖吸收，增加胰島素敏感性和細胞的糖攝入，並且抑制肝糖合成。鹽酸丁二胍和其他雙胍類口服降糖藥一樣，不是以直接降血糖為主要作用機理，而是對抗血糖水平過高。服用不會產生低血糖的現象，但能夠有效降低糖尿病人的空腹與餐後血糖 Enrique Ravina Hugo Kubinyi The Evolution of Drug Discovery From Traditional Medicines to Modern Drugs Wiley 2011 p 215。 劑量 日常給藥劑量為 150300 毫克 口服 Gustav Kuschinsky Heinz Lüllmann Textbook of pharmacology Academic Press p 225 1973。 副作用與用藥禁忌 常見副作用為食慾匱乏，噁心，腹瀉，口中有金屬味和體重減輕。有糖尿病昏迷，酮酸中毒，嚴重感染或創傷者停用。 毒性 鹽酸丁二胍由於可能導致乳酸堆積的機率增加，而在一些國家被下市。目前在羅馬尼亞、匈牙利、臺灣和日本仍作為處方藥被應用。Hankó B Tukarcs E Kumli P Vincze Z Antidiabetic drug utilization in Hungary Pharm World Sci 2005 Jun27 32635Hankó BZ Reszegi CA Kumli P Vincze Z Practice of antidiabetic therapy in Hungary Acta Pharm Hung 200575 27786Jerry L Schlesser Gale Research Inc Drugs available abroad Derwent Publications Ltd 1990 p28Chou CH Cheng CL Huang CC A validated HPLC method with ultraviolet detection for the determination of buformin in plasma Biomed Chromatogr 2004 May18 42548Takeda Announces Submission Of Application For Additional Indication Of Actos In Japan Concomitant Therapy With Biguanides For Type 2 Diabetes Medical News Today 28 Jan 2007 乳酸堆積症一般只在鹽酸丁二胍血漿濃度超過的 060 微克 毫升的病人中發生，在腎功能正常的患者中十分罕見。Wittmann P Haslbeck M Bachmann W Mehnert H Lactic acidosis in diabetics on biguanides authors translation Deutsche Medizinische Wochenschrift 102 1510 1977Berger W MehnertAner S Mülly K Heierli C Ritz R 10 cases of lactic acidosis during biguanide therapy buformin and phenformin Schweizerische medizinische Wochenschrift 10618301834 1976 抗癌作用 鹽酸丁二胍和二甲雙胍還有苯乙雙胍一樣，抑制癌細胞生長和發育 Sakae Saito Aki Furuno Junko Sakurai Asami Sakamoto HaeRyong Park Kazuo Shinya Takashi Tsuruo and Akihiro Tomida Chemical Genomics Identifies the Unfolded Protein Response as a Target for Selective Cancer Cell Killing during Glucose Deprivation Cancer Research 200969 10422534Vladimir N Anisimov InsulinIGF1 signaling pathway driving aging and cancer as a target for pharmacological intervention Experimental Gerontology Volume 38 Issue 10 October 2003 Pages 10411049Valery A Alexandrov Vladimir N Anisimov Natalia M Belous Inna A Vasilyeva and Vera B Mazon The inhibition of the transplacental blastomogenic effect of nitrosomethylurea by postnatal administration of buformin to rats Carcinogenesis Volume 1 Issue 12 Pp 975978 1980Anisimov VN Ostroumova MN Dilman VM Inhibition of the blastomogenic effect of 712dimethylbenz a anthracene in female rats by buformin diphenin a polypeptide pineal extract and LDOPA Bulletin of Experimental Biology and Medicine Volume 89 Number 6 819822 1980Vladimir N Anisimov Lev M Berstein Irina G Popovich Mark A Zabezhinski Peter A Egormin Margarita L Tyndyk Ivan V Anikin Anna V Semenchenko Anatoli I Yashin Central and Peripheral Effects of InsulinIGF1 Signaling in Aging and Cancer Antidiabetic Drugs as Geroprotectors and Anticarcinogens Annals of the New York Academy of Sciences 1057220234 2005。其抗癌機制是由於其可以阻斷瓦氏效應，並且將癌細胞的供能途徑從細胞基質糖解逆轉回依靠線粒體的丙酮酸途徑。Matthew G Vander Heiden Lewis C Cantley and Craig B Thompson Understanding the Warburg Effect The Metabolic Requirements of Cell Proliferation Science 324 5930 10291033 2009 Shaw RJ Lamia KA Vasquez D Koo SH Bardeesy N Depinho RA Montminy M Cantley LC The kinase LKB1 mediates glucose homeostasis in liver and therapeutic effects of metformin Science 2005 Dec 9310 575416426 參考文獻 Category 雙胍 Category 糖尿病藥物