列管於運動禁藥監控計畫中的Telmisartan

Telmisartan in the Doping Monitoring Program

10.6127/JEPF.2016.23.02

張值維(Chih-Wei Chang)；陳昭彥(Chao-Yen Chen)；許美智(Mei-Chich Hsu)

血管張力素II接受體阻斷劑 ； 世界運動禁藥管制機構 ； 荷爾蒙及代謝調節劑 ； 高血壓 ； 美度銨 ； angiotensin II receptor blocker ； World Anti-Doping Agency ； hormone and metabolic modulators ； hypertension ； meldonium

運動生理暨體能學報

23輯（2016 / 12 / 01）

13 - 22

繁體中文

背景：Telmisartan是一血管張力素II接受體阻斷劑（angiotensin II receptor blockers），用以治療高血壓及降低心血管風險，它擁有比起其他同類藥物更多的優勢，如一天一錠的用法、老年／腎功能不佳者可服用、更專一的藥效作用等，因而暢銷於世界各地，但也因其擁有能提升運動表現的潛在藥效，使它在體育界備受關注。Telmisartan藉由AMP-activated protein kinase（AMPK）/ peroxisome proliferator activated receptor δ（PPAR δ）路徑預防脂肪合成、增進運動耐力及運動後的氧氣消耗、增加慢肌纖維的比例。在2014年年底，Telmisartan與莎拉波娃所服用的美度銨（Meldonium）同時被世界運動禁藥管制機構（World Anti-Doping Agency, WADA）列入2015運動禁藥賽內及賽外的監控計畫。現今，美度銨被列入運動禁藥，而Telmisartan則尚在監控計畫中。WADA此時不會對服用Telmisartan之運動員進行懲罰，但正密切監控其是否被濫用，隨時都可能跟美度銨一樣，正式被列入運動禁藥。目的：本文將詳細介紹Telmisartan藥品發展與臨床應用、作用機轉與運動表現的關聯、藥物動力學與檢驗方法及替代藥物的選擇。

Background: Telmisartan belongs to angiotensin II receptor blockers and is used for treating essential hypertension and reducing cardiovascular risk. Telmisartan is considered as an attractive and world-wide popular ARB owing to its numerous merits, e.g., the usage of a tablet per day, good tolerance in elderly and patients with renal impairment, and high specificity of action. However, telmisartan is now in a perilous state, because it may potentially elevate exercise performance. Studies have demonstrated that telmisartan may prevent fat synthesis, enhance execise endurance and postexercise oxygen consumption, and increase slow-twitch skeletal muscle fibres via AMP-activated protein kinase (AMPK) / peroxisome proliferator activated receptor δ (PPAR δ) pathway. In the end of 2014, telmisartan and meldonium, which Sharapova took, were simultaneously listed in the 2015 Monitoring Program by the World Anti-Doping Agency (WADA). Nowadays, meldonium is prohibited so far, whereas telmisartan is still in monitoring program. WADA would not make the punishment on athletes who are taking telmisartan, but is currently monitoring the abuse substances seriously. Telmisartan could be officially prohibited in anytime, just like meldonium. Purpose: This literature review introduces the development and clinical indications, mechanism of actions, the link between exercise performance, metabolism and excretion, detection methods as well as alternative medications of telmisartan.

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