活性代謝產物

活性代謝產物(active metabolite)是藥物經代謝後產出，具有生理活性的分子。

藥物的代謝產物

藥物分子經身體代謝，被修改後仍繼續對身體造成影響者，即為活性代謝產物。通常這些影響與原分子相似且較弱，但仍可有可觀影響(如11-hydroxy-THC（英語：11-hydroxy-THC）, morphine-6-glucuronide（英語：morphine-6-glucuronide）)。有些藥如可待因以及曲馬多有比母藥強的代謝產物(各自為嗎啡以及O-desmethyltramadol（英語：O-Desmethyltramadol） )^[1]^[2]^[3]，在這些案例代謝產物可能為療效貢獻了一大部分。有時代謝產物具有毒性，必須小心監控以避免在體內累積。如哌替啶和dextropropoxyphene（英語：Dextropropoxyphene）.^[3]^[4]

有些藥物一開始的狀態沒有活性，被設計成在體內代謝後產生活性成分。這類藥物叫做前驅藥物。藥物被如此設計可能是因為:藥物在製造及儲存階段更穩定。或是更能被身體吸收，擁有較好的藥物代謝動力學特性。(如 lisdexamphetamine).^[5]

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^ ^3.0 ^3.1 Zhou SF, Zhou ZW, Yang LP, Cai JP. Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Current Medicinal Chemistry. 2009, 16 (27): 3480–675. PMID 19515014. doi:10.2174/092986709789057635.
^ Coller JK, Christrup LL, Somogyi AA. Role of active metabolites in the use of opioids. European Journal of Clinical Pharmacology. February 2009, 65 (2): 121–39. PMID 18958460. doi:10.1007/s00228-008-0570-y.
^ Müller CE. Prodrug approaches for enhancing the bioavailability of drugs with low solubility. Chemistry & Biodiversity. November 2009, 6 (11): 2071–83. PMID 19937841. doi:10.1002/cbdv.200900114.

Nedderman, Angus N.R. & Walker, Don K. Metabolite testing in drug development. Bonate, Peter L. (編). Pharmacokinetics in Drug Development: Advances and Applications, Volume 3. Springer. 2011 [2016-03-04]. ISBN 9781441979360. （原始內容存檔於2014-07-29）.