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（英语：11-hydroxy-THC）, morphine-6-glucuronide（英语：morphine-6-glucuronide）)。有些藥如可待因以及曲马多有比母藥強的代謝產物(各自為嗎啡以及O-desmethyltramadol（英语：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（英语：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，擁有較好的药物代谢动力学特性。(如 lisdexamphetamine).^[5]

[1]
Haffen E, Paintaud G, Berard M, Masuyer C, Bechtel Y, Bechtel PR. On the assessment of drug metabolism by assays of codeine and its main metabolites. Therapeutic Drug Monitoring. June 2000, 22 (3): 258–65. PMID 10850391. doi:10.1097/00007691-200006000-00005.
[2]
Raffa RB. A novel approach to the pharmacology of analgesics. The American Journal of Medicine. July 1996, 101 (1A): 40S–46S. PMID 8764759. doi:10.1016/s0002-9343(96)00137-4.
[3]
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.
[4]
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.
[5]
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. (编). Pharmacokinetics in Drug Development: Advances and Applications, Volume 3. Springer. 2011 [2016-03-04]. ISBN 9781441979360. （原始内容存档于2014-07-29）.

[pmid10850391-1] [1]
Haffen E, Paintaud G, Berard M, Masuyer C, Bechtel Y, Bechtel PR. On the assessment of drug metabolism by assays of codeine and its main metabolites. Therapeutic Drug Monitoring. June 2000, 22 (3): 258–65. PMID 10850391. doi:10.1097/00007691-200006000-00005.

[pmid8764759-2] [2]
Raffa RB. A novel approach to the pharmacology of analgesics. The American Journal of Medicine. July 1996, 101 (1A): 40S–46S. PMID 8764759. doi:10.1016/s0002-9343(96)00137-4.

[pmid19515014-3] [3]
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.

[pmid18958460-4] [4]
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.

[pmid19937841-5] [5]
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.

[1]

[2]

[3]

[4]

[5]

活性代謝產物

Wikiwand in your browser!

活性代謝產物

Wikiwand in your browser!

藥物的代謝產物

前驅藥物

參考資料

延伸閱讀

參見