活性代谢产物

活性代谢产物(active metabolite)是药物经代谢后产出，具有生理活性的分子。

药物的代谢产物

药物分子经身体代谢，被修改后仍继续对身体造成影响者，即为活性代谢产物。通常这些影响与原分子相似且较弱，但仍可有可观影响(如11-hydroxy-THC（英语：11-hydroxy-THC）, morphine-6-glucuronide（英语：morphine-6-glucuronide）)。有些药如可待因以及曲马多有比母药强的代谢产物(各自为吗啡以及O-desmethyltramadol（英语：O-Desmethyltramadol） )^[1]^[2]^[3]，在这些案例代谢产物可能为疗效贡献了一大部分。有时代谢产物具有毒性，必须小心监控以避免在体内累积。如哌替啶和dextropropoxyphene（英语：Dextropropoxyphene）.^[3]^[4]

前驱药物

有些药物一开始的状态没有活性，被设计成在体内代谢后产生活性成分。这类药物叫做前驱药物。药物被如此设计可能是因为:药物在制造及储存阶段更稳定。或是更能被身体吸收，拥有较好的药物代谢动力学特性。(如 lisdexamphetamine).^[5]

参考资料

[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.

延伸阅读

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）.

参见

[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]