WordNet

a person who is a participating member of an organization; "the club issues a list of members, both the actives and the retirees"
tending to become more severe or wider in scope; "active tuberculosis"
in operation; "keep hope alive"; "the tradition was still alive"; "an active tradition" (同)alive
engaged in or ready for military or naval operations; "on active duty"; "the platoon is combat-ready"; "review the fighting forces" (同)combat-ready, fighting
(used of verbs (e.g. `to run' (同)dynamic
taking part in an activity; "an active member of the club"; "he was politically active"; "the participating organizations" (同)participating
(of e.g. volcanos) capable of erupting
(of e.g. volcanos) erupting or liable to erupt; "active volcanos"
(of the sun) characterized by an increased occurrence of sunspots and flares and radio emissions
characterized by energetic activity; "an active toddler"; "active as a gazelle"; "an active man is a man of action"
disposed to take action or effectuate change; "a director who takes an active interest in corporate operations"; "an active antagonism"; "he was active in drawing attention to their grievances"
engaged in full-time work; "active duty"; "though past retirement age he is still active in his profession"
exerting influence or producing a change or effect; "an active ingredient"
expressing that the subject of the sentence has the semantic function of actor: "Hemingway favors active constructions"
full of activity or engaged in continuous activity; "an active seaport"; "an active bond market"; "an active account"
any substance involved in metabolism (either as a product of metabolism or as necessary for metabolism)

PrepTutorEJDIC

『活動的な』,活発な,活気のある / 『有効な』,(薬の効力などが)まだ働いている,機能している / (軍務で)現役の / 『積極的な』,実際的な / 能動態の
代謝物質(新陳代謝によって生じる物質)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/04/04 12:29:51」(JST)

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[Wiki en表示]

An active metabolite is an active form of a drug after it has been processed by the body.

Prodrugs

Sometimes drugs are formulated deliberately so they will break down inside the body to form the active drug. These are called prodrugs. The reason for this may be because the drug is more stable during manufacture and storage as the prodrug form, or because the prodrug is better absorbed by the body or has superior pharmacokinetics (e.g., lisdexamphetamine).^[1]

Metabolites of drugs

Another kind of active metabolite results when a drug is broken down by the body into a modified form which continues to produce effects in the body. Usually these effects are similar to those of the parent drug but weaker, although they can still be significant (see e.g. 11-hydroxy-THC, morphine-6-glucuronide). Certain drugs such as codeine and tramadol have metabolites that are stronger than the parent drug (morphine and O-desmethyltramadol respectively)^[2]^[3]^[4] and in these cases the metabolite may be responsible for much of the therapeutic action of the parent drug. Sometimes, however, metabolites may produce toxic effects and patients must be monitored carefully to ensure they do not build up in the body. This is an issue with some well known drugs such as pethidine (meperidine) and dextropropoxyphene.^[4]^[5]

References

^ Müller CE (November 2009). "Prodrug approaches for enhancing the bioavailability of drugs with low solubility". Chemistry & Biodiversity 6 (11): 2071–83. doi:10.1002/cbdv.200900114. PMID 19937841.
^ Haffen E, Paintaud G, Berard M, Masuyer C, Bechtel Y, Bechtel PR (June 2000). "On the assessment of drug metabolism by assays of codeine and its main metabolites". Therapeutic Drug Monitoring 22 (3): 258–65. PMID 10850391.
^ Raffa RB (July 1996). "A novel approach to the pharmacology of analgesics". The American Journal of Medicine 101 (1A): 40S–46S. PMID 8764759.
^ ^a ^b Zhou SF, Zhou ZW, Yang LP, Cai JP (2009). "Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development". Current Medicinal Chemistry 16 (27): 3480–675. PMID 19515014.
^ Coller JK, Christrup LL, Somogyi AA (February 2009). "Role of active metabolites in the use of opioids". European Journal of Clinical Pharmacology 65 (2): 121–39. doi:10.1007/s00228-008-0570-y. PMID 18958460.

UpToDate Contents

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1. ステロイド誘発性骨粗鬆症の予防および治療 prevention and treatment of glucocorticoid induced osteoporosis
2. リウマチ性疾患および腎疾患におけるシクロホスファミドの使用の一般原則 general principles of the use of cyclophosphamide in rheumatic and renal disease
3. 内因性および外因性ステロイドの尿中排泄の測定 measurement of urinary excretion of endogenous and exogenous glucocorticoids
4. 薬と肝臓：代謝および肝障害の機序 drugs and the liver metabolism and mechanisms of injury
5. 異常分娩：遷延分娩および分娩停止 abnormal labor protraction and arrest disorders

English Journal

Metabonomic analysis of HIV-infected biofluids.

Sitole LJ, Williams AA, Meyer D.SourceDepartment of Biochemistry, University of Pretoria, Pretoria 0002, South Africa. Debra.Meyer@up.ac.za.
Molecular bioSystems.Mol Biosyst.2013 Jan 27;9(1):18-28. doi: 10.1039/c2mb25318f. Epub 2012 Nov 1.
Monitoring the progression of HIV infection to full-blown acquired immune deficiency syndrome (AIDS) and assessing responses to treatment will benefit greatly from the identification of novel biological markers especially since existing clinical indicators of disease are not infallible. Nuclear magn
PMID 23114495

Japanese Journal

Regulation of central carbon metabolism in Saccharomyces cerevisiae by metabolic inhibitors(MICROBIAL PHYSIOLOGY AND BIOTECHNOLOGY)

Matsuda Fumio,Shirai Tomokazu,Ishii Jun,Kondo Akihiko
Journal of bioscience and bioengineering 116(1), 59-64, 2013-07
… Among the 6 active inhibitors, the effects of pyrazole (alcohol dehydrogenase inhibitor) and TTA (2-thenoyltrifluoloacetone, succinate dehydrogenase inhibitor) were analyzed in detail. … The multi-targeted metabolic profiling analysis revealed that, although the TTA and pyrazole treatments affected the profiles of all central carbon metabolites in distinct manners, the level of fructose-1,6-bisphosphate commonly increased in the TTA- and pyrazole-treated S. …
NAID 110009634746

活性型ビタミンD誘導体の臨床応用と医薬品化(<特集>「ビタミン誘導体の臨床応用」(第64回大会シンポジウム))

久保寺登
ビタミン 87(2), 95-103, 2013-02-25
… The second is the elucidation of the vitamin D activation pathway in the body and the discovery of the biologically active metabolites of vitamin D. … The clinical application of active vitamin D or its prodrug was also attempted to make up for the deficiency caused by poor vitamin D activation. … The third is characterized by the discovery of the differentiation-inducing properties of active vitamin D. …
NAID 110009594132

「active」

　　[★]

adj.

活動性の、活動期の、活動的な、行動的な、積極的な、活発な、能動的な、有効な、アクティブな

関: active stage、actively、activity、aggressive、behaviorally、brisk、briskly、effective、efficacious、offensive、positive、positively、valid、vigorous、vigorously

[pmid19937841-1] Müller CE (November 2009). "Prodrug approaches for enhancing the bioavailability of drugs with low solubility". Chemistry & Biodiversity 6 (11): 2071–83. doi:10.1002/cbdv.200900114. PMID 19937841.

[pmid10850391-2] Haffen E, Paintaud G, Berard M, Masuyer C, Bechtel Y, Bechtel PR (June 2000). "On the assessment of drug metabolism by assays of codeine and its main metabolites". Therapeutic Drug Monitoring 22 (3): 258–65. PMID 10850391.

[pmid8764759-3] Raffa RB (July 1996). "A novel approach to the pharmacology of analgesics". The American Journal of Medicine 101 (1A): 40S–46S. PMID 8764759.

[pmid19515014-4] Zhou SF, Zhou ZW, Yang LP, Cai JP (2009). "Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development". Current Medicinal Chemistry 16 (27): 3480–675. PMID 19515014.

[pmid18958460-5] Coller JK, Christrup LL, Somogyi AA (February 2009). "Role of active metabolites in the use of opioids". European Journal of Clinical Pharmacology 65 (2): 121–39. doi:10.1007/s00228-008-0570-y. PMID 18958460.

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active metabolites