Journals / İstanbul Journal of Pharmacy / 2023 / Cilt: 53 Sayı: 2

Importance and review of drug metabolite synthesis

Pages
251–269
Publication Date
2023-08-30
DOI
—
🏛️Bibliographic metadata and full text access for this article are provided via DergiPark.
DergiPark Record ↗
✨

AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

Moreover, it showed that there was much more research available for Phase I than Phase II in the literature.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Phase I and Phase II metabolic reactions are involved in the pharmacokinetic properties of drugs after administration.
📊
Key Findings & Data:These reactions mainly aim to make drugs more polar and eliminate them safely.
💡
Conclusion & Impact:Moreover, it showed that there was much more research available for Phase I than Phase II in the literature.
🔬Design:Review & Systematic Survey
📍Scope:Comprehensive Sample
⚙️Variables:Drug metabolite · metabolism · synthesis

Abstract

Phase I and Phase II metabolic reactions are involved in the pharmacokinetic properties of drugs after administration. These reactions mainly aim to make drugs more polar and eliminate them safely. However, some of these metabolites have the potential to exhibit a toxicological effect. Industry and/or academia have to consider these metabolites in terms of their pharmacodynamic and pharmacokinetic properties. These metabolites are not only residual intermediates from the synthetic process of the main drug but also unique structures produced by metabolic enzymes in the human organism. Thus, metabolite synthesis by synthetic or semi-synthetic methods is a key feature in the pharmaceutical industry. In this review, synthetic methods of the metabolites from all known metabolic pathways are reviewed from the literature. It was observed that both synthetic and semi-synthetic methods require more attention as they are as important and complex as drug synthesis. Moreover, it showed that there was much more research available for Phase I than Phase II in the literature.

🔖

Cite This Article

ŞAHİN, Z., ÖZGEN, P. S. O., ROLLAS, S. (2023). Importance and review of drug metabolite synthesis. İstanbul Journal of Pharmacy, Cilt: 53 Sayı: 2, 251–269. https://ajindex.com/articles/963650

📄 Full Text PDF Viewer

📄

PDF görüntüleyici hazırlanıyor...

References (1)

  1. Adamczyk, M., & Fino, J. R. (1996). Synthesis of procainamide me-tabolites, N-acetyl desethylprocainamide, and desethylprocain-amide. Organic Preparations and Procedures International, 28(4), 470-474. doi:Doi 10.1080/00304949609356555 google scholar Althuis, T. H., & Hess, H. J. (1977). Synthesis and identification of the major metabolites of prazosin formed in dog and rat. Journal of Medicinal Chemistry, 20(1), 146-149. doi:10.1021/jm00211a031 google scholar Arewang, C. J., Lahmann, M., Oscarson, S., & Tiden, A. K. (2007). Synthesis of urine drug metabolites: glucuronic acid glycosides of phenol intermediates. Carbohydrate Research, 342(7), 970-974. doi:10.1016/j.carres.2007.01.014 google scholar Argikar, U. A. (2012). Unusual glucuronides. Drug Metabolism & Disposition, 40(7), 1239-1251. doi:10.1124/dmd.112.045096 google scholar Asha, S., & Vidyavathi, M. (2009). Cunninghamella--a microbial model for drug metabolism studies--a review. Biotechnology Ad-vances, 27(1), 16-29. doi:10.1016/j.biotechadv.2008.07.005 google scholar Bailey, M. J., & Dickinson, R. G. (2003). Acyl glucuronide reactiv-ity in perspective: biological consequences. Chemico-Biological Interactions, 145(2), 117-137. doi:10.1016/s0009-2797(03)00020-6 google scholar Baillie, T. A., Cayen, M. N., Fouda, H., Gerson, R. J., Green, J. D., Grossman, S. J.,. Shipley, L. A. (2002). Drug metabolites in safety testing. Toxicology and Applied Pharmacology, 182(3), 188-196. doi:10.1006/taap.2002.9440 google scholar Baldwin, B. C., Robinson, D., & Williams, R. T. (1960). Studies in detoxi-cation. 82. The fate of benzoic acid in some domestic and other birds. The Biochemical Journal, 76(3), 595-600. doi:10.1042/bj0760595 google scholar Boerner, U. (1975). The metabolism of morphine and heroin in man. Drug Metabolism Reviews, 4(1), 39-73. doi:10.3109/03602537508993748 google scholar Bradshaw, P. R., Athersuch, T. J., Stachulski, A. V., & Wilson, I. D. (2020). Acyl glucuronide reactivity in perspective. Drug Discovery Today, 25(9), 1639-1650. doi:10.1016/j.drudis.2020.07.009 google scholar Brown, D. D., Axelrod, J., & Tomchick, R. (1959). Enzymatic N-Methylation of Histamine. Nature, 183(4662), 680-680. doi:10.1038/183680a0 google scholar Cai, X., Sha, M., Guo, C., & Pan, R. M. (2012). Synthesis of Tertiary Amine N-oxides—A Review. Asian Journal of Chemistry, 24(9), 3781-3784. google scholar Caswell, J. M., O’Neill, M., Taylor, S. J., & Moody, T. S. (2013). Engi-neering and application of P450 monoo