Journal articles: 'Biotransformation of drugs'

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Svensson, Craig K. "Biotransformation of Drugs in Human Skin." Drug Metabolism and Disposition 37, no. 2 (November 12, 2008): 247–53. http://dx.doi.org/10.1124/dmd.108.024794.

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Tong, Wang-Yu, and Xiang Dong. "Microbial Biotransformation: Recent Developments on Steroid Drugs." Recent Patents on Biotechnology 3, no. 2 (June 1, 2009): 141–53. http://dx.doi.org/10.2174/187220809788700157.

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Velı́k, J., V. Baliharová, J. Fink-Gremmels, S. Bull, J. Lamka, and L. Skálová. "Benzimidazole drugs and modulation of biotransformation enzymes." Research in Veterinary Science 76, no. 2 (April 2004): 95–108. http://dx.doi.org/10.1016/j.rvsc.2003.08.005.

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Fink-Gremmels, J., and A. S. J. P. A. M. van Miert. "Veterinary drugs: disposition, biotransformation and risk evaluation." Analyst 119, no. 12 (1994): 2521. http://dx.doi.org/10.1039/an9941902521.

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Tang, Xia, Jerry W. Hayes, II, Louis Schroder, William Cacini, John Dorsey, R. C. Elder, and Katherine Tepperman. "Determination of Biotransformation Products of Platinum Drugs in Rat and Human Urine." Metal-Based Drugs 4, no. 2 (January 1, 1997): 97–109. http://dx.doi.org/10.1155/mbd.1997.97.

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Cisplatin is an extremely effective cancer chemotherapeutic agent, but its use is often accompanied by toxicity. Second generation drugs such as carboplatin are becoming more widely used because of reduced toxicity. Since biotransformation products have been implicated in the toxic responses, we have begun to investigate the reactions of cisplatin and carboplatin with potential biological ligands. Reaction products were characterized using HPLC with inductively coupled plasma - mass spectrometry (HPLC-ICP-MS), H1 and C13 NMR and fast atom bombardment - mass spectrometry (FAB-MS). Three Pt-creatinine complexes, cis-[Pt(NH3)2Cl(Creat)]+, cis-[Pt(NH3)2(H2O)(Creat)]2+ and cis-[Pt(NH3)2(Creat)2]2+, were synthesized and the platinum was shown to coordinate to the ring nitrogen, N(3). Human urine samples from patients on cisplatin chemotherapy were shown to contain cisplatin, its hydrolysis product and biotransformation products containing Pt-creatinine, Pt-urea and Pt-uric acid complexes. Urine from carboplatin patients shows fewer biotransformation products. Studies with control and diabetic (protected against cisplatin toxicity) rats showed systematic differences in the biotransformation products formed on administration of cisplatin.

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Ravindran, Selvan, Amlesh J. Tambe, Jitendra K. Suthar, Digamber S. Chahar, Joyleen M. Fernandes, and Vedika Desai. "Nanomedicine: Bioavailability, Biotransformation and Biokinetics." Current Drug Metabolism 20, no. 7 (August 7, 2019): 542–55. http://dx.doi.org/10.2174/1389200220666190614150708.

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Background: Nanomedicine is increasingly used to treat various ailments. Biocompatibility of nanomedicine is primarily governed by its properties such as bioavailability, biotransformation and biokinetics. One of the major advantages of nanomedicine is enhanced bioavailability of drugs. Biotransformation of nanomedicine is important to understand the pharmacological effects of nanomedicine. Biokinetics includes both pharmacokinetics and toxicokinetics of nanomedicine. Physicochemical parameters of nanomaterials have extensive influence on bioavailability, biotransformation and biokinetics of nanomedicine. Method: We carried out a structured peer-reviewed research literature survey and analysis using bibliographic databases. Results: Eighty papers were included in the review. Papers dealing with bioavailability, biotransformation and biokinetics of nanomedicine are found and reviewed. Bioavailability and biotransformation along with biokinetics are three major factors that determine the biological fate of nanomedicine. Extensive research work has been done for drugs of micron size but studies on nanomedicine are scarce. Therefore, more emphasis in this review is given on the bioavailability and biotransformation of nanomedicine along with biokinetics. Conclusion: Bioavailability results based on various nanomedicine are summarized in the present work. Biotransformation of nanodrugs as well as nanoformulations is also the focus of this article. Both in vitro and in vivo biotransformation studies on nanodrugs and its excipients are necessary to know the effect of metabolites formed. Biokinetics of nanomedicine is captured in details that are complimentary to bioavailability and biotransformation. Nanomedicine has the potential to be developed as a personalized medicine once its physicochemical properties and its effect on biological system are well understood.

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Da Silva, Vinicius Barreto, Daniel Fábio Kawano, Ivone Carvalho, Edemilson Cardoso Conceição, Osvaldo Freitas, and Carlos Henrique Tomich de Paula Silva. "Psoralen and Bergapten: In Silico Metabolism and Toxicophoric Analysis of Drugs Used to Treat Vitiligo." Journal of Pharmacy & Pharmaceutical Sciences 12, no. 3 (December 9, 2009): 378. http://dx.doi.org/10.18433/j3w01d.

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PURPOSE: to discuss the contribution of psoralen and bergapten metabolites on psoralens toxicity. METHODS: Computational chemistry prediction of metabolic reactions and toxicophoric groups based on the expert systems Derek and Meteor. RESULTS: a total of 15 metabolites were suggested for both psoralen and bergapten based on phase 1 and 2 biotransformations until the 3rd generation. Five toxicophoric substructures were shared among psoralen, bergapten and their corresponding metabolites; one toxicophoric marker (resorcinol) was only identified in bergapten and its biotransformation products. CONCLUSION: Although the toxic effects of psoralens are well known and documented, there is little information concerning the role of their metabolites in this process. We believe this work add to the knowledge of which molecular substructures are relevant to the process of metabolism and toxicity induction, thus guiding the search and development of more effective and less toxic drugs to treat vitiligo.

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Rekka, Eleni A., Panos N. Kourounakis, and Maria Pantelidou. "Xenobiotic Metabolising Enzymes: Impact on Pathologic Conditions, Drug Interactions and Drug Design." Current Topics in Medicinal Chemistry 19, no. 4 (April 11, 2019): 276–91. http://dx.doi.org/10.2174/1568026619666190129122727.

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Background: The biotransformation of xenobiotics is a homeostatic defensive response of the body against bioactive invaders. Xenobiotic metabolizing enzymes, important for the metabolism, elimination and detoxification of exogenous agents, are found in most tissues and organs and are distinguished into phase I and phase II enzymes, as well as phase III transporters. The cytochrome P450 superfamily of enzymes plays a major role in the biotransformation of most xenobiotics as well as in the metabolism of important endogenous substrates such as steroids and fatty acids. The activity and the potential toxicity of numerous drugs are strongly influenced by their biotransformation, mainly accomplished by the cytochrome P450 enzymes, one of the most versatile enzyme systems. Objective: In this review, considering the importance of drug metabolising enzymes in health and disease, some of our previous research results are presented, which, combined with newer findings, may assist in the elucidation of xenobiotic metabolism and in the development of more efficient drugs. Conclusion: Study of drug metabolism is of major importance for the development of drugs and provides insight into the control of human health. This review is an effort towards this direction and may find useful applications in related medical interventions or help in the development of more efficient drugs.

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Klinger, W. "Biotransformation of Drugs and other Xenobiotics during Postnatal development." Experimental and Toxicologic Pathology 48 (June 1996): 1–88. http://dx.doi.org/10.1016/s0940-2993(96)80104-7.

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PINZA, M., and G. PIFFERI. "ChemInform Abstract: Synthesis and Biotransformation of 3-Hydrazinopyridazine Drugs." ChemInform 26, no. 17 (August 18, 2010): no. http://dx.doi.org/10.1002/chin.199517276.

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PINZA, M., and G. PIFFERI. "ChemInform Abstract: Synthesis and Biotransformation of 3-Hydrazinopyridazine Drugs." ChemInform 26, no. 19 (August 18, 2010): no. http://dx.doi.org/10.1002/chin.199519155.

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Domaradzka, Dorota, Urszula Guzik, and Danuta Wojcieszyńska. "Biodegradation and biotransformation of polycyclic non-steroidal anti-inflammatory drugs." Reviews in Environmental Science and Bio/Technology 14, no. 2 (March 28, 2015): 229–39. http://dx.doi.org/10.1007/s11157-015-9364-8.

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Krawczyk-Łebek, Agnieszka, Monika Dymarska, Tomasz Janeczko, and Edyta Kostrzewa-Susłow. "Fungal Biotransformation of 2′-Methylflavanone and 2′-Methylflavone as a Method to Obtain Glycosylated Derivatives." International Journal of Molecular Sciences 22, no. 17 (September 5, 2021): 9617. http://dx.doi.org/10.3390/ijms22179617.

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Methylated flavonoids are promising pharmaceutical agents due to their improved metabolic stability and increased activity compared to unmethylated forms. The biotransformation in cultures of entomopathogenic filamentous fungi is a valuable method to obtain glycosylated flavones and flavanones with increased aqueous solubility and bioavailability. In the present study, we combined chemical synthesis and biotransformation to obtain methylated and glycosylated flavonoid derivatives. In the first step, we synthesized 2′-methylflavanone and 2′-methylflavone. Afterwards, both compounds were biotransformed in the cultures of two strains of entomopathogenic filamentous fungi Beauveria bassiana KCH J1.5 and Isaria fumosorosea KCH J2. We determined the structures of biotransformation products based on NMR spectroscopy. Biotransformations of 2′-methyflavanone in the culture of B. bassiana KCH J1.5 resulted in three glycosylated flavanones: 2′-methylflavanone 6-O-β-d-(4″-O-methyl)-glucopyranoside, 3′-hydroxy-2′-methylflavanone 6-O-β-d-(4″-O-methyl)-glucopyranoside, and 2-(2′-methylphenyl)-chromane 4-O-β-d-(4″-O-methyl)-glucopyranoside, whereas in the culture of I. fumosorosea KCH J2, two other products were obtained: 2′-methylflavanone 3′-O-β-d-(4″-O-methyl)-glucopyranoside and 2-methylbenzoic acid 4-O-β-d-(4′-O-methyl)-glucopyranoside. 2′-Methylflavone was effectively biotransformed only by I. fumosorosea KCH J2 into three derivatives: 2′-methylflavone 3′-O-β-d-(4″-O-methyl)-glucopyranoside, 2′-methylflavone 4′-O-β-d-(4″-O-methyl)-glucopyranoside, and 2′-methylflavone 5′-O-β-d-(4″-O-methyl)-glucopyranoside. All obtained glycosylated flavonoids have not been described in the literature until now and need further research on their biological activity and pharmacological efficacy as potential drugs.

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Noten, J. B. G. M., W. M. A. Verhoeven, S. Tuinier, and D. Touw. "Therapeutic drug monitoring." Acta Neuropsychiatrica 11, no. 1 (March 1999): 15–16. http://dx.doi.org/10.1017/s0924270800036309.

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SUMMARYThe cytochrome P450 iso-enzyme system plays a key role in the biotransformation of many drugs, including psychotropics. Its activity is determined by both genetic and environmental factors. The most important iso-enzymes for psychiatry in general are P450 IID6, 3A4 and 1A2. Knowledge about the involvement of these enzymes and biotransformation processes is mandatory because of the individual variability in their metabolic capacity. Regular measurement of plasmaconcentrations of (psycho)pharmacological compounds is therefore essential. In addition, the potential value of pheno- and/or genotyping has to be investigated.

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Kearns, Gregory L. "Hepatic Drug Metabolism in Cystic Fibrosis: Recent Developments and Future Directions." Annals of Pharmacotherapy 27, no. 1 (January 1993): 74–79. http://dx.doi.org/10.1177/106002809302700117.

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OBJECTIVE: To review the most current information pertaining to hepatic drug metabolism in patients with cystic fibrosis (CF) and to explore the possible association between CF and specific pathways for the hepatic biotransformation of xenobiotics. DATA SOURCES: A MEDLINE search (key terms: cystic fibrosis, pharmacokinetics, metabolism, pharmacogenetics) was used to identify pertinent literature, including reviews. Research findings from the author's laboratory are also presented. STUDY SELECTION: Only recently reported (from 1988 to present), controlled, clinical investigations of hepatic drug metabolism in patients with CF are included. These investigations examined a mechanistic basis for altered drug biotransformation. Although uncontrolled clinical trials, case reports, and review articles are not included in the discussion, appropriate reference citations are made to these works. DATA EXTRACTION: Data from well-designed, controlled, clinical and basic investigations of altered hepatic drug biotransformation in patients with CF are summarized and discussed. New data from an ongoing study concerning the renal excretion of antipyrine metabolites in these patients are presented. DATA SYNTHESIS: In vivo studies of the formation clearance for metabolites of fleroxacin, sulfamethoxazole, and theophylline clearly demonstrate increased activity for important P-450 isoenzymes. These data are supported by an in vitro study that confirmed increased microsomal metabolism of theophylline to 1-methylxanthine, 3-methylxanthine, and 1,3-dimethyluric acid in a liver specimen from a patient with CF. These findings not only substantiate disease-specific increases in hepatic phase I biotransformation in patients with CF, but also verify the premise of substrate specificity for this pharmacogenetic phenomenon. Likewise, pharmacokinetic studies of drugs that undergo significant hepatic phase II biotransformation (e.g., furosemide, lorazepam, ibuprofen) appear to support increased hepatic drug clearance in patients with CF. This assertion has also been confirmed by a study of acetaminophen disposition, which demonstrated significantly increased formation clearance of the sulfate and glucuronide conjugates of the drug. Finally, the marked increase in the plasma clearance of indocyanine green, a pharmacologic probe for the biliary uptake and excretion of drugs, lends credence to the assertion that increased hepatic clearance of drugs in the presence of CF may be the consequence of disease-specific changes in both enzyme activity and/or drug transport within the liver. CONCLUSIONS: Investigations of drug biotransformation in CF have revealed disease-specific increases in the formation of drug metabolites. Future application of techniques in molecular biology and biochemical pharmacology will need to characterize the mechanistic basis for altered drug metabolism in CF and expand our knowledge of the relationship between drug metabolism phenotype and genotype; the impact of growth, development, and disease severity on drug metabolism; the potential role of CF gene products (i.e., CFTR) on intrahepatic drug transport and biotransformation; and the pharmacogenetic determinants of substrate specificity for hepatic drug metabolism in CF.

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Kulkarni, Arun. "Role of Biotransformation in Conceptal Toxicity of Drugs and Other Chemicals." Current Pharmaceutical Design 7, no. 9 (June 1, 2001): 833–57. http://dx.doi.org/10.2174/1381612013397735.

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Hoogenboom, L. A. P., F. J. H. Pastoor, W. E. Clous, S. E. Hesse, and H. A. Kuiper. "The use of porcine hepatocytes for biotransformation studies of veterinary drugs." Xenobiotica 19, no. 11 (January 1989): 1207–19. http://dx.doi.org/10.3109/00498258909043173.

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Sousa, Tiago, Ronnie Paterson, Vanessa Moore, Anders Carlsson, Bertil Abrahamsson, and Abdul W. Basit. "The gastrointestinal microbiota as a site for the biotransformation of drugs." International Journal of Pharmaceutics 363, no. 1-2 (November 2008): 1–25. http://dx.doi.org/10.1016/j.ijpharm.2008.07.009.

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Diehl-Jones, William, and Debbie Fraser Askin. "The Neonatal Liver, Part 1: Embryology, Anatomy, and Physiology." Neonatal Network 21, no. 2 (March 2002): 5–12. http://dx.doi.org/10.1891/0730-0832.21.2.5.

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The liver is the largest organ in the body and is critical to a number of metabolic, regulatory, and detoxification processes. These include the production of bile, metabolic processing of nutrients, synthesis and regulation of plasma proteins and glucose, and biotransformation of drugs and toxins.

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Asakawa, Yoshinori, Toshihiro Hashimoto, and Yoshiaki Noma. "Biotransformation of Terpenoids from the Crude Drugs and Animal Origin by Microorganisms." HETEROCYCLES 54, no. 1 (2001): 529. http://dx.doi.org/10.3987/rev-00-sr(i)7.

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Srisilam, Keshetty, and Ciddi Veeresham. "RETRACTED: Biotransformation of drugs by microbial cultures for predicting mammalian drug metabolism." Biotechnology Advances 21, no. 1 (March 2003): 3–39. http://dx.doi.org/10.1016/s0734-9750(02)00096-4.

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Moo-Young, Murray. "Article retraction: Biotransformation of drugs by microbial cultures for predicting drug metabolism." Biotechnology Advances 22, no. 8 (November 2004): 617. http://dx.doi.org/10.1016/j.biotechadv.2004.07.001.

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Prasse, Carsten, Manfred Wagner, Ralf Schulz, and Thomas A. Ternes. "Biotransformation of the Antiviral Drugs Acyclovir and Penciclovir in Activated Sludge Treatment." Environmental Science & Technology 45, no. 7 (April 2011): 2761–69. http://dx.doi.org/10.1021/es103732y.

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Shen, Winston W. "The metabolism of psychoactive drugs: A review of enzymatic biotransformation and inhibition." Biological Psychiatry 41, no. 7 (April 1997): 814–26. http://dx.doi.org/10.1016/s0006-3223(96)00180-1.

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Braun, F., U. Christians, S. Laabs, K. Elias, M. Shipkova, E. Schütz, and B. Ringe. "An ex vivo model to study the intestinal biotransformation of immunosuppressive drugs." Transplantation Proceedings 32, no. 7 (November 2000): 1999. http://dx.doi.org/10.1016/s0041-1345(00)01529-3.

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Gorrod, John William. "Genetic influences on the biotransformation of drugs and xenobiotics and their toxicity." Pharmacological Research 26 (September 1992): 23. http://dx.doi.org/10.1016/1043-6618(92)90757-3.

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Sabatine, Marc S., and Jessica L. Mega. "Pharmacogenomics of antiplatelet drugs." Hematology 2014, no. 1 (December 5, 2014): 343–47. http://dx.doi.org/10.1182/asheducation-2014.1.343.

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Abstract Clopidogrel, a platelet P2Y12 inhibitor, is one of the most widely prescribed drugs in cardiovascular medicine because it reduces ischemic and thrombotic complications. It is a prodrug requiring biotransformation into the active metabolite by the hepatic cytochrome 450 system, especially the CYP2C19 enzyme. Candidate gene studies and genome-wide association studies have identified loss-of-function CYP2C19 variants to be associated with a diminished pharmacologic response. Specifically, compared with noncarriers, carriers of at least one copy of a loss-of-function CYP2C19 allele have ∼30% lower levels of active clopidogrel metabolite and ∼25% relatively less platelet inhibition with clopidogrel. Moreover, in patients treated with clopidogrel predominantly for percutaneous coronary intervention, carriers of 1 or 2 CYP2C19 loss-of-function alleles are at increased risk for major adverse cardiovascular outcomes, with an ∼1.5-fold increase in the risk of cardiovascular death, myocardial infarction, or stroke as well as an ∼3-fold increase in risk for stent thrombosis. Tripling the dose of clopidogrel in carriers of a CYP2C19 loss-of-function allele can achieve on-treatment platelet reactivity comparable to that seen with the standard 75 mg dose in wild-type individuals, but the impact on clinical outcomes remains unknown. Alternatively, 2 third-generation P2Y12 inhibitors are available: prasugrel and ticagrelor. These drugs are superior to clopidogrel in reducing ischemic outcomes and are unaffected by CYP2C19 loss-of-function alleles.

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Chałupka, Joanna, Adam Sikora, Aleksandra Kozicka, and Michał Piotr Marszałł. "Overview: Enzyme-catalyzed Enantioselective Biotransformation of Chiral Active Compounds Used in Hypertension Treatment." Current Organic Chemistry 24, no. 23 (December 28, 2020): 2782–91. http://dx.doi.org/10.2174/1385272824999201020204256.

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Enzymatic kinetic resolution is one of the methods which allows for the synthesis of enantiomerically pure various active pharmaceutical ingredients. In contrast to chemical routes, enzymatic reactions have characteristics, including mild reaction conditions, a few byproducts, and relatively high activity of the used enzymes. β-adrenolytic drugs are widely used in the treatment of hypertension and cardiovascular disorders. Due to the fact that β- blockers possess an asymmetric carbon atom in their structure, they are presented in two enantiomeric forms. It was reported by many studies that only the (S)-enantiomers of these drugs possess the desired therapeutic effect, whereas the administration of the racemate may cause dangerous side effects, such as bronchoconstriction or diabetes. Nevertheless, β- blockers are still commercially available drugs mainly used in medicine as racemates, whereas there are several methods that are widely used in order to obtain enantiomerically pure compounds.

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Marks, Gerald S. "The 1986 Upjohn Award Lecture. Interaction of chemicals with hemoproteins: implications for the mechanism of action of porphyrinogenic drugs and nitroglycerin." Canadian Journal of Physiology and Pharmacology 65, no. 6 (June 1, 1987): 1111–19. http://dx.doi.org/10.1139/y87-175.

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The ferrochelatase inhibitory activity of a variety of analogues of 3,5-diethoxycarbonyl-1,4-dihydro-2,4,6-trimethylpyridine (DDC) was studied in chick embryo liver cells. The ferrochelatase inhibitory activity of the 4-butyl, 4-pentyl, and 4-hexyl analogues was considered to be due to catalytic activation by cytochrome P-450 leading to heme alkylation and formation of the corresponding N-alkylporphyrins. The relative ferrochelatase inhibitory activity of the DDC analogues has implications for a postulated model of the binding of porphyrins in the ferrochelatase active site. 3-[2-(2,4,6-Trimethylphenyl)thioethyl]-4-methylsydnone (TTMS) was shown to be a potent porphyrinogenic agent and to inhibit ferrochelatase in chick embryo liver cells. A related sydnone, 3-benzyl-4-phenylsydnone did not inhibit ferrochelatase activity. These results supported the idea that the porphyrinogenicity of TTMS was due to catalytic activation by cytochrome P-450 leading to heme alkylation and formation of N-vinylprotoporphyrin which inhibits ferrochelatase. Polychlorinated biphenyls, phenobarbital, nifedipine, and a large number of structurally different chemicals which are porphyrinogenic in chick embryo liver cells inhibit uroporphyrinogen decarboxylase by an unknown mechanism. Thus drug-induced porphyrin biosynthesis in chick embryo liver cell culture appears to be caused by inhibition of either ferrochelatase or uroporphyrinogen decarboxylase. The biotransformation of nitroglycerin by human red blood cells is due to a combination of a sulfhydryl-dependent enzymatic process and an interaction with reduced hemoglobin. Biotransformation of nitroglycerin was shown to occur only with the deoxy form of hemoglobin and to involve a two-electron denization, resulting in the oxidation of two molecules of heme iron (II) per mole of nitroglycerin biotransformed to glyceryl dinitrate and nitrite anion. Since nitroglycerin biotransformation appears to be involved in the mechanism of nitroglycerin-induced vasodilation, we have suggested the following hypothesis: biotransformation of nitroglycerin in vascular smooth muscle might occur by interaction of nitroglycerin with the iron (ferrous) of guanylate cyclase-bound heme. The nitrite ion formed may be converted via nitrous acid to nitric oxide. This in turn would combine with the heme moiety of guanylate cyclase to activate the enzyme and through a series of enzymatic reactions cause vasodilation.

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Ahmad, Saeed, Farhan Hameed Khaliq, Asadullah Madni, Muhammad Nabeel Shahid, and Irfan Pervaiz. "Microbial biotransformation of beclomethasone dipropionate by Aspergillus niger." Brazilian Journal of Pharmaceutical Sciences 50, no. 4 (December 2014): 903–9. http://dx.doi.org/10.1590/s1984-82502014000400026.

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In the present research, the steroidal anti-asthmatic drug beclomethasone dipropionate was subjected to microbial biotransformation by Aspergillus niger. Beclomethasone dipropionate was transformed into various metabolites first time from microbial transformation. New drug metabolites produced can act as new potential drug molecules and can replace the old drugs in terms of safety, efficacy, and least resistance. They were purified by preparative thin layer chromatography technique, and their structures were elucidated using modern spectroscopic techniques, such as 13C NMR, 1H NMR, HMQC, HMQC, COSY, and NOESY, and mass spectrometry, such as EI-MS. Four metabolites were purified: (i) beclomethasone 17-monopropionate, (ii) beclomethasone 21-monopropionate, (iii) beclomethasone, and (iv) 9beta,11beta-epoxy-17,21-dihydroxy-16beta-methylpregna-1,4-diene-3,20-dione 21-propionate.

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Zendulka, O., M. Sabová, J. Juřica, M. Machalíček, P. Švéda, M. Farková, and A. Šulcová. "The Effect of Methamphetamine on Biotransformation of Ethanol: Pilot Study." Acta Facultatis Pharmaceuticae Universitatis Comenianae 59, no. 2 (December 28, 2012): 63–71. http://dx.doi.org/10.2478/v10219-012-0026-4.

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AbstractMethamphetamine is one of the most popular recreational drugs in Central Europe and is often combined with ethanol. Various interactions between these two substances have been described including the influence of administered ethanol on biotransformation of methamphetamine. The aim of the present study was to describe the opposite effect - the influence of methamphetamine on biotransformation of ethanol in rats. Methamphetamine was administered for 10 days (10 mg/kg/day) i.p. and ethanol was delivered as an intragastric bolus (2 g/kg) on the10th day of experiment to both methamphetamine administered rats and control animals. The pharmacokinetic experiment on the whole animal was performed and plasma samples were drawn at the 40th, 120th, 210th and 300th minute after ethanol administration. Ethanol plasmatic levels reached significantly lower values in the 40th and 120th interval when compared to controls. Differences were insignificant in the last two intervals. Our results suggest that chronic methamphetamine administration induces ethanol biotransformation. We suppose that this effect is caused by induction of alcohol dehydrogenase metabolic activity or by allosteric interaction of methamphetamine and this enzyme. More studies have to be conducted to confirm or disprove our hypothesis.

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Moyseyenko, V., T. Nykula, and I. Burzhynskaya. "CHRONIC KIDNEY DISEASE AND VISCERAL CANDIDIASIS." Ukrainian Journal of Nephrology and Dialysis, no. 4(48) (August 25, 2015): 61–64. http://dx.doi.org/10.31450/ukrjnd.4(48).2015.11.

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Kidneys play a significant role in metabolism, detoxification, biotransformation of dietary, medicinal and other substances. The mainstay of treatment of patients with chronic kidney disease, including pyelonephritis is antibiotic therapy; of glomerulonephritis - glucocorticoids, cytostatics. The presence of comorbidities, diabetes increases the total number of drugs used. Frequent prolonged use of drugs causes secondary immunodeficiency, gastrointestinal tract dysbiosis, clinical manifestations of which are oral mucosa candidiasis; the progression of kidney damage, kidney transplant may cause visceral candidiasis. Control of immunosuppressive therapy, parenteral infusion ofantifungal agents and timely diagnosis prevent candidiasis in patients with chronic kidney disease.

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Strobel, Henry W., Jun Geng, Hidenori Kawashima, and Huamin Wang. "Cytochrome P450-Dependent Biotransformation of Drugs and Other Xenobiotic Substrates in Neural Tissue." Drug Metabolism Reviews 29, no. 4 (January 1997): 1079–105. http://dx.doi.org/10.3109/03602539709002244.

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Letelier, M. E., P. Izquierdo, L. Godoy, A. M. Lepe, and M. Faúndez. "Liver microsomal biotransformation of nitro-aryl drugs: mechanism for potential oxidative stress induction." Journal of Applied Toxicology 24, no. 6 (November 2004): 519–25. http://dx.doi.org/10.1002/jat.999.

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Wong, Yin Cheong, Shuai Qian, and Zhong Zuo. "Regioselective biotransformation of CNS drugs and its clinical impact on adverse drug reactions." Expert Opinion on Drug Metabolism & Toxicology 8, no. 7 (May 8, 2012): 833–54. http://dx.doi.org/10.1517/17425255.2012.688027.

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Klinger, Wolfgang. "Developmental pharmacology and toxicology: Biotransformation of drugs and other xenobiotics during postnatal development." European Journal of Drug Metabolism and Pharmacokinetics 30, no. 1-2 (March 2005): 3–17. http://dx.doi.org/10.1007/bf03226403.

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Gascon, M. P., and P. Dayer. "In vitro forecasting of drugs which may interfere with the biotransformation of midazolam." European Journal of Clinical Pharmacology 41, no. 6 (December 1991): 573–78. http://dx.doi.org/10.1007/bf00314987.

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Jaladanki, Chaitanya K., Samima Khatun, Holger Gohlke, and Prasad V. Bharatam. "Reactive Metabolites from Thiazole-Containing Drugs: Quantum Chemical Insights into Biotransformation and Toxicity." Chemical Research in Toxicology 34, no. 6 (April 26, 2021): 1503–17. http://dx.doi.org/10.1021/acs.chemrestox.0c00450.

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Blaschke, G., M. Meyring, C. Mühlenbrock, and B. Chankvetadze. "Recent results of biotransformation of drugs: investigation of the in vitro biotransformation of thalidomide using a dual cyclodextrin system in capillary electrophoresis." Il Farmaco 57, no. 7 (July 2002): 551–54. http://dx.doi.org/10.1016/s0014-827x(02)01258-2.

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Sargautiene, Vanda, Renāte Ligere, Ineta Kalniņa, Ida Jākobsone, Vizma Nikolajeva, and Aleksejs Derovs. "The Effect of 5-Aminosalicylic Acid on Intestinal Microbiota." Proceedings of the Latvian Academy of Sciences. Section B. Natural, Exact, and Applied Sciences. 74, no. 2 (April 1, 2020): 53–57. http://dx.doi.org/10.2478/prolas-2020-0008.

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AbstractThe article discusses the possible relationships between intestinal microbiota and the therapeutic efficacy of 5-aminosalicylic acid (5-ASA) in inflammatory bowel diseases. Intestinal microbiota may be involved in 5-ASA enzymatic biotransformation, but the metabolism of drugs by the intestinal microbiota has been studied in less detail, and little is known about the relationships between anti-inflammatory efficacy of 5-ASA with bacterial viability, quantity and activity. It remains unclear whether 5-ASA affects the microbiota depending on the different segments of gastrointestinal tract. Drugs and diet can both improve and worsen the composition of the intestinal microbiota. However, it is not known whether drugs affect the intestinal microbiota regardless of diet. Further research is needed to answer these questions.

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Ivanova, Lada, Ilia G. Denisov, Yelena V. Grinkova, Stephen G. Sligar, and Christiane K. Fæste. "Biotransformation of the Mycotoxin Enniatin B1 by CYP P450 3A4 and Potential for Drug-Drug Interactions." Metabolites 9, no. 8 (July 27, 2019): 158. http://dx.doi.org/10.3390/metabo9080158.

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Enniatins (ENNs) are fungal secondary metabolites that frequently occur in grain in temperate climates. Their toxic potency is connected to their ionophoric character and lipophilicity. The biotransformation of ENNs predominantly takes place via cytochrome P450 3A (CYP 3A)-dependent oxidation reactions. Possible interaction with ENNs is relevant since CYP3A4 is the main metabolic enzyme for numerous drugs and contaminants. In the present study, we have determined the kinetic characteristics and inhibitory potential of ENNB1 in human liver microsomes (HLM) and CYP3A4-containing nanodiscs (ND). We showed in both in vitro systems that ENNB1 is mainly metabolised by CYP3A4, producing at least eleven metabolites. Moreover, ENNB1 significantly decreased the hydroxylation rates of the typical CYP3A4-substrate midazolam (MDZ). Deoxynivalenol (DON), which is the most prevalent mycotoxin in grain and usually co-occurrs with the ENNs, was not metabolised by CYP3A4 or binding to its active site. Nevertheless, DON affected the efficiency of this biotransformation pathway both in HLM and ND. The metabolite formation rates of ENNB1 and the frequently used drugs progesterone (PGS) and atorvastatin (ARVS) lactone were noticeably reduced, which indicated a certain affinity of DON to the enzyme with subsequent conformational changes. Our results emphasise the importance of drug–drug interaction studies, also with regard to natural toxins.

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Karaźniewicz-Łada, Marta, Anna K. Główka, Aniceta A. Mikulska, and Franciszek K. Główka. "Pharmacokinetic Drug–Drug Interactions among Antiepileptic Drugs, Including CBD, Drugs Used to Treat COVID-19 and Nutrients." International Journal of Molecular Sciences 22, no. 17 (September 3, 2021): 9582. http://dx.doi.org/10.3390/ijms22179582.

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Anti-epileptic drugs (AEDs) are an important group of drugs of several generations, ranging from the oldest phenobarbital (1912) to the most recent cenobamate (2019). Cannabidiol (CBD) is increasingly used to treat epilepsy. The outbreak of the SARS-CoV-2 pandemic in 2019 created new challenges in the effective treatment of epilepsy in COVID-19 patients. The purpose of this review is to present data from the last few years on drug–drug interactions among of AEDs, as well as AEDs with other drugs, nutrients and food. Literature data was collected mainly in PubMed, as well as google base. The most important pharmacokinetic parameters of the chosen 29 AEDs, mechanism of action and clinical application, as well as their biotransformation, are presented. We pay a special attention to the new potential interactions of the applied first-generation AEDs (carbamazepine, oxcarbazepine, phenytoin, phenobarbital and primidone), on decreased concentration of some medications (atazanavir and remdesivir), or their compositions (darunavir/cobicistat and lopinavir/ritonavir) used in the treatment of COVID-19 patients. CBD interactions with AEDs are clearly defined. In addition, nutrients, as well as diet, cause changes in pharmacokinetics of some AEDs. The understanding of the pharmacokinetic interactions of the AEDs seems to be important in effective management of epilepsy.

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Pereverzev, A. P., O. D. Ostroumova, and A. I. Kochetkov. "Drug-induced liver damage with cholestasis." Kachestvennaya klinicheskaya praktika, no. 3 (September 27, 2020): 61–74. http://dx.doi.org/10.37489/2588-0519-2020-3-61-74.

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The liver is the main organ responsible for the biotransformation and elimination of drugs, and therefore its function is often impaired by different medications. In this article, the authors inform practical health care professionals about the possible liver damage with cholestasis caused by drugs (DILI). Most often, DILI is caused some antibacterial drugs, steroids, barbiturates and some other drugs. DILI has no pathognomonic clinical manifestations. tte scientific literature describes both an asymptomatic increase of “liver” enzymes and the development of acute liver failure. Important diagnostic methods are the collection of anamnesis (especially the medicinal one), analysis of blood biochemical tests, and data from visual diagnostic methods. If the patient has DILI, it is necessary, whenever possible, to stop intake of a drug. ttere are no specific drugs recommended for pharmacotherapy of DILI but there is some the positive effect of ademetionine and ursodeoxycholic acid. ttere are no specific preventive measures for DILI. Healthcare practitioners are recommended not to use drugs off-label, optimize pharmacotherapy and fight with polypharmacy, monitore biochemical tests regularly etc.

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Murray, Michael. "Cytochromes P450: Roles in the Biotransformation of Chemicals in Cigarette Smoke and Impact of Smoking Cessation on Concurrent Drug Therapy." Journal of Smoking Cessation 5, no. 2 (December 1, 2010): 107–14. http://dx.doi.org/10.1375/jsc.5.2.107.

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AbstractCigarette smoke contains polycyclic aromatic hydrocarbons (PAHs) that activate the expression of cytochrome P450 family 1 (CYP1) enzymes in liver and other tissues; this process is dependent on the aryl hydrocarbon receptor (AhR) transcription factor. An important CYP1 enzyme, CYP1A2, has a critical role in the oxidation of drugs such as clozapine, olanzapine and theophylline; these drugs exhibit a high incidence of adverse effects that are linked to plasma concentrations. This article reviews the impact of smoking and smoking cessation on therapy with toxic drugs that undergo CYP-mediated elimination. PAHs in cigarette smoke activate the AhR and upregulate CYP1A2, which enhances the clearance of these drugs, diminishes their efficacy and necessitates the use of higher doses. However, smoking cessation decreases PAH exposure, which leads to a decline in clearance of CYP1A2 substrate drugs. Dose reductions and close therapeutic monitoring for such drugs are recommended in patients who cease smoking.

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Venisetty, R., and V. Ciddi. "Application of Microbial Biotransformation for the New Drug Discovery Using Natural Drugs as Substrates." Current Pharmaceutical Biotechnology 4, no. 3 (June 1, 2003): 153–67. http://dx.doi.org/10.2174/1389201033489847.

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Manosroi, Jiradej, Masahiko Abe, and Aranya Manosroi. "Biotransformation of steroidal drugs using microorganisms screened from various sites in Chiang Mai, Thailand." Bioresource Technology 69, no. 1 (July 1999): 67–73. http://dx.doi.org/10.1016/s0960-8524(98)00163-1.

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Bacinschi, Nicolae, Ina Pogonea, Lilia Podgurschi, Maria Mihalachi-Anghel, Emil Ștefănescu, Bogdan Socea, and Marin Chianu. "The role of biotransformation processes in mediating interactions between psychotropic drugs and natural products." Journal of Mind and Medical Sciences 7, no. 1 (April 4, 2020): 9–15. http://dx.doi.org/10.22543/7674.71.p915.

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Hashimoto, Toshihiro, Yoshiaki Noma, and Yoshinori Asakawa. "ChemInform Abstract: Biotransformation of Terpenoids from the Crude Drugs and Animal Origin by Microorganisms." ChemInform 32, no. 17 (April 24, 2001): no. http://dx.doi.org/10.1002/chin.200117259.

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Langner, A., M. F. Melzig, and S. Kempa. "P213 the use of lymphocyte cultures for the investigation of the biotransformation of drugs." European Journal of Pharmaceutical Sciences 2, no. 1-2 (September 1994): 172. http://dx.doi.org/10.1016/0928-0987(94)90386-7.

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Opriș, Ocsana, Maria-Loredana Soran, Ildikó Lung, Alexandra Ciorîță, and Lucian Copolovici. "Biotransformation of Non-steroidal Anti-inflammatory Drugs Induces Ultrastructural Modifications in Green Leafy Vegetables." Journal of Soil Science and Plant Nutrition 21, no. 2 (March 2, 2021): 1408–20. http://dx.doi.org/10.1007/s42729-021-00449-5.

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Journal articles on the topic 'Biotransformation of drugs'

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