Monitoring Free Drug Concentration

Dasgupta, Amitava

doi:10.1016/b978-0-12-802025-8.00004-0

Cited by 6 publications

(4 citation statements)

References 95 publications

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“…Population pharmacokinetic analyses have been instrumental in formulating dosing recommendations for digoxin tailored to specific patient subsets, such as Japanese patients with atrial fibrillation and heart failure [ 33 ]. However, despite such efforts, individual factors like age, renal function, and concurrent drug interactions continue to influence digoxin response, mandating personalized dosing strategies and vigilant monitoring [ 34 ]. Studies have revealed substantial variations in serum digoxin concentration levels even among patients sharing similar clinical characteristics, underscoring the imperative for meticulous monitoring and individualized therapy management [ 35 , 36 ].…”

Section: Reviewmentioning

confidence: 99%

“…However, despite such efforts, individual factors like age, renal function, and concurrent drug interactions continue to influence digoxin response, mandating personalized dosing strategies and vigilant monitoring [34]. Studies have revealed substantial variations in serum digoxin concentration levels even among patients sharing similar clinical characteristics, underscoring the imperative for meticulous monitoring and individualized therapy management [35,36].…”

Section: Individual Variability In Responsementioning

confidence: 99%

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A Comprehensive Review on Unveiling the Journey of Digoxin: Past, Present, and Future Perspectives

Khandelwal,

Vagha,

Meshram

et al. 2024

Cureus

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Digoxin, a cardiac glycoside derived from the foxglove plant ( Digitalis spp.), has been utilized for centuries in managing various cardiac conditions due to its ability to increase myocardial contractility and regulate heart rate. This comprehensive review explores the historical context, pharmacological properties, clinical applications, efficacy, safety profile, challenges, and future perspectives of digoxin. Tracing its journey from traditional medicine to modern cardiovascular therapeutics, we delve into its mechanism of action, therapeutic indications, and clinical guidelines. While digoxin remains a cornerstone therapy for heart failure and atrial fibrillation, its narrow therapeutic index and individual variability in response pose challenges in clinical practice. Nevertheless, ongoing research efforts aim to elucidate its role in emerging therapeutic areas and technological advancements in drug delivery. Despite the advent of newer pharmacological agents, digoxin's enduring relevance lies in its established efficacy, affordability, and global accessibility. This review underscores the symbiotic relationship between tradition and progress in cardiovascular medicine, highlighting the timeless pursuit of medical innovation to optimize patient care.

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Section: Reviewmentioning

confidence: 99%

Section: Individual Variability In Responsementioning

confidence: 99%

A Comprehensive Review on Unveiling the Journey of Digoxin: Past, Present, and Future Perspectives

Khandelwal,

Vagha,

Meshram

et al. 2024

Cureus

View full text Add to dashboard Cite

show abstract

“…Drugs are transported in the circulation either in a free form, dissolved in the aqueous phase of plasma, or in complex bonds with plasma proteins [ 11 ] in varying degrees [ 12 ]. Following the principle of reversible equilibrium and the law of mass action [ 13 ], an equilibrium exists between bound and free (unbound) molecular forms—additionally because binding is generally reversible [ 12 ]. Only the free form is capable of diffusing through membranes and from the vascular space into tissues, being eliminated by metabolism or excretion [ 14 ], and therefore pharmacological activity is exerted by the free drug concentration [ 15 , 16 ].…”

Section: Introductionmentioning

confidence: 99%

“…This concept is important because the total plasma concentration is what is usually measured and not the unbound concentration, which is only occasionally determined. Although at the therapeutic concentration of most drugs, the molar concentration of unbound drugs is usually low in comparison with the molar concentration of the protein binding sites [ 13 , 21 ], in some pathophysiological conditions, the free drug fraction can be reduced/increased with ensuing changes in the distribution process, either by an altered protein–drug affinity or by a change in plasma protein levels [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

Insights into the Binding of Dietary Phenolic Compounds to Human Serum Albumin and Food-Drug Interactions

et al. 2020

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The distribution of drugs and dietary phenolic compounds in the systemic circulation de-pends on, among other factors, unspecific/specific reversible binding to plasma proteins such as human serum albumin (HSA). Phenolic substances, present in plant-derived feeds, foods, beverages, herbal medicines, and dietary supplements, are of great interest due to their biological activity. Recently, considerable research has been directed at the formation of phenol–HSA complexes, focusing above all on structure–affinity relationships. The nucleophilicity and planarity of molecules can be altered by the number and position of hydroxyl groups on the aromatic ring and by hydrogenation. Binding affinities towards HSA may also differ between phenolic compounds in their native form and conjugates derived from phase II reactions. On the other hand, food–drug interactions may increase the concentration of free drugs in the blood, affecting their transport and/or disposition and in some cases provoking adverse or toxic effects. This is caused mainly by a decrease in drug binding affinities for HSA in the presence of flavonoids. Accordingly, to avoid the side effects arising from changes in plasma protein binding, the intake of flavonoid-rich food and beverages should be taken into consideration when treating certain pathologies.

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A novel human pluripotent stem cell-based assay to predict developmental toxicity

et al. 2020

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There is a great need for novel in vitro methods to predict human developmental toxicity to comply with the 3R principles and to improve human safety. Human-induced pluripotent stem cells (hiPSC) are ideal for the development of such methods, because they are easy to retrieve by conversion of adult somatic cells and can differentiate into most cell types of the body. Advanced three-dimensional (3D) cultures of these cells, so-called embryoid bodies (EBs), moreover mimic the early developing embryo. We took advantage of this to develop a novel human toxicity assay to predict chemically induced developmental toxicity, which we termed the PluriBeat assay. We employed three different hiPSC lines from male and female donors and a robust microtiter plate-based method to produce EBs. We differentiated the cells into cardiomyocytes and introduced a scoring system for a quantitative readout of the assay—cardiomyocyte contractions in the EBs observed on day 7. Finally, we tested the three compounds thalidomide (2.3–36 µM), valproic acid (25–300 µM), and epoxiconazole (1.3–20 µM) on beating and size of the EBs. We were able to detect the human-specific teratogenicity of thalidomide and found the rodent toxicant epoxiconazole as more potent than thalidomide in our assay. We conclude that the PluriBeat assay is a novel method for predicting chemicals’ adverse effects on embryonic development.

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Monitoring Free Drug Concentration

Cited by 6 publications

References 95 publications

A Comprehensive Review on Unveiling the Journey of Digoxin: Past, Present, and Future Perspectives

A Comprehensive Review on Unveiling the Journey of Digoxin: Past, Present, and Future Perspectives

Insights into the Binding of Dietary Phenolic Compounds to Human Serum Albumin and Food-Drug Interactions

A novel human pluripotent stem cell-based assay to predict developmental toxicity

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