Catalog of Herbs
James A. Duke in Handbook of Medicinal Herbs, 2018
Often planted as an ornamental. Dried leaves are used medicinally because of the effect on the central nervous system, the heart, and blood vessels. It contains glucosides which act as heart tonic, stimulant, and diuretic. Its most important use is in congestive heart failure because it increases the force of systolic contractions. It also provides more rest between those contractions. Also, lowers the venous pressure in hypertensive heart disease. Elevates blood pressure due to impaired heart function and reduces the size of dilated hearts. Diuresis and reduction of edema follow as a result of improved circulation. According to Farnsworth and Morris, digoxin occurred in circa 11 million (0.73% of all prescriptions), digitoxin in circa 5 million (0.33%), and digitalis extracts in 2.5 million (0.16%).98 The drug digitoxin is 1000 times stronger than the powdered leaves. Used as an antidote for aconite. Nineteenth century artist, van Gogh, is speculated to have taken digitalis for epilepsy. Digitalis causes yellow vision, visions of yellow rings, as well as other visual and psychic disturbances, some of which show up in his art.
Skin Absorption Databases and Predictive Equations
Richard H. Guy, Jonathan Hadgraft in Transdermal Drug Delivery, 2002
Names of compounds listed in the FV database (Table Al) with permeability coefficient values in the Flynn database are contained within brackets. Updated values (2) have replaced the n-alcohol permeability coefficients appearing in the Flynn database (34). (The only practical difference is that a lower permeability coefficient for propanol [1.2 × 10 3 cm h−1] replaced the value [1.4 × 103 cm h−1] included in the Flynn database.) In vivo measurements included in the Flynn database [ethylbenzene, styrene, and toluene from (35,36)] were excluded from the current analysis. The measured permeability coefficient of hydrocortisone (37), determined from a 5% ethanol vehicle, and the permeability of naproxen, determined from an aqueous gel vehicle, were placed in the excluded database. Likewise, etorphine was excluded since Jolicoeur and others (33) identified it as being very different from quite similar compounds, and much different in hairless mouse skin. Digitoxin was excluded since the measurement was probably not at steady state. Subsequent investigations for morphine (38) and fentanyl and sufentanil (4) were considered in addition to the prior investigation (5) cited in the Flynn database. Various compounds from the Flynn database were excluded because more than 90% of the compound was ionized in the experiments.
Endogenous Digitalis-Like Factors: Past Progress and Future Prospects
Antonio Coca, Ricardo P. Garay in Ionic Transport in Hypertension: New Perspectives, 2019
This substance may at times exist in a form that has antigenic determinants which allow it to be recognized by antidigoxin antibodies. A potential explanation for this is that the chemical groups contributing to the recognition may be important for binding to transport proteins in blood. The basis for this hypothesis is that the 12ß hydroxyl group of digoxin is the only point in its structure in which it differs from digitoxin, yet this hydroxyl group governs the large difference in plasma protein binding between these two cardiac glycosides. If antibodies that are specific for digoxin, but not digitoxin, recognize an endogenous factor, then it is likely that the antigenic determinant in digoxin which is recognized by the antibody includes the 12β hydroxyl. Rather than the antibody serving as a model of the Na,K-ATPase binding site, as we initially hypothesized, it may be serving as a model of the plasma protein binding site for digoxin.
Cardiotonic steroids as potential Na+/K+-ATPase inhibitors – a computational study
Published in Journal of Receptors and Signal Transduction, 2019
Chirag N. Patel, Sivakumar Prasanth Kumar, Krunal M. Modi, Mehul N. Soni, Nainesh R. Modi, Himanshu A. Pandya
The determination of optimal poses of CTS was performed by introspecting multiple dock poses of CTS in terms of lowest binding energy and interactions with key residues. Upon observation of these docked complexes, we found the dominance of hydrophobic and aromatic properties in the intermolecular interactions which were responsible for the binding hot-spots of selected CTS. The best docked pose of digoxigenin exhibited 11 van der Waals interactions, 2 hydrogen bonds, 1 carbon-hydrogen bond and 1 π-alkyl interactions with residues such as Ala 114, Asn 129, Leu 132, Ile 322, Phe 323, Gly 326, Ile 327, Ile 328, Val 329, Ala 330, Glu 786, Ile 787, Phe 790, Leu 800, Leu 802, Gly 803, Thr 804 and Ile 807 (Figure 3). Two hydrogen bonding have been observed between Ala 330 and Thr 804 with 3.59 and 4.07 Å respectively. Eight hydrophobic interactions were detected with Ile 16, Val 21, Phe 41, Ile 95, Tyr 158, Leu 197 and Ala 198 with distance of 3.7, 3.6, 3.3, 3.6, 4.0, 3.5, 3.8 and 3.9 Å respectively. Based on the docking experiments, we can conclude that digoxigenin as the potential phytochemical candidate for testing conditions of congestive heart failure and has been taken for further analysis. The remaining CTS in complex with Na+/K+-ATPase is shown in Figures S3–S7 along with their binding energy and contacting residues listed above. Cardiac glycosides including Digoxin, β-methyl digoxin, digoxigenin, digitoxigenin and digitoxin are validated to be the known inhibitors of Na+/K+-ATPase [48].
Digitalis therapy in patients with ventricular tachyarrhythmias
Published in Scandinavian Cardiovascular Journal, 2022
Tobias Schupp, Julian Müller, Max von Zworowsky, Mohammad Abumayyaleh, Kathrin Weidner, Jonas Rusnak, Kambis Mashayekhi, Thomas Bertsch, Ibrahim Akin, Michael Behnes
During the study period from 2002 until 2015, treatment with digitalis decreased from 46.9 to 7.5%. This trend was observed both in patients suffering from AF and HF. The present study suggests that digitalis treatment (digoxin in 67% and digitoxin in 37%) is not associated with increased mortality in patients with ventricular tachyarrhythmias. However, digitalis treatment may increase the risk of the composite endpoint and the risk of cardiac rehospitalization, which was consistent after multivariable Cox regression analyses and which was seen both in patients with AF and HF, as well as in those patients suffering from both AF and HF. Finally, digitoxin may be associated with increased mortality as compared to digoxin.
Foxglove poisoning: diagnostic and therapeutic differences with medicinal digitalis glycosides overdose
Published in Acta Clinica Belgica, 2022
Koen R. Maes, Pieter Depuydt, Joris Vermassen, Peter De Paepe, Walter Buylaert, Cathelijne Lyphout
There are important pharmacokinetic differences between cardiac glycosides with regard to the degree of protein binding, lipid solubility and biotransformation. Digoxin and digitoxin have been used for medicinal purposes. The preference for digoxin in therapeutic use is because of its relatively short half-life of 40 hours, low protein binding and renal excretion with little biotransformation or enterohepatic cycling. These factors make digoxin the most predictable compound in terms of obtaining therapeutic serum concentrations [11].