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ACS Omega Jul 2017Digitalis drugs are selective inhibitors of the plasma membrane Na/K-ATPase. There are many studies on molecular mechanisms of digitalis interaction with purified pig...
Digitalis drugs are selective inhibitors of the plasma membrane Na/K-ATPase. There are many studies on molecular mechanisms of digitalis interaction with purified pig kidney enzyme, with the tacit assumption that it is a good model of human kidney enzyme. However, previous studies on crude or recombinant human kidney enzymes are limited, and have not resulted in consistent findings on their digitalis sensitivities. Hence, we prepared comparably purified enzymes from human and pig kidneys and determined inhibitory constants of digoxin, ouabain, ouabagenin, bufalin, and marinobufagenin (MBG) on enzyme activity under optimal turnover conditions. We found that each compound had the same potency against the two enzymes, indicating that (i) the pig enzyme is an appropriate model of the human enzyme, and (ii) prior discrepant findings on human kidney enzymes were either due to structural differences between the natural and recombinant enzymes or because potencies were determined using binding constants of digitalis for enzymes under nonphysiological conditions. In conjunction with previous findings, our newly determined inhibitory constants of digitalis compounds for human kidney enzymes indicate that (i) of the compounds that have long been advocated to be endogenous hormones, only bufalin and MBG may act as such at kidney tubules, and (ii) beneficial effects of digoxin, the only digitalis with extensive clinical use, does not involve its inhibitory effect on renal tubular Na/K-ATPase.
PubMed: 28782051
DOI: 10.1021/acsomega.7b00591 -
South African Medical Journal =... Dec 2014Digoxin is one of the oldest of drugs acting on the heart and still one of the most frequently used. While in atrial fibrillation digoxin continues to have a valid role... (Meta-Analysis)
Meta-Analysis Review
Digoxin is one of the oldest of drugs acting on the heart and still one of the most frequently used. While in atrial fibrillation digoxin continues to have a valid role in the control of ventricular rate when added to beta-blockers and calcium antagonists, digoxin for heart failure is no longer a supportable option in view of the negative recent meta-analysis.
Topics: Anti-Arrhythmia Agents; Atrial Fibrillation; Digitalis; Digoxin; Heart Failure; Humans; Plant Preparations
PubMed: 26242504
DOI: 10.7196/samj.8634 -
Anatolian Journal of Cardiology 2015Digitalis preparations are commonly used by children and adults with heart diseases worldwide, although excessive doses may cause cardiac effects. The aim of the study...
OBJECTIVE
Digitalis preparations are commonly used by children and adults with heart diseases worldwide, although excessive doses may cause cardiac effects. The aim of the study is to evaluate the antiarrhythmic effect of Crataegus oxyacantha extract on digoxin-induced arrhythmias in anesthetized Wistar rats.
METHODS
Control and experimental groups were evaluated for arrhythmias induced by digoxin. Fifteen rats (7 as controls and 8 as the experimental group) were included in the study. The dry fruits of 100 mg Crataegus oxyacantha were extracted by percolation method. Digoxin, at a dose of 40 µg/kg/min, was infused to form the arrhythmias in all rats. Simultaneously, the extract was infused into the experimental group, while 0.9% NaCl was infused into control group. Electrocardiographic QRS prolongation and arterial blood pressure changes were analyzed.
RESULTS
The experimental group lived longer (62.13±2.20 min) than the controls (p=0.002). On the other hand, the time to beginning of QRS prolongation did not differ between the two groups (p=0.812). Bradycardia was significant in the control group (288.01±10.54 beat/min and p=0.01). The maximum QRS duration was observed in the control group during the digoxin and 0.9% NaCl infusion period (53.29±3.99 ms and p=0.001). Also, the durations of atrial and ventricular arrhythmias were shorter in the experimental group. However, arterial blood pressure dipping was significant in the experimental group (23.67±10.89 mm Hg and p<0.001).
CONCLUSION
Crataegus oxyacantha alcoholic extract produced an antiarrhythmic effect that was induced by digoxin in Wistar rats. However, in the clinical use of this extract, the hypotensive effect should be considered. Also, the alcoholic extract of Crataegus oxyacantha may be an alternative treatment medication for arrhythmias induced by digoxin toxicity in humans.
Topics: Animals; Anti-Arrhythmia Agents; Arrhythmias, Cardiac; Crataegus; Digoxin; Disease Models, Animal; Heart Rate; Male; Phytotherapy; Plant Extracts; Random Allocation; Rats; Rats, Wistar
PubMed: 25880053
DOI: 10.5152/akd.2014.5869 -
Journal of Nephropharmacology 2015Herbal therapy is a holistic therapy, integrating emotional, mental and spiritual levels. Life style, emotional, mental and spiritual considerations are part of any... (Review)
Review
Herbal therapy is a holistic therapy, integrating emotional, mental and spiritual levels. Life style, emotional, mental and spiritual considerations are part of any naturopathic approach. The use of herbs does not generally involve "drug" actions or adverse effects. Although medicinal plants are widely used and assumed to be safe, however, they can potentially be toxic. Where poisoning from medicinal plants has been reported, it usually has been due to misidentification of the plants in the form, in which they are sold, or incorrectly preparation and administration by inadequately trained personnel. There are some "drug like" plants remedies that their actions approach that of pharmaceuticals. Herbalists use these plants in treatment strategies and in countries such as Britain their vast availability is restricted by law. Digitalis is one of these examples and the number of these plants is not a lot. The mechanisms by which the herbs generally act are not established, however, most of medicinal plants possess antioxidant activities. The plants have been shown to effective by this property is various conditions including cancer, memory deficit and Alzheimer, atherosclerosis, diabetes and other cardiovascular diseases. Antioxidant activities of herbal medicines are also effective in reducing the toxicities of toxic agents or other drugs.
PubMed: 28197471
DOI: No ID Found -
Hepato-gastroenterology Sep 2014The objective of this study was to evaluate the efficacy and safety of landiolol hydrochloride, a newly developed ultra-short-acting β1-selective blocker, for... (Comparative Study)
Comparative Study
BACKGROUND/AIMS
The objective of this study was to evaluate the efficacy and safety of landiolol hydrochloride, a newly developed ultra-short-acting β1-selective blocker, for postoperative tachyarrhythmia after esophagectomy.
METHODOLOGY
In total 231 patients underwent transthoracic esophagectomy at the Department of Gastroenterological Surgery (Surgery II), Nagoya University Graduate School of Medicine from 2007 to 2012. Twenty-four patients who were treated with either landiolol hydrochloride (n = 11) or conventional agents (combination of calcium channel blocker and digitalis preparation; control group, n = 13) for postoperative tachyarrhythmia after transthoracic esophagectomy were retrospectively analyzed. Tachyarrhythmia was defined as a heart rate of >120 bpm or atrial fibrillation. Hemodynamic changes, conversion rates, and adverse events were evaluated.
RESULTS
The reduction in the heart rate at 1 h after medication was seen significantly more frequent in the landiolol group than in the control group. The time to conversion to sinus rhythm was also significantly shorter in the landiolol group. There were no significant differences between the two groups in blood pressure either before or after the medication. One patient in the landiolol group showed hypotension and bradycardia, without serious consequences.
CONCLUSIONS
Landiolol hydrochloride can be effectively and safely used in patients who develop tachyarrhythmia after esophagectomy.
Topics: Adrenergic beta-1 Receptor Antagonists; Aged; Anti-Arrhythmia Agents; Atrial Fibrillation; Calcium Channel Blockers; Digitalis Glycosides; Drug Therapy, Combination; Esophagectomy; Female; Heart Rate; Humans; Japan; Male; Middle Aged; Morpholines; Retrospective Studies; Tachycardia; Treatment Outcome; Urea
PubMed: 25436340
DOI: No ID Found -
Cardiology 2014
Topics: Digitalis; Digitoxin; Famous Persons; Heart Failure; History, 18th Century; History, 19th Century; Humans; Medicine in the Arts; Mental Disorders; Paintings; Phytotherapy; Plant Preparations
PubMed: 24401658
DOI: 10.1159/000355335 -
Theriaca 2014The article series provides a written and pictorial account of the Danish pharmaceutical industry's products from their introduction until about 1950. Part 6 deals with...
The article series provides a written and pictorial account of the Danish pharmaceutical industry's products from their introduction until about 1950. Part 6 deals with products from A/S Pharmacia. A/S Pharmacia was established in Copenhagen in 1922 as a Danish limited company by the enterprising pharmacist Edward Jacobsen. Pharmacia was not Jacobsen's first pharmaceutical company as previously he had established a pharmaceutical agency already in 1913 which in 1919 was reorganized to a limited company by the name of A/S Edward Jacobsen. This agency was later extended to include a production of generics. Jacobsen remained the co-owner and manager of Pharmacia until 1934 where he resigned and established another company, A/S Ejco, for the manufacture of generics. It is worth mentioning that already in 1911 a Swedish pharmaceutical company was established named AB Pharmacia. Today we do not know whether Edward Jacobsen knew about this Swedish company. Later on in 1936 AB Pharmacia and A/S Pharmacia made a contract concerning mutual market sharing, and a research cooperation was brought about between the two companies which resulted in an increase of turnover for A/S Pharmacia. In 1955 the cooperation between the two companies was increased as the Swedish company joined as principal shareholder with the purpose of continuing and developing the Danish company as an independent pharmaceutical company with its own research and development as well as manufacture, control and marketing. Therefore Pharmacia in Denmark was able to establish a synthesis factory in Koge and move the domicile to new premises in Hillered. In 1993 Pharmacia was presented in a printed matter as "The largest Nordic pharmaceutical company" as a result of the merger between the Swedish Kabi Pharmacia, formerly established by a merger between Kabi Vitrum and AB Pharmacia, and the Italian Farmitalia Carlo Erba. Only two years later in 1995 Pharmacia merged with the American pharmaceutical company The Upjohn Company under the name of Pharmacia & Upjohn. In 2000 this company was merged with the chemical group Monsanto under a new name, Pharmacia Corporation. Pharmacia Corporation was taken over by Pfizer in 2003. The early activities of A/S Pharmacia included not only the import of raw materials and ready-made articles, such as medicinal products, but also the manufacture of own medicinal products. This is not surprising considering the founder Edward Jacobsen's pharmaceutical career. Pharmacia's early manufacture of own medicinal products consisted mainly of generics, however, not only the expensive foreign medicinal products, but also any available Danish generics such as easily manufactured pharmacopeia products. It is thus worth mentioning that Pharmacia's own technological production capacity at that time was limited and required a cooperation with other (Danish) pharmaceutical companies. Pharmacia was able to produce tablet cores, but the sugarcoating had to be made by external business partners. Pharmacia was able to produce digitalis preparations, but the standardization of these had to be effected elsewhere. The total production of one of Pharmacia's products took place at an external business partner. Pharmacia was established at a time where the increasing use of industrially manufactured medicinal products, both Danish and foreign ones, had resulted in a considerable decrease in sales of pharmacy produced medicinal products. This had for a long time worried The Danish Association of Pharmacies, and this resulted in a reaction from the association, namely the DAK-products which by nature were produced in Denmark and thus became the most essential element in the fight against the industrially manufactured products--a fight which according to the association had to be fought with all legal means. Therefore The Danish Association of Pharmacies obviously reacted precipitated when in 1926 the association in writing stated that Pharmacia's products were not manufactured in Denmark in spite of the fact that they were labelled as such according to agreement with Landsforeningen Dansk Arbejde, i.e., The National Association Danish Work, which in 1925 allowed Pharmacia to use the labels of the association. The unemployment was high in the 1920'ies and increasing so when Pharmacia subsequently took legal action against the Association of Pharmacies and claimed that the statement was unjustified and might harm Pharmacia, it may indicate that the public of that time looked positively upon the manufacture and the use of Danish manufactured products. The Danish Association of Pharmacies lost the case as the claim according to the court was unjustified and thus unlawful. The suspicions of the association were not supported by facts, however, they were not either completely groundless. Following this The National Association Danish Work gave notice to terminate the contract with Pharmacia concerning the right to use the labels of the association. By expanding the cooperation and later on by merging with the Swedish Pharmacia AB the Danish A/S Pharmacia succeeded in continuing and developing a company where research, development and production of innovative medicinal products as well as of generics could take place in Denmark.
Topics: Denmark; Drug Industry; History, 20th Century; History, 21st Century; Pharmaceutical Preparations; Research; Technology, Pharmaceutical
PubMed: 25816560
DOI: No ID Found -
Canadian Journal of Physiology and... Oct 2012Natriuretic peptides and digitalis-like compounds serve as regulators of homeostasis, including control of volume expansion and blood pressure. The aim of the present...
Natriuretic peptides and digitalis-like compounds serve as regulators of homeostasis, including control of volume expansion and blood pressure. The aim of the present study was to explore possible interactions between atrial natriuretic peptide (ANP) and ouabain in the heart. ANP (1 nmol/L) had no effect in papillary muscle preparations from guinea pigs. Ouabain (1 µmol/L) induced positive inotropic effect. The addition of ANP prior to ouabain resulted in a significant decrease in the ouabain-induced positive inotropic effect, manifested as an attenuated increase in twitch maximal upward force slope and resting muscular tension. In addition, ANP caused an increase in Na⁺-K⁺-ATPase activity in heart microsomal preparations. The effect of ouabain on Na⁺-K⁺-ATPase activity was shown in a biphasic manner. Ouabain (0.01-1 nmol/L) had a small but significant increase on pump activity, but higher doses of ouabain inhibited activity. ANP attenuated ouabain-induced Na⁺-K⁺-ATPase activity. Furthermore, ouabain (50 nmol/L) or ANP (10 nmol/L) alone induced Akt activation in cardiomyocytes. However, ANP blocked ouabain-induced Akt activation. These results point to the existence of interactions between ANP and ouabain on Na⁺-K⁺-ATPase signaling and function in the heart, which may be mediated by regulation of Na⁺-K⁺-ATPase activity and (or) signal transduction mechanisms.
Topics: Animals; Atrial Natriuretic Factor; Cardiotonic Agents; Cells, Cultured; Guinea Pigs; In Vitro Techniques; Male; Mice; Mice, Transgenic; Microsomes; Muscle Tonus; Myocardial Contraction; Myocytes, Cardiac; Ouabain; Papillary Muscles; Proto-Oncogene Proteins c-akt; Rats; Rats, Wistar; Signal Transduction; Sodium-Potassium-Exchanging ATPase; Up-Regulation
PubMed: 22966876
DOI: 10.1139/y2012-112 -
Journal of Analytical Methods in... 2012Serially diluted and agitated (SAD) drugs available commercially are in use with great faith because of the astonishing results they produce. The scientific viewpoint...
Serially diluted and agitated (SAD) drugs available commercially are in use with great faith because of the astonishing results they produce. The scientific viewpoint attached to the centuries-old therapy with SAD drugs, as in homeopathy, remained doubtful for want of appropriate research and insufficient evidence base. The conflicting points related to SAD drug mostly related to the level of concentrations/dilutions, use of drug in contradictory clinical conditions compared to the modern system of medicine, identification of medicinally active ingredient in concentrations and dilutions used in commercially available SAD drugs, and lack of laboratory-based pharmacological data vis-à-vis modern medicine. Modus operandi of SAD drug is also unknown. To address some of these issues an analytical study was carried out wherein commercially available SAD drug Digitalis purpurea, commonly used in different systems of medicine, was put to test. Various concentrations of commercially available Digitalis purpurea were analyzed using analytical methods: cyclic voltammetry, emission spectroscopy, and UV-VIS spectroscopy. These analytical methods apparently identified the medicinal ingredients and effect of serial dilution in commercial preparation of the drugs.
PubMed: 22606641
DOI: 10.1155/2012/109058 -
International Dental Journal Dec 2011Herbs have been used for centuries to prevent and control disease. Herbal extracts are effective because they interact with specific chemical receptors within the body... (Review)
Review
Herbs have been used for centuries to prevent and control disease. Herbal extracts are effective because they interact with specific chemical receptors within the body and are in a pharmacodynamic sense, drugs themselves. By using herbal medicines, patients have averted the many side effects that generally come with traditional medicines, but this does not mean that side effects do not occur. Only knowledgeable practitioners can prescribe the right herb and its proper dosage. Herbal medicines had been considered in every culture, however, pharmaceutical companies overturned this type of thinking. Now, pharmaceuticals are called traditional and herbs are libeled as the 'alternative'. The biggest challenge and problem is lack of information about the effect of herbs in oral tissues, mechanism of effect, and side effects. Several popular conventional drugs on the market are derived from herbs. These include aspirin (from white willow bark), digitalis (from foxglove), and sudafed (modelled after a component in the plant ephedra). Herbal products can vary in their potency. Therefore, care must be taken in selecting herbs, even so, herbal medicines have dramatically fewer side effects and are safer to use than conventional medications. The herbs described in this article are Bloodroot, Caraway, Chamomile, Echinacea, Myrrh, Peppermint, Rosemary, Sage, Thyme, Aloe Vera, Propolis, and a summary of other herbs that are useful in dentistry. Herbs may be good alternatives to current treatments for oral health problems but it is clear that we need more research.
Topics: Anti-Infective Agents; Complementary Therapies; Humans; Pharmaceutical Preparations, Dental; Phytotherapy; Plant Extracts; Plants, Medicinal; Propolis
PubMed: 22117784
DOI: 10.1111/j.1875-595X.2011.00064.x