34525-Article Text-162102-1-6-20190720

Total Page:16

File Type:pdf, Size:1020Kb

34525-Article Text-162102-1-6-20190720 International Journal of Pharmacy and Pharmaceutical Sciences Print ISSN: 2656-0097 | Online ISSN: 0975-1491 Vol 11, Issue 9, 2019 Original Article PRESCRIPTION PATTERN OF CARDIOVASCULAR AND/OR ANTIDIABETIC DRUGS IN ABUJA DISTRICT HOSPITALS NKEIRUKA GRACE OSUAFOR *, CHINWE VICTORIA UKWE, MATTEW JEGBEFUME OKONTA Department of Clinical Pharmacy and Pharmacy Management, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, PMB 410001 Enugu State, Nigeria Email: [email protected] Received: 10 Jun 2019 Revised and Accepted: 25 Jul 2019 ABSTRACT Objective: The study aimed to describe the prescription pattern of cardiovascular and/or anti-diabetic drugs and adherence to the World Health Organization (WHO) prescribing indicators in Abuja District Hospitals. Methods: This descriptive retrospective study was carried out in Asokoro and Maitama District Hospitals Abuja. One thousand and nine prescriptions that contained a cardiovascular drug (CVD) and/or anti-diabetic drug issued between June 2017 and May 2018 from the Medical Outpatient Department were analyzed. Data were collected from the pharmacy electronic database, prescription pattern and adherence to WHO prescribing indicators were assessed. The analysis was done using descriptive statistics. Results were presented as percentages, means, and standard deviations. Results: The frequency of treatment was higher among women (58.8%) and the age group of 41–60 (54.8%). The average number of drugs prescribed was 3.3±1.6: the percentage of drugs prescribed in generic was (64%) and (78.8%) were from the Essential Drug List (EDL). Calcium Channel Blockers (CCB, 71.7%) and Biguanides (B, 92.4%) were the most prescribed CVD and anti-diabetic drug. The majority of the CVD (74.5%) and diabetes (63.6%) patients were on combination therapy. The most frequent CVD combination was CCB plus Angiotensin-Converting Enzyme Inhibitors/Angiotensin Receptor Blockers (29.7%). Compared to men, the proportion of females taking one or more CVD (61.3%) or antidiabetic (56.4%) was higher. Conclusion: The prescribing indicators are not optimal in Abuja district hospitals. Women received more treatment for cardiovascular and diabetes diseases than men while the age range of 41-60 was more treated than other age groups. Keywords: Cardiovascular, Anti-diabetic, Prescription pattern, Prescribing indicators, District hospitals © 2019 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open-access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/) DOI: http://dx.doi.org/10.22159/ijpps.2019v11i9.34525 INTRODUCTION The district hospitals in FCT are at the center of the provision of care for CVD and diabetes, and make a good site for an investigation into Non-Communicable Diseases (NCDs) is a global health threat the prescription pattern. affecting men and women in their most productive years. In 2016, NCDs were responsible for more than 70% of the global deaths [1]. There are variations in the reports of prescription patterns for CVDs Presently an epidemiological transition has taken place in lower- and diabetes drugs, studies have reported Calcium Channel Blockers middle-income countries [2] where NCDs constitute more than 60% (CCB) [11–13] or Angiotensin-Converting Enzyme Inhibitor (ACEI) of deaths in the region [1]. Cardiovascular diseases (CVDs) and [14, 15] as the most utilized class of antihypertensive drugs. Other diabetes were responsible for more than 50% of mortality due to studies have documented diuretics [16, 17] as the most utilized CVD. NCDs in lower-middle-income countries [1]. Global Health Estimates Reports on the prescription pattern of anti-diabetics documented in 2016 showed that CVDs and diabetes accounted for 29% of Years sulphonylureas [14,18] or metformin [19] as the most utilized class of Life Lost and 40.7% of deaths due to NCDs among Nigerian men of diabetes drug. However, inherent differences exist in prescription and women [1, 3]. In Nigeria, the prevalence of CVDs has not been patterns across countries and even among similar health institutions established but existing evidence shows an increase in the of the same country, which necessitates more information on the prevalence of risk factors like hypertension and obesity [4, 5]. The pattern of use of drugs for these diseases. With more drugs being prevalence of diabetes in Nigeria ranges between 4.04% [6] to registered in Nigeria, there is always a gap in the knowledge of the 5.77% [7]. With these increases, hospital consultations and use of drugs. Also, the guidelines on the management of CVDs and attendant drug prescription which is an integral part of the diabetes are not gender or age-specific on classes of a drug to use and it is not clear whether the prescription is the same for different management of CVDs and diabetes are likely to assume an upward gender and age group. This study was undertaken to assess and different trend. Consequently, there is a need to evaluate the prescription patterns for CVD and diabetes and adherence to WHO quality of care received by the patients in terms of prescription. prescribing indicators in two secondary health institutions. Existing evidence suggests that Cardiovascular (CV) drugs and anti- diabetic drugs are among the highest therapeutic drug class MATERIALS AND METHODS prescribed in the outpatient [8, 9]. The WHO recognizes the investigation of prescription as an objective method to describe drug Methods use in health facilities [10]. Evaluation of prescription pattern and Study design and setting prescribing indicators can describe the prevailing prescription trend and assess the extent of rational drug use. Drug use study can be This retrospective study was conducted in Abuja District Hospitals used to evaluate the healthcare needs of people according to age and in Nigeria from June to August 2018. Abuja is the Federal Capital sex at various levels of the health care system and this may Territory (FCT). FCT has thirteen district hospitals that are contribute to adjustments in the drug policy of a country's health established and managed by the FCT Hospital Management Board. care system. This is particularly important in Nigeria where drug The operations of clinical services in these hospitals differ to some products exist both as a single agent and fixed-dose combinations. extent as they do not all have the same type of specialists. Two Osuafor et al. Int J Pharm Pharm Sci, Vol 11, Issue 9, 21-27 district hospitals were purposively selected out of the thirteen Analysis of data district hospitals. Asokoro and Maitama District Hospitals were chosen because they maintain an accessible electronic medical The data were coded into Statistical Package for the Social Sciences database that covers the period of the study and runs a Medical for Window (IBM SPSS version 21) and subsequently analyzed using Outpatient Department (MOPD). Information in the database of descriptive statistics. Association between prescriptions, gender, pharmacy department include patient identification number, date of and age were tested with chi-square. P-value<or = to 0.05 was birth, date of prescription, sex, occupation, drugs prescribed, clinic considered statistically significant. Results were expressed in where the prescription is being generated from, source of funding frequencies, percentages, numbers, means and standard deviations. for the treatment, The Medical Outpatient Department (MOPD) To evaluate the prescription pattern, the number of cardiovascular holds a CV and diabetes clinic on two separate days of the week. and antidiabetic drugs was determined for each prescription. The drugs were classified according to the Anatomical Therapeutic A sampling of the prescriptions Chemical (ATC) code. The cardiovascular drugs include calcium Using the information provided from the pharmacy records on the channel blockers-C08, agents acting on the rennin angiotensin number of cardiovascular (CV) drugs and anti-diabetics dispensed system-C09, diuretics-C03, beta-blocking agents-C07, centrally for the period, the total prescriptions containing a cardiovascular acting drugs-C02A, and cardiac therapy-C01. The anti-diabetic was drug and/or anti-diabetic were estimated to be 7279. The classified into biguanides-A10BA, sulfonylureas-A10BB, dipeptidyl consultation days and prescriptions containing cardiovascular (CV) peptidase (DPP-4) inhibitors-A10BH and insulin-A10A. The and/or anti-diabetic drugs were selected using systematic random prescription pattern for cardiovascular and anti-diabetic drugs was sampling. The two consultation days were listed and alternate days evaluated according to gender and age. The percentage of were selected. On each day, every fourth prescription from MOPD cardiovascular and anti-diabetic drugs prescribed in generic and was selected. Prescriptions included in the study were those from the Essential Drug List (EDL) was also assessed. Nigeria and containing at least one CV and/or anti-diabetic drug prescribed from FCT EDL were utilized. The WHO prescribing indicators as MOPD for patients above 18 y. cardiovascular drugs are those used recognized by the World Health Organization/International for hypertension and heart failure. Excluded prescriptions are those Network for Rational Use of Drugs (WHO/INRUD) were analyzed for written without sex, age. There was no replacement. the prescriptions. The prescribing indicators include the average number of drugs per prescription, percentage of drugs prescribed by Data collection
Recommended publications
  • Quinidine, Beta-Blockers, Diphenylhydantoin, Bretylium *
    Pharmacology of Antiarrhythmics: Quinidine, Beta-Blockers, Diphenylhydantoin, Bretylium * ALBERT J. WASSERMAN, M.D. Professor of Medicine, Chairman, Division of Clinical Pharmacology, Medical College of Virginia, Health Sciences Division of Virginia Commonwealth University, Richmond, Virginia JACK D. PROCTOR, M.D. Assistant Professor of Medicine, Medical College of Virginia, Health Sciences Division of Virginia Commonwealth University, Richmond, Virginia The electrophysiologic effects of the antiar­ adequate, controlled clinical comparisons are virtu­ rhythmic drugs, presented elsewhere in this sym­ ally nonexistent. posium, form only one of the bases for the selec­ A complete presentation of the non-electro­ tion of a therapeutic agent in any given clinical physiologic pharmacology would include the follow­ situation. The final choice depends at least on the ing considerations: following factors: 1. Absorption and peak effect times 1. The specific arrhythmia 2. Biotransformation 2. Underlying heart disease, if any 3. Rate of elimination or half-life (t1d 3. The degree of compromise of the circula­ 4. Drug interactions tion, if any 5. Toxicity 4. The etiology of the arrhythmia 6. Clinical usefulness 5. The efficacy of the drug for that arrhythmia 7. Therapeutic drug levels due to that etiology 8. Dosage schedules 6. The toxicity of the drug, especially in the As all of the above data cannot be presented in given patient with possible alterations in the limited space available, only selected items will volume of distribution, biotransformation, be discussed. Much of the preceding information and excretion is available, however, in standard texts ( 1 7, 10). 7. The electrophysiologic effects of the drug (See Addendum 1) 8. The routes and frequency of administration Quinidine.
    [Show full text]
  • Malaysian STATISTICS on MEDICINE 2005
    Malaysian STATISTICS ON MEDICINE 2005 Edited by: Sameerah S.A.R Sarojini S. With contributions from Goh A, Faridah A, Rosminah MD, Radzi H, Azuana R, Letchuman R, Muruga V, Zanariah H, Oiyammal C, Sim KH, Fong AYY, Tamil Selvan M, Basariah N, Hooi LS, Zaki Morad, Fadilah O, Lim V.K.E., Tan KK, Biswal BM, Lim YS, Lim GCC, Mohammad Anwar H.A, Ahmad Sabri O, Mary SC, Marzida M, Benjamin Chan TM, Suarn Singh, Zoriah A, Noor Ratna N , Abdul Razak M, Norzila Z, Shamsinah H A publication of the Pharmaceutical Services Division and the Clinical Research Centre Ministry of Health Malaysia Malaysian Statistics On Medicine 22005005 Edited by: Sameerah S.A.R Sarojini S. With contributions from Goh A, Faridah A, Rosminah MD, Radzi H, Azuana R, Letchuman R, Muruga V, Zanariah H, Oiyammal C, Sim KH, Fong AYY, Tamil Selvan M, Basariah N, Hooi LS, Zaki Morad, Fadilah O, Lim V.K.E., Tan KK, Biswal BM, Lim YS, Lim GCC, Mohammad Anwar H.A, Ahmad Sabri O, Mary SC, Marzida M, Benjamin Chan TM, Suarn Singh, Zoriah A, Noor Ratna N , Abdul Razak M, Norzila Z, Shamsinah H A publication of the Pharmaceutical Services Division and the Clinical Research Centre Ministry of Health Malaysia Malaysian Statistics On Medicine 2005 April 2007 © Ministry of Health Malaysia Published by: The National Medicines Use Survey Pharmaceutical Services Division Lot 36, Jalan Universiti 46350 Petaling Jaya Selangor, Malaysia Tel. : (603) 4043 9300 Fax : (603) 4043 9400 e-mail : [email protected] Web site : http://www.crc.gov.my/nmus This report is copyrighted.
    [Show full text]
  • Pharmaceutical Services Division and the Clinical Research Centre Ministry of Health Malaysia
    A publication of the PHARMACEUTICAL SERVICES DIVISION AND THE CLINICAL RESEARCH CENTRE MINISTRY OF HEALTH MALAYSIA MALAYSIAN STATISTICS ON MEDICINES 2008 Edited by: Lian L.M., Kamarudin A., Siti Fauziah A., Nik Nor Aklima N.O., Norazida A.R. With contributions from: Hafizh A.A., Lim J.Y., Hoo L.P., Faridah Aryani M.Y., Sheamini S., Rosliza L., Fatimah A.R., Nour Hanah O., Rosaida M.S., Muhammad Radzi A.H., Raman M., Tee H.P., Ooi B.P., Shamsiah S., Tan H.P.M., Jayaram M., Masni M., Sri Wahyu T., Muhammad Yazid J., Norafidah I., Nurkhodrulnada M.L., Letchumanan G.R.R., Mastura I., Yong S.L., Mohamed Noor R., Daphne G., Kamarudin A., Chang K.M., Goh A.S., Sinari S., Bee P.C., Lim Y.S., Wong S.P., Chang K.M., Goh A.S., Sinari S., Bee P.C., Lim Y.S., Wong S.P., Omar I., Zoriah A., Fong Y.Y.A., Nusaibah A.R., Feisul Idzwan M., Ghazali A.K., Hooi L.S., Khoo E.M., Sunita B., Nurul Suhaida B.,Wan Azman W.A., Liew H.B., Kong S.H., Haarathi C., Nirmala J., Sim K.H., Azura M.A., Asmah J., Chan L.C., Choon S.E., Chang S.Y., Roshidah B., Ravindran J., Nik Mohd Nasri N.I., Ghazali I., Wan Abu Bakar Y., Wan Hamilton W.H., Ravichandran J., Zaridah S., Wan Zahanim W.Y., Kannappan P., Intan Shafina S., Tan A.L., Rohan Malek J., Selvalingam S., Lei C.M.C., Ching S.L., Zanariah H., Lim P.C., Hong Y.H.J., Tan T.B.A., Sim L.H.B, Long K.N., Sameerah S.A.R., Lai M.L.J., Rahela A.K., Azura D., Ibtisam M.N., Voon F.K., Nor Saleha I.T., Tajunisah M.E., Wan Nazuha W.R., Wong H.S., Rosnawati Y., Ong S.G., Syazzana D., Puteri Juanita Z., Mohd.
    [Show full text]
  • 110499 Calcium-Antagonist Drugs
    DRUG THERAPY Review Article Drug Therapy smooth muscle (arteriolar and venous), nonvascular smooth muscle (bronchial, gastrointestinal, genitouri- nary, and uterine), and noncontractile tissues (pan- A LASTAIR J.J. WOOD, M.D., Editor creas, pituitary, adrenal glands, salivary glands, gastric mucosa, white cells, platelets, and lacrimal tissue). Blockade of L-type channels in vascular tissues results CALCIUM-ANTAGONIST DRUGS in the relaxation of vascular smooth muscle and in cardiac tisssue results in a negative inotropic effect. DARRELL R. ABERNETHY, M.D., PH.D., The ability of these drugs to decrease smooth-muscle AND JANICE B. SCHWARTZ, M.D. and myocardial contractility results in both clinically desirable antihypertensive and antianginal effects and undesirable myocardial depression. RUGS classified as calcium antagonists or Other calcium channels with electrophysiologic calcium-channel blockers were introduced properties have also been identified. These channels, into clinical medicine in the 1960s and are to which the calcium antagonists do not bind, in- D clude the N-type channels in neuronal tissue, P-type now among the most frequently prescribed drugs for the treatment of cardiovascular diseases.1 Although channels in Purkinje tissues, and T-type (transient potential) channels in cardiac nodal structures and the currently available calcium antagonists are chem- 4,5 ically diverse, they share the common property of vascular smooth muscle. blocking the transmembrane flow of calcium ions Regulation of the L-type channels may differ in through voltage-gated L-type (slowly inactivating) different types of cells. In cardiac myocytes, these channels.2 These drugs have proved effective in pa- channels are activated by catecholamines and other stimuli that activate adenylyl cyclase or cyclic aden- tients with hypertension, angina pectoris, and cardi- 6-8 ac arrhythmias and may be beneficial in patients with osine monophosphate–dependent protein kinase.
    [Show full text]
  • Protective Effect of Eicosapentaenoic Acid on Ouabain Toxicity in Neonatal
    Proc. Nati. Acad. Sci. USA Vol. 87, pp. 7834-7838, October 1990 Medical Sciences Protective effect of eicosapentaenoic acid on ouabain toxicity in neonatal rat cardiac myocytes (cardiac glycoside toxicity/w-3 fatty acid effect/cytosolic calcium overload/cardiac antiarrhythmic/Na,K-ATPase inhibition) HAIFA HALLAQ*t, ALOIS SELLMAYERt, THOMAS W. SMITH§, AND ALEXANDER LEAF* *Department of Preventive Medicine, Harvard Medical School and Massachusetts General Hospital, Boston, MA 02114; tInstitut fur Prophylaxe und Epidemiologie der Kreislaufkrankheiten, Universitat Munchen, Pettenkofer Strasse 9, 8000 Munich 2, Federal Republic of Germany; and §Cardiovascular Division, Departments of Medicine, Brigham and Women's Hospital and Harvard Medical School, Boston, MA 02114 Contributed by Alexander Leaf, June 26, 1990 ABSTRACT Isolated neonatal cardiac myocytes have been sarcolemmal membranes of the heart cells. Furthermore, a utilized as a model for the study of cardiac arrhythmogenic prospective randomized clinical trial (7) showed that, among factors. The myocytes respond to the toxic effects of a potent men who had recently suffered a myocardial infarction, those cardiac glycoside, ouabain at 0.1 mM, by an increase in their that were advised to eat fish two or three times a week had spontaneous beating rate and a reduction in amplitude of a 29% reduction in fatal myocardial infarctions over a sub- contractions resulting within minutes in a lethal state of sequent 2-year period compared to those patients not given contracture. Incubating the isolated myocytes for 3-S5 days in such advice. There was, however, no significant difference in culture medium enriched with 5 ,IM arachidonic acid [20:4 cardiac events; those eating fish just did not die as frequently (n-6)] had no effect on the development of lethal contracture of their myocardial infarctions.
    [Show full text]
  • Cardenolide Biosynthesis in Foxglove1
    Review 491 Cardenolide Biosynthesis in Foxglove1 W. Kreis2,k A. Hensel2, and U. Stuhlemmer2 1 Dedicated to Prof. Dr. Dieter He@ on the occasion of his 65th birthday 2 Friedrich-Alexander-Universität Erlangen, Institut für Botanik und Pharmazeutische Biologie, Erlangen, Germany Received: January 28, 1998; Accepted: March 28, 1998 Abstract: The article reviews the state of knowledge on the genuine cardiac glycosides present in Digitalis species have a biosynthesis of cardenolides in the genus Digitalis. It sum- terminal glucose: these cardenolides have been termed marizes studies with labelled and unlabelled precursors leading primary glycosides. After harvest or during the controlled to the formulation of the putative cardenolide pathway. Alter- fermentation of dried Digitalis leaves most of the primary native pathways of cardenolide biosynthesis are discussed as glycosides are hydrolyzed to yield the so-called secondary well. Special emphasis is laid on enzymes involved in either glycosides. Digitalis cardenolides are valuable drugs in the pregnane metabolism or the modification of cardenolides. medication of patients suffering from cardiac insufficiency. In About 20 enzymes which are probably involved in cardenolide therapy genuine glycosides, such as the lanatosides, are used formation have been described "downstream" of cholesterol, as well as compounds obtained after enzymatic hydrolysis including various reductases, oxido-reductases, glycosyl trans- and chemical saponification, for example digitoxin (31) and ferases and glycosidases as well as acyl transferases, acyl es- digoxin, or chemical modification of digoxin, such as metildig- terases and P450 enzymes. Evidence is accumulating that car- oxin. Digitalis lanata Ehrh. and D.purpurea L are the major denolides are not assembled on one straight conveyor belt but sources of the cardiac glycosides most frequently employed in instead are formed via a complex multidimensional metabolic medicine.
    [Show full text]
  • Quo Vadis Cardiac Glycoside Research?
    toxins Review Quo vadis Cardiac Glycoside Research? Jiˇrí Bejˇcek 1, Michal Jurášek 2 , VojtˇechSpiwok 1 and Silvie Rimpelová 1,* 1 Department of Biochemistry and Microbiology, University of Chemistry and Technology Prague, Technická 5, Prague 6, Czech Republic; [email protected] (J.B.); [email protected] (V.S.) 2 Department of Chemistry of Natural Compounds, University of Chemistry and Technology Prague, Technická 3, Prague 6, Czech Republic; [email protected] * Correspondence: [email protected]; Tel.: +420-220-444-360 Abstract: AbstractCardiac glycosides (CGs), toxins well-known for numerous human and cattle poisoning, are natural compounds, the biosynthesis of which occurs in various plants and animals as a self-protective mechanism to prevent grazing and predation. Interestingly, some insect species can take advantage of the CG’s toxicity and by absorbing them, they are also protected from predation. The mechanism of action of CG’s toxicity is inhibition of Na+/K+-ATPase (the sodium-potassium pump, NKA), which disrupts the ionic homeostasis leading to elevated Ca2+ concentration resulting in cell death. Thus, NKA serves as a molecular target for CGs (although it is not the only one) and even though CGs are toxic for humans and some animals, they can also be used as remedies for various diseases, such as cardiovascular ones, and possibly cancer. Although the anticancer mechanism of CGs has not been fully elucidated, yet, it is thought to be connected with the second role of NKA being a receptor that can induce several cell signaling cascades and even serve as a growth factor and, thus, inhibit cancer cell proliferation at low nontoxic concentrations.
    [Show full text]
  • Diagnosis and Treatment of Digoxin Toxicity
    Postgrad Med J: first published as 10.1136/pgmj.69.811.337 on 1 May 1993. Downloaded from Postgrad Med J (1993) 69, 337 - 339 i) The Fellowship of Postgraduate Medicine, 1993 Review Article Diagnosis and treatment ofdigoxin toxicity Gregory Y.H. Lip, Malcolm J. Metcalfe and Francis G. Dunn Department ofCardiology, Stobhill General Hospital, Glasgow G21 3UW, UK Introduction Cardiac glycosides are unusual in having a narrow important to emphasize that the clinical diagnosis therapeutic range, which is idiosyncratic to the of toxicity is of fundamental importance and individual. In view of this it is perhaps not surpris- should not be discarded because of 'normal' ing that toxicity is a common occurrence, being plasma digoxin concentrations. reported in up to 35% of digitalized patients.' There are several mechanisms which can lead to Use ofplasma concentration measurements this problem. Firstly, digoxin is excreted mainly by the kidneys, and therefore, any impairment ofrenal In an attempt to improve digoxin therapy, it is function may lead to higher than expected plasma frequently advocated that the plasma digoxin con- concentrations. Congestive cardiac failure, renal centration should be measured. Trough plasma failure and advanced age can also cause toxicity by concentrations below 0.8 ng/ml (1.0 nmol/l) are reducing the volume of distribution of the drug. considered sub-therapeutic and levels greater than Concomitant electrolyte imbalance, notably 2.0 ng/ml (2.56 nmol/l) toxic. Unfortunately, there hypokalaemia, hypomagnesaemia and hypercal- is a marked overlap of measured plasma levels copyright. caemia can potentiate digoxin toxicity. Approx- between groups of patients with and without imately 30% of digoxin is plasma protein bound evidence of toxicity.3'4 For example, one patient and thus certain other drugs such as amiodarone may exhibit evidence of toxicity at a measured and calcium antagonists can lead to higher than plasma drug level ofonly 0.8 ng/ml, whilst another expected plasma concentrations.
    [Show full text]
  • Studies on Myocardial Metabolism. V. the Effects of Lanatoside-C on the Metabolism of the Human Heart
    STUDIES ON MYOCARDIAL METABOLISM. V. THE EFFECTS OF LANATOSIDE-C ON THE METABOLISM OF THE HUMAN HEART J. M. Blain, … , A. Siegel, R. J. Bing J Clin Invest. 1956;35(3):314-321. https://doi.org/10.1172/JCI103280. Research Article Find the latest version: https://jci.me/103280/pdf STUDIES ON MYOCARDIAL METABOLISM. V. THE EFFECTS OF LANATOSIDE-C ON THE METABOLISM OF THE HUMAN HEART 1 By J. M. BLAIN, E. E. EDDLEMAN, A. SIEGEL, AND R. J. BING (From the Departments of Experimental Medicine and Clinical Physiology, The Medical College of Alabama, Birmingham, Alabama, and the Veterans' Administration Hospital, Birmingham, Ala.) (Submitted for publication Septenber 6, 1955; accepted November 16, 1955) Since 1785 when Withering undertook the first this method should aid in elucidating the meta- systemic study of the effects of digitalis, a large bolic pathways within the heart muscle; thus reac- amount of data has been accumulated describing tions determined by more precise in vitro methods its pharmacological effects. Despite intensive could be re-evaluated in the light of data obtained study, the underlying mechanism responsible for on the human heart in vivo. the beneficial results in patients with heart failure The various cardiac glycosides differ in time of remains obscure. Although digitalis in small doses onset and persistence of action. Lanatoside-C, the may affect the heart rate through its vagal effect, preparation used in this study, is a purified deriva- it is agreed that the predominant action of this tive of digitalis lanata which can be given intra- drug is on the heart muscle directly (1).
    [Show full text]
  • Profiling and Structural Analysis of Cardenolides in Two Species of Digitalis Using Liquid Chromatography Coupled with High-Resolution Mass Spectrometry
    bioRxiv preprint doi: https://doi.org/10.1101/864959; this version posted December 5, 2019. The copyright holder for this preprint (which was not certified by peer review) is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under aCC-BY-NC 4.0 International license. Profiling and structural analysis of cardenolides in two species of Digitalis using liquid chromatography coupled with high-resolution mass spectrometry Baradwaj Gopal Ravi1†, Mary Grace E. Guardian2†, Rebecca Dickman2, Zhen Q. Wang1* 1Department of Biological Sciences, University at Buffalo, State University of New York, Buffalo, NY 14260, United States 2Department of Chemistry, Chemistry Instrumentation Center, University at Buffalo, State University of New York, Buffalo, NY 14260, United States †These authors contributed equally to this work. *Correspondent author: Tel: (+1)7166454969 [email protected] Keywords: cardiac glycoside; foxglove; Digitalis purpurea; Digitalis lanata; digoxin; digitoxin Abstract Plants of the Digitalis genus contain a cocktail of cardenolides commonly prescribed to treat heart failure. Cardenolides in Digitalis extracts have been conventionally quantified by high- performance liquid chromatography yet the lack of structural information compounded with possible co-eluents renders this method insufficient for analyzing cardenolides in plants. The goal of this work is to structurally characterize cardiac glycosides in fresh-leaf extracts using liquid chromatography coupled with tandem mass spectrometry (LC/MS/MS) that provides exact masses. Fragmentation of cardenolides is featured by sequential loss of sugar units while the steroid aglycon moieties undergo stepwise elimination of hydroxyl groups, which distinguishes different aglycones. The sequence of elution follows diginatigenindigoxigeningitoxigeningitaloxigenindigitoxigenin for cardenolides with the same sugar units but different aglycones using a reverse-phase column.
    [Show full text]
  • Oleandrin: a Cardiac Glycosides with Potent Cytotoxicity
    PHCOG REV. REVIEW ARTICLE Oleandrin: A cardiac glycosides with potent cytotoxicity Arvind Kumar, Tanmoy De, Amrita Mishra, Arun K. Mishra Department of Pharmaceutical Chemistry, Central Facility of Instrumentation, School of Pharmaceutical Sciences, IFTM University, Lodhipur, Rajput, Moradabad, Uttar Pradesh, India Submitted: 19-05-2013 Revised: 29-05-2013 Published: **-**-**** ABSTRACT Cardiac glycosides are used in the treatment of congestive heart failure and arrhythmia. Current trend shows use of some cardiac glycosides in the treatment of proliferative diseases, which includes cancer. Nerium oleander L. is an important Chinese folk medicine having well proven cardio protective and cytotoxic effect. Oleandrin (a toxic cardiac glycoside of N. oleander L.) inhibits the activity of nuclear factor kappa‑light‑chain‑enhancer of activated B chain (NF‑κB) in various cultured cell lines (U937, CaOV3, human epithelial cells and T cells) as well as it induces programmed cell death in PC3 cell line culture. The mechanism of action includes improved cellular export of fibroblast growth factor‑2, induction of apoptosis through Fas gene expression in tumor cells, formation of superoxide radicals that cause tumor cell injury through mitochondrial disruption, inhibition of interleukin‑8 that mediates tumorigenesis and induction of tumor cell autophagy. The present review focuses the applicability of oleandrin in cancer treatment and concerned future perspective in the area. Key words: Cardiac glycosides, cytotoxicity, oleandrin INTRODUCTION the toad genus Bufo that contains bufadienolide glycosides, the suffix-adien‑that refers to the two double bonds in the Cardiac glycosides are used in the treatment of congestive lactone ring and the ending-olide that denotes the lactone heart failure (CHF) and cardiac arrhythmia.
    [Show full text]
  • Ouabain - the Insulin of the Heart Hauke Fürstenwerth
    Ouabain - The Insulin of the Heart Hauke Fürstenwerth To cite this version: Hauke Fürstenwerth. Ouabain - The Insulin of the Heart. International Journal of Clinical Practice, Wiley, 2010, 64 (12), pp.1591. 10.1111/j.1742-1241.2010.02395.x. hal-00599542 HAL Id: hal-00599542 https://hal.archives-ouvertes.fr/hal-00599542 Submitted on 10 Jun 2011 HAL is a multi-disciplinary open access L’archive ouverte pluridisciplinaire HAL, est archive for the deposit and dissemination of sci- destinée au dépôt et à la diffusion de documents entific research documents, whether they are pub- scientifiques de niveau recherche, publiés ou non, lished or not. The documents may come from émanant des établissements d’enseignement et de teaching and research institutions in France or recherche français ou étrangers, des laboratoires abroad, or from public or private research centers. publics ou privés. International Journal of Clinical Practice For PeerOuabain – TheReview Insulin of the HeartOnly Journal: International Journal of Clinical Practice Manuscript ID: IJCP-12-09-0760.R1 Manuscript Type: Perspective Date Submitted by the 18-Jan-2010 Author: Complete List of Authors: Fürstenwerth, Hauke; Hauke Fürstenwerth, consultant Specialty area: International Journal of Clinical Practice Page 1 of 9 International Journal of Clinical Practice 1 2 Title: Ouabain – The Insulin of the Heart 3 4 Author: Dr. Hauke Fürstenwerth 5 6 Unterölbach 3A 7 D-51381 Leverkusen 8 Germany 9 Phone: +49-2171-733740 10 e-mail: [email protected] 11 12 corresponding author: Dr.
    [Show full text]