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KAUNAS UNIVERSITY of MEDICINE Department of Basic & Clinical Pharmacology KAUNAS UNIVERSITY OF MEDICINE Department of Basic & Clinical Pharmacology Trends in the use of Angiotensin converting enzyme inhibitors and Angiotensin II antagonists in Lithuania on 2005 – 2007 years The author: Asta Dičkutė a student of Pharmacy faculty of Kaunas University of Medicine Work supervisor: Lekt. Edmundas Kaduševičius Kaunas 2008 1 TABLE OF CONTENTS Abbreviations.......................................................................................................................................3 1. Introduction and novelty of the master work...................................................................................4 2. Objective and tasks..........................................................................................................................8 3. The renin-angiotensin aldosterone system: physiological role and pharmacologic inhibition .. ...9 3.1 Components of the renin-angiotensin aldosterone system.............................................................9 3.2.Description and clasification of AT1 and AT2 receptors............................................................11 3.3 Classical Endocrine Pathway of Angiotensin Biosynthesis………………………..…………...12 3.4 Tissue renin-angiotensin aldosterone system and Alternative Pathways of Angiotensin Biosynthesis………………………………………………………………………………………...13 3.5 Dysregulation of the renin-angiotensin aldosterone system in Cardiovascular Disorders…..…16 3.6 Renin-angiotensin aldosterone system inhibition. Early Preclinical Findings…………………17 3.7. Pharmacologic Intervention in the Renin-Angiotensin System Cascade…………………..….17 4. Angiotensin – converting enzyme inhibitors. History. Chemical structure. Pharmacokinetics....19 4.1 History…….....…………………………………………………………………………………19 4.2 Chemical structure…………….………………………………………………………………..20 4.3 Pharmacokinetics of the ACE inhibitors…………………..……………………………….......23 5. Angiotensin II antagonists. History. Chemical structure. Pharmacokinetics…………..………..25 5.1 History……………………………………………………………………….…………………25 5.2 Chemical structure………………………………………….………………………………….25 5.3 Pharmacokinetics of angiotensin II antagonists………………………………………………..27 6. Head-to-head efficacy comparisons………………………………………………………….….29 7. Results …………………………………………………...................…………………………...37 8. Discussion ……………………………………………………….……………………………..65 9. Acknowledgments……………………………………………………………………………….67 10. Conclusions. ………………………………………………………………….…..…………….68 11. Summary……………………………………………………………………………………….69 13 Santrauka…………………………………………………………………………………….….71 14. Literatures……………………………………………………………………………….……..73 15. Annexes…………………………………………………………………………..……………75 2 ABBREVIATIONS ACE-I - angiotensin-converting enzyme inhibitors ARA - angiotensin receptor antagonists BP – blood pressure BKR-2 - the bradykinin receptor type 2 CAGE - chymostatin-sensitive angiotensin generating enzyme CVD – cardiovascular diseases EU - Europe Union GFR - glomerular filtration rate HgbA1c - glycated hemoglobin IHD – isheamic heart diseases JG - juxtaglomerular cells LV – left ventricular mRNA - messenger ribonucleic acid PGE-2 - prostaglandin E2 PGI-2 - prostaglandin I2 PRA - plasma renin activity RAAS – the renin-angiotensin aldosterone system RAS – the renin–angiotensin system RCT - randomized controlled trial UK - United Kingdom USA - United States of America WHO – World Health Organisation 3 1. INTRODUCTION AND NOVELTY OF THE MASTER WORK Cardiovascular disease is one of the main causes of death in the world in 2005. Among the 58 million deaths in the world in 2005, noncommunicable diseases were estimated to account for 35 million. Sixteen million of the 35 million deaths occur in people aged under 70 years. The majority of deaths (80%) from noncommunicable diseases occur in low and middle income countries, where most of the world‘s population lives, and the rates are higher than in high income countries. Deaths from noncommunicable diseases occur at earlier ages in low and middle income countries than in high income countries.[1]. Among the noncommunicable diseases, cardiovascular diseases are the leading cause of death, responsible for 30% of all deaths – or about 17.5 million people – in 2005[1]. In addition to the high death toll, noncommunicable diseases cause disability. The most widely used summary measure of the burden of disease is disability-adjusted life years (DALYs), which combines years of healthy life lost to premature death with time spent in less than full health. Almost half of the global burden of disease is caused by noncommunicable diseases, compared with 13% by injuries and 39% by communicable diseases, maternal and perinatal conditions, and nutritional deficiencies combined. While the share of cardiovascular diseases, chronic respiratory diseases and cancer decreases, other noncommunicable diseases increase from 9% to 28%, primarily due to a larger share for mental disorders, and to a lesser extent due to impairments of the sense organs (sense and hearing) and musculoskeletal system (mainly arthritis). [1] Cardiovascular diseases remain the major cause of death across Europe, and a major cause of morbidity and loss of quality of life. [2] Every year more than 4 million Europeans die from diseases of the heart and blood vessels. The prevalence of many cardiovascular diseases increases exponentially with ageing, especially coronary heart disease, heart failure, atria fibrillation, hypertension and aortic stenosis. This is a challenge for modern cardiology since all surveys show that management of elderly patients often differs from management in younger patients. Specific attention is needed for guideline development and adherence with respect to elderly. [2] The population in Europe is ageing rapidly. At present (latest available data ≈ 2004), 13.7% of the European population is aged 65 years or older which is twice the world level. [2] 4 Figure 1. Population of Europe in 2004. [2] There is an apparent west-east gradient with more elderly people in the Western countries. [2] This reflects the longer life-expectancy in Western countries, which is partly a result of the lower age-specific mortality from cardiovascular diseases. Cardiovascular disease is the main cause of death in most countries in Europe. At present (latest available data ≈ 2004), the average age standardised cardiovascular mortality ratio is 5.1 per 1,000 inhabitants for men, and 3.4 for women. [2] CVD is the main cause of death before the age of 65 for men in 28 of the 49 countries of Europe for which we have mortality data and for women in 17 countries. In women, the countries where CVD is the main cause of death before the age of 65 are all Central and Eastern European countries. [3] CVD is the main cause of death before the age of 65 for men in ten countries in the EU (Estonia, Finland, Greece, Ireland, Latvia, Lithuania, Poland, Slovakia, Sweden and the UK). [3] Lithuania is ascribed to the states of high risk cardiovascular diseases by World Health Organisation and Europen Society of Cardiology. [4] About 55 percent of all deaths and 25-50 percent of disablement and 15-20 percent of all medical consultations are because of cardiovascular diseases. Cardiovascular diseases are one of the main causes of death and disablement among middle aged and elder men and women in Lithuania. Mortality from cardiovascular diseases increased 16.6 percent since 2000 till 2005. [4] Cardiovascular diseases are the leading cause of death, responsible for more than a half of all deaths (or 23,8 thousand of 43,8 thousand people) in Lithuania in 2005. Among the cardiovascular diseases, an ischemic heart disease is the leading cause of death (15 thousand deaths in 2005). [4] 5 Almost 89 percent of all deaths from cardiovascular diseases occur in people aged 60 years old and more. The biggest rate of mortality from cardiovascular diseases is in Alytus, Utena, Taurage districts in Lithuania in 2005. [4] Almost 52 percent of all deaths (or 562 people of 1090.86 total deaths) are from cardiovascular diseases in Lithuania in 2006. [4] Age adjusted death rates by cause of death, 2006 Deaths per 100 000 European standard population Causes of death Total 1090,86 Malignant neoplasms 195,45 Diseases of the circulatory system 562,05 External causes of death 149,77 Intentional self-harm 28,94 Table.1. Age adjusted death rates by cause of deaths in Lithuania in 2006 [4] Among the cardiovascular diseases ischaemic heart diseases are the leading cause of death, responsible for 56 percent of all deaths – or about 13.7 thousand people – in 2006 in Lithuania. Almost 82 percent of all deaths from cardiovascular diseases occur in people aged 65 years and more. [4] The morbidity of cardiovascular diseases increases between young and able-bodied population. [4] The decrease of risk factors is one of the main components of the IHD medical treatment strategy. It is important to decrease risk factors for healthy people and patients with IHD symptoms (primary and secondary prevention of the disease). The other not less important component of secondary prevention is the treatment with medicine. It is set that people sick with IHD and using every of the main medicines (aspirin, BAB, AKF inhibitor or statin) have ¼ less isheamic heart attacks, people who use drugs combinations decrease heart attacks till ¾ ones. [5] Drugs that inhibit the renin–angiotensin system (RAS), namely angiotensin-converting enzyme inhibitors (ACE-I) and angiotensin receptor antagonists (ARA) are gaining increasing popularity as initial medications for the management of
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