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ACE Inhibitors
Angiotensin-converting-enzyme inhibitors (ACE inhibitors) are a class of medication used primarily for the treatment of hypertension, high blood pressure and heart failure. This class of medicine works by causing relaxation of blood vessels as well as a decrease in blood volume, which leads to lower blood pressure and decreased oxygen demand from the heart. ACE inhibitors Enzyme inhibitor, inhibit the activity of angiotensin-converting enzyme, an important component of the renin–angiotensin system which converts angiotensin I to angiotensin II, and hydrolyses bradykinin. Therefore, ACE inhibitors decrease the formation of angiotensin II, a vasoconstrictor, and increase the level of bradykinin, a peptide vasodilator. This combination is synergistic in lowering blood pressure. As a result of inhibiting the ACE enzyme in the bradykinin system, the ACE inhibitor drugs allow for increased levels of bradykinin which would normally be degraded. Bradykinin produces prostaglandin. Thi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Captopril
Captopril, sold under the brand name Capoten among others, is an ACE inhibitor, angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first oral ACE inhibitor found for the treatment of hypertension. It does not cause fatigue as associated with beta-blockers. Captopril was patented in 1976 and approved for medical use in 1980. Structure–activity relationship Captopril has an L-proline group which allows it to be more bioavailable in oral formulations. The thiol moiety within the molecule has been associated with two significant adverse effects: the hapten or immune response. This immune response, also known as agranulocytosis, can explain the adverse drug events which may be seen in captopril with the allergic response which includes hives, severe stomach pain, difficulty breathing, and swelling of the face, lips, tongue or throat. In terms of interaction with the enzyme, the molec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peptide
Peptides are short chains of amino acids linked by peptide bonds. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Da or more are called proteins. Chains of fewer than twenty amino acids are called oligopeptides, and include dipeptides, tripeptides, and tetrapeptides. Peptides fall under the broad chemical classes of biological polymers and oligomers, alongside nucleic acids, oligosaccharides, polysaccharides, and others. Proteins consist of one or more polypeptides arranged in a biologically functional way, often bound to ligands such as coenzymes and cofactors, to another protein or other macromolecule such as DNA or RNA, or to complex macromolecular assemblies. Amino acids that have been incorporated into peptides are termed residues. A water molecule is released during formation of each amide bond.. All peptides except cyclic peptides have an N-terminal (amine group) and C-terminal (carboxyl g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diabetes Mellitus
Diabetes mellitus, commonly known as diabetes, is a group of common endocrine diseases characterized by sustained hyperglycemia, high blood sugar levels. Diabetes is due to either the pancreas not producing enough of the hormone insulin, or the cells of the body becoming unresponsive to insulin's effects. Classic symptoms include polydipsia (excessive thirst), polyuria (excessive urination), polyphagia (excessive hunger), Weight loss#Unintentional, weight loss, and blurred vision. If left untreated, the disease can lead to various health complications, including disorders of the Cardiovascular disease, cardiovascular system, Diabetic retinopathy, eye, Diabetic nephropathy, kidney, and Diabetic neuropathy, nerves. Diabetes accounts for approximately 4.2 million deaths every year, with an estimated 1.5 million caused by either untreated or poorly treated diabetes. The major types of diabetes are Type 1 diabetes, type 1 and Type 2 diabetes, type 2. The most common treatment for ty ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heart Failure
Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome caused by an impairment in the heart's ability to Cardiac cycle, fill with and pump blood. Although symptoms vary based on which side of the heart is affected, HF typically presents with shortness of breath, Fatigue (medical), excessive fatigue, and bilateral peripheral edema, leg swelling. The severity of the heart failure is mainly decided based on ejection fraction and also measured by the severity of symptoms. Other conditions that have symptoms similar to heart failure include obesity, kidney failure, liver disease, anemia, and thyroid disease. Common causes of heart failure include coronary artery disease, heart attack, hypertension, high blood pressure, atrial fibrillation, valvular heart disease, alcohol use disorder, excessive alcohol consumption, infection, and cardiomyopathy. These cause heart failure by altering the structure or the function of the heart or in some cases both. There are ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Myocardial Infarction
A myocardial infarction (MI), commonly known as a heart attack, occurs when Ischemia, blood flow decreases or stops in one of the coronary arteries of the heart, causing infarction (tissue death) to the heart muscle. The most common symptom is retrosternal Angina, chest pain or discomfort that classically radiates to the left shoulder, arm, or jaw. The pain may occasionally feel like heartburn. This is the dangerous type of acute coronary syndrome. Other symptoms may include shortness of breath, nausea, presyncope, feeling faint, a diaphoresis, cold sweat, Fatigue, feeling tired, and decreased level of consciousness. About 30% of people have atypical symptoms. Women more often present without chest pain and instead have neck pain, arm pain or feel tired. Among those over 75 years old, about 5% have had an MI with little or no history of symptoms. An MI may cause heart failure, an Cardiac arrhythmia, irregular heartbeat, cardiogenic shock or cardiac arrest. Most MIs occur d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ACE Inhibitors Drug Design
The discovery of an orally inactive peptide from snake venom established the important role of angiotensin converting enzyme (ACE) inhibitors in regulating blood pressure. This led to the development of captopril, the first ACE inhibitor. When the adverse effects of captopril became apparent new derivates were designed. Then after the discovery of two active sites of ACE: N-domain and C-domain, the development of domain-specific ACE inhibitors began. Development of first generation ACE inhibitors The development of the nonapeptide teprotide ( Glu- Trp- Pro- Arg-Pro- Gln- Ile-Pro-Pro), which was originally isolated from the venom of the Brazilian pit viper '' Bothrops jararaca'', greatly clarified the importance of ACE in hypertension. However, its lack of oral activity limited its therapeutic utility. L- benzyl succinic acid (2(R)-benzyl-3-carboxypropionic acid) was described to be the most potent inhibitor of carboxypeptidase A in the early 1980s. The authors referred to it ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ramipril
Ramipril, sold under the brand name Altace among others, is an ACE inhibitor type medication used to treat high blood pressure, heart failure, and diabetic kidney disease. It can also be used as a preventative medication in patients over 55 years old to reduce the risk of having a heart attack, stroke or cardiovascular death in patients shown to be at high risk, such as some diabetics and patients with vascular disease. It is a reasonable initial treatment for high blood pressure. It is taken by mouth. Common side effects include headaches, dizziness, fatigue, and cough. Serious side effects may include liver problems, angioedema, kidney problems, and high blood potassium. Use in pregnancy and breastfeeding is not recommended. It is an ACE inhibitor and works by decreasing renin-angiotensin-aldosterone system activity. Ramipril was patented in 1981 and approved for medical use in 1989. It is available as a generic medication. In 2022, it was the 187th most commonly prescr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lisinopril
Lisinopril is a medication belonging to the drug class of angiotensin-converting enzyme (ACE) inhibitors and is used to treat hypertension (high blood pressure), heart failure, and heart attacks. For high blood pressure it is usually a first-line treatment. It is also used to prevent kidney problems in people with diabetes mellitus. Lisinopril is taken orally (swallowed by mouth). Full effect may take up to four weeks to occur. Common side effects include headache, dizziness, feeling tired, cough, nausea, and rash. Serious side effects may include low blood pressure, liver problems, hyperkalemia (high blood potassium), and angioedema. Use is not recommended during the entire duration of pregnancy as it may harm the baby. Lisinopril works by inhibiting the renin–angiotensin–aldosterone system. Lisinopril was patented in 1978 and approved for medical use in the United States in 1987. It is available as a generic medication. In 2022, it was the third most commonly presc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enalapril
Enalapril, sold under the brand name Vasotec among others, is an ACE inhibitor medication used to treat high blood pressure, diabetic kidney disease, and heart failure. For heart failure, it is generally used with a diuretic, such as furosemide. It is given by mouth or by injection into a vein. Onset of effects are typically within an hour when taken by mouth and last for up to a day. Common side effects include headache, tiredness, feeling lightheaded with standing, and cough. Serious side effects include angioedema and low blood pressure. Use during pregnancy is believed to result in harm to the baby. It is in the angiotensin-converting-enzyme (ACE) inhibitor family of medications. Enalapril was patented in 1978, and came into medical use in 1984. It is on the World Health Organization's List of Essential Medicines. In 2022, it was the 141st most commonly prescribed medication in the United States, with more than 4million prescriptions. It is available as a gener ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Captopril
Captopril, sold under the brand name Capoten among others, is an ACE inhibitor, angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first oral ACE inhibitor found for the treatment of hypertension. It does not cause fatigue as associated with beta-blockers. Captopril was patented in 1976 and approved for medical use in 1980. Structure–activity relationship Captopril has an L-proline group which allows it to be more bioavailable in oral formulations. The thiol moiety within the molecule has been associated with two significant adverse effects: the hapten or immune response. This immune response, also known as agranulocytosis, can explain the adverse drug events which may be seen in captopril with the allergic response which includes hives, severe stomach pain, difficulty breathing, and swelling of the face, lips, tongue or throat. In terms of interaction with the enzyme, the molec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trandolapril
Trandolapril is an ACE inhibitor used to treat high blood pressure. It may also be used to treat other conditions. It is similar in structure to another ramipril but has a cyclohexane group. It is a prodrug that must be metabolized into its active form. It has a longer half-life when compared to other agents in this class. It was patented in 1981 and approved for medical use in 1993. It is marketed by Abbott Laboratories under the brand name Mavik. Side effects Side effects reported for trandolapril include nausea, vomiting, diarrhea, headache, dry cough, dizziness or lightheadedness when sitting up or standing, hypotension, or fatigue. Possible drug interactions Patients also on diuretics may experience an excessive reduction of blood pressure after initiation of therapy with trandolapril. It can reduce potassium loss caused by thiazide diuretics and increase serum potassium when used alone. Therefore, hyperkalemia is a possible risk. Increased serum lithium levels can ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Perindopril
Perindopril is a medication used to treat high blood pressure, heart failure, or stable coronary artery disease. As a long-acting ACE inhibitor, perindopril works by inhibiting production of the vasoconstriction hormone, angiotensin, thereby relaxing blood vessels, increasing urine output, and decreasing blood volume, leading to a reduction of blood pressure. It also increases blood renin activity and decreases aldosterone secretion, causing increased urine production and excretion of sodium. As a prodrug, perindopril is hydrolyzed in the liver to its active metabolite, perindoprilat. It was patented in 1980 and approved for medical use in 1988. Perindopril is taken in the form of perindopril arginine/amlodipine or perindopril erbumine. Both forms are therapeutically equivalent and interchangeable, but the dose prescribed to achieve the same effect may differ between the two forms. Perindopril should not be used during pregnancy, as it may harm the fetus. Some people ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
