Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.Angiotensin-Converting Enzyme Inhibitors: A class of drugs whose main indications are the treatment of hypertension and heart failure. They exert their hemodynamic effect mainly by inhibiting the renin-angiotensin system. They also modulate sympathetic nervous system activity and increase prostaglandin synthesis. They cause mainly vasodilation and mild natriuresis without affecting heart rate and contractility.Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic.Peptidyl-Dipeptidase A: A peptidyl-dipeptidase that catalyzes the release of a C-terminal dipeptide, -Xaa-*-Xbb-Xcc, when neither Xaa nor Xbb is Pro. It is a Cl(-)-dependent, zinc glycoprotein that is generally membrane-bound and active at neutral pH. It may also have endopeptidase activity on some substrates. (From Enzyme Nomenclature, 1992) EC 3.4.15.1.Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.Antihypertensive Agents: Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.Angiotensin I: A decapeptide that is cleaved from precursor angiotensinogen by RENIN. Angiotensin I has limited biological activity. It is converted to angiotensin II, a potent vasoconstrictor, after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME.Hypertension: Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Renin-Angiotensin System: A BLOOD PRESSURE regulating system of interacting components that include RENIN; ANGIOTENSINOGEN; ANGIOTENSIN CONVERTING ENZYME; ANGIOTENSIN I; ANGIOTENSIN II; and angiotensinase. Renin, an enzyme produced in the kidney, acts on angiotensinogen, an alpha-2 globulin produced by the liver, forming ANGIOTENSIN I. Angiotensin-converting enzyme, contained in the lung, acts on angiotensin I in the plasma converting it to ANGIOTENSIN II, an extremely powerful vasoconstrictor. Angiotensin II causes contraction of the arteriolar and renal VASCULAR SMOOTH MUSCLE, leading to retention of salt and water in the KIDNEY and increased arterial blood pressure. In addition, angiotensin II stimulates the release of ALDOSTERONE from the ADRENAL CORTEX, which in turn also increases salt and water retention in the kidney. Angiotensin-converting enzyme also breaks down BRADYKININ, a powerful vasodilator and component of the KALLIKREIN-KININ SYSTEM.Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.Enalaprilat: The active metabolite of ENALAPRIL and a potent intravenously administered angiotensin-converting enzyme inhibitor. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.Oliguria: Decreased URINE output that is below the normal range. Oliguria can be defined as urine output of less than or equal to 0.5 or 1 ml/kg/hr depending on the age.Fosinopril: A phosphinic acid-containing angiotensin-converting enzyme inhibitor that is effective in the treatment of hypertension. It is a prodrug that is converted to its active metabolite fosinoprilat.Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.Double-Blind Method: A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.Nephrosis: Pathological processes of the KIDNEY without inflammatory or neoplastic components. Nephrosis may be a primary disorder or secondary complication of other diseases. It is characterized by the NEPHROTIC SYNDROME indicating the presence of PROTEINURIA and HYPOALBUMINEMIA with accompanying EDEMA.Sodium Chloride Symporter Inhibitors: Agents that inhibit SODIUM CHLORIDE SYMPORTERS. They act as DIURETICS. Excess use is associated with HYPOKALEMIA.Diuretics: Agents that promote the excretion of urine through their effects on kidney function.Pharmaceutical Services, Online: Pharmacy services accessed via electronic means.Pharmacies: Facilities for the preparation and dispensing of drugs.Perfume: A substance, extract, or preparation for diffusing or imparting an agreeable or attractive smell, especially a fluid containing fragrant natural oils extracted from flowers, woods, etc., or similar synthetic oils. (Random House Unabridged Dictionary, 2d ed)Internet: A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.Beauty: Characteristics or attributes of persons or things which elicit pleasurable feelings.Legislation, Pharmacy: Laws and regulations, pertaining to the field of pharmacy, proposed for enactment or enacted by a legislative body.Counterfeit Drugs: Drugs manufactured and sold with the intent to misrepresent its origin, authenticity, chemical composition, and or efficacy. Counterfeit drugs may contain inappropriate quantities of ingredients not listed on the label or package. In order to further deceive the consumer, the packaging, container, or labeling, may be inaccurate, incorrect, or fake.Pharmacy: The practice of compounding and dispensing medicinal preparations.Commerce: The interchange of goods or commodities, especially on a large scale, between different countries or between populations within the same country. It includes trade (the buying, selling, or exchanging of commodities, whether wholesale or retail) and business (the purchase and sale of goods to make a profit). (From Random House Unabridged Dictionary, 2d ed, p411, p2005 & p283)Education, Pharmacy: Formal instruction, learning, or training in the preparation, dispensing, and proper utilization of drugs in the field of medicine.Schools, Pharmacy: Educational institutions for individuals specializing in the field of pharmacy.Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.Blogging: Using an INTERNET based personal journal which may consist of reflections, comments, and often hyperlinks.Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.ItalyHydrogenation: Addition of hydrogen to a compound, especially to an unsaturated fat or fatty acid. (From Stedman, 26th ed)Erectile Dysfunction: The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction.Genetic Testing: Detection of a MUTATION; GENOTYPE; KARYOTYPE; or specific ALLELES associated with genetic traits, heritable diseases, or predisposition to a disease, or that may lead to the disease in descendants. It includes prenatal genetic testing.Carbolines: A group of pyrido-indole compounds. Included are any points of fusion of pyridine with the five-membered ring of indole and any derivatives of these compounds. These are similar to CARBAZOLES which are benzo-indoles.Penile Erection: The state of the PENIS when the erectile tissue becomes filled or swollen (tumid) with BLOOD and causes the penis to become rigid and elevated. It is a complex process involving CENTRAL NERVOUS SYSTEM; PERIPHERAL NERVOUS SYSTEMS; HORMONES; SMOOTH MUSCLES; and vascular functions.Orphan Drug Production: Production of drugs or biologicals which are unlikely to be manufactured by private industry unless special incentives are provided by others.Impotence, Vasculogenic: Inability to achieve and maintain an erection (ERECTILE DYSFUNCTION) due to defects in the arterial blood flow to the PENIS, defect in venous occlusive function allowing blood drainage (leakage) from the erectile tissue (corpus cavernosum penis), or both.Penis: The external reproductive organ of males. It is composed of a mass of erectile tissue enclosed in three cylindrical fibrous compartments. Two of the three compartments, the corpus cavernosa, are placed side-by-side along the upper part of the organ. The third compartment below, the corpus spongiosum, houses the urethra.Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.Tablets: Solid dosage forms, of varying weight, size, and shape, which may be molded or compressed, and which contain a medicinal substance in pure or diluted form. (Dorland, 28th ed)Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed)FormocresolsArthritis, Rheumatoid: A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.Root Canal Irrigants: Chemicals used mainly to disinfect root canals after pulpectomy and before obturation. The major ones are camphorated monochlorophenol, EDTA, formocresol, hydrogen peroxide, metacresylacetate, and sodium hypochlorite. Root canal irrigants include also rinsing solutions of distilled water, sodium chloride, etc.Graft Rejection: An immune response with both cellular and humoral components, directed against an allogeneic transplant, whose tissue antigens are not compatible with those of the recipient.Calcium Hydroxide: A white powder prepared from lime that has many medical and industrial uses. It is in many dental formulations, especially for root canal filling.Kidney Transplantation: The transference of a kidney from one human or animal to another.
Patchett A, Harris E, Tristram E, Wyvratt M, Wu M, Taub D, Peterson E, Ikeler T, ten Broeke J, Payne L, Ondeyka D, Thorsett E, Greenlee W, Lohr N, Hoffsommer R, Joshua H, Ruyle W, Rothrock J, Aster S, Maycock A, Robinson F, Hirschmann R, Sweet C, Ulm E, Gross D, Vassil T, Stone C (1980). "A new class of angiotensin-converting enzyme inhibitors". Nature 288 (5788): 280-3. PMID 6253826. doi:10.1038/288280a0. ...
آنزیم ۲ مبدل آنژیوتانسین (به انگلیسی: Angiotensin-converting enzyme 2) یا به اختصار ACE2، یک اگزوپپتیداز است که موجب تبدیل آنژیوتانسین ۱ به «آنژیوتانسین ۹-۱» (نُه پپتیدی)،[۳] یا تبدیل آنژیوتانسین ۲ به «آنژیوتانسین ۷-۱» می‌گردد.[۴][۵] این آنزیم اثرات مستقیمی بر عملکرد قلب دارد،a و بیشتر در لایهٔ داخلی رگ‌های خونی، قلب و کلیه‌ها بیان می‌شود.[۶] داروهای بازدارندهٔ آنزیم مبدل آنژیوتانسین که در درمان فشار خون بالا استفاده می‌شوند، اثری بر آنزیم ACE2 ندارند.[۷] مشخص شده که گیرنده‌های ACE2، نقطهٔ ورود برخی از انواع کروناویروس‌ها به سلول‌های بدن انسان هستند.[۸] دو گروه مجزا از ...
Sheer Heart Attack》은 1974년 11월 8일 영국의 EMI 레코드와 미국의 엘렉트라 레코드에 의해 발매된 영국의 록 밴드 퀸의 세 번째 스튜디오 음반이다. 그들의 첫 두 음반에 수록된 프로그레시브 주제에서 발췌한 이 음반은 더 전통적인 록 트랙을 특징으로 하고 "클래식" 퀸 사운드를 향한 발걸음을 내디뎠다.[1] 그 음반은 밴드와 로이 토머스 베이커에 의해 제작되었고 영국과 전 세계에서 퀸을 주류로 만들었다. 이 음반의 첫 번째 싱글 음반인 〈Killer Queen〉은 영국 차트에서 2위에 올랐고 빌보드 싱글 차트에서 12위를 차지하며 미국에서 그들의 첫 번째 톱 20 히트곡을 제공했다. 《Sheer Heart Attack》은 1975년에 12위를 차지하며 미국 탑 20을 기록한 첫 번째 퀸 음반이었다. 이 음반은 "뛰어난 하드 록 기타 트랙"을 많이 포함하고 있는 것으로 인정받았다.[2] 돌이켜 보면, 이 ...
... s (ARBs), also known as angiotensin II receptor antagonists , AT1 receptor antagonists or sartans, are a group of pharmaceuticals that modulate the renin-angiotensin system. Their main uses are in the treatment of hypertension (high blood pressure), diabetic nephropathy (kidney damage due to diabetes) and congestive heart failure. They block the activation of AT1 receptors, preventing the binding of angiotensin II. Angiotensin II receptor blockers are used primarily for the treatment of hypertension where the patient is intolerant of ACE inhibitor therapy. They do not inhibit the breakdown of bradykinin or other kinins, and are thus only rarely associated with the persistent dry cough and/or angioedema that limit ACE inhibitor therapy.[citation needed] More recently, they have ...
... (rINN) /ˌkændɪˈsɑːrtən/ is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. The prodrug candesartan cilexetil is marketed by AstraZeneca and Takeda Pharmaceuticals, commonly under the trade names Diceran,Blopress, Atacand, Amias, and Ratacand. It is available in generic form. As with other angiotensin II receptor antagonists, candesartan is indicated for the treatment of hypertension. Results from the CHARM study (early 2000s) demonstrated the morbidity and mortality reduction benefits of candesartan therapy in congestive heart failure. Thus, while ACE inhibitors are still considered first-line therapy in heart failure, candesartan can be used in combination with an ACE to achieve improved mortality and morbidity vs. an ACE alone and additionally is an alternative in patients intolerant of ACE ...
... is an ACE inhibitor used to treat high blood pressure, it may also be used to treat other conditions. It is marketed by Abbott Laboratories under the brand name Mavik. Trandolapril is a prodrug that is de-esterified to trandolaprilat. It is believed to exert its antihypertensive effect through the renin-angiotensin-aldosterone system. Trandolapril has a half-life of about 6 hours, and trandolaprilat has a half life of about 10 h. Trandolaprilat has about eight times the activity of its parent drug. About one-third of trandolapril and its metabolites are excreted in the urine, and about two-thirds of trandolapril and its metabolites are excreted in the feces. Serum protein binding of trandolapril is about 80%. Trandolapril acts by competitive inhibition of angiotensin converting enzyme (ACE), a key enzyme in the renin-angiotensin system which plays an ...
... (marketed under the brand name Accupril by Pfizer) is an angiotensin-converting enzyme inhibitor (ACE inhibitor) used in the treatment of hypertension and congestive heart failure. A prodrug, it is converted to its active metabolite, quinaprilat, in the liver. Quinapril inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I. Angiotensin II is a powerful vasoconstrictor and increases blood pressure through a variety of mechanisms. Due to reduced angiotensin production, plasma concentrations of aldosterone are also reduced, resulting in increased excretion of sodium in the urine and increased concentrations of potassium in the blood. Quinapril is indicated for the treatment of high blood pressure ...
... , brand name Lotensin (Novartis), is an ACE inhibitor used primarily in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing the renal and retinal complications of diabetes. ACE inhibitors relax blood vessels, and decrease blood volume, which lowers blood pressure and decreases oxygen demand from the heart. They inhibit angiotensin-converting enzyme, which is part of the renin-angiotensin-aldosterone system. Benazepril is a prodrug which is metabolized by the liver into its active form benazeprilat via cleavage of the drug's ester group. Patients with advanced renal insufficiency taking benazepril show "substantial" kidney benefits. A long-term study of patients' ...
... hydrochloride is a potent orally active nonsulfhydryl angiotensin converting enzyme inhibitor (ACE inhibitor) which is used for the treatment of hypertension and congestive heart failure. Moexipril can be administered alone or with other antihypertensives or diuretics. It works by inhibiting the conversion of angiotensin I to angiotensin II. Moexipril is available from Schwarz Pharma under the trade name Univasc. Moexipril is available as a prodrug moexipril hydrochloride, and is metabolized in the liver to form the pharmacologically active compound moexiprilat. Formation of moexiprilat is caused by hydrolysis of an ethyl ester group. Moexipril is incompletely absorbed after oral administration, and its bioavailability is low. The long pharmacokinetic half-life and persistent ACE inhibition of moexipril allows once-daily administration. Moexipril is ...
Common adverse drug reactions include: hypotension, cough, hyperkalemia, headache, dizziness, fatigue, nausea, and kidney impairment.[21][22] ACE inhibitors might increase inflammation-related pain, perhaps mediated by the buildup of bradykinin that accompanies ACE inhibition.[23][24][25]. The main adverse effects of ACE inhibition can be understood from their pharmacological action. The other reported adverse effects are hepatotoxicity and effect on the fetus.[22] Renal impairment is a significant potential adverse effect of all ACE inhibitors that directly follows from their mechanism of action. Patients starting on an ACE inhibitor usually have a modest reduction in glomerular filtration rate (GFR) that stabilizes after several days. However, the decrease may be significant in conditions of decreased renal perfusion, such as renal artery stenosis, heart ...
First-line therapy for people with heart failure due to reduced systolic function should include angiotensin-converting enzyme (ACE) inhibitors (ACE-I) or angiotensin receptor blockers (ARBs) if the person develops a long term cough as a side effect of the ACE-I.[60] Use of medicines from this class is associated with improved survival and quality of life in people with heart failure.[61]. Beta-adrenergic blocking agents (beta blockers) also form part of the first line of treatment, adding to the improvement in symptoms and mortality provided by ACE-I/ARB.[61][62] The mortality benefits of beta blockers in people with systolic dysfunction who also have atrial fibrillation (AF) is more limited than in those who do not have AF.[63] If the ejection fraction is not diminished (HFpEF), the benefits of beta blockers is more modest; a decrease in mortality has ...
As enzymes have evolved to bind their substrates tightly, and most reversible inhibitors bind in the active site of enzymes, it is unsurprising that some of these inhibitors are strikingly similar in structure to the substrates of their targets. Inhibitors of DHFR are prominent examples[2][3][1]. Other example of these substrate mimics are the protease inhibitors, a very successful class of antiretroviral drugs used to treat HIV.[24] The structure of ritonavir, a protease inhibitor based on a peptide and containing three peptide bonds, is shown on the right. As this drug resembles the protein that is the substrate of the HIV protease, it competes with this substrate in the enzyme's active site. Enzyme inhibitors are often designed to mimic the transition state or intermediate of an enzyme-catalyzed reaction. This ensures that the inhibitor exploits the transition state ...
آنزیم ۲ مبدل آنژیوتانسین (به انگلیسی: Angiotensin-converting enzyme 2) یا به اختصار ACE2، یک اگزوپپتیداز است که موجب تبدیل آنژیوتانسین ۱ به «آنژیوتانسین ۹-۱» (نُه پپتیدی)،[۳] یا تبدیل آنژیوتانسین ۲ به «آنژیوتانسین ۷-۱» می‌گردد.[۴][۵] این آنزیم اثرات مستقیمی بر عملکرد قلب دارد،a و بیشتر در لایهٔ داخلی رگ‌های خونی، قلب و کلیه‌ها بیان می‌شود.[۶] داروهای بازدارندهٔ آنزیم مبدل آنژیوتانسین که در درمان فشار خون بالا استفاده می‌شوند، اثری بر آنزیم ACE2 ندارند.[۷] مشخص شده که گیرنده‌های ACE2، نقطهٔ ورود برخی از انواع کروناویروس‌ها به سلول‌های بدن انسان هستند.[۸] دو گروه مجزا از ...
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