Super detailed comparison of 5 major classes of antihypertensive drugs! (collection)

Author: Gao Lili

Source: Center for Drug Evaluation

Currently There are five types of antihypertensive drugs commonly used in clinical practice: angiotensin-converting enzyme inhibitors (ACEIs), angiotensin receptor blockers (ARBs), calcium channel blockers (CCBs), diuretics, and beta-blockers stagnation agent, etc. Only by grasping the difference between the 5 types of antihypertensive drugs can rational drug use. I. Types and differences between ACEI and ARBACEI works by blocking RAAS (renin-angiotensin-aldosterone) system) and KKS (kallikrein-kinin system), such as captopril, enalapril, etc. ARBs work by blocking angiotensin II1 (AT1) type receptors, such as losartan, valsartan, irbesartan, telmisartan, etc. ACEI or ARB is generally preferred for hypertension with heart failure, left ventricular hypertrophy, previous myocardial infarction, cardiac insufficiency, atrial fibrillation, coronary heart disease, diabetic nephropathy, CKD, microalbuminuria or proteinuria, patients with metabolic syndrome. ARBs can be used as an alternative treatment for patients with ACEI allergy or intolerance. Captopril has a high incidence of irritating dry cough due to sulfhydryl groups, which can cause cytopenia, rash, and dysgeusia. Imidapril has a low incidence of cough. ARBs have an affinity for AT1 receptor as telmisartan>candesartan>valsartan>losartan. The combination of ACEI and ARB is generally not recommended due to the increased incidence of adverse events, including hyperkalemia, hypotension, syncope, and renal insufficiency. II. Types and differences of CCBAccording to its affinity with arterial blood vessels and heart and its effect ratio, CCB can be divided into dihydropyridine CCB and Non-dihydropyridine CCBs. Dihydropyridine CCBsmainly act on arteries, with better selectivity to blood vessels, and are mainly used for the treatment of hypertension. Such as nifedipine, amlodipine, levamlodipine, felodipine, etc. Dihydropyridine CCBs are preferred for patients with volumetric hypertension (eg elderly hypertension, isolated systolic hypertension and low renin activity or low sympathetic activity) and hypertensive patients with atherosclerosis (eg, hypertension with stable angina, carotid atherosclerosis, coronary atherosclerosis, and hypertension with peripheral vascular disease). Dihydropyridine CCBs can be divided into first generation, second generation and third generation according to their pharmacokinetic and pharmacodynamic characteristics. The difference between nifedipine ordinary tablet, sustained-release tablet and controlled-release tablet:The difference between amlodipine and levamlodipine:Most CCBs have negative inotropic effects, which can worsen cardiac function and cause heart failure decompensation and increased mortality, so Patients with heart failure should avoid the use, especially short-acting dihydropyridine CCBs and non-dihydropyridine CCBs with negative inotropic effects. When heart failure patients with severe hypertension or angina pectoris cannot be controlled by other drugs and need to use CCB, amlodipine or felodipine with better safety can be selected. The use of felodipine extended-release tablets in patients with severe heart failure does not increase the mortality rate, and it is relatively safe for patients with underlying heart disease and heart failure, but requires Be aware of its negative inotropic effects, especially when combined with beta-blockers. In patients with severe heart failure, amlodipine has not been shown to increase mortality or other adverse effects.good reaction. Nifedipine, amlodipine and felodipine are mainly metabolized by hepatic CYP3A4. CYP3A4 strong inhibitors such as itraconazole, fluconazole, clarithromycin, etc. can significantly slow down its metabolism and enhance the antihypertensive effect, which may can cause severe hypotension;CYP3A4 strong inducers such as rifampicin, carbamazepine, phenobarbital, phenytoin, etc. can accelerate its metabolism and cause blood pressure to rise or blood pressure to fluctuate violently. Clinically, it should be avoided or Use with caution. In addition, amlodipine has a moderate inhibitory effect on CYP3A4. When combined with simvastatin, the daily dose of simvastatin should not exceed 20 mg. III. Types and differences of diureticsDiuretics play an antihypertensive effect mainly by diuretic natriuresis and reducing volume load. Commonly used diuretics include loop diuretics (such as furosemide, torasemide), thiazide diuretics (such as hydrochlorothiazide, indapamide), potassium-sparing diuretics, etc. Among them, loop diuretics and thiazide diuretics are called potassium-sparing diuretics. potassium-sparing diureticsinclude aldosterone receptor antagonists such as spironolactone, eplerenone, and the aldosterone-independent triamterene, adrenalin Mirolli. At present, the most commonly used antihypertensive drugs are thiazide diuretics, which are especially suitable for elderly patients with hypertension, refractory hypertension, heart failure complicated with hypertension, and salt-sensitive hypertension. Comparison of potassium-sparing diuretics:antagonists against aldosterone synthesis by blocking spironolactone receptors Androgenic effects can cause adverse reactions such as impotence, loss of libido, gynecomastia or menstrual disorders in women. Eplerenone is a highly selective aldosterone receptor antagonist with weaker receptor blocking effect than aldosterone, and does not antagonize androgen and progesterone receptors, the adverse reactions were significantly less than spironolactone. IV. Types and differences of β-blockersβ-blockers mainly inhibit the excessively activated sympathetic nerve activity, inhibit the Myocardial contractility, slowing heart rate and exerting antihypertensive effect. Commonly used beta-blockers include selective beta1-blockers (eg, metoprolol, atenolol, bisoprolol), and alpha1/beta-blockers (such as arolol, carvedilol, labetalol, etc.). β-blockers are especially suitable for patients with tachyarrhythmia, coronary heart disease, chronic heart failure, aortic dissection, increased sympathetic nerve activity and high blood pressure. The difference between metoprolol, atenolol, and bisoprolol:The difference between Metoprolol Tartrate Tablets and Metoprolol Succinate Extended Release Tablets:The difference between carvedilol, arolol, labetalol:< img class="content_title" height="300" layout="respons ive" sizes="(min-width: 320px) 320px, 100vw" src="https://mmbiz.qpic.cn/mmbiz_png/CB0BZ6GAshhw8nV7LwRVgFk7rkYoCUnJBZhHtTpK9rcKSDHVjaib5MuSsibeMkhUhyBJojC6fD3SGyUJZefXfaYA/640"img>hypertension Accompanied by increased heart rate, the first choice is a beta-blocker that can also slow down the heart rate. The selective beta-1 receptor blockers, metoprolol and bisoprolol, are recommended. α1/β receptor blockers: can significantly dilate peripheral blood vessels, inhibit sympathetic nerve activity and block cardiac β1 receptors, and can directly Stimulates heat production in brown adipose tissue, has a certain effect on weight control, and is suitable for hypertension characterized by increased diastolic blood pressure; Eliminate abnormal glucose and lipid metabolism caused by β-receptor blockade, improve glucose and lipid metabolism disorders, reduce atherosclerotic lesions, and also remove and inhibit the generation of oxygen free radicals. It is suitable for patients with glucose or lipid metabolism disorders. Hypertension. In hypertensive patients with cerebral thrombosis or tremor, in addition to reducing blood pressure, arolol can also increase cerebral blood flow and significantly reduce tremor symptoms. Labetalol can directly expand blood vessels, lower blood pressure, and has minimal adverse effects on fetal growth and development, and does not affect placental and renal blood flow. It can also promote fetal lung maturation and can be used to treat pregnancy period hypertension. References:

1 Guidelines for the diagnosis and treatment of hypertension in traditional Chinese medicine[J].China Journal of Traditional Chinese Medicine,2011,9(23 ):108

2 Zhu Yizhen et al. Pharmacology [M]. Beijing: People’s Health Publishing House, 2016:95-99,179-192

3 Guidelines for Rational Drug Use in Hypertension (Second Edition)[J].Chinese Journal of Medical Frontiers,2017,9(7):28-70

< h1>4 The 2018 revision of the Chinese Guidelines for the Prevention and Treatment of Hypertension[J].Cardiovascular and Cerebrovascular Disease Prevention and Treatment, 2019,19(1):1-32

Expert consensus on the correct application of ACE inhibitors in kidney disease[J].Chinese Journal of Nephrology,2006,22(1):57-58

6 Tong Rongsheng et al. Drug comparison and clinical rational selection – cardiovascular disease volume [M]. Beijing: People’s Health Publishing House, 2013: 23-33, 44-47, 98-103, 108-109, 173-177< /span>

7 Angiotensin-Converting Enzyme Inhibitor Application Chinese Expert Consensus in Patients with Coronary Heart Disease[J].Chinese Journal of Circulation,2016,31(5):420-424

span>

8 Chinese expert consensus on the application of angiotensin-converting enzyme inhibitors in cardiovascular diseases[J].Chinese Journal of Cardiovascular Diseases,2007,35(2):97-104

span>

9China Guidelines for the Management of Renal Hypertension 2016 (Simple Version)[J].Chinese Journal of Medicine,2017,97(20):1551

span>

10 Guidelines for Rational Drug Use in Heart Failure (Second Edition)[J].Chinese Journal of Frontiers in Medicine,2019,11(7):1-78< /span>

11 Guidelines for Rational Drug Use for Coronary Heart Disease (Second Edition) [J]. Frontiers in Chinese Medicine, 2018,10(6):1-130

12 Guidelines for the diagnosis and treatment of stable coronary heart disease[J].Chinese Journal of Cardiovascular Diseases,2018,46(9):685

13 Yang Mingna et al. General practice prescription case reviews: cardiovascular disease [M]. Beijing: Peking University Medical Press, 2017: 30-41

14 Expert consensus on the safety management of multiple drug use in the elderly[J].Chinese Journal of Diabetes,2018,26(9):708

15Clinical application of levamlodipine besylate Expert consensus[J].Chinese Journal of Internal Medicine,2010,49(11):987-988

16 Chinese expert advice on clinical application of amlodipine besylate[J]. Chinese Journal of Internal Medicine, 2009, 48(11): 974-978

17 Qian Zhiyu. Pharmacology [M]. Beijing: China Medical Science and Technology Press, 2009: 404 -410,442-452

18 Chinese expert consensus on the treatment of hypertension with diuretics[J].Chinese Journal of Hypertension,2011,19(3):214-220

Expert consensus on the application of 19β-adrenergic receptor blockers in cardiovascular diseases[J].Chinese Journal of Cardiovascular Diseases,2009,37(3):195-207

Expert consensus on the application of 20 β-blockers in hypertension[J].Frontiers in Chinese Medicine,2019,11(4):29-36< /p>

21 Chinese expert advice on the standardized clinical application of intravenous beta-adrenergic receptor blockers[J].Chinese Journal of Heart Failure and Cardiomyopathy,2017,1(1):7- 14

22 α/β-blockers in the treatment of hypertension Chinese expert consensus[J]. Journal of Hypertension, 2016, 24(6):522-525

23 α/β blockers in the treatment of hypertension in chronic kidney disease as a practical guideline[J] ]. Chinese Medical Journal, 2013, 93(48): 3812-3815

24 Chinese Expert Consensus on Heart Rate Management in Hypertensive Patients [J]. Frontiers in Chinese Medicine, 2017, 9(8):32-33

Contributions are welcome

WeChat: druglive, vipnote< /p>

Manuscript requirements: professional articles related to clinical drug use

Manuscript format: word document

Remuneration: determined according to the quality of the article

Listen to the Drug Evaluation Center and make a little progress every day!