Hypertension is the most common cardiovascular disease and a major risk factor for cardiovascular, cerebrovascular and renal failure. Therefore, lowering hypertension and reducing the incidence of complications are of great clinical importance to improve the quality of life.
Currently, the commonly used antihypertensive drugs can be categorized into five major groups, namely diuretics, beta receptor antagonists, calcium channel blockers (CCB), angiotensin converting enzyme inhibitors (ACEI) and angiotensin II receptor antagonists (ARB).
1.Diuretics
The antihypertensive effect is mainly through sodium excretion, reducing extracellular volume and lowering peripheral vascular resistance. The onset of antihypertensive effect is smooth and slow, with a relatively long duration and long-lasting effect. It is suitable for mild and moderate hypertension, and for simple systolic hypertension. Salt-sensitive hypertension, combined with obesity or diabetes, menopausal women, combined with heart failure and hypertension in the elderly have a strong antihypertensive effect. Diuretics may increase the efficacy of other antihypertensive drugs.
Thiazides: hydrochlorothiazide, indapamide, etc.
tabular diuretics: furosemide.
Potassium-preserving diuretics: spironolactone steroids.
Major adverse effects: hypokalemia and effects on lipid, glucose, and blood uric acid metabolism, often occurring at high doses, so low doses are recommended. Others include malaise and increased urine output, and are contraindicated in patients with gout. Potassium-preserving diuretics can cause hyperthermia and should not be used in combination with ACEI and ARB, and should be used with caution in renal insufficiency. The tab diuretics are mainly used for hypertensive patients with combined renal insufficiency.
2.β-receptor antagonists
These drugs can inhibit myocardial contractility and slow down heart rate by inhibiting central and peripheral RAAS to exert antihypertensive effects. The onset of antihypertensive effect is strong and rapid, and the duration of antihypertensive effect varies among different β receptor antagonists. It is suitable for patients with different degrees of hypertension, especially for middle-aged and young patients with fast heart rate or combined with angina pectoris and chronic heart failure, but is relatively ineffective in elderly hypertension.
Commonly used drugs are: propranolol (Jinan), metoprolol (betaxolol), atenolol (amiloride), bisoprolol (Bosu), labetalol, carvedilol.
Major adverse effects: bradycardia, weakness, chills in the extremities. beta-receptor antagonists inhibit myocardial contractility, sinus node and atrioventricular node function, and increase airway resistance. Acute heart failure, pathological sinus node syndrome, atrioventricular block patients are prohibited.
3.Calcium channel blockers
Calcium channel blockers have rapid onset of antihypertensive effect, relatively strong antihypertensive efficacy and magnitude, with less individual variability in efficacy. Calcium channel blockers have no significant effect on blood lipids and blood glucose, and have good compliance with medication. Compared with other antihypertensive drugs, calcium channel blockers also have the following advantages: better antihypertensive efficacy in elderly patients; high sodium intake and non-steroidal anti-inflammatory drugs do not affect the antihypertensive efficacy; significant antihypertensive effect in patients with alcoholism; can be used in patients with combined diabetes, coronary artery disease or peripheral blood shutdown; long-term treatment also has anti-atherosclerotic effect.
Representative drugs (long-acting).
Long half-life drugs: amlodipine, levamlodipine, etc.
Lipid-soluble membrane-controlled drugs: lacidipine, lercanidipine, etc.
Extended or controlled-release formulations: felodipine extended-release tablets, nifedipine controlled-release tablets, etc.
The main disadvantages are: reflex sympathetic activity is enhanced at the beginning of treatment, causing increased heart rate, facial flushing, headache, lower limb edema, etc., especially when using short-acting preparations.
4.Angiotensin converting enzyme inhibitors
The antihypertensive effect is mainly through the inhibition of circulatory and tissue ACE, so that the production of ATⅡ is reduced, and the degradation of bradykinin is reduced by the inhibition of kinase. The onset of antihypertensive effect is slow, and the maximum effect is reached in 3~4 weeks. Restriction of sodium intake or combined use of diuretics can make the onset of effect rapid and enhance the effect.
Representative drugs: Captopril, Enalapril, Benazepril, Lenopril, Ramipril, Fosinopril, Cilazapril, Perindopril, etc.
Main adverse effects: irritating dry cough and angioedema. The incidence of dry cough is about 10%-20%, which may be related to the increase of bradykinin in the body and may disappear after discontinuation. Contraindicated in hyperkalemia, pregnant women and patients with bilateral renal artery stenosis. Caution should be exercised when using in patients with blood creatinine over 3mg/dl, and blood creatinine and potassium levels should be tested regularly.
5.Angiotensin II receptor antagonists
Slow onset of antihypertensive effect, but long-lasting and smooth. Low-salt diet or combined with diuretics can significantly enhance the efficacy. Most ARBs have an enhanced antihypertensive effect with increasing volume, and have a wide therapeutic dose window. The most important feature is that there are fewer adverse reactions directly related to the drug, which generally do not cause irritating dry cough and high compliance with continuous treatment.
Representative drugs: Crosartan, valsartan, irbesartan, telmisartan, olmesartan, candesartan, etc.
Treatment targets and contraindications are the same as ACEI.
In addition to the above five major classes of antihypertensive drugs, there are some other drugs in the history of antihypertensive drug development, including sympathetic nerve inhibitors, such as reserpine, colistin; direct vasodilators, such as hydrazidiazide; α1 receptor antagonists, such as prazosin, terazosin, doxazosin, had been used for many years in clinical and have certain antihypertensive efficacy, but because of more side effects, it is not advocated to be used alone, but can be used in compound The use of prazosin, terazosin, and doxazosin has been used for many years with some antihypertensive effect.