400-859-2883
Current Location:Home > Industry Information

Industry Information

Date of publication:2020/10/22 17:17:13

According to the mechanism of action and whether they are first-line antihypertensive drugs, antihypertensive drugs can be classified as follows, of which the first five categories are first-line antihypertensive drugs.
 

hypertension

1. Diuretics: ①Thiazide diuretics: such as epitizide, hydrochlorothiazide, bendroflumethiazide, methyclothiazide, polythiazide; ②Loop diuretics: such as furosemide, torasemide, bumetanide; ③Potassium-sparing diuretics: such as amiloride, Triamterene, spironolactone, eplerenone; ④ Thiazide-like diuretics: such as indapamide, chlorthalidone, metalozone, Xipamide, Clopamide.

2. Adrenergic receptor antagonists: ①Non-selective β receptor antagonists: such as propranolol, etc.; ②Highly selective β1 receptor antagonists: such as metoprolol, bisoprolol, etc.; ③ Mixed α, β receptors Antagonists: such as Labetrol.

3. Calcium channel blockers: ①Dihydropyridines: representative drugs are nifedipine; ②Non-dihydropyridines: representative drugs are diltiazem and verapamil.

4. Angiotensin-converting enzyme (ACE) inhibitors: such as captopril, perindopril, benazepril, etc.

5. Angiotensin II receptor antagonists: such as valsartan, losartan, telmisartan, irbesartan, olmesartan, etc.

6. Other alpha-receptor antagonists such as prazosin, doxazosin, etc.; Alpha-2 adrenergic receptor agonists such as clonidine, reserpine, methyldopa, etc. Compound preparations such as new types of compound preparations include irbesartan hydrochlorothiazide, valsartan hydrochlorothiazide, valsartan amlodipine, perindopril hydrochlorothiazide and so on.

Characteristics of antihypertensive drugs

There are many types of antihypertensive drugs, and various drugs have their own characteristics.

1. Diuretics

It is often used alone to combat mild hypertension, and also used in combination with other drugs to treat moderate to severe hypertension, especially for patients with heart failure and edema. Representative drugs include hydrochlorothiazide, indapamide, and compound amiloride hydrochloride tablets.

Long-term use of these drugs can easily lead to impaired glucose tolerance, increased blood sugar, hyperuricemia and other metabolic disorders, as well as increased blood cholesterol and triglycerides, decreased high-density lipoprotein, decreased libido and other complications. Therefore, it is generally used intermittently under the guidance of a physician.

Diuretics play a hypotensive effect through natriuretic drainage and reducing volume load. The commonly used diuretics are hydrochlorothiazide and indapamide. Such drugs are especially suitable for elderly hypertension, isolated systolic hypertension, and hypertension with heart failure. The side effects are closely related to the dose, so small doses are usually used. Common adverse reactions include hypokalemia and hyperuricemia, so it should be noted that blood potassium should be rechecked and patients with gout should be disabled.

2. Calcium channel blockers

It is suitable for all types of hypertension, especially for patients with severe hypertension with coronary heart disease, angina pectoris, cerebrovascular accident, and kidney disease.

Representative drugs are nifedipine, amlodipine, nicardipine, nitrendipine, felodipine, diltiazem and so on. Calcium channel blockers are the most widely used antihypertensive drugs. Its effect is not affected by salt intake and has no serious side effects.

But the pathogenesis of hypertension is complicated. Everyone has different causes of increased blood pressure, and not everyone can achieve the best results with calcium channel blockers. Calcium channel blockers mainly play the role of expanding blood vessels and lowering blood pressure by blocking calcium channels on vascular smooth muscle cells. It is most suitable for elderly hypertension, simple systolic hypertension (only high systolic blood pressure, not high diastolic blood pressure), high blood pressure with stable angina, high blood pressure with coronary or carotid atherosclerosis and peripheral vascular disease.

3. Beta receptor antagonist

It is widely used in patients with mild and moderate hypertension, especially in young hypertensive patients and the treatment of exertional angina. It is not suitable for patients with heart failure, bronchial asthma, and diabetes.

The main drugs are propranolol, metoprolol, atenolol, bisoprolol, labetalol, carvedilol and so on. β-receptor antagonists mainly reduce blood pressure by inhibiting sympathetic nerve activity, inhibiting renin release, inhibiting myocardial contractility, and slowing down heart rate.

β-receptor antagonists are most suitable for hypertensive patients with coronary heart disease (including angina pectoris, myocardial infarction), rapid heart rate or premature contractions and other rapid arrhythmia, chronic heart failure, hyperthyroidism, anxiety and other symptoms, especially for young people. Common adverse reactions include fatigue, cold limbs, agitation, bradycardia, etc., and may also affect glucose and lipid metabolism. People with slow heart rate (<45 beats/min), sinus bradycardia, arrhythmia and bronchial asthma are contraindicated.

Long-term use of β-receptor antagonists will have a "rebound" phenomenon after sudden withdrawal, such as increased blood pressure, tachycardia, angina pectoris, anxiety, etc. Therefore, the drug must be stopped gradually under the guidance of a doctor. Never stop the medicine suddenly by yourself.

4. Angiotensin-converting Enzyme inhibitor (ACE inhibitor)

This class of drugs has a good effect on essential hypertension and renal hypertension. It can improve glucose and lipid metabolism, prevent and treat cardiac insufficiency, and reverse ventricular hypertrophy. It is often used in patients with ventricular hypertrophy, heart failure, diabetes, hyperlipidemia, and elderly patients with moderate or severe hypertension.

It should be used with caution in patients with serum creatinine> 3 mg and contraindicated in patients with bilateral renal artery stenosis and in the middle and late stages of pregnancy.

Commonly used drugs are captopril, enalapril, perindopril, benazepril, fosinopril, ramipril, quinapril, and so on. ACE inhibitors mainly act to dilate blood vessels by inhibiting the renin-angiotensin-aldosterone system, thereby reducing blood pressure.

The advantages of ACE inhibitors are that they have no adverse effects on glucose and lipid metabolism, and can improve glucose metabolism, reduce new-onset diabetes, reduce urine protein in diabetic patients, and protect the heart and kidneys. Such drugs are especially suitable for hypertensive patients with diabetes, nephropathy, proteinuria, metabolic syndrome, chronic heart failure, and myocardial infarction. The most common adverse reaction is a persistent dry cough, which is more common in the initial stage of medication. Those with mild symptoms can try to continue taking the medication, and those who cannot tolerate it should be changed. Other adverse reactions include hypotension, skin rash, and occasionally angioedema. Once these adverse reactions occur, the drug should be discontinued and no ACE inhibitors should be used. Pay attention to review blood potassium and renal function during medication. Patients with severe renal insufficiency, hyperkalemia, bilateral renal artery stenosis and pregnant women should not use such drugs.

5. Angiotensin II receptor antagonist (ARB)

Such antihypertensive drugs have good effects and small side effects. Commonly used drugs include Losartan, Valsartan, Irbesartan, Candesartan, Telmisartan, Olmesartan, etc. ARB is the youngest member of the family of antihypertensive drugs. Its mechanism of action is similar to that of ACE inhibitors. Its applicable population, adverse reactions and contraindications are also similar to ACE inhibitors.

Conclusion

Diuretics have a long-lasting effect, but it is necessary to pay attention to their influence on glucose and lipid metabolism.

Beta-receptor antagonists lower blood pressure mainly by reducing heart rate and myocardial contractility. Its antihypertensive effect is weak, and non-selective β receptor antagonists and high-dose highly selective β1 receptor antagonists can have a certain effect on glucose and lipid metabolism and bronchial smooth muscle.

ACE inhibitors can cause the accumulation of bradykinin, and the incidence of dry cough is relatively high. Pay attention to monitoring renal function and electrolytes during use.

In short, all kinds of antihypertensive drugs have certain limitations, and often need to be used in combination to ensure that the blood pressure meets the standard and reduce adverse drug reactions.

Huateng Pharma, a professional pharmaceutical intermediates and APIs manufacturer in China, is able to provide the services of antihypertensive drugs intermediates' process development and scale-up production with capacities varying from gram to kilograms and multi tons. Find intermediates of antihypertensive drugs like Candesartan, Telmisartan, Losartan, Irbesartan, Olmesartan from Huateng Pharma now.