From this article you will learn: what medications for hypertension belong to the last generation, and whether they are really better than earlier antihypertensive drugs.
- Angiotensin-converting enzyme inhibitors
- Calcium channel blockers
- Beta-blockers
- Angiotensin-2 receptor blockers
- Direct renin inhibitors( aliskiren)
The term "last generation" of antihypertensive drugs does not have an exact definition or years of release. Most often this term is used for advertising purposes, promoting a certain drug - not necessarily the most effective or new - in the pharmaceutical market. But medical science does not stand still. Testing of new drugs against hypertension is ongoing, however, their introduction into clinical practice is not a matter of one year. Not every new tool demonstrates higher efficiency and safety, compared to older, but also better tested means. Almost every year on the pharmacological market, new tablets are taken from hypertension, containing for a long time already known active substances or a combination thereof.
Still worth noting that some antihypertensive drugs do exist, in such cases it can be said about the last generation of drugs from high blood pressure.
Most of the representatives from the list of drugs from the new generation of hypertension are issued in the form of tablets for oral use. The only exception is labetalol, a beta-blocker, available as a solution for intravenous administration. There are other preparations for parenteral use( for example, nitrates, benzohexonium, sodium nitroprusside), but they are difficult to classify as new drugs. Almost always intravenous administration of antihypertensive drugs is used to treat hypertensive crises.
In any case, before using the novelties in the treatment of hypertension, it is necessary to consult a cardiologist. It is also possible to independently search for information on the scientific studies of the effectiveness and safety of this drug in comparison with the already well-studied means.
Further in the article, groups of drugs are sorted by "age": from old to more modern.
Angiotensin-converting enzyme inhibitors
Angiotensin-converting enzyme inhibitors( abbreviated as ACE inhibitors) are pharmaceutical drugs that are used primarily to treat high blood pressure and heart failure. This group of drugs inhibits the activity of the angiotensin-converting enzyme, which converts inactive angiotensin 1 into active angiotensin 2, thereby expanding the blood vessels and reducing the burden on the heart.
The first drug ACEI( captopril) was discovered more than 40 years ago, since that time 12 drugs from this group have been introduced into clinical practice.
Currently, most commonly used ACE inhibitors, which were invented back in the 1990s. Their list:
- Ramipril.
- Perindopril.
- Zofenopril.
- Quinapril.
- Fosinopril.
Despite the fairly long-established introduction to clinical practice, these drugs continue to lead confidently among all ACE inhibitors, proving their high efficacy and safety in many studies. Moreover, many scientific evidence indicate that there are almost no significant differences in the efficacy and safety of different representatives of ACE inhibitors. Effectively reduce blood pressure can both lisinopril and fosinopril, although the cost of these drugs in the pharmacy can vary at times.
In addition to the treatment of hypertension, ACE inhibitors are used with:
- Heart failure - these drugs reduce the burden on the heart.
- Diabetic nephropathy - ACE inhibitors help maintain the functional state of the kidneys.
- Chronic kidney disease - ACEI can help slow the progression of these diseases.
- Myocardial infarction.
People who should not take ACE inhibitors:
- Pregnant and lactating women.
- Patients with hypersensitivity to these drugs.
- Patients with certain renal diseases - for example, renal artery stenosis.
The most frequent side effect of all - even the newest - ACEI is a dry cough, developing in about 10% of people taking these drugs. Less common are edema on the lips, tongue or around the eyes, as well as worsening kidney function.
Calcium channel blockers
Calcium channel blockers( abbreviated as CCB), sometimes called calcium antagonists, are a group of drugs that affect the ingress of calcium ions into certain muscle cells. They are used to treat various diseases, including arterial hypertension, angina pectoris, Raynaud's syndrome and cardiac arrhythmias, and to stop preterm labor during pregnancy.
List of the three main groups of the CCB:
- Group of nifedipine( dihydropyridines).A group of diltiazem( benzothiazepines).
- Group of verapamil( phenylalkylamines).
To reduce blood pressure, dihydropyridines are most often used, which were developed in the 1960s.
There are 4 generations of drugs from the group of nifedipine:
- 1 generation - nifedipine;
- 2nd generation - nicardipine, felodipine;
- 3rd generation - amlodipine;
- 4th Generation - Cilnidipine.
In clinical practice most often used drugs of the first three generations, cilnidipine doctors are appointed rarely.
Amlodipine is perhaps the most commonly prescribed drug from the BCC group. It began to be used in 1990.Amlodipine has demonstrated high efficacy in the treatment of hypertension, as well as safety.
Cilnidipine is a new drug of the 4th generation from the BCC group, which has certain advantages over other calcium antagonists. Compared with representatives of the first three generations, which affect only the L-type calcium channels, cilnidipine can also block their N-type. This property can have useful clinical value, manifested by suppression of reflex tachycardia and reduction of edema, which are sometimes observed with the use of amlodipine and other, older, CCBs. Cilnidipine has a high lipophilicity, due to which it has a prolonged effect. Cilnidipine is produced under the trade names "Duocard", "Cilacar", "Atelek".
Contraindications to the appointment of dihydropyridines include allergic reactions to a particular drug.
| Also, calcium antagonists should be used with caution in the following situations. | Possible side effects of CCA from the dihydropyridine group include |
|---|---|
| Myocardial infarction and unstable angina | Edema on the legs |
| Arterial hypotension | Fatigue |
Aortic stenosis  Click on photo for enlarge | Nausea |
| Pregnancy and breastfeeding | Dizziness |
| Renal and hepatic failure | Rapid heart rate |
| Severe heart failure | Tides( sensation of heat spreading throughout the body, especially in the face and neck) |
Beta-blockers
Beta-blockers( BB) are a class of drugs that block the receptors of endogenous catecholamines( noradrenaline and epinephrine), thereby applyingto reduce blood pressure, treatment of heart rhythm disorders, secondary prevention of myocardial infarction.
The first OB( propranolol) was synthesized in 1964.Many doctors and scientists agree that the discovery of this group of drugs is one of the most important events in the clinical medicine and pharmacology of the XX century.
Since that time, a lot of BB has been developed. Some of them act on all types of beta-adrenergic receptors, others - only on one of them. It is on these properties and distinguish three generations of BB:
- 1 generation - propranolol, timolol, sotalol( nonselective, block beta-1 and beta-2 adrenergic receptors)
- 2nd generation - metoprolol, bisoprolol, esmolol( selective, block only beta 1 adrenergic receptors)
- 3rd generation - carvedilol, nebivolol, labetalol(have additional vasodilating properties).
Carvedilol is one of the third generation BB that has the additional property of vasodilation. It acts on beta-1 and beta-2-adrenergic receptors, and also blocks alpha-adrenergic receptors in the vessels. Due to these effects, carvedilol more reduces blood pressure, less affects the heart rate, does not increase lipid and blood glucose levels. The drawback of the drug is its effect on beta-2-adrenoreceptors, which increases the risk of bronchoconstriction. Take carvedilol twice a day, which is not very convenient for the patient.
Nebivolol is a drug that selectively acts on beta-1-adrenergic receptors, which additionally has vasodilating properties due to increased synthesis of nitric oxide( NO) in the vascular endothelium. Due to these effects, nebivolol better reduces blood pressure, less affects the heart rate, does not increase lipid and blood glucose levels, does not cause erectile dysfunction. The negative property of this drug is a rather weak effect on beta-blockers, so it is most often used in elderly people with heart failure.
Labetalol is a drug that has non-selective beta-blocking properties and effects on alpha receptors. Labetalol is used mainly in the form of intravenous administration, in which it has a very short duration of action, which allows to achieve good control over the effects of the drug. This is the most effective beta-blocker for the treatment of hypertensive crises. It is often used with pheochromocytoma( adrenal tumor) and pre-eclampsia( late toxicosis in pregnant women).
| Contraindications to the use of beta blockers | Also these drugs are used with caution in patients with |
|---|---|
| Bronchial asthma and obstructive pulmonary disease | Diabetes mellitus |
| Atrioventricular blockade of 2 and 3 degrees | Myasthenia |
| Severe obliterating diseases of peripheral arteries | Bradycardia |
| Severe, unstable heart failure | Arterial hypotension |
List of common side effects for beta-blockers:
- Bradycardia.
- Atrioventricular block.
- Deterioration of symptoms of heart failure.
- Bronchospasm.
- Spasm of peripheral vessels.
- Increase in glucose and lipids in the blood.
- Erectile dysfunction.
- Sleep disorders( due to decreased production of melatonin).
Angiotensin Receptor Blockers 2
Angiotensin 2 receptor blockers( ARBs), or sartans, are the newest group of drugs commonly used to treat hypertension. The first sartan( losartan) was introduced into practice in 1986.
The action of Sartans is based on the blockade of the last level of the renin-angiotensin system, that is, on the prevention of the binding of angiotensin 2 to its receptors. Due to these effects, ARBs cause vasodilation, reduce the secretion of vasopressin and aldosterone( hormones that help to retain fluid and sodium in the body), which leads to lower blood pressure.
The most recent ARBs approved for clinical use are olmesartan( Cardosal), fimasartan( Canarb) and azilsartan( Edarby).
Indications for use of sartans, including the newest drugs:
- Arterial hypertension.
- Heart failure.
- Kidney pathology in diabetes mellitus.
- Chronic kidney disease.
As can be seen, indications for the use of Sartans are almost the same as for the use of another group of drugs that affect the renin-angiotensin system - ACE inhibitors. In most cases, ARBs are prescribed in those situations where the administration of ACEI led to the occurrence of side effects( dry cough).It should be borne in mind that older ACE inhibitors have almost the same efficacy in lowering blood pressure, cost less and have certain advantages over Sartans in the treatment of patients with diabetes mellitus.
Sartans are usually well tolerated by most patients.
| Contraindications to the use of ARBs | Most frequent side effects may include |
|---|---|
| Increased sensitivity to a particular drug | Dizziness |
| pregnancy and breastfeeding | Headaches |
| Bilateral renal artery stenosis with impaired kidney function | Increase in blood potassium levels |
| Orthostatic hypotension | |
| Diarrhea |
Directinhibitors of renin( aliskiren)
Aliskiren is a cure for hypertension of a new generation that has not yet acquired a largeth prevalence. The only drug of this class is aliskiren, which received permission for clinical use in 2007.
Aliskiren binds to renin, suppressing its interaction with angiotensinogen, thereby preventing the formation of angiotensin 1 and angiotensin 2.
Aliskiren is used only for the treatment of hypertension, and even with this disease it is not recommended to be used as the first line of therapy.
| Contraindications to the use of aliskiren | List of side effects of aliskiren |
|---|---|
| Increased sensitivity to aliskirenum | Angioedema |
| Renal failure | Increased potassium levels in the blood( especially when used in combination with ACE inhibitors in patients with diabetes mellitus) |
| Joint use with ARB or ACE inhibitors in patientswith diabetes | Drop in blood pressure |
| Pregnancy or breastfeeding | Diarrhea and other symptoms of gastrointestinal disturbances |
| Headache Dizziness Coughing | |
