Valsartan for high blood pressure

Valsartan for high blood pressure

Valsartan is a prescription drug that helps against high blood pressure. Like candesartan and losartan, it belongs to the sartan group of substances. Valsartan was developed and patented in 1991. Here, you can find out what you should consider regarding intake and dosage, possible side effects, and whether valsartan is carcinogenic.

What is Valsartan used for?

Valsartan is – just like amlodipine , ramipril , hydrochlorothiazide ( HCT ) or bisoprolol – a blood pressure lowering agent. In this area of ​​application, valsartan is one of the drugs of choice.

The active ingredient is often taken as an alternative to ACE inhibitors (e.g. ramipril) because these can trigger a dry cough in many people. The reason for this is that ACE inhibitors inhibit not only the “angiotensin converting enzyme” (ACE) but also the breakdown of bradykinin. This is a substance that can trigger a dry cough.

Valsartan can also be used in the treatment of heart failure, i.e. heart failure or after a heart attack. In both cases, it is intended to protect against consequential damage caused by changes in the heart.

 

What else can valsartan do?

Permanently high blood pressure is harmful to the body. As a result, the blood vessels become calcified. Strokes, heart attacks and many other diseases are also triggered by permanently high blood pressure. Taking valsartan thus reduces the risk of developing such diseases.

ACE inhibitors and sartans have been shown to protect kidney function from harmful influences. It was also demonstrated that sartans and ACE inhibitors could prevent negative remodelling processes in the heart after a heart attack. They are also often used when kidney damage has occurred due to diabetes mellitus. Here, too, the drug has a protective effect on the kidneys.

Use in combination with other antihypertensives.

According to the guidelines from 2018 1, two drugs are often used in combination at the beginning of the therapy for high blood pressure. Here, the doctor has the choice between different alternatives:

  • a calcium channel blocker such as amlodipine,
  • a diuretic such as HCT,
  • an ACE inhibitor such as ramipril or
  • a sartan such as valsartan

Because Spartans and ACE inhibitors work similarly, they are not combined. However, they still have the same status in treating high blood pressure.

Each of these drugs has different advantages and disadvantages; the doctor must find the right drug or combination for each patient.

 

How is valsartan dosed?

Valsartan is taken in tablet form with 80 mg, 160 mg, or the maximum daily dose of 320 mg. The doctor determines the dosage and depends on the extent of the blood pressure reduction required. The dose is usually chosen to be relatively low at the beginning and then increased if necessary during treatment. This increase continues until the desired blood pressure reduction is achieved. 

If, despite the increase, more than two medications are needed, a third is added. Taking several tablets is only sometimes necessary – sometimes combined preparations are also available. For example, Valsartan 160/25 is a combination drug of 160 mg valsartan and 25 mg HCT. The two active ingredients are often prescribed in this combination since the effects complement each other.

Instructions for taking valsartan

Depending on the prescription, valsartan is taken once or twice a day with a bit of water. The tablets can be taken with or without food. 

If a dose is forgotten, it can be made up for later. However, a double dose should not be taken if it is already time for the next dose. The drug should only be discontinued by consulting a doctor, as this can lead to a worsening of the disease.

Valsartan can also be used as an oral solution if you have difficulty swallowing or if the person is fed by tube.

A drug with different names

Many different manufacturers produce drugs with the active ingredient valsartan. The following trade names are available in Germany, for example:

  • Valsartan dura®
  • Valsartan comp®
  • Valsacor®
  • Cordinate®
  • Valsartan Hexal®

 

How does valsartan work?

Valsartan is one of the sartans. These are also called AT 1 antagonists or angiotensin II receptor blockers. This designation already indicates the drug’s mode of action: valsartan blocks the angiotensin receptor.

This receptor is found in the heart, the brain, the kidneys, and above all, in the blood vessels. Here, Valsartan influences the so-called RAAS (renin-angiotensin-aldosterone system). This system is essential in regulating blood pressure and works in the following ways: 

  • Renin is produced by the kidneys when their blood flow is reduced when the kidneys “detect” that blood pressure is inadequate.
  • Renin then causes angiotensinogen to be converted to angiotensin I.
  • The ACE, i.e. the angiotensin-converting enzyme, then converts angiotensin I into angiotensin II.
  • This, in turn, activates the hormone aldosterone.
  • This leads to the kidneys excreting less water and the blood vessels constricting. This raises blood pressure.

By blocking this system, the kidney excretes more water, and the blood vessels widen. The blood pressure is therefore less increased and falls.

After valsartan has exerted its effect, 30 per cent of it is excreted through the kidneys. The remaining 70 per cent is metabolized in the liver.

Effect of other means in comparison

Many drugs can block the mechanism just described in different ways:

  • Some drugs inhibit renin, such as aliskiren, one of these active ingredients.
  • The ACE is reduced in its function by ACE inhibitors such as ramipril.
  • The Spartans block the angiotensin receptor. This means that angiotensin can no longer develop its blood pressure-increasing effect.
  • Last but not least, aldosterone can also be inhibited by aldosterone antagonists such as spironolactone.

What are the side effects of valsartan?

Like many other antihypertensives, valsartan may be associated with an excessive reduction in blood pressure. This leads, for example, to side effects such as dizziness, trembling hands or tachycardia up to and including collapse. In addition, sartans can trigger headaches, coughs, and gastrointestinal problems.

Valsartan can also cause blood potassium to increase. Therefore, it may be necessary to have regular blood tests while taking valsartan. If kidney function is reduced, the drug dose must be adjusted, or it may even have to be discontinued. 

 

Interactions of Valsartan

The following medications can affect how Valsartan works:

If it is necessary to take any of these drugs regularly, the dose of valsartan may need to be adjusted.

When not to take valsartan?

When taking valsartan, the contraindications should be observed. Valsartan should not be taken during pregnancy or breastfeeding as it may adversely affect the health of the child.

In addition, it must not be taken if both renal arteries are narrowed. Otherwise, there is a risk of sudden kidney failure. Because valsartan can cause an increase in blood potassium, it must not be used if you have a known increase in blood potassium (hyperkalaemia).

Valsartan may also be used in children and adolescents from six. However, caution should be exercised when using valsartan in people under the age of 18 and with severe impairment of kidney or liver function, as there is little experience in such cases.

Is the drug valsartan carcinogenic?

In 2018, there was a scandal related to valsartan, which made the active ingredient widely known. A major recall was launched by the manufacturer, Zhejiang Huahai Pharmaceutical, after evidence of contamination of its drug. The company’s license to manufacture this drug was subsequently revoked. 2

The substance that caused the contamination and thus the recall is called N-nitrosodimethylamine (NDMA). The substance is considered a probable carcinogen in humans. Between 3.7 and 22 micrograms of NDMA were detectable in the affected drugs. For comparison, a European absorbs an average of 0.3 micrograms of this substance daily; it is 17 to 85 micrograms for a smoker.

In addition, as early as 2010, a large-scale meta-analysis indicated that taking ACE inhibitors or sartans could increase the risk of developing lung cancer. This finding was attributed to the influence of the RAAS on cell growth. Another large-scale meta-analysis a year later was able to refute these results. Thus, no increased risk of cancer is to be expected when taking valsartan and other sartans.

 

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