How Valsartan works
Valsartan blocks the receptors (docking sites) of the hormone angiotensin-II – more precisely, the AT-1 receptors, which means that the hormone can no longer exert its effect. This prevents a rise in blood pressure and thus relieves the heart and kidneys.
The salt and water balance in the human body is regulated by the hormonal RAA system (renin-angiotension-aldosterone system). At the same time, blood pressure is also regulated via the RAAS.
Angiotensin II is one of the hormones in this system. When it binds to its receptors on the inside of the blood vessels, the vessels constrict – blood pressure rises. There are also angiotensin II receptors in the kidneys. Here, the hormone ensures that less salt is released into the urine, meaning that more salt and thus water remain in the body. This also increases blood pressure.
Absorption, breakdown and excretion
In the body, about one-fifth of the amount of active ingredient is metabolized to inactive degradation products, the rest is excreted unchanged. Excretion takes place largely via the bile in the stool. Approximately six hours after ingestion, half of the administered amount has been excreted.
When is valsartan used?
Valsartan is approved for the treatment of:
- High blood pressure
- recent heart attack
- heart failure (heart failure)
How Valsartan is used
The most common form of valsartan is oral tablets. For patients who have difficulty swallowing or are tube-fed, oral solutions are available.
The dosage depends largely on the area of application and is usually between 80 and 160 milligrams once daily. The maximum dosage is 320 milligrams. Sometimes this daily dose is also divided into two intakes (morning and evening).
What are the side effects of valsartan?
In controlled clinical trials, valsartan did not cause side effects more often than drug-free placebo. One in one hundred to one thousand people treated experienced dizziness, fatigue, cough, and abdominal pain as the most common side effects.
The erectile dysfunction often triggered by blood pressure medications generally does not occur with valsartan. Sometimes sartans such as losartan and valsartan can even have a positive effect on impotence (erectile dysfunction).
What should I be aware of when taking valsartan?
Contraindications
Valsartan must not be taken in the following cases:
- hypersensitivity to the active substance or to any of the other components of the drug
- severe liver dysfunction
- cholestasis (bile stasis)
- concomitant use of aliskiren (blood pressure medication) in patients with diabetes or chronic renal dysfunction
- second and third trimesters of pregnancy
Interactions
The additional use of other medications that affect the RAAS or blood pressure should be closely monitored by the physician, especially at the beginning, so that the blood pressure does not drop too much.
In combination with preparations that can increase the potassium level in the body, the potassium level must be monitored. Such preparations include potassium-sparing diuretics and potassium supplements. Low-sodium table salt is also one of them.
Age restriction
Valsartan is approved for treatment in children six years of age and older.
Pregnancy and breastfeeding
Since valsartan can harm the unborn child, the antihypertensive drug must not be used during pregnancy – especially in the second and third trimesters.
No information is available on the use of valsartan during breastfeeding. Breastfeeding mothers should therefore not take the active substance.
How to obtain medication with valsartan
Medicines containing valsartan are subject to prescription in Germany, Austria and Switzerland.
How long has valsartan been known?
The first sartan – losartan – was launched on the market in the USA in 1995. Later, other active ingredients were developed which, among other things, are better utilized in the body and have a longer effect.
Valsartan scandal
In 2018, numerous generics produced in China with the active ingredient valsartan had to be recalled from the market because the approved limits of the carcinogenic substance N-nitrosodimethylamine were exceeded in individual batches. The contamination most likely resulted from a change in the production process at the manufacturing company.
Pharmaceuticals in which the contained valsartan was produced in Europe were not affected.
