Valsartan

Valsartan is an AT1 receptor blocker (sartan) for the treatment of high blood pressure, heart failure, and after a heart attack.

Valsartan is available as a single-ingredient product and in various combinations: with HCT, with amlodipine (Exforge®, Dafiro®), or as a triple combination. Well-known brand names are Diovan® and Valsartan-1 A Pharma®.

Valsartan blocks the AT1 receptor for angiotensin II:

Mechanism of action:

• Selective blockade of the AT1 receptor
• Prevents the action of angiotensin II on the blood vessels
• Widening of the blood vessels and lowering of blood pressure
• Reduced aldosterone release

Clinical effect:

• Lowers systolic blood pressure by 10-15 mmHg
• Organ protection for the heart and kidneys
• No effect on the breakdown of bradykinin (cough less common than with ACE inhibitors)

Study data: Valsartan is well supported by large studies (VALUE, Val-HeFT, VALIANT) for the treatment of high blood pressure, heart failure, and after a heart attack.

Valsartan is suitable for:

• Adults with high blood pressure
• Heart failure
• Following a heart attack with heart failure
• Patients with ACE inhibitor intolerance

Particularly suitable:

• When combination therapy is needed (many combination products available)
• After a heart attack with impaired heart function

Not suitable:

• Pregnancy and breastfeeding
• Severe hepatic insufficiency
• Biliary cirrhosis, cholestasis

High blood pressure:

• Starting dose: 80 mg once daily
• Usual dose: 80-160 mg once daily
• Maximum dose: 320 mg daily

Heart failure:

• Starting dose: 40 mg twice daily
• Target dose: 160 mg twice daily

After a heart attack:

• Starting dose: 20 mg twice daily (half a 40 mg tablet)
• Gradual increase over several weeks
• Target dose: 160 mg twice daily

Available strengths:

• 40 mg, 80 mg, 160 mg, 320 mg

Combination products:

• Valsartan + HCT
• Valsartan + amlodipine (Exforge®, Dafiro®)
• Valsartan + amlodipine + HCT (Exforge HCT®)

How to take:

• Once daily (high blood pressure) or twice daily (heart failure)
• Regardless of meals
• Take with water
• Always at the same time of day

Dose adjustment:

• Gradual increase every 2-4 weeks
• Regular blood pressure and laboratory checks
• In heart failure: closer monitoring

Important notes:

• Do not stop abruptly
• Drink enough fluids
• Avoid potassium salts and potassium-rich dietary supplements

Valsartan must not be taken in cases of:

• Hypersensitivity to valsartan
• Pregnancy in the 2nd and 3rd trimesters
• Severe hepatic insufficiency, biliary cirrhosis
• Concomitant use with aliskiren in diabetes or impaired kidney function (GFR below 60 ml/min/1.73 m²)

Caution in:

• Renal insufficiency
• Renal artery stenosis
• Hyperkalemia
• Dehydration or salt depletion
• Aortic stenosis

Pregnancy and breastfeeding: Valsartan is not recommended in the 1st trimester of pregnancy and is contraindicated in the 2nd and 3rd trimesters. Sartans can cause severe malformations and kidney damage in the unborn child. Treatment should not be started during pregnancy. If pregnancy is detected, treatment must be stopped immediately and, if necessary, another therapy started. Valsartan is not recommended during breastfeeding.

Common (1-10%):

• Dizziness
• Orthostatic hypotension (drop in blood pressure when standing up)
• Changes in kidney function

Uncommon (0.1-1%):

• Angioedema
• Elevated potassium levels
• Headache
• Fatigue
• Gastrointestinal complaints
• Cough (significantly less often than with ACE inhibitors)

Frequency not known:

• Skin rash
• Elevated liver function values
• Muscle pain

Generally well tolerated: The rate of side effects is often barely higher than with placebo.

Contraindicated:

• Aliskiren in diabetes or renal insufficiency
• Sacubitril (except as the fixed combination product Entresto®)

Caution with:

• Potassium-sparing diuretics → hyperkalemia
• NSAIDs → reduced effect, kidney damage
• Lithium → increased levels
• Cyclosporine → increased potassium levels

Note on Entresto®: Sacubitril/valsartan (Entresto®) is a combination product for heart failure. It must not be combined with ACE inhibitors. When switching between an ACE inhibitor and Entresto®, there must be a gap of at least 36 hours in either direction. It should not be combined with other sartans.