Valsartan

Products

Valsartan is commercially available in the form of film-coated tablets and has been approved since 1996 (Diovan, generic). The active ingredient is also combined fixed with other agents:

Hydrochlorothiazide (co-Diovan, Exforge HCT with amlodipine, generics).
Amlodipine (Exforge, generic).
Sacubitril (Entresto)

Valsartan scandal: in July 2018, numerous generic drugs had to be recalled from the market because individual batches were contaminated with the carcinogenic substance -nitrosodimethylamine during production of the active ingredient at the supplier Zhejiang Huahai Pharmaceutical. Not all drugs were affected. The drugs were recalled down to the retail level. This contamination occurred after a change in the production process starting in 2012 (!)

Structure and properties

Valsartan (C₂₄H₂₉N₅O₃, M_r = 435.5 g/mol) is a nonpeptidic biphenyltetrazole derivative. The drug contains the amino acid valine (abbreviation: val), which gives it its name (val-sartan). Valsartan exists as a white, hygroscopic powder and is practically insoluble in water.

Effects

Valsartan (ATC C09CA03) has antihypertensive properties by abolishing the physiologic effects of angiotensin II. Angiotensin II has potent vasoconstrictor effects and increases aldosterone release, which in turn causes increased water and sodium retention. The effects of valsartan are due to selective antagonism at the AT1 receptor.

Indications

Essential hypertension (high blood pressure).
Heart failure (cardiac insufficiency)
Long-term prophylaxis after a heart attack

Dosage

According to the professional information. The dose depends on the indication. The drug can be taken regardless of meals, but should always be administered at the same time of day.

Contraindications

Hypersensitivity
Pregnancy and lactation
Severe renal dysfunction
Hereditary angioedema
Patients who have developed angioneurotic edema during treatment with an ACE inhibitor or a sartan
Concurrent use of sartans or ACE inhibitors with aliskiren in patients with diabetes mellitus, as well as in patients with impaired renal function

For complete precautions, see the drug label.

Interactions

Valsartan has a potential for drug-drug interactions. Interactions have been described with other inhibitors of the RAAS, lithium, agents that increase potassium levels, and NSAIDs, among others.

Adverse effects

The most common adverse effects include viral infections, drowsiness, orthostatic hypotension, and increased blood creatinine and urea levels.