Valsartan is a medicine for high blood pressure (hypertension), also used in heart failure and after myocardial infarction. It belongs to the angiotensin II receptor blocker (ARB) class. It is generally well tolerated; it can cause dizziness, fatigue and, less often, increased potassium or changes in kidney function.
Also known as: Diovan
Dual RAAS blockade (ACE+ARB) with risk of hypotension, hyperkalaemia and renal decline.
Dual RAAS blockade with an ARB and an ACE inhibitor adds the effects on renal haemodynamics and potassium balance. The captopril label documents "Dual Blockade of the Renin-Angiotensin System (RAS)" as associated with "increased risks of hypotension, hyperkalaemia, and changes in renal function (including acute renal failure)" and recommends close monitoring of BP, renal function and electrolytes when the combination is unavoidable; the valsartan label states "Dual inhibition of the RAS: Increased risk of renal impairment, hypotension, and hyperkalemia". Major trials (ONTARGET, ALTITUDE) showed that dual blockade does not reduce mortality and increases renal adverse events and hyperkalaemia. Avoid in most hypertensive patients; consider only under specialist supervision in selected HF (Val-HeFT, PARADIGM-HF), with rigorous monitoring of BP, creatinine and potassium one week after initiation/adjustment and whenever therapy changes.
Valsartan + captopril: dual RAAS blockade — higher risk of hypotension, hyperkalaemia and renal impairment. Avoid in most patients.
Enhanced RAAS blockade removes renal compensation and raises potassium.
Potassium, creatinine, blood pressure.
Hypotension or hyperkalaemia.
Avoid routinely; if used, monitor potassium, creatinine and BP.
DailyMed (FDA) — approved Valsartan label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1a8af3d9-4053-4233-82a7-e8c7bc9e302f ; approved Captopril label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=563737c5-4d63-4957-8022-e3bc3112dfac — additional reference: Prontuário Terapêutico do INFARMED (11th ed., 2012)
Dual RAAS blockade (ACE+ARB) with risk of hypotension and renal injury.
Combining an ARB (valsartan) with an ACE inhibitor (ramipril) blocks the RAAS at two steps, adding the risk of hyperkalaemia, hypotension and renal function deterioration. The valsartan label states that "Dual inhibition of the RAS" increases the "risk of renal impairment, hypotension, and hyperkalemia"; the ramipril label documents "Dual Blockade of the Renin-Angiotensin System" among the warnings and "Agents Increasing Serum Potassium" in interactions, and the risk is higher in patients with renal impairment, diabetes or volume depletion. The ONTARGET trial with telmisartan+ramipril showed more renal adverse events without mortality benefit. Avoid in most patients; if absolutely necessary (refractory HF), monitor BP, creatinine and potassium 1–2 weeks after initiation or dose adjustment and reduce the doses of both.
Valsartan + ramipril: dual RAAS blockade — higher risk of hypotension, hyperkalaemia and renal impairment. Avoid; monitor BP, K+ and creatinine if unavoidable.
Enhanced blockade lowers intraglomerular pressure, impairing renal function and raising potassium.
Creatinine, diuresis, potassium.
Hypotension or renal worsening.
Avoid unless proven benefit; monitor renal function.
DailyMed (FDA) — approved Ramipril label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3806abdc-6aec-4252-bd79-e2c115b849aa ; approved Valsartan label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1a8af3d9-4053-4233-82a7-e8c7bc9e302f — additional reference: Prontuário Terapêutico do INFARMED (11th ed., 2012)
ARB with a potassium-sparing diuretic raises hyperkalaemia risk.
Both valsartan (ARB) and spironolactone (aldosterone antagonist) reduce renal potassium excretion through complementary pathways — valsartan decreases aldosterone by blocking the AT1 receptor, and spironolactone blocks the mineralocorticoid receptor at the effector end. The spironolactone label classifies "ARBs" among the "agents that increase serum potassium" and recommends "checking serum potassium levels when ACE inhibitor or ARB therapy is altered in patients receiving spironolactone"; the valsartan label warns that "potassium-sparing diuretics, potassium supplements or salt substitutes may lead to increases in serum potassium". The combination is used in HF (RALES demonstrated benefit) but requires rigorous monitoring. Contraindicated if K+ > 5,0 mEq/L or creatinine clearance < 30 mL/min; stop potassium supplements; monitor K+ and creatinine at 3–7 days and 1 month, then quarterly.
Valsartan + spironolactone: additive hyperkalaemia (ARB + K-sparing diuretic). Monitor potassium and renal function; avoid in CKD or K+ > 5,0.
Both spare potassium; risk rises with reduced renal function.
Potassium, heart rhythm.
Hyperkalaemia or arrhythmia.
Monitor potassium; avoid in advanced renal failure.
DailyMed (FDA) — approved Valsartan label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1a8af3d9-4053-4233-82a7-e8c7bc9e302f ; approved Spironolactone label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=57d1c333-c229-54aa-e063-6394a90a84ce — additional reference: Prontuário Terapêutico do INFARMED (11th ed., 2012)
As with ACE inhibitors, ARBs can raise serum potassium; high potassium intake or salt substitutes increase the risk of hyperkalaemia.
Avoid potassium supplements and salt substitutes without supervision; monitor potassium in at-risk patients.
EMC-UK (MHRA) — approved Valsartan SmPC: https://www.medicines.org.uk/emc/product/14212/smpc
Valsartan is contraindicated in previous ARB-associated angioedema or hereditary angioedema.
Do not use in patients with a history of angioedema.
EMC-UK (MHRA) — approved Valsartan SmPC: https://www.medicines.org.uk/emc/product/14212/smpc
Valsartan is contraindicated in bilateral renal artery stenosis (or stenosis in a single functioning kidney) because of the risk of acute renal failure.
Do not use; assess renal function before starting an ARB.
EMC-UK (MHRA) — approved Valsartan SmPC: https://www.medicines.org.uk/emc/product/14212/smpc
ARBs are contraindicated in pregnancy: they may cause fetal renal injury, oligohydramnios and skull hypoplasia, especially in the 2nd and 3rd trimesters.
Do not start in pregnancy; if pregnancy is detected, stop valsartan immediately.
Not recommended during breastfeeding; prefer an alternative with an established safety profile.
Women of childbearing age must use effective contraception during treatment.
EMC-UK (MHRA) — approved Valsartan SmPC: https://www.medicines.org.uk/emc/product/14212/smpc
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Blocks angiotensin II-induced vasoconstriction and aldosterone secretion. An oral 80 mg dose inhibits the pressor effect of angiotensin II by about 80% at peak, with about 30% inhibition persisting at 24 hours. It does not inhibit ACE (no effect on bradykinin — less cough) and does not interfere with other hormone receptors or relevant ion channels.
Selective competitive antagonist of angiotensin II AT1 receptors (affinity ~20,000-fold greater for AT1 than AT2), independent of angiotensin II synthesis pathways. Blockade removes the negative feedback on renin (2-3-fold rise in plasma renin) without overcoming the antihypertensive effect.
Peak plasma levels 2-4 hours after dosing; absolute bioavailability ~25% (range 10-35%). Food reduces exposure by ~40% (AUC) and peak by ~50%, without requiring adjustment. Small volume of distribution (17 L); protein binding ~95%.
Limited metabolism: the main metabolite (valeryl-4-hydroxy-valsartan, about 9% of the dose) is formed via CYP2C9. Does not inhibit CYP450 enzymes at clinically relevant concentrations — metabolic interactions unlikely. Eliminated mainly in faeces (~83%) and urine (~13%), mostly as unchanged drug.
Mean elimination half-life of about 6 hours (bi-exponential decay); no appreciable accumulation with repeated dosing. Exposure is ~70% higher and half-life 35% longer in the elderly; doubles in patients with mild-to-moderate liver disease.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
