VALSARTAN

Clinical safety rating: avoid

Contraindicated (not allowed)

How it works

Valsartan is an angiotensin II receptor antagonist (ARB) that selectively blocks the binding of angiotensin II to the AT1 receptor, resulting in vasodilation, reduced aldosterone secretion, and decreased blood pressure.

What the body does with it

Metabolism	Valsartan is primarily metabolized by CYP2C9 (minor pathways include CYP2C8 and CYP3A4). It undergoes glucuronidation via UGT1A3 and UGT2B7.
Excretion	Primarily eliminated unchanged in feces (83%) via biliary excretion, and approximately 13% in urine as unchanged drug. Renal clearance accounts for ~30% of total clearance.
Half-life	Terminal elimination half-life is approximately 6 hours (range 4–9 hours) in healthy adults. In patients with hepatic impairment, half-life is similar due to lack of significant metabolism.
Protein binding	94–97% bound, primarily to serum albumin.
Volume of Distribution	Volume of distribution at steady state is approximately 17 L (0.23 L/kg). This indicates limited extravascular distribution, consistent with high protein binding.
Bioavailability	Oral bioavailability is about 25% (range 10–35%). Food decreases absorption and reduces peak concentration by about 50% but does not affect AUC significantly.
Onset of Action	Oral: 2 hours for peak serum concentration; antihypertensive effect begins within 2 weeks of therapy, but maximal effect may require 4 weeks.
Duration of Action	Duration of antihypertensive effect is 24 hours with once-daily dosing. Blood pressure reduction is sustained over the dosing interval, with a trough-to-peak ratio of 60–70%.

Classification & Brands

Dosing & administration

80-320 mg orally once daily; initial dose typically 80 mg or 160 mg once daily.

Dosage form	TABLET
Renal impairment	No adjustment for GFR ≥30 mL/min; for GFR <30 mL/min, caution and consider lower starting dose (e.g., 80 mg once daily) due to limited data; not dialyzable.
Liver impairment	Child-Pugh Class A: no adjustment; Child-Pugh Class B: caution, consider starting dose of 80 mg once daily; Child-Pugh Class C: not recommended due to lack of data.
Pediatric use	Children 6-16 years: starting dose 1.3 mg/kg (up to 40 mg) orally once daily, titrate to maximum 2.7 mg/kg (up to 160 mg) once daily. Children 1-5 years: starting dose 0.4 mg/kg (up to 20 mg) once daily, titrate to maximum 1.0 mg/kg (up to 80 mg) once daily.
Geriatric use	No specific dose adjustment; initiate at lower end of dosing range (80 mg once daily) due to potential for decreased renal function and increased sensitivity; monitor blood pressure and renal function.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

NSAIDs may diminish the antihypertensive effect Lithium levels may be increased Use in pregnancy can cause injury and death to the developing fetus.

Breastfeeding	Excreted into breast milk in low amounts; M/P ratio not established. Avoid use in breastfeeding due to potential adverse effects on neonatal renal and cardiovascular systems.
Teratogenic Risk	First trimester: Limited human data, but potential risk of renal and cardiac malformations based on animal studies and angiotensin II receptor blocker (ARB) class effects. Second and third trimesters: Fetal oligohydramnios, renal injury (including renal failure), skull ossification defects, limb contractures, hypotension, and neonatal death. Avoid use in pregnancy.

Warnings & precautions

■ FDA Black Box Warning

Fetal toxicity: Drugs acting directly on the renin-angiotensin system can cause injury and death to the developing fetus. Discontinue as soon as possible when pregnancy is detected.

Side Effect Profile

Common Effects	heart failure
Serious Effects

Absolute Contraindications

["Hypersensitivity to valsartan or any component","Pregnancy","Coadministration with aliskiren in patients with diabetes"]

Clinical Precautions

Precautions

["Hypotension in volume- or salt-depleted patients","Worsening renal function, especially in patients with renal artery stenosis","Hyperkalemia, particularly with concurrent use of potassium-sparing diuretics or supplements","Angioedema","Hepatic impairment"]

Clinical Tips & Counseling

Drug interactions

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