DIOVAN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DIOVAN (DIOVAN).

How it works

Angiotensin II receptor antagonist (ARB) that selectively blocks the binding of angiotensin II to the AT1 receptor, thereby inhibiting vasoconstriction, aldosterone secretion, and renal sodium reabsorption.

What the body does with it

Metabolism	Primarily glucuronidation via UGT1A3, UGT2B7, and UGT1A8; minor CYP2C9 oxidation; unchanged drug eliminated in feces (83%) and urine (13%).
Excretion	Primarily biliary/fecal (83% of dose) as unchanged drug; renal excretion accounts for 13% (mostly unchanged).
Half-life	Terminal elimination half-life: approximately 6 hours (range 4–8 hours) in healthy adults; not significantly altered in renal or hepatic impairment.
Protein binding	Highly protein-bound (95%), primarily to albumin.
Volume of Distribution	Volume of distribution at steady state (Vdss): approximately 17 L (0.24 L/kg for 70 kg adult); indicates limited extravascular distribution.
Bioavailability	Oral bioavailability: approximately 25% (range 10–35%); food reduces absorption by about 40% (Cmax and AUC decrease).
Onset of Action	Oral: onset of antihypertensive effect within 2 hours; peak effect at 4–6 hours.
Duration of Action	Duration of antihypertensive effect is approximately 24 hours with once-daily dosing; trough-to-peak ratio >60%.

Classification & Brands

Dosing & administration

80-320 mg orally once daily; initial dose 80 mg; titrate to 160-320 mg daily based on response.

Dosage form	CAPSULE
Renal impairment	No adjustment required for GFR ≥30 mL/min; for GFR <30 mL/min, use with caution; no data for dialysis.
Liver impairment	Mild to moderate (Child-Pugh A/B): no adjustment; severe (Child-Pugh C): contraindicated.
Pediatric use	1-16 years: weight-based, initial 1.3 mg/kg/day (max 40 mg) orally, titrate up to 2.7 mg/kg/day (max 160 mg); 6-16 years: 80-160 mg once daily if weight ≥35 kg.
Geriatric use	Initial dose 80 mg once daily; titrate slowly; monitor renal function and blood pressure closely due to increased sensitivity.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DIOVAN (DIOVAN).

Breastfeeding	Not recommended. Valsartan is excreted in human milk in low concentrations (M/P ratio approximately 0.12); however, due to potential adverse effects on neonatal renal function and hypotension, breastfeeding is advised against.
Teratogenic Risk	FDA Pregnancy Category D for 2nd and 3rd trimesters. First trimester: limited data, potential risk of fetal renal dysfunction and oligohydramnios; second and third trimesters: associated with oligohydramnios, fetal renal impairment, skull ossification defects, and neonatal hypotension, hyperkalemia, and anuria.

Warnings & precautions

■ FDA Black Box Warning

When used during pregnancy, drugs that act directly on the renin-angiotensin system (RAS) can cause injury and even death to the developing fetus. Discontinue as soon as possible once pregnancy is detected.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to valsartan or any component of the formulation","Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m²)","Pregnancy"]

Clinical Precautions

Precautions

["Fetal toxicity (see black box warning)","Hypotension in volume- or salt-depleted patients","Monitor renal function; risk of acute renal failure in patients with renal artery stenosis","Hyperkalemia, especially in patients with renal impairment or on potassium supplements","Avoid concomitant use with aliskiren in patients with diabetes or renal impairment (eGFR <60 mL/min)"]

Clinical Tips & Counseling

Drug interactions

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DIOVAN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DIOVAN (DIOVAN).

How it works

What the body does with it

Metabolism	Primarily glucuronidation via UGT1A3, UGT2B7, and UGT1A8; minor CYP2C9 oxidation; unchanged drug eliminated in feces (83%) and urine (13%).
Excretion	Primarily biliary/fecal (83% of dose) as unchanged drug; renal excretion accounts for 13% (mostly unchanged).
Half-life	Terminal elimination half-life: approximately 6 hours (range 4–8 hours) in healthy adults; not significantly altered in renal or hepatic impairment.
Protein binding	Highly protein-bound (95%), primarily to albumin.
Volume of Distribution	Volume of distribution at steady state (Vdss): approximately 17 L (0.24 L/kg for 70 kg adult); indicates limited extravascular distribution.
Bioavailability	Oral bioavailability: approximately 25% (range 10–35%); food reduces absorption by about 40% (Cmax and AUC decrease).
Onset of Action	Oral: onset of antihypertensive effect within 2 hours; peak effect at 4–6 hours.
Duration of Action	Duration of antihypertensive effect is approximately 24 hours with once-daily dosing; trough-to-peak ratio >60%.

Classification & Brands

Dosing & administration

80-320 mg orally once daily; initial dose 80 mg; titrate to 160-320 mg daily based on response.

Dosage form	CAPSULE
Renal impairment	No adjustment required for GFR ≥30 mL/min; for GFR <30 mL/min, use with caution; no data for dialysis.
Liver impairment	Mild to moderate (Child-Pugh A/B): no adjustment; severe (Child-Pugh C): contraindicated.
Pediatric use	1-16 years: weight-based, initial 1.3 mg/kg/day (max 40 mg) orally, titrate up to 2.7 mg/kg/day (max 160 mg); 6-16 years: 80-160 mg once daily if weight ≥35 kg.
Geriatric use	Initial dose 80 mg once daily; titrate slowly; monitor renal function and blood pressure closely due to increased sensitivity.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for DIOVAN (DIOVAN).

Breastfeeding	Not recommended. Valsartan is excreted in human milk in low concentrations (M/P ratio approximately 0.12); however, due to potential adverse effects on neonatal renal function and hypotension, breastfeeding is advised against.
Teratogenic Risk	FDA Pregnancy Category D for 2nd and 3rd trimesters. First trimester: limited data, potential risk of fetal renal dysfunction and oligohydramnios; second and third trimesters: associated with oligohydramnios, fetal renal impairment, skull ossification defects, and neonatal hypotension, hyperkalemia, and anuria.

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to valsartan or any component of the formulation","Concomitant use with aliskiren in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m²)","Pregnancy"]