Cardovan

Approved Indications:

• Hypertension (High Blood Pressure):
• For the treatment of essential hypertension in adults and children ≥6 years.
• Reduces the risk of cardiovascular events such as stroke and myocardial infarction.
• Heart Failure:
• Used in adult patients with NYHA Class II–IV heart failure to reduce hospitalization and cardiovascular mortality.
• Often part of guideline-directed medical therapy (GDMT).
• Post-Myocardial Infarction (MI):
• Indicated in clinically stable patients with left ventricular systolic dysfunction or symptomatic heart failure post-MI to improve survival and reduce cardiovascular risk.

Clinically Accepted Off-Label Uses:

• Diabetic Nephropathy (in patients intolerant to ACE inhibitors)
• Left Ventricular Hypertrophy (LVH)
• Marfan syndrome (aortic root dilation management, second-line)
• Proteinuria reduction in chronic kidney disease (CKD)

General Guidelines:

• Route: Oral
• May be administered with or without food.
• Swallow whole with water.

Adults:

• Hypertension:
• Starting dose: 80 mg once daily
• Maintenance: 80–320 mg once daily
• Maximum: 320 mg/day
• Heart Failure:
• Starting dose: 40 mg twice daily
• Target dose: 160 mg twice daily, as tolerated
• Post-MI:
• Initial: 20 mg twice daily
• Titrate over several weeks up to 160 mg twice daily

Pediatric (Age 6–16 years):

• Hypertension:
• Dose based on body weight:
• <35 kg: 40 mg once daily
• ≥35 kg: 80–160 mg once daily

Elderly:

• No initial dose adjustment generally required; monitor renal function and blood pressure.

Renal Impairment:

• Mild to moderate (CrCl >30 mL/min): No dose adjustment.
• Severe (CrCl <30 mL/min): Use with caution; monitor closely.

Hepatic Impairment:

• Mild to moderate hepatic impairment (without cholestasis): Use with caution.
• Severe impairment or biliary cirrhosis: Not recommended.

Valsartan is a selective angiotensin II type 1 (AT1) receptor blocker (ARB). It competitively inhibits the binding of angiotensin II to AT1 receptors in vascular smooth muscle and the adrenal gland, preventing vasoconstriction and aldosterone secretion. This leads to vasodilation, reduction in blood pressure, and decreased preload and afterload in heart failure. Unlike ACE inhibitors, it does not interfere with bradykinin metabolism, thus resulting in fewer cough-related side effects.

• Absorption: Rapid but incomplete; absolute bioavailability ≈ 25%
• Time to Peak Concentration (Tmax): 2–4 hours post-dose
• Distribution: Volume of distribution ≈ 17 L; plasma protein binding ≈ 94–97%
• Metabolism: Minimal; primarily excreted unchanged; no significant CYP450 involvement
• Elimination:
• Half-life: ≈ 6 hours
• Excretion: ~83% in feces, ~13% in urine (mostly unchanged)

• Pregnancy: Category D
• Contraindicated during the 2nd and 3rd trimesters due to risk of fetal toxicity (e.g., renal failure, skull hypoplasia, death).
• Discontinue immediately if pregnancy is detected.
• Lactation:
• Unknown if valsartan is excreted in human milk.
• Due to potential for serious adverse reactions in infants, breastfeeding is not recommended during treatment.

• Primary Class: Angiotensin II Receptor Blocker (ARB)
• Subclass: Selective AT1 receptor antagonist
• Generation: Second-generation ARB

• Known hypersensitivity to valsartan or any excipients
• Pregnancy (especially 2nd/3rd trimester)
• Concomitant use with aliskiren in patients with diabetes mellitus
• Severe hepatic impairment or biliary cirrhosis
• Hereditary conditions of galactose intolerance (due to excipients in some formulations)

• Fetal Toxicity: Can cause injury/death to fetus; discontinue when pregnancy detected.
• Hypotension Risk: Especially in volume- or salt-depleted patients; correct depletion before use.
• Hyperkalemia: Monitor potassium, especially in renal impairment or with potassium-sparing agents.
• Renal Function Monitoring: Caution in patients with bilateral renal artery stenosis; may worsen renal function.
• Angioedema: Rare but possible; discontinue if observed.
• Liver Dysfunction: Avoid in severe hepatic impairment; monitor transaminases if used.

Common:

• Central Nervous System: Headache, dizziness
• Gastrointestinal: Nausea, diarrhea, abdominal pain
• General: Fatigue, viral infection (in pediatrics)

Less Common:

• Cough (less frequent than ACE inhibitors)
• Back pain
• Arthralgia

Serious/Rare:

• Hypotension
• Hyperkalemia
• Angioedema
• Acute renal failure
• Hepatitis, elevated liver enzymes
• Rhabdomyolysis (rare reports)

• Potassium supplements & K-sparing diuretics (e.g., spironolactone):
• Increased risk of hyperkalemia
• NSAIDs: May reduce antihypertensive effect; increased risk of renal dysfunction
• Lithium: Risk of lithium toxicity; monitor serum lithium levels
• Diuretics: Volume depletion may intensify hypotension
• Aliskiren: Contraindicated in diabetic patients due to renal impairment risk
• CYP450: Not a substrate, inducer, or inhibitor of major CYP enzymes — low interaction potential

• ACC/AHA Hypertension Guidelines: Valsartan remains a preferred ARB for monotherapy or combination therapy.
• ESC 2023 Heart Failure Guidelines: Recommended in patients intolerant to ACE inhibitors or as part of ARNi.
• FDA Warning (ongoing monitoring): Surveillance continues for nitrosamine impurities (e.g., NDMA) in some valsartan batches, though current formulations are compliant.

• Temperature: Store below 25°C (77°F); brief excursions permitted up to 30°C.
• Humidity: Protect from moisture; store in a tightly closed container.
• Light Protection: Store in original packaging to protect from light.
• Handling: Do not use tablets that are chipped, broken, or discolored.