Valsartil40 mg

Valsartil is an angiotensin II receptor blocker (ARB) with the following evidence-based uses:

Established / FDA-approved uses

• Hypertension: Treatment of high blood pressure in adults and children aged 6 years and older, alone or in combination with other antihypertensive agents.
• Heart failure: Treatment of symptomatic heart failure (NYHA Class II-IV) in adults who are intolerant of ACE inhibitors or, in some cases, as add-on therapy, to reduce hospitalization for heart failure.
• Post-myocardial infarction: Treatment of clinically stable patients with left ventricular failure or left ventricular systolic dysfunction following a heart attack, to reduce cardiovascular mortality.

Guideline-supported / adjunct uses

• As part of combination therapy (e.g., with a diuretic or calcium channel blocker) when blood pressure is not controlled with Valsartil alone.
• Used off-label in some patients with diabetic kidney disease for its renal-protective (antiproteinuric) effect, although losartan and irbesartan have more extensive outcome-trial data for this specific use.

Valsartil should not be used in patients who are pregnant due to the risk of fetal harm (see Pregnancy and Lactation).

Each film-coated tablet of Valsartan typically contains Valsartan as the active ingredient, commonly available in strengths of 40 mg, 80 mg, 160 mg, and 320 mg. Excipients vary by manufacturer and may include microcrystalline cellulose, crospovidone, magnesium stearate, colloidal silicon dioxide, and a film-coating system. Valsartan is also marketed in fixed-dose combinations with hydrochlorothiazide, amlodipine, or sacubitril in some markets; this document refers to Valsartan as a single-ingredient product unless otherwise specified.

Valsartil is a synthetic, orally active angiotensin II receptor antagonist that acts on the AT1 receptor subtype. It is chemically distinct from the biphenyl-tetrazole class in some structural aspects but shares the core pharmacology of ARBs. Valsartil does not inhibit ACE (kininase II), the enzyme that generates angiotensin II and also degrades bradykinin, which is why it is associated with a lower incidence of dry cough and angioedema compared with ACE inhibitors, though angioedema can still rarely occur.

Valsartil is used to manage hypertension, chronic heart failure, and to improve survival after a heart attack in appropriate patients, by reducing the harmful cardiovascular and renal effects of angiotensin II.

Valsartil belongs to the therapeutic class of Angiotensin II Receptor Blockers (ARBs), also called angiotensin receptor antagonists. This class is used primarily in the management of hypertension, heart failure, and cardiovascular/renal protection.

Valsartan selectively blocks the binding of angiotensin II to the AT1 receptor found in vascular smooth muscle and the adrenal gland. Angiotensin II is a potent vasoconstrictor and the primary active hormone of the renin-angiotensin-aldosterone system (RAAS); it also stimulates aldosterone secretion. By blocking AT1 receptors, Valsartan:

• Reduces vasoconstriction, lowering peripheral vascular resistance and blood pressure.
• Reduces aldosterone release, which decreases sodium and water retention.
• Does not affect bradykinin metabolism (unlike ACE inhibitors), leading to a lower incidence of cough.

Pharmacokinetics: After oral administration, Valsartan has an absolute bioavailability of about 23%, with peak plasma concentrations reached in 2-4 hours. Food reduces systemic exposure (AUC) by about 40-50%, but this is not considered clinically significant and Valsartan can be taken with or without food. It is highly protein bound (~95%), undergoes minimal hepatic metabolism, and is eliminated mainly unchanged, primarily via bile/feces (~83%) and to a lesser extent in urine (~13%). The elimination half-life is approximately 6 hours.

Valsartil tablets should be swallowed whole with a glass of water, with or without food, at approximately the same time(s) each day to maintain consistent blood levels. Do not crush or chew the tablet unless advised by a physician or pharmacist. If a dose is missed, it should be taken as soon as remembered unless it is almost time for the next dose, in which case the missed dose should be skipped; doses should not be doubled.

Clinically significant drug interactions with Valsartil include:

• ACE inhibitors: Combining Valsartil with an ACE inhibitor increases the risk of hyperkalemia, hypotension, and renal impairment without added cardiovascular benefit; dual RAAS blockade is generally not recommended.
• Aliskiren: Concomitant use of Valsartil with aliskiren is contraindicated in patients with diabetes and not recommended in patients with renal impairment (eGFR <60 mL/min/1.73m²), due to increased risk of hyperkalemia, hypotension, and renal impairment.
• Potassium-sparing diuretics, potassium supplements, or salt substitutes containing potassium: May increase serum potassium; concomitant use requires monitoring.
• NSAIDs (including selective COX-2 inhibitors): May reduce the antihypertensive effect of Valsartil and increase the risk of renal impairment, particularly in elderly, volume-depleted, or renally impaired patients.
• Lithium: Valsartil can increase serum lithium concentrations and lithium toxicity; monitor lithium levels closely during concomitant use.
• Other antihypertensive agents or diuretics: Additive blood-pressure-lowering effect; may increase the risk of symptomatic hypotension.

Most patients tolerate Valsartil well. Reported adverse effects include:

Common

• Dizziness or lightheadedness
• Headache
• Fatigue
• Upper respiratory tract infection symptoms
• Abdominal pain
• Hyperkalemia (elevated blood potassium)

Less common / serious (seek medical attention)

• Symptomatic hypotension, especially in volume- or salt-depleted patients
• Worsening renal function or acute kidney injury, particularly in patients with pre-existing renal impairment or renal artery stenosis
• Angioedema (swelling of the face, lips, tongue, or throat) — rare but requires immediate discontinuation and emergency care
• Rare cases of elevated liver enzymes or hepatic dysfunction
• Rare cases of decreased hemoglobin/hematocrit or neutropenia

Pregnancy: Valsartil is contraindicated during pregnancy. Drugs that act directly on the renin-angiotensin system, including Valsartil, can cause injury and death to the developing fetus when used in the second and third trimesters, including fetal renal failure, oligohydramnios, skull hypoplasia, and neonatal death. If pregnancy is detected, Valsartil should be discontinued as soon as possible and the patient switched to an alternative antihypertensive under medical supervision. Women of childbearing potential should discuss reliable contraception with their physician while taking Valsartil.

Lactation: It is not known whether Valsartil is excreted in human breast milk. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue breastfeeding or discontinue Valsartil, taking into account the importance of the drug to the mother; use only if clearly needed and after consulting a physician.

The following precautions apply to the use of Valsartil:

• Hypotension: Symptomatic hypotension may occur, particularly in patients who are volume- or salt-depleted (e.g., from diuretic therapy, dietary salt restriction, dialysis, vomiting, or diarrhea). Correct volume depletion before starting Valsartil, or begin under close medical supervision.
• Renal impairment: Monitor renal function periodically, especially in patients with renal artery stenosis, pre-existing kidney disease, or heart failure, as changes in renal function including acute renal failure can occur.
• Hyperkalemia: Monitor serum potassium periodically, particularly in patients with renal impairment, diabetes, or those taking potassium supplements, potassium-sparing diuretics, or salt substitutes containing potassium.
• Angioedema: Discontinue Valsartil immediately and do not readminister if angioedema (swelling of face, lips, tongue, throat, or difficulty breathing) occurs.
• Dual RAAS blockade: Avoid combining Valsartil with an ACE inhibitor or aliskiren (see Interactions).
• Hepatic impairment: Use with caution in mild-to-moderate hepatic impairment; not recommended in patients with severe hepatic impairment, biliary cirrhosis, or biliary obstruction.

Overdose with Valsartil may cause marked hypotension, dizziness, and tachycardia or bradycardia. If overdose is suspected, seek immediate medical attention or contact a poison control center right away. Treatment is supportive and may include monitoring of vital signs and, if needed, intravenous fluids or other supportive measures administered by medical professionals; Valsartil is not effectively removed by hemodialysis due to its high protein binding. Do not attempt to manage an overdose at home without medical guidance.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Elderly: No overall differences in effectiveness were observed between elderly and younger patients; however, elderly patients may be more sensitive to blood-pressure-lowering effects, so caution is advised.

Renal impairment: No initial dosage adjustment is routinely required in mild-to-moderate renal impairment, but renal function and potassium should be monitored. Use with caution in severe renal impairment.

Hepatic impairment: No dosage adjustment needed in mild-to-moderate hepatic impairment; not recommended in severe hepatic impairment or biliary obstruction.

Pediatric patients: Safety and efficacy of Valsartil for hypertension are established in children aged 6 years and older; not established in children under 6 years or for heart failure/post-MI indications in children.

Pregnancy: Contraindicated (see Pregnancy and Lactation).

Valsartil is typically used as a long-term, often lifelong, maintenance therapy for chronic conditions such as hypertension and heart failure, since these conditions generally require continuous blood pressure and cardiovascular risk control. In post-myocardial infarction patients, treatment is usually continued indefinitely unless discontinued by the treating physician. The duration of therapy should be determined by the prescribing physician based on the underlying condition, response, and tolerability; Valsartil should not be stopped abruptly without medical advice.

Valsartan is classified as an Angiotensin II Receptor Blocker (ARB), within the broader category of renin-angiotensin-aldosterone system (RAAS) inhibitors, which also includes ACE inhibitors and direct renin inhibitors.

Valsartan works by selectively blocking the AT1 subtype of angiotensin II receptors, preventing angiotensin II from causing vasoconstriction and aldosterone release. This results in vasodilation, reduced peripheral vascular resistance, decreased sodium and water retention, and consequently lowers blood pressure and reduces cardiac workload, which is beneficial in hypertension, heart failure, and after a heart attack.

D

Valsartil is approved for the treatment of hypertension in children aged 6 to 16 years, with weight-based starting doses (see Dosage and Administration). Use in children under 6 years of age is not established, and use for heart failure or post-myocardial infarction indications has not been established in pediatric patients. As with adults, Valsartil is contraindicated in pregnant adolescents due to the risk of fetal harm. Growing children on long-term therapy should have periodic monitoring of renal function, electrolytes, and blood pressure by their physician.