Valsartan

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• Cough: While much less common than with ACE inhibitors, some patients still develop a dry, persistent cough.
• Abdominal Pain: Discomfort or cramping in the stomach area.
• Diarrhea: Loose or frequent stools.
• Back Pain: General muscle aches in the lower or upper back.
• Viral Infections: Such as the common cold or flu-like symptoms.

• Angioedema: Swelling of the deeper layers of the skin, often around the face, lips, tongue, or throat. This is a medical emergency.
• Rhabdomyolysis: A rare condition where muscle tissue breaks down, releasing a damaging protein into the blood. Symptoms include unexplained muscle pain, tenderness, or weakness, and dark-colored urine.
• Impaired Renal Function: In susceptible individuals, Valsartan can cause a decline in kidney function, especially if the patient is dehydrated or taking other medications that affect the kidneys.

> Warning: Stop taking Valsartan and call your doctor immediately if you experience any of the following:

• Signs of an Allergic Reaction: Hives, difficulty breathing, or swelling of your face, lips, tongue, or throat.
• Fainting or Severe Lightheadedness: This may indicate that your blood pressure has dropped too low.
• Signs of High Potassium: Nausea, weakness, tingly feeling, chest pain, irregular heartbeats, or loss of movement.
• Kidney Problems: Little or no urination, painful or difficult urination, swelling in your feet or ankles, or feeling tired or short of breath.
• Liver Problems: Loss of appetite, stomach pain (upper right side), tiredness, itching, dark urine, or jaundice (yellowing of the skin or eyes).

Long-term use of Valsartan is generally considered safe and is often necessary for the chronic management of hypertension and heart failure. However, prolonged use requires regular monitoring of kidney function and electrolyte levels (especially potassium). In some patients, long-term use may lead to a gradual increase in serum creatinine levels, signifying changes in renal filtration. There is no evidence to suggest that Valsartan causes cumulative toxicity or dependency over several years of use.

Fetal Toxicity: Valsartan carries a prominent FDA Black Box Warning regarding its use during pregnancy. Drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, Valsartan should be discontinued as soon as possible. Exposure to ARBs during the second and third trimesters has been associated with fetal lung hypoplasia (underdeveloped lungs), skeletal deformations, and neonatal skull hypoplasia. It can also lead to oligohydramnios (decreased amniotic fluid), which is a sign of decreased fetal renal function.

Report any unusual symptoms to your healthcare provider immediately. Side effects can often be managed by adjusting the dose or switching to a different medication within the same class.

• Anaphylaxis and Angioedema: Patients with a history of angioedema (swelling of the face, lips, or throat) while taking other medications (especially ACE inhibitors like Lisinopril) should use Valsartan with extreme caution. If swelling occurs, the drug must be stopped immediately and emergency care sought.
• Hypotension (Low Blood Pressure): Patients who are volume- or salt-depleted (e.g., those on high-dose diuretics) may experience excessive hypotension. Blood pressure should be monitored closely during the initiation of therapy.
• Impaired Renal Function: Valsartan can cause changes in kidney function, including acute renal failure, particularly in patients with pre-existing kidney disease or those with renal artery stenosis (narrowing of the arteries to the kidneys).
• Hyperkalemia: Because Valsartan can increase potassium levels, patients should avoid using potassium supplements or salt substitutes containing potassium without consulting their doctor.

To ensure the safe use of Valsartan, healthcare providers will require regular laboratory tests:

• Blood Pressure: Frequent monitoring, especially when starting or changing doses, to ensure the target range is met without causing hypotension.
• Serum Potassium: Periodic checks to ensure potassium levels do not become dangerously high (hyperkalemia).
• Serum Creatinine and BUN: Tests to monitor kidney function, particularly in patients with known renal impairment or heart failure.

Valsartan may cause dizziness or lightheadedness, especially during the first few days of treatment or after a dose increase. Patients should observe how they react to the medication before driving, operating heavy machinery, or performing tasks that require alertness.

Alcohol can enhance the blood pressure-lowering effect of Valsartan, which may lead to increased dizziness, lightheadedness, or fainting. It is generally advised to limit alcohol consumption while taking this medication.

Do not stop taking Valsartan abruptly. While it does not typically cause a "withdrawal syndrome" in the traditional sense, stopping the medication can lead to a rapid rebound in blood pressure, which increases the risk of heart attack or stroke. If discontinuation is necessary, your doctor will provide a tapering schedule.

> Important: Discuss all your medical conditions, including any history of liver disease, kidney disease, or heart valve problems, with your healthcare provider before starting Valsartan.

• Non-Steroidal Anti-Inflammatory Drugs (NSAIDs): Drugs like Ibuprofen, Naproxen, and Celecoxib can reduce the antihypertensive effect of Valsartan. More importantly, in patients who are elderly, volume-depleted, or have compromised kidney function, the combination can lead to a further deterioration of renal function, including possible acute renal failure.
• Other Antihypertensives: Taking Valsartan with other blood pressure medications (calcium channel blockers, beta-blockers) will have an additive effect. While often intended, it requires careful monitoring to prevent blood pressure from dropping too low.

• Potassium-Rich Foods: While a healthy diet is encouraged, patients on Valsartan should avoid excessive consumption of high-potassium foods (like bananas, spinach, and potatoes) or salt substitutes that use potassium chloride instead of sodium chloride, as this can lead to hyperkalemia.
• Grapefruit: Unlike some other heart medications, Valsartan does not have a significant interaction with grapefruit juice.
• High-Fat Meals: As noted in the pharmacokinetics section, food can reduce the absorption rate of Valsartan, but this is usually not clinically significant. It is best to be consistent—either always take it with food or always without.

• St. John's Wort: May potentially reduce the effectiveness of Valsartan by inducing certain metabolic pathways, though the clinical impact is usually minimal.
• Natural Licorice: Can cause the body to retain salt and water, which counteracts the blood pressure-lowering effects of Valsartan.
• Hawthorn: This herb may have mild blood pressure-lowering properties and could theoretically increase the effects of Valsartan, leading to hypotension.

Valsartan does not typically interfere with common laboratory tests, but it will directly affect results for:

• Plasma Renin Activity: Levels may increase as a compensatory mechanism for AT1 receptor blockade.
• Serum Potassium and Creatinine: These levels may be elevated due to the drug's pharmacological action.

For each major interaction, the management strategy usually involves dose adjustment, more frequent monitoring of lab values, or selecting an alternative medication.

> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter pain relievers and cold medicines.

• Bilateral Renal Artery Stenosis: In patients with narrowing of the arteries to both kidneys, Valsartan can cause a rapid decline in renal function and acute kidney failure because these patients rely on the renin-angiotensin system to maintain glomerular filtration.
• Severe Hepatic Impairment: Since the liver and biliary system are the primary routes of elimination for Valsartan, patients with severe liver disease or biliary obstruction may experience dangerously high levels of the drug.
• Severe Congestive Heart Failure: While Valsartan is used to treat heart failure, in very severe cases where renal function depends on the RAAS, ARBs can cause oliguria (low urine output) or progressive azotemia (high nitrogen levels in the blood).
• Volume Depletion: Patients who are severely dehydrated or have low salt levels should have their condition corrected before starting Valsartan to prevent severe hypotension.

While Valsartan is chemically distinct from ACE inhibitors, patients who have experienced angioedema while taking an ACE inhibitor (like Lisinopril or Benazepril) may have a slightly higher risk of experiencing the same reaction with Valsartan. This is not a strict contraindication, but it requires extreme vigilance during the start of therapy.

> Important: Your healthcare provider will evaluate your complete medical history, including any history of kidney or liver issues, before prescribing Valsartan.

Clinical studies did not identify overall differences in the safety or effectiveness of Valsartan between elderly patients (65 and older) and younger patients. However, older adults are more likely to have decreased renal or hepatic function and are more susceptible to hypotension. Therefore, healthcare providers may start with lower doses and monitor blood pressure and kidney function more frequently in this population.

For patients with mild to moderate renal impairment, no initial dose adjustment is needed. However, in patients with severe renal impairment (Creatinine Clearance < 10 mL/min) or those on dialysis, Valsartan should be used with caution. The drug is not removed by hemodialysis because it is highly bound to plasma proteins.

In patients with mild to moderate chronic liver disease, the exposure (AUC) to Valsartan is approximately twice that of healthy volunteers. While no specific starting dose adjustment is mandated, providers should use the lowest effective dose and monitor the patient closely. Valsartan should be avoided or used with extreme caution in patients with severe hepatic impairment or biliary cirrhosis.

> Important: Special populations require individualized medical assessment to ensure the benefits of Valsartan therapy outweigh the potential risks.

| Parameter | Value |

|---|---|

| Bioavailability | ~25% (Oral) |

| Protein Binding | 95% (Mainly Albumin) |

| Half-life | 6 to 9 hours |

| Tmax | 2 to 4 hours |

| Metabolism | Minimal (~20%), inactive metabolites |

| Excretion | Fecal 83%, Renal 13% |

• Molecular Formula: C24H29N5O3
• Molecular Weight: 435.5 g/mol
• Solubility: Soluble in ethanol and methanol; slightly soluble in water.
• Structure: Valsartan is a tetrazole derivative and a non-peptide molecule. Its structure allows it to mimic the C-terminal end of Angiotensin II, enabling competitive inhibition at the receptor site.

Valsartan is classified as an Angiotensin II Receptor Blocker (ARB). Other drugs in this class include Losartan, Candesartan, and Olmesartan. Within the broader therapeutic area of cardiovascular medicine, it is considered a first-line agent for hypertension management and a core component of Guideline-Directed Medical Therapy (GDMT) for heart failure.