valsartan/amlodipine

Action and Spectrum

Actions and Spectrum:

Actions:

valsartan: valsartan is an angiotensin receptor blocker (ARB) that works by blocking the effects of angiotensin II, a hormone that can cause blood vessels to constrict and increase blood pressure. By blocking this hormone, valsartan allows blood vessels to relax and widen, which can lead to a decrease in blood pressure. valsartan is effective in reducing both systolic and diastolic blood pressure.

amlodipine: amlodipine is a calcium channel blocker that relaxes the blood vessels and reduces the heart’s workload. It does this by blocking calcium entry into the smooth muscle cells of blood vessels and the heart, which can cause these muscles to contract. Amlodipine helps to relax the blood vessels, improve blood flow, and decrease blood pressure by blocking the entry of calcium. Amlodipine is effective in reducing both systolic and diastolic blood pressure.

Spectrum of effects: When used together, valsartan and amlodipine can provide complementary effects to lower blood pressure. valsartan helps to relax blood vessels by blocking the effects of angiotensin II, while amlodipine relaxes blood vessels by blocking calcium entry. This combination can be particularly effective in people with high blood pressure, providing more significant reductions than drugs alone. Additionally, the combination may have other beneficial effects, such as reducing the risk of heart failure, stroke, and other cardiovascular events.

Drug Interaction

Adverse Reaction

Frequency Defined

>10%:

Headache

Increased BUN (6-17%)

1-10%:

Peripheral edema (5-8%)

Upper respiratory infection (3%)

Dizziness (2%)

Anxiety (3%)

Nasopharyngitis (4%)

Diarrhea (3%)

Abdominal pain (3%)

Nausea (3%)

Cough (2%)

Somnolence (3%)

Increased potassium (3%)

<1%:

Syncope

Orthostatic hypotension

Visual disturbance

Exanthema

Tinnitus

Black Box Warning

Black Box Warning:

If pregnancy is detected, discontinue the dose as soon as possible. The drug affects the RAS, causing oligohydramnios. It may result in injury/death of the fetus.

Contraindication / Caution

Contraindication/Caution

Contraindications:

• Contraindication in pregnancy: As mentioned in a previous answer, medications that affect the renin-angiotensin system (including valsartan) are contraindicated in pregnancy. Therefore, if a woman is pregnant or planning to become pregnant, valsartan and amlodipine should not be used.
• Severe liver disease: Both valsartan and amlodipine are metabolized by the liver, so people with severe liver disease should use these medications with caution, as they may not be able to properly metabolize and eliminate the drugs from their system.
• Severe kidney disease: People with severe kidney Contraindication in pregnancy: As mentioned in a previous answer, medications that affect the renin-angiotensin system (including valsartan) are contraindicated. Therefore, valsartan and amlodipine should not be used if a woman is pregnant or planning to become pregnant.
• Severe liver disease: Both valsartan and amlodipine are metabolized by the liver, so people with severe liver disease should use these medications with caution, as they may not be able to properly metabolize and eliminate the drugs from their system.
• Severe kidney disease: People with severe kidney disease may need to adjust their dosages. The medications may not be cleared from the body as effectively in people with impaired kidney function.
• Hypotension: valsartan and amlodipine are used to lower blood pressure; use with caution in people with low blood pressure. In some cases, the medications may cause excessive lowering of blood pressure, which can lead to dizziness or fainting.
• Allergy or sensitivity to the medications: People with allergic reactions or sensitivity to valsartan or amlodipine should not use these medications.
• Heart failure: valsartan and amlodipine are often used to treat heart failure with caution in people with severe or not stabilized on other heart failure medications.
• As with any medication, discussing valsartan and amlodipine with a healthcare provider is essential, especially if any pre-existing conditions or medications are being taken that could interact with these drugs.Top of Form

Cautions:

• Drug interactions: valsartan and amlodipine may interact with other medications, including over-the-counter drugs, supplements, and prescription medications. It is important to inform the healthcare provider of all medications being taken to avoid potential drug interactions.
• Electrolyte imbalances: valsartan and amlodipine may cause electrolyte imbalances, such as low levels of sodium or high levels of potassium. People taking these medications should have their electrolyte levels monitored regularly.
• Liver function: valsartan and amlodipine are metabolized in the liver, so people with impaired liver function should use these medications with caution.
• Kidney function: valsartan and amlodipine are eliminated from the body through the kidneys. People with impaired kidney function should adjust their dosages and be monitored closely for adverse effects.
• Fluid and salt imbalances: valsartan and amlodipine can cause fluid and salt imbalances, especially in people with congestive heart failure. It is important to monitor fluid intake and restrict salt intake as directed by the healthcare provider.
• Pregnancy and breastfeeding: As previously mentioned, valsartan and amlodipine are contraindicated in pregnancy and should not be used during breastfeeding without consulting a healthcare provider.
• Hypotension: valsartan and amlodipine can cause hypotension (low blood pressure), which can cause dizziness, lightheadedness, and fainting. People should rise slowly from a sitting or lying position and avoid activities that require mental alertness or coordination if they experience these symptoms.

Pregnancy / Lactation

Pregnancy consideration:

The drug is not safe during pregnancy. Discontinue the drug if pregnancy is achieved.

Breastfeeding warnings:

The drug is excreted in the breast milk. It shows adverse effects in breastfed infants.

Pregnancy category:

• Category A: well-controlled and satisfactory studies do not show risk to the fetus in the first/later trimester.      
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
• Category N: No data is available for the drug under this category.

Pharmacology

Pharmacology:

amlodipine is a calcium channel blocker that works by inhibiting the influx of calcium ions into smooth muscle cells, resulting in the relaxation of the smooth muscle and dilation of blood vessels. It leads to a decrease in peripheral vascular resistance, which lowers blood pressure. amlodipine also has cardioprotective effects, like reducing the workload on the heart and improving coronary blood flow.

valsartan is an angiotensin receptor blocker (ARB) that works by blocking the action of angiotensin II, a hormone that causes blood vessels to constrict and blood pressure to increase. valsartan explicitly blocks the angiotensin II type 1 receptor, leading to vasodilation and a reduction in blood pressure. valsartan also has some cardioprotective effects, such as reducing the workload on the heart and improving cardiac function.

Pharmacodynamics:

amlodipine is a calcium channel blocker that works by inhibiting the influx of calcium ions into smooth muscle cells, resulting in the relaxation of the smooth muscle and dilation of blood vessels. It leads to a decrease in peripheral vascular resistance, which lowers blood pressure. Amlodipine also has cardioprotective effects, such as reducing the workload on the heart and improving coronary blood flow.

valsartan is an angiotensin receptor blocker (ARB) that works by blocking the action of angiotensin II, a hormone that causes blood vessels to constrict and blood pressure to increase. valsartan explicitly blocks the angiotensin II type 1 receptor, which leads to vasodilation and a reduction in blood pressure. valsartan also has some cardioprotective effects, such as reducing the workload on the heart and improving cardiac function.

Pharmacokinetics:

The pharmacokinetics of amlodipine/valsartan are as follows

amlodipine:

• Absorption: amlodipine is rapidly absorbed after oral administration, with peak blood concentrations occurring 6-12 hours after a dose.
• Distribution: amlodipine is highly bound to plasma proteins (about 97%) and has a large volume of distribution (about 21 L/kg).
• Metabolism: amlodipine is extensively metabolized in the liver. It changes into inactive metabolites, with less than 10% of the drug excreted unchanged in urine.
• Elimination: amlodipine and its metabolites are mainly eliminated in the feces, with a small proportion excreted in the urine. The elimination half-life of amlodipine is about 35-50 hours, which means it takes several days for the drug to be eliminated from the body.

valsartan:

• Absorption: valsartan is well absorbed after oral administration, with peak blood concentrations occurring 2-4 hours after a dose.
• Distribution: valsartan is highly bound to plasma proteins (about 94-97%) and has a moderate volume of distribution (about 17 L/kg).
• Metabolism: valsartan is minimally metabolized in the liver, and most of the drug is excreted unchanged in the feces or urine.
• Elimination: valsartan has a terminal elimination half-life of about 9-14 hours, which means it is eliminated relatively quickly from the body.

Elimination/Excretion

The drug is excreted in urine

Adminstartion

Administration:

• amlodipine and valsartan should be taken with or without food but should be taken at the same time each day to maintain consistent blood levels of the drugs.
• The tablets should be swallowed with water and not crushed or chewed.
• amlodipine and valsartan should be taken as directed by a healthcare provider. Only change the dosage or frequency of the medication after consulting a healthcare provider.
• amlodipine and valsartan should be used regularly to obtain the maximum benefit of the medication.
• The duration of treatment with amlodipine and valsartan may vary depending on the individual patient’s condition. It is essential to continue taking the medication even if the patient feels well, as high blood pressure often has no symptoms.

Patient Information Leaflet

Patient information leaflet

Generic Name: amlodipine/valsartan

Pronounced: am-LOE-de-peen-val-SAR-tan

Why do we use amlodipine/valsartan?

amlodipine and valsartan are used to treat high blood pressure (hypertension). Hypertension is a common condition in which the blood pressure in the arteries is consistently elevated. Left untreated, it can lead to serious health problems like heart disease, stroke, kidney disease, and vision loss.