Heart health is a major concern today as more people are becoming obese and fewer people exercise enough to accommodate for higher daily caloric intake. Coronary heart disease, the most common type of heart disease in adults, occurs when plaque (a waxy substance) collects against the inner walls of the coronary arteries. The coronary arteries are what carry oxygen-rich blood to the heart.

Two serious problems, angina and hypertension, are warning signs of coronary heart disease and a possible heart attack. Hypertension is the term doctors use to describe high blood pressure, which measures the force (as the heart pumps blood through the body) against the walls of the arteries; and angina is the term for chest pains caused when heart muscles don’t receive enough oxygen-rich blood. Amlodipine besylate is a long-acting compound used as a treatment for angina and as an antihypertensive.

Amlodipine besylate is a calcium channel blocker that can reduce blood pressure by relaxing the smooth muscle

in the arterial wall. In angina cases, this relaxation can help to increase blood flow to the heart muscles.

 

What amlodipine besylate does, and medications that contain it

Amlodipine besylate works by inhibiting the transmembrane influx of

calcium ions in cardiac muscle and vascular smooth muscle. The flexibility of these muscles is dependent upon extracellular calcium ions and how they move through ion channels. Amlodipine besylate selectively inhibits the in-flow of calcium ion, mainly on the vascular smooth muscle. This causes a reduction in vascular resistance which in turn reduces blood pressure.

Several medications utilize amlodipine besylate as an active ingredient, including Caduet and Norvasc, and three combination drugs: Azor, Exforge and Lotrel.

 

Help manage hypertension and angina

Amlodipine can be used to prevent chest pains, increasing the ability to exercise and decreasing angina attacks. Because it is slow-flowing and long-acting, it cannot treat chest pain or high blood pressure attacks. Instead, it reduces the risk of attacks by treating the symptoms. Amlodipine besylate is used alone and in combination of other antihypertensives to manage hypertension. It is the preferred method of therapy in patients with higher risks of developing coronary artery disease (CAD).

Hypertension has no symptoms, which means people who are not monitored can develop kidney problems and heart disease without realizing they have high blood pressure. People who are obese, have diabetes, have a high sodium intake, smoke, are African American, are stressed, drink too much alcohol or have a family history of high blood pressure are the most at-risk. Many aging adults see higher blood pressure as their blood vessels stiffen with age. The bottom line is that high blood pressure significantly increases the possibility of having a heart attack or heart failure, a stroke, kidney disease or an early death. That is why is it so important to talk to your doctor about symptoms and treatment options. Calcium-channel blocking agents, such as amlodipine besylate, are a preferred initial therapy for patients with hypertension, especially those with coexisting angina, geriatric patients with isolated systolic hypertension and patients with diabetes.

Angina is commonly caused by plaque buildup. Plaque buildup in the arteries is detrimental no matter what type of plaque is present. Hard plaque causes arteries to become stiff and narrow, limiting blood flow. Other plaque is softer and can rupture, causing blood clots. A blood clot can completely block an artery. Both types of plaque can cause angina and lead to a heart attack if they go untreated. Angina affects men and women equally.

There are four types of angina, each with different treatments and symptoms.

• Stable angina is the most common form and occurs when a heart works harder than usual. This type of angina has a pattern, meaning a pattern is formed based on what factors trigger it, how severe the attack is and how often the angina occurs. This is not a heart attack but can be indicative of a future heart attack. Pain usually subsides when medication is administered. Causes include overexertion, stress, smoking and overeating.

• Unstable angina does not follow a pattern and may occur more often (and more severely) than stable angina. This type of angina can be very serious, requires immediate medical treatment and is more often found in older adults. Heart attacks often follow unstable angina. Medication may not relieve unstable angina. Blood clots are the primary cause for unstable angina.

• Variant (or Prinzmetal’s) angina is more rare than the other types, accounting for approximately two our of every 100 cases. Spasms in a coronary artery cause variant angina, and it typically happens while a body is at rest, between midnight and early morning. It is also more often found in younger angina sufferers. Variant angina can be relieved with medication. Spasms can occur due to stress, smoking, use of cocaine, medications that restrict blood vessels and exposure to cold temperatures.

• Microvascular angina may not be treated with medication and can last longer than other types of angina. This type of angina is likely a symptom of coronary microvascular disease (MVD), a disease affecting the smallest coronary arteries in the heart. Microvascular angina is more typically found in women during menopause.

Amlodipine besylate can be used to manage variant angina and chronic stable angina, as calcium-channel blockers are the preferred treatment in those types of angina. It is also used in people with recent CAD.

 

Side effects of drugs containing amlodipine besylate

Most side effects of amlodipine besylate are minor and can include headache, dizziness, chest pain, weakness, jaundice and swollen feet/ankles and hands. If any side effects worsen, consult a physician. A doctor may conclude that persistent mild side effects are less of a risk than those posed by hypertension or angina.

Allergic reactions can be severe, so receive medical attention if the following occur: swelling of face, lips, tongue or throat; difficulty breathing; hives or fast or irregular heartbeat.

As drugs can affect each person differently, other side effects are possible. Do not judge whether a side effect is mild or severe without consulting a doctor. U.S. residents may report serious side effects to the FDA at 1-800-FDA-1088. Residents of Canada can report to Health Canada at 1-866-234-2345.

 

Precautions and risks associated with amlodipine besylate

It is hard to estimate how a new drug will affect a patient, so it is important to be cautious until the body is used to the drug and its effects. Always discuss any allergies with a doctor prior to starting a new drug regimen to decrease risks. Other factors may cause unwanted side effects, so discuss your medical history with your doctor before starting amlodipine besylate.

Also, take precautions for safety and never drive, operate heavy machinery the first time taking amlodipine besylate. And in some cases, amlodipine besylate may cause dizziness, so you should limit activities while taking it. Always give a doctor or dentist a complete list of medications before undergoing any surgical procedures.

Amlodipine besylate should be used only when needed, so discuss side effects and risks with your doctor if you are pregnant or breast-feeding, as it is unknown if amlodipine besylate passes into breast milk.

 

Inactive ingredients

Substances found in medications that do not (or are not intended to) treat symptoms or conditions are call inactive ingredients. Components that bind a pill together, colors, flavors and preservatives are all considered inactive ingredients. In tablets containing amlodipine besylate, these ingredients are magnesium stearate, dibasic calcium phosphate anhydrous, microcrystalline cellulose and sodium starch glycolate.

An inactive ingredient search database is available from the FDA at www.accessdata.fda.gov/scripts/cder/iig/index.cfm.

 

Dosage

Consult a doctor for the recommended dosage of any medication. The following information is the typical dosage in studies and experiments. Do not take more amlodipine besylate than directed as overdoses can cause death. Dosages should start low and be adjusted according to the patient’s response over the course of seven to 14 days.

The range of dosage for adults with CAD and chronic stable angina is 5 mg-10 mg once per day for NORVASC, according to information gained through double-blind, placebo-controlled, randomized studies involving patients (http://www.rxlist.com/norvasc-drug/clinical-pharmacology.htm#CS).

Elderly patients should start on 2.5 mg once per day for hypertension. Children should also start at 2.5 mg once per day and can increase to 5 mg per day.

Classification information of amlodipine besylate

Amlodipine besylate is in the class of dihydropyridines.

CAS Number: 111470-99-6

VA Class: CV200

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