High Quality EP/USP standard Amlodipine Besylate CAS 111470-99-6 with best price

Amlodipine Besylate More Info

Amlodipine besylate, commonly known by the brand name Norvasc, is a long-acting calcium channel blocker used to treat hypertension (high blood pressure) and angina (chest pain). It works by relaxing the arteries and increasing their diameter, a process known as vasodilation.

Mechanism of Action

Amlodipine is a dihydropyridine calcium channel blocker that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. It primarily affects vascular smooth muscle cells, causing vasodilation and reducing peripheral vascular resistance, which lowers blood pressure. Amlodipine can also prevent excessive constriction in the coronary arteries.
The mechanisms by which amlodipine relieves angina are:
Stable angina: Amlodipine reduces the total peripheral resistance (afterload) against which the heart works, reducing myocardial oxygen demand.
Variant angina: Amlodipine blocks spasm of the coronary arteries and restores blood flow.

Applications

Amlodipine besylate is primarily used to treat:
Hypertension (high blood pressure)
Chronic stable angina (chest pain)
Vasospastic angina (Prinzmetal's angina)
It can be used alone or in combination with other medications to manage these conditions. A fixed-dose combination of amlodipine and perindopril, an angiotensin converting enzyme inhibitor, is also available.

Routes of Administration

Amlodipine besylate is administered orally as tablets

Safety and Side Effects

The most common side effects of amlodipine include:
Edema (swelling of the legs and ankles)
Headache
Fatigue
Dizziness
Flushing (hot or warm feeling in the face)
Stomach pain and nausea
Less common side effects include1:
Acid or sour stomach
Belching
Feeling of warmth
Heartburn
Indigestion
Lack or loss of strength
Muscle cramps
Redness of the face, neck, arms, and occasionally, upper chest
Sleepiness or unusual drowsiness
Stomach discomfort, upset, or pain
Serious side effects are rare but require immediate medical attention:
Increased angina or heart attack
Decreased blood pressure (hypotension)
Rapid, pounding, or irregular heartbeat
Fainting
Severe stomach pain, with or without diarrhea, feeling sick and being sick (nausea and vomiting) – these can be signs of pancreatitis
Yellowing of the skin or eyes – this can be a sign of liver problems.

Pharmacokinetics

Amlodipine is well absorbed after oral administration.
Bioavailability: Amlodipine has a mean oral bioavailability of around 60%.
Half-life: The half-life of amlodipine is about 30 to 50 hours, and steady-state plasma concentrations are achieved after 7 to 8 days of daily dosing.
Protein Binding: In the blood, amlodipine has high plasma protein binding of 97.5%.
Metabolism: Amlodipine is slowly metabolized in the liver by CYP3A4 into inactive pyridine metabolites.
Excretion: Renal elimination is the major route of excretion, with about 60% of an administered dose recovered in urine, largely as inactive pyridine metabolites. Approximately 20-25% of the drug is excreted in the feces.

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For ready stock samples, they are usually shipped within 3 working days after payment received.
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For sample orders: 
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A full set of shipment documents as well as package photos can be provided in scan-copy and original, to help customers complete the customs clearance process.

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