1.What is Amlodipine Besylate?
Definition
Amlodipine is the besylate salt of amlodipine, a drug belonging to a class of drugs known as dihydropyridine calcium channel blockers. Approved by the FDA in 1987, it has antihypertensive and antianginal effects. Dihydropyridine calcium channel blockers selectively act on myocardial and peripheral blood vessels, resulting in dilation of arteries.
Therefore, the drug is used for the treatment of hypertension and different types of angina.
Chemical & Physical features:
Chemical Structure:
Synonyms: Amlodipine besilate, Amdepin, Amlodin, Amdipin
Molecular weight: 567.1
Molecular formula: C26H31ClN2O8S
CAS number: 111470-99-6
DrugBank Accession number: DB00381
IUPAC Name: Benzenesulfonic acid;3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
Form: White crystalline powder
Solubility: Slightly soluble in water, sparingly soluble in ethanol
Brand names:
Amlobenz, Lotrel, Norvasc, Prestalia,
2.Amlodipine Besylate forms and specifications
Amlodipine Base powder 99%
The formula is available at a purity of 99.64%. It is a long-acting calcium channel blocker used for hypertension and the relief of chest pain. It is insoluble in water and can be stored for 3 years in powder form at a temperature of -20°C.
Amlodipine Besylate API powder 99%
Pfizer is one of the originators of this product and supplies it in the form of a white powder with a solubility of >20 mg/mL. It is sold in a glass bottle of either 10 or 50 mg and used to treat hypertension and angina pectoris.
Amlodipine Maleate API powder 99%
Depending on the weight, it is available at different costs. It is stored in a closed container at low temperature and kept away from moisture, heat and light. Being suitable for adults, it is used for treating hypertension, chronic stable angina and variant angina.
The product has a shelf life of 2 years.
Amlodipine besylate 10mg tablets （5mg)
Amlodipine besylate tablets are available in multiple strengths under the brand name NORVASC, including 2.5 mg, 5 mg, and 10 mg. The 5 mg tablets are white, octagon-shaped tablets with NORVASC and 5 engraved on one side, while the 10 mg tablets are white and round with NORVASC and 10 engraved on one side.
These tablets are stored in air-tight, light-resistant containers at 15-30°C.
3.Amlodipine besylate vs. amlodipine
Amlodipine besylate is basically amlodipine combined with another salt to improve drug delivery. The former is used on animals as well, while the latter is only used on humans.
4.Amlodipine Besylate vs. Amlodipine Maleate
Amlodipine maleate is also another salt combined with amlodipine. There is no difference in the efficacy of both. However, amlodipine besylate has a higher incidence of adverse effects.
5.Amlodipine vs lisinopril
Lisinopril is an ACE inhibitor used in the treatment of hypertension and heart failure. According to a study, amlodipine controls blood pressure better than lisinopril, which showed the best results during the daytime.
6.Mechanism of action of Amlodipine Besylate
The influx of calcium ions is needed for the contractility of cardiac muscle cells and vascular smooth muscle cells. The besylate salt of amlodipine is a dihydropyridine calcium antagonist. Therefore it inhibits the influx of calcium ions into these cells by blocking the calcium channel. The effect is greater on vascular smooth muscle cells than cardiac muscle cells, and consequently, peripheral vascular resistance and blood pressure are decreased.
7.Amlodipine Besylate manufacturing process
Phtaloyl amlodipine is the starting material used by the manufacturer to prepare amlodipine and its salts. It is processed with aqueous solutions of primary amines in water-immiscible solvents such as methylene chloride, ethylene dichloride, chloroform ethyl acetate, and toluene. This is known as the deprotection reaction. Afterward, it is treated with benzene sulfonic acid, and the final product is obtained.
8.Amlodipine Besylate uses
Treat high blood pressure
By selectively blocking the calcium ion influx across cell membranes, it dilates the main coronary and systemic arteries. It leads to a reduction in peripheral vascular resistance, which in turn decreases blood pressure.
Chest pain
The drug is used to treat angina, which is chest pain. It dilates peripheral arterioles, reducing total peripheral resistance (afterload) against which the heart works. This leads to a decrease in the myocardial oxygen demand and alleviates exertional angina.
The arteriolar dilation also increases oxygen delivery to the heart in patients experiencing a coronary artery spasm, making the drug valuable in the case of Prinzmetal's or variant angina.
9.Amlodipine Besylate dosage
The oral antihypertensive dose for adults is 5 mg once daily, with the maximum being 10 mg daily. For older patients, it is started at 2.5 mg once daily.
With regards to angina and coronary artery disease, the dose is 5-10 mg once daily.
10.Amlodipine Besylate side effects
The side effects include swelling in the legs and ankles, stomachache and nausea, dizziness, flushing, arrhythmias, palpitations, muscle rigidity, and tremors. However, these are usually mild in nature.
11.Amlodipine Besylate API price
$130.6/kg
12.Amlodipine Besylate API manufacturers in China
Below are some manufacturers who are professional in making API ingredients.
Jiangsu Simcere Pharmaceutical Co., Ltd
The company was established in March 1995. The factory is located in Simcere Hainan, and the main sales markets are North America, Central/South America, Western Europe, Eastern Europe, Australia, Asia, Middle East, and Africa.
Category: Finished Dosage > Cardiovascular Preparations
Description: White round tablet
Strength: 2.5mg
Contact Details: Liu Huan, Tel: +86-25-85566666
Changzhou Ruiming Pharmaceuticals Co., Ltd.
Established in 2003, with Asia as its main sales market, the company actively builds connections with China Pharmaceutical University, the University of Shanghai for Science and Technology, etc. Two of its products, propafenone hydrochloride and felodipine, also passed the Chinese GMP inspection in July 2009.
Category: Active Pharmaceutical Ingredients > Antibiotics > Other Antibiotics
CAS Number: 111470-99-6
Standards: In-house Standards
Contact Details: Ms Xia, Tel: +86-519-85095533
TAIZHOU SUNZONE PHARMACEUTICAL LIMITED
The company's main sales markets are Central/South America, Eastern Europe, Asia, Middle East, and Africa, and it specializes in antibiotics, biological drugs, medical instruments, pharmaceutical machinery, etc. It ships to over 30 countries.
Contact Details: Sophie Hong, Tel: +86-576-81816607
China Chinopharma Ltd.
Category: Bio Products > Technology Service > Biocatalysts
Contact Details: Wu Alice, Tel: +86-21-33592000-256
The company has introduced many good quality APIs and exports products to several countries around the world.
Nanjing Hicin Pharmaceutical Co., Ltd
Category: Active Pharmaceutical Ingredients
Contact Details: Chen Hui, Tel: +86-25-83222911
With a staff of more than 300 people, and sales markets in North America, Central/South America, Western Europe, Eastern Europe, Australia, Asia, the Middle East, and Africa, the company is known for the production of raw materials, intermediates, and finished products, which include both preparations and APIs.
13.FAQ:
What’s the market size of Amlodipine Besylate?
With the rising number of cases of hypertension, the market size is increasing in the Asia Pacific region and is expected to increase drastically between 2021 and 2026.
Is amlodipine a beta-blocker?
No, it is not. However, it is used in combination with beta-blockers for hypertensive patients.
Is amlodipine an ace inhibitor?
No, it is not. However, it is used in combination with ace inhibitors for hypertensive patients.
References:
1. https://pubchem.ncbi.nlm.nih.gov/compound/Amlodipine-besylate
2. https://go.drugbank.com/drugs/DB00381
3. https://www.rxlist.com/norvasc-drug.htm#description
4. https://patents.google.com/patent/WO2005023769A1/en
5. http://www.differencebetween.net/science/health/difference-between-amlodipine-and-amlodipine-besylate/
6. https://journals.lww.com/jhypertension/Abstract/2018/10003/A18046_Levamlodipine_Maleate_or_AmlodipineBesylate.1057.aspx
7. https://www.pharmacompass.com/price/amlodipine-besylate
8. https://www.pharmasources.com
9. https://www.marketwatch.com/press-release/amlodipine-besylate-market-size-2021-future-trends-share-competitive-analysis-and-growth-in-future-global-analysis-by-forecast-to-2026-2021-06-14
10. https://www.medicines.org.uk/emc/product/5701/smpc#gref
11. https://www.selleckchem.com/products/Amlodipine(Norvasc).html
12. https://www.sigmaaldrich.com/PK/en/product/sigma/a5605
13. https://julong.en.made-in-china.com/product/BwothQxuOnrM/China-Factory-Supply-99-Purity-CAS-88150-47-4-Amlodipine-Maleate.html
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