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Amlodipine Besylate

Amlodipine Besylate structure

CAS No:
111470-99-6
Formula:
C20H25ClN2O5.C6H6O3S
Chemical Name:
Amlodipine Besylate
Synonyms:
Vazkor;3-Ethyl 5-Methyl 2-(2-Aminoethoxy)methyl-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate Benzenesulfonate 2-(2-Aminoethoxy)methyl-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic Acid 3-Ethyl 5-Methyl Ester Benzenesulfona;3-ethyl 5-Methyl 2-((2-aMinoethoxy)Methyl)-4-(2-chlorophenyl)-6-Methyl-1,4-dihydropyridine-3,5-dicarboxylate benzenesulfonate;AMlodipine bes;Amlodipine besilate (crystalline);2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester benzenesulfonate;raw material amlodipine besylate;Amlodipine Beaylate
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

White Crystalline SolidChEBI: The benzenesulfonate salt of amlodipine.Amlodipine (generic name Amlodipine Besylate) is a class of calcium channel blockers. One of the amlodipine product on the market is Norvasc®.Amlodipine functionalizes by the dilation of blood vessels and the improvement of blood flow, which lead to lowered blood pressure. Thereby, it is used to treat high bold pressure (hypertension).

Amlodipine benzenesulfonate is the benzenesulfonate salt of amlodipine. It has a role as a vasodilator agent, a calcium channel blocker and an antihypertensive agent. It contains an amlodipine.|A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.

Anilodipine besylate is a new, once-daily, dihydropyridine calcium antagonist useful in the treatment of hypertension and angina.

White Crystalline Solid

ChEBI: The benzenesulfonate salt of amlodipine.

Amlodipine Besylate Basic Attributes

Molecular Weight：

567.05

Exact Mass：

566.149

EC Number：

1312995-182-4

NSC Number：

758922

DSSTox ID：

DTXSID2043909

Color/Form：

white

ATC Code：

C09DB01|C09DX01|QC08CA01

HScode：

29333990

Characteristics

PSA：

163

XLogP3：

5.30950

Appearance：

white solid

Density：

1.227g/cm3

Melting Point：

199-201°C

Boiling Point：

527.2°C at 760 mmHg

Flash Point：

272.6ºC

Water Solubility：

Soluble in DMSO (20 mg/mL), water (10 mM), chloroform, ethanol (14 mg/mL), and methanol.

Storage Conditions：

Store at RT

Vapor Pressure：

3.34E-11mmHg at 25°C

PKA：

8.6

Collision Cross Section：

187.4 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Critical Temperature & Pressure：

2-8°C

Safety Information

wgk germany：

hazard class code：

safety instructions：

26-36

RTECS Number：

US7967700

Marks：

Storage features：

Room temperature

Precautionary statement(s)：

P201, P202, P264, P270, P281, P301+P310, P308+P313, P321, P330, P405, P501

Hazard Statements：

22-36/37/38-20/21/22

GHS Classification：

|Danger|H302 (97.08%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P273, P280, P301+P312, P302+P352, P304+P312, P304+P340, P305+P351+P338, P310, P312, P321, P330, P332+P313, P337+P313, P362, P391, P403+P233, P405, and P501|Aggregated GHS information provided by 171 companies from 24 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|H300 (100%): Fatal if swallowed [Danger Acute toxicity, oral]|P201, P202, P264, P270, P281, P301+P310, P308+P313, P321, P330, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501

Drug Information

Drug Indication：

Treatment of essential hypertension., , Amlodipine/Valsartan Mylan is indicated in adults whose blood pressure is not adequately controlled on amlodipine or valsartan monotherapy.,|Treatment of essential hypertension as substitution therapy in adult patients whose blood pressure is adequately controlled on the combination of amlodipine, valsartan and hydrochlorothiazide (HCT), taken either as three single-component formulations or as a dual-component and a single-component formulation.|Treatment of systemic arterial hypertension in cats.|Prevention of cardiovascular events, Treatment of dyslipidaemia, Treatment of hypertension, Treatment of ischemic coronary artery disorders|Treatment of hypertension|Treatment of essential hypertension|Treatment of elevated cholesterol, Treatment of hypertension, Treatment of ischemic coronary artery disorders|Prevention of cardiovascular events in hypertensive patients and diabetes mellitus type II patients with multiple risk factors for cardiovascular disease, Treatment of concomitant angina and dyslipidaemia, Treatment of concomitant hypertension and dyslipidaemia|Prevention of cardiovascular events in hypertensive patients and diabetes mellitus type II patients with multiple risk factors for cardiovascular disease, Treatment of concomitant angina and dyslipidaemia|Cardiovascular-event prophylaxis, Treatment of dyslipidaemia, Treatment of elevated cholesterol, Treatment of heart failure, Treatment of ischaemic coronary artery disorders, Treatment of vascular hypertensive disorders|Prevention of acute myocardial infarction, Prevention of atherosclerotic heart disease, Prevention of stroke, Treatment of essential hypertension, Treatment of heart failure, Treatment of Prinzmetal's angina|Prevention of cardiovascular events in hypertensive patients and diabetes mellitus type II patients with multiple risk factors for cardiovascular disease, Treatment of concomitant angina and dyslipidemia, Treatment of concomitant hypertension and dyslipidemia|Prevention of heart failure, Prevention of stroke, Treatment of acute myocardial infarction, Treatment of atherosclerotic heart disease, Treatment of heart failure, Treatment of Prinzmetal's angina|Treatment of arterial hypertension|Hypertension with dyslipidemia|Chronic stable angina pectoris, Treatment of hypertension|Essential hypertension|Prevention of atherosclerotic heart disease|Arterial hypertension

MeSH：

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)|A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)

MeSH Entry Terms：

Amlodipine

Amlodipine Besylate Use and Manufacturing

Uses

A dihydropyridine calcium channel blocker. Used as an antianginal and antihypertensive Angiotensin II inhibitor prodrug, antihypertensive Amlodipine besylate is a L-type calcium channel blocker which may be used for the treatment of angina pectoris and hypertension. Amlodipine also inhibits growth of human epidermoid carcinoma A431 cells and has antireproductive effects in male rats.L-type calcium channel blocker that displays antihypertensive properties. Inhibits Ca 2+ -induced co

A dihydropyridine calcium channel blocker. Used as an antianginal and antihypertensive

Angiotensin II inhibitor prodrug, antihypertensive

Use Classification：

Human drugs -> Amlodipine / Valsartan Mylan -> EMA Drug Category|Agents acting on the renin-angiotensin system -> Human pharmacotherapeutic group|Human drugs -> Dafiro HCT -> EMA Drug Category|Human drugs -> Exforge HCT -> EMA Drug Category|Veterinary drugs -> Lodipressin -> EMA Drug Category|Calcium channel blockers -> Veterinary pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Drug Function and Efficacy

Calcium channel blockers block calcium ions from entering myocardial and vascular smooth muscle cells across the membrane. The mechanism of antihypertensive effect is to directly relax vascular smooth muscle. By dilating peripheral arterioles and coronary arteries, reducing total peripheral vascular resistance, relieving coronary artery spasm, reducing cardiac afterload, reducing cardiac energy consumption and oxygen demand, angina pectoris can be relieved.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Acetylcysteine effervescent tablets
Ingredients	Amlodipine besylate. Molecular weight: C20H25N2O5Cl·C6H6O3S
Indication	In vitro study data show that amlodipine does not affect the binding of digoxin, phenytoin, warfarin or indomethacin to plasma proteins. Effects of other drugs on this product Cimetidine: Combination with cimetidine does not change the pharmacokinetics of amlodipine. Grapefruit juice: 20 healthy volunteers took 240ml grapefruit juice and a dose of 10mg amlodipine at the same time, and no significant effect on the pharmacokinetics of amlodipine was found. Aluminum/magnesium (antacids): Taking aluminum/magnesium antacids and a single dose of amlodipine at the same time did not have a significant effect on the pharmacokinetics of amlodipine. Sildenafil: A single dose of 100mg sildenafil (Viagra) did not affect the pharmacokinetics of amlodipine in patients with essential hypertension.
Specifications	0.6g

Amlodipine Besylate Dispersible Tablets
Ingredients	Amlodipine besylate. Chemical name: 3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate
Indication	This product is safe when used in combination with the following drugs: thiazide diuretics, а-adrenergic receptor blockers, β-adrenergic receptor blockers, angiotensin converting enzyme inhibitors, long-acting nitrates, sublingual nitroglycerin, nonsteroidal anti-inflammatory drugs, antibiotics and oral hypoglycemic drugs. In vitro study data using human plasma showed that this product does not affect the plasma protein binding rate of digoxin, phenytoin sodium, warfarin or indomethacin. Effects of other drugs on amlodipine: Cimetidine: Co-administration with cimetidine does not change the pharmacokinetics of amlodipine. Grapefruit juice: 20 healthy volunteers took grapefruit juice and 10 mg of amlodipine at the same time, and no significant effect on the pharmacokinetics of amlodipine was observed. Aluminum/magnesium (antacids): Taking aluminum/magnesium antacids and a single dose of amlodipine at the same time,
Specifications	5mg (calculated as amlodipine)
Manufacturer	Guangzhou Yipinhong Pharmaceutical Co., Ltd.

Amlodipine Besylate Tablets
Ingredients	The main ingredients of this product are: Amlodipine Besylate Tablets.
Indication	Cimetidine, grapefruit juice, acidogens: The pharmacokinetics of this product are not changed when used together. Atorvastatin, digoxin, ethanol: This product does not affect their pharmacokinetics. Sildenafil: A single dose of sildenafil (Viagra) in patients with essential hypertension has no effect on the pharmacokinetics of this product. The two drugs produce an independent antihypertensive effect when used together. Warfarin: This product does not change the prothrombin action time of warfarin. Digoxin, phenytoin and warfarin: The combination with this product has no effect on the plasma protein binding rate. Anesthetics: Inhaled hydrocarbons combined with this product can cause hypotension. Nonsteroidal anti-inflammatory drugs: Indomethacin in particular can weaken the antihypertensive effect of this product. -Blockers: The combination with this product is well tolerated, but it can cause excessive hypotension and rarely aggravate heart failure. Estrogen: The combination can cause fluid retention and increase blood pressure. Sulfinpyrazone: The combination can increase the protein binding rate of this product and produce changes in blood drug concentration. Lithium: Co-administration may cause neurotoxicity, nausea, vomiting, diarrhea, ataxia, tremor and/or numbness, so be cautious. Sympathomimetic amines: May weaken the antihypertensive effect of this product. Sublingual nitroglycerin and long-acting nitrate preparations: Co-administration with this product may enhance the anti-anginal effect. Although rebound effects have not been reported, the dosage should be gradually reduced under the guidance of a doctor when the drug is discontinued. Thiazide diuretics, ACEI, digoxin, warfarin, antibiotics and oral hypoglycemic drugs: Can be safely used with this product.
Specifications	5mg (calculated as amlodipine)
Manufacturer	Liaoning Kangboshi Pharmaceutical Co., Ltd.

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