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Q. Will single-pill, fixed-dose combinations lead to better BP control?
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Atorvastatin is a synthetic lipid-lowering agent. Atorvastatin is an inhibitor of 3-hydroxy-3-methyglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis. Atorvastatin calcium is [R-(R*,R*)]-2-(4-fluorophenyl)- ß-d--dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino) carbonyl]-1H-pyrrole-1-heptanoic acid, calcium salt (2:1) trihydrate. The empirical formula of atorvastatin calcium is (C33H34FN2O5)2Ca.3H2O and its molecular weight is 1209.42.

 

 

Amlodipine besilate is a dihydropyridine calcium channel blocker. It is a peripheral and coronary vasodilator but has little or no effect on cardiac conduction and negative inotropic activity is rarely seen at therapeutic doses. The molecular formula of amlodipine is C20H25ClN2O.C6H6O3S with a molecular weight of 567.1. On the other hand, lisinopril is an angiotensin converting enzyme inhibitor resulting in inhibition of the renin-angiotensin-aldosterone system. It is also a vasodilator and reduces peripheral vascular resistance. The molecular formula of lisinopril is C21H31N3O5.2H2O with a molecular weight of 441.5.

 

The drug is a fixed dose combination of two lipid-lowering agents. Ezetimibe and Atorvastatin. Ezetimibe is a selective cholesterol absorption inhibitor. The chemical name of zetimibe is 1-(4- flouoropheny)-3(R)-[3-(4-fluorophenyl)-3-hydroxyphenyl)-2-azetidinone. The empirical formula is C24H21F2NO3. Its molecular weight is 409.4. The chemical structure of ezetimibe is as follows :- Atorvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMGCoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.

 

Losartan potassium, the first of a new class of antihypertensives, is an angiotensin II receptor (AT1) antagonist. Losartan potassium, a nonpeptide molecule, is chemically described as 2- butyl-4- chloro -1- [p - (0-1 H - tetrazol - 5-yl phenyl)-benzyl] imidazole -5- methanol monopotassium salt. Its empirical formula is C22H22Cl K N6O and its molecular weight is 461.01.

 

 

 

Amlodipine besilate is a dihydropyridine calcium channel blocker with an empirical formula of C20H25ClN2O5.C6H6O3S and a molecular weight of 567.1. On the other hand, losartan potassium is a non-peptide angiotensin II receptor (AT I) antagonist with an empirical formula of C22H22ClKN6O and a molecular weight of 461.01

Losacar-H is a fixed dose combination of an angiotensin II receptor (type AT1) antagonist, losartan potassium, and a diuretic, hydrochlorothiazide. Losartan potassium, a non-peptide molecule, is chemically described as 2-butyl-4-chloro-1-[p-(o-1H-tetrazol-5-yl phenyl)benzyl]imidazole-5-methanol mono-potassium salt. Its empirical formula is C22H22ClKN6O, and its molecular weight is 461.01. On the other hand, hydrochlorothiazide is 6-chloro-3,4-dihydro-2H-1,24- benzothiadiazine-7-sulfonamide 1,1-dioxide. Its empirical formula is C7H8ClN3O4S2 and its molecular weight is 297.74.

 

 

NEBULA tablets contain Nebivolol hydrochloride which is a cardio-selective beta- blocker and is a recemante of two enantiomers: SRRR-nebivolol (or d-nebivolol) which is responsible for its competitive and selective beta-receptor antagonist activity and RSSS - nebivolol (or l-nebivolol) which is resposible for its mild vacodilating properties due to an interaction with the L-arginine / nitric oxide pathway. single and repeated doses of nebivolol deduce heart rate and blood pressure at rest and during exercise, both in normotensive subjects and in hypertensive patinets.

 

 

 

 

 

 

Solotrate-SR tablet is an oral extended-release formulation of isosorbide mononitrate, the major active metabolite of isosorbide dinitrate ; most of the clinical activity of the dinitrate is attributable to the mononitrate. The principal pharmacological action of isosorbide mononitrate and all organic nitrates in general is relaxation of vascular smooth muscle, producing dilatation of peripheral arteries and veins, especially the latter. Dilatation of the veins promotes peripheral
pooling of blood, decreases venous return to the heart, thereby reducing left ventricular end-diastolic pressure and pulmonary capillary wedge pressure (preload). Arteriolar relaxation reduces systemic vascular resistance, and systolic arterial pressure and mean arterial pressure (afterload). Dilatation of the coronary arteries also occurs.

 

TORGET Tablets contain torsemide which is a diuretic of the pyridine-sulfonylurea class. Its chemical name is 1-isopropyl- 3-[(4-m-toluidino-3-pyridyl)sulfonyl]urea. Its empirical formula is C16H20N4O3S, its pKa is 7.1, and its molecular weight is 348.43.

 

 

 
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