we wish to express our indebtedness to our faculty, Dr.Bidyut, Chairman, Department of Pharmacy, Stamford University of Bangladesh; for his invaluable suggestions, continued encouragement and unfailing enthusiasm throughout the process of completing this report. We hope that finding of this report will provide useful institutional information about “AMLODIPINE” drug and this experience will help us in our pharmacy studies……..
Amlodipine (Norvasc (Pfizer) and generics) (as besylate, mesylate or maleate) is a long-acting calcium channel blocker (dihydropyridine (DHP) class) used as an anti-hypertensive and in the treatment of angina. Like other calcium channel blockers, amlodipine acts by relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance and hence reducing blood pressure; in angina it increases blood flow to the heart muscle (although DHP-class calcium channel blockers are more selective for arteries than myocardium, as the cardiac calcium channels are not of the dihydropyridine-type).
Systematic (IUPAC) name
(RS)-3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate.
Amlodipine is a chiral calcium antagonist, currently on the market and in therapeutic use as a racemate [1:1 mixture of (R)-(+)- and (S)-(–)-amlodipine]] A method for the semi-preparative chromatographic purification of the enantiomers (S)-(–)-amlodipine and (R)-(+)-amlodipine has been reported.
Enantiomer of amlodipine
NORVASC® is the besylate salt of amlodipine, a long-acting calcium channel blocker. Amlodipine besylate is chemically described as 3-Ethyl-5-methyl (±)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate, monobenzenesulphonate. Its empirical formula is C 20 H 25 CIN 2 O 5 •C 6 H 6 O 3 S, and its structural formula is:
Amlodipine besylate is a white crystalline powder with a molecular weight of 567.1. It is slightly soluble in water and sparingly soluble in ethanol. NORVASC (amlodipine besylate) tablets are formulated as white tablets equivalent to 2.5, 5 and 10 mg of amlodipine for oral administration. In addition to the active ingredient, amlodipine besylate, each tablet contains the following inactive ingredients: microcrystalline cellulose, dibasic calcium phosphate anhydrous, sodium starch glycolate, and magnesium stearate.
Patent Information and Present Market Condition:
* Pfizer patent protection on Norvasc lasted until 2007.Total patent expiration occurred later in 2007.A number of generic versions are available. * In the United Kingdom tablets of amlodipine from different supplies may contain different salts. The strength of the tablets is expressed in terms of amlodipine base, i.e., without the salt. * The efficacy and tolerability of a fixed dose combination of amlodipine 5mg and perindopril 4mg, an angiotensin converting enzyme (ACE) inhibitor, have recently been confirmed in a prospective, observational multicenter trial of 1250 hypertensive patients.
BRABD NAMES,MANUFACTURES AND DOSAE FORMS AVAILABLE IN B ANGLADESH FOR AMLODIPINE
Brand Name | Contains| Dosage Form | Manufacturer| Price(Tk.)| AMDIN | Amlodipine 5mg & 10mg/tablet| Tablet| Alco Pharma Ltd.| 5mg x 50s pack: 150.00 MRP ; 10mg x 30s pack: 150.00 MRP| AMDOCAL| Amlodipine 5mg & 10mg/tablet| Tablet| Beximco Pharmaceuticals Ltd.| 5mg x 100s pack: 500.00 IP; 10mg x 60s pack: 420.00 IP| AMDOPER | Amlodipine 5mg/tablet| Tablet| Hallmark Pharmaceuticals Ltd.| 5mg x 30s pack: 90.00 MRP| AMDOPIN | Amlodipine 5mg/tablet| Tablet| Ziska Pharmaceuticals Ltd.| 5mg x 50s pack: 175.00 MRP| AMLO...