Monday, March 18, 2013

AMLODIPINE


Amlodipine is a longacting calcium channel blocker,  it used as an antihypertensive and in the treatment of angina pectoris. Amlodipine  relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance thereby reducing blood pressure; in angina, Amlodipine increases blood flow to the heart muscle.


(RS) -3-ethyl 5-methyl  2-[(2-aminoethoxy)methyl]-4- (2-chlorophenyl) -6-methyl-1, 4-dihydropyridine-3, 5-dicarboxylate

use
Amlodipine taken orally. It is usually taken once a day. To help you remember to take amlodipine, take it around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take amlodipine exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor will probably start you on a low dose of amlodipine and gradually increase your dose.
Amlodipine controls high blood pressure and chest pain  but does not cure them. Continue to take amlodipine even if you feel well. Do not stop taking amlodipine without talking to your doctor.

Dosage 
Hypertension
Adults
 Initial dose is 5 mg daily (max, 10 mg daily). 2.5 mg daily when adding amlodipine to other antihypertensive therapy.
Children 6 to 17 years  -   2.5 to 5 mg once daily.

CAD
Adults  -   5 to 10 mg once daily.
Chronic stable or vasospastic angina
Adults   -    5 to 10 mg once daily.
Elderly -   Start with 5 mg once daily.

Hepatic Impairment
Hypertension
Initially 2.5 mg every day.

Chronic stable or vasospastic angina
Start with 5 mg once daily.
Elderly  -  Initially 2.5 mg every day.

MECHANISM OF ACTION
Amlodipine is a dihydropyridine calcium antagonist that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects can be detected in vitro, but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound , and its kinetic interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect.
Amlodipine is a peripheral arterial vasodilator acts directly on vascular  muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
Amlodipine does also act as a functional inhibitor of acid sphingomyelinase.
The precise mechanisms by which amlodipine relieves angina have not been fully delineated, but are thought to include:
Exertional angina
In patients with exertional angina, amlodipine reduces the total peripheral resistance against which the heart works and reduces the rate pressure product, so lowers myocardial oxygen demand, at any given level of exercise.
Vasospastic angina
Amlodipine has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium, epinephrine, serotonin, and thromboxane A2 analog in experimental animal models and in human coronary vessels in vitro. This inhibition of coronary spasm is responsible for the effectiveness of amlodipine in vasospastic angina.

Amlodipine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
swelling of the hands, feet, ankles, or lower legs
headache   ,      upset stomach      ,      stomach pain     ,      dizziness or lightheadedness
drowsiness    ,      excessive tiredness    ,      flushing (feeling of warmth)
Some side effects can be serious. The following symptoms are uncommon, but if you experience any of them, call your doctor immediately:
more frequent or more severe chest pain
rapid, pounding, or irregular heartbeat
fainting
Administration's (FDA) MedWatch Adverse Event Reporting program online [at http:// If you experience a serious side effect, you or your doctor may send a report to the Food and Drug www.fda.gov/Safety/MedWatch] or by phone [1-800-332-1088].
BRANDS
Aforbes    by Merck Inc.               Philippines
Agen       by Zentiva in the            Czech Republic
Aken       by Kendrick Farmaceutica     in Mexico
Amcard in Bangladesh by Apex Pharma Ltd
Amdepin by Cadila Pharmaceuticals in India
Amdipin in Colombia by Laboratorios Lafrancol
Amlodine by Dainippon Sumitomo Pharmaceuticals in Japan, and in Philippines by Westfield Pharmaceuticals, a division of InnoGen
Amlodipine 5 in Indonesia by PT KALBE FARMA Tbk, Bekasi
Amlong in India by Micro Labs
Amlopin by Lek
Amlopin in Bangladesh by The Acme Laboratories Ltd
Amlopine in Thailand by Berlin (Thailand) Pharmaceutical Industry Co Ltd
Amlostin in the United Kingdom by Discovery Pharmaceuticals
Amlosun in Bangladesh by Sun Pharmaceutical (Bangladesh) Ltd
Amlovas in India by Macleods Pharmaceticals Ltd
Amlovasc in the United Kingdom by Dr. Reddy's Laboratories
Amlozek in Poland by Adamed
Asomex by Emcure Pharmaceuticals India
Atecard-AM in India by Alembic Ltd
Camlodin in Bangladesh by Square Pharmaceuticals Ltd
Dailyvasc by Xeno Pharmaceuticals
Hipril is a combination of lisinopril with amlodipine (5 mg each) in India
Istin in the United Kingdom and Ireland
Lama in India by Stadmed Private Limited, Kolkata
Lodopin in Pakistan by Merck Pakistan
Lopin in Bangladesh by Edruc Ltd
Nelod in Bangladesh by The Kemiko Pharmaceuticals Ltd
Nopidin in Bangladesh by Ad-din Pharmaceuticals Ltd
Norvasc by Pfizer in North America, some European countries, China, Japan, and Pakistan
Norvasc, Perivasc and Nordip in Australia
Pharex Amlodipine in the Philippines by PHAREX HealthCorp
Tenox b


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