Coram, is a dihydropyridine derivative, slightly soluble in water and sparingly soluble in ethanol. Amlodipine (Coram) is a calcium ion flux inhibitor (slow channel blocker or calcium ion antagonist inhibits the transmembrane influx of calcium ions into cardiac and smooth muscle). The mechanism of the antihypertensive action of Amlodipine is due to direct relaxant effect on vascular smooth muscle.
The precise mechanism by which Amlodipine relives angina has not been fully determined but Amlodipine reduces total ischemic burden by the following actions
Amlodipine dilates peripheral arterioles thus, reduces the total peripheral resistance (after load) against which the heart works. Since there is no associated reflex tachycardia, this unloading of the heart reduces myocardial energy consumption and oxygen requirements and probably accounts for the effectiveness of amlodipine in myocardial ischemic regions. This increases myocardial oxygen delivery in patients with coronary artery spasm (Prinzmetal’s or variant angina)
After oral administration of therapeutic doses, Coram is well absoebed with peak blood levels attaining between 6-12 hours postdose. The terminal plasma elimination half-life is about 35-50 hours and is consistent with once daily dosing. Steady state plasma levels are reached after 7-8 days of consecutive dosing. Amlodipine is extensively metabolized by the liver to inactive metabolites excreted in the urine.
In patients with hypertension once daily dosing provides clinically significant reduction of blood pressure in both the supine and standing positions throughout the 24 hours interval.
In patients with angina, once daily administration of amlodipine increases total exercise time and decreases both angina attack frequency and nitroglcerine tablet consumption. Coram (Amlodipine) has not been associated with any adverse metabolic effects or changes in plasma lipids and is suitable for use in patients with asthma, diabetes and gout.
Amlodipine (Coram) is indicated for the first line treatment of hypertension and can be used as the sole agent to control blood pressure in the majority of patients. Patients not adequately controlled on a single antihypertensive agent may benefit from the addition of Amlodipine, which has been used in combination with thiazide diuretic, beta adrenoceptor blocking agent, or an angiotensin converting enzyme inhibitor.
Amlodipine (Coram) is indicated for the first line treatment of myocardial ischemia whether due to fixed obstruction (stable angina) and/ or vasoconstriction (prinzmetal’s or variant angina) of coronary vasculature.
Amlodipine may be used when the clinical presentation suggests a possible vasospastic/ vasoconstrictive component but where vasospasm / vasoconstriction has not been confirmed. Amlodipine may be used alone, as mono therapy or in combination with other anti-anginal drugs in patients with angina that is refractory to nitrates and/ or adequate doses of beta blocker.
Dosage and administration
For both hypertension and angina, the usual initial dose is 5mg amlodipine, once daily which may be increased to a maximum dose of 10mg depending on the individual patient’s response. No dose adjustment of amlodipine is required upon concomitant administration of thiazide diuretics, beta blockers and angiotensin converting enzyme inhibitor.
- Generally: Edema in ankle, headache, dizziness, flushed and feeling hot, fatigue, urticarial, itching, dyspepsia, stomachaches, nausea
- Circulation: Excessive hypotension, palpitation, chest pain, extrasystole
- Musculoskeletal: Arthragia, muscular pain
- CNS: Sleep disorders, cramps
- Respiration: Dyspnea