|Each Amlodipine Ultra Medica tablet contains :
Amlodipine besylate equivalent to Amlodipine 2.5 mg.
Amlodipine besylate equivalent to Amlodipine 5 mg.
Amlodipine besylate equivalent to Amlodipine 10 mg.
|Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle.
Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells.
Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.
The precise mechanisms by which amlodipine relieves angina have not been fully delineated, but are thought to include the following:
Exertional Angina : In patients with exertional angina, amlodipine reduces the total peripheral resistance (afterload) against which the heart works and reduces the rate pressure product, and thus 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.
This inhibition of coronary spasm is responsible for the effectiveness of amlodipine in vasospastic
(Prinzmetal’s or variant) angina.
|• Hypertension Amlodipine is indicated for the treatment of hypertension. It may be used
alone or in combination with other antihypertensive agents.
• Chronic Stable Angina : Amlodipine is indicated for the symptomatic treatment of chronic stable angina. Amlodipine may be used alone or in combination with other antianginal agents.
• Vasospastic Angina (Prinzmetal’s or Variant Angina) : Amlodipine is indicated for the treatment of confirmed or suspected vasospastic angina. Amlodipine may be used as monotherapy or in combination with other antianginal agents.
• Angiographically Documented CAD In patients with recently documented CAD by angiography and without heart failure or an ejection fraction <40%, amlodipine is indicated to reduce the risk of hospitalization due to angina and to reduce the risk of a coronary revascularization procedure.
|In general, treatment with amlodipine was well-tolerated at doses up to 10 mg daily. Most adverse reactions reported during therapy with amlodipine were of mild severity: Headache, Edema, Dizziness, Flushing, Palpitation, Somnolence, abdominalgia, and nausea.|
|Amlodipine is contraindicated in patients with known sensitivity to amlodipine or cardiac shock , unstable angina , oarctation of aorta , acute porphyria .|
|Warnings and precautions|
|Because amlodipine is extensively metabolized by the liver and the plasma elimination half-life (t 1/2) is 56 hours in patients with impaired hepatic function, titrate slowly when administering amlodipine to patients with severe hepatic impairment.|
|Pregnancy and lactation|
Pregnancy Category C There are no adequate and well-controlled studies in pregnant women. Amlodipine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
NURSING MOTHERS :
It is not known whether amlodipine is excreted in human milk. In the absence of this information, it is recommended that nursing be discontinued while amlodipine is administered .
|In vitro data indicate that amlodipine has no effect on the human plasma protein binding of digoxin, phenytoin, warfarin, and indomethacin.
Cimetidine: Co-administration of amlodipine with cimetidine did not alter the pharmacokinetics of amlodipine.Grapefruit Juice: Administration of amlodipine with grapefruit or grapefruit juice is not recommended since bioavailability may be increased in certain patients resulting in increased
blood pressure lowering effects.
Magnesium and Aluminum Hydroxide Antacid: Co-administration of a magnesium and aluminum hydroxide antacid with a single dose of Amlodipine had no significant effect on the pharmacokinetics of amlodipine.
Sildenafil: A single 100 mg dose of sildenafil in subjects with essential hypertension had no effect on the pharmacokinetic parameters of amlodipine.
Atorvastatin: Co-administration of multiple 10 mg doses of amlodipine with 80 mg of atorvastatin resulted in no significant change in the steady-state pharmacokinetic parameters of atorvastatin.
Ethanol: Single and multiple 10 mg doses of amlodipine had no significant effect on the pharmacokinetics of ethanol.
CYP3A4 Inhibitors: Strong inhibitors of CYP3A4 (e.g., ketoconazole) may increase the plasma concentrations of amlodipine to a greater extent than diltiazem. Amlodipine should be used with caution together with CYP3A4 Inhibitors however, no adverse events attributable to such interaction have been reported.
CYP3A4 Inducers: There is no data available regarding the effect of CYP3A4 Inducers: on amlodipine.
Amlodipine should be used with caution together with CYP3A4 inducers .
|DOSAGE & ADMINISTRATION|
Elderly patients, or patients with hepatic insufficiency : may be started on 2.5 mg once daily and this dose may be used when adding amlodipine to other antihypertensive therapy.Adjust dosage according to each patient’s need.
In general, titration should proceed over 7 to 14 days so that the physician can fully assess the patient’s response to each dose level.
The recommended dose for chronic stable or vasospastic angina is 5–10 mg, with the lower dose suggested in the elderly and in patients with hepatic insufficiency. The recommended dose range
for patients with coronary artery disease is 5–10 mg once daily. In clinical studies, the majority of patients required 10 mg .
The effective antihypertensive oral dose in pediatric patients ages 6–17 years is 2.5 mg to 5 mg once daily.
|If massive overdose occur, initiate active cardiac and respiratory monitoring.
Frequent blood pressure measurements are essential. When hypotension occur, provide cardiovascular support including elevation of the extremities and the judicious administration of fluids.
If hypotension remains unresponsive to these conservative measures, consider administration of vasopressors (such as phenylephrine) with attention to circulating volume and urine output.
As amlodipine is highly protein bound, hemodialysis is not likely to be of benefit.
|2 X 10 tablets packed in PVC/Aluminum blisters inside a cartoon box with a leaflet.|
|Keep Away From Children, Store at room temperature (15- 30 C), away from light.|