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Amlodipine (Norvasc )

When ingested, amlodipine becomes completely absorbed in the small intestine. Neither absorbability nor bioavailability of the drug changes when administered with food. Renal elimination of ten inactive metabolites formed in the liver is the only way of excretion. Users with renal insufficiency experience just a slight difference in the main pharmacokinetic parameters of amlodipine. It ensures safe treatment of the elderly, who often have some degree of renal dysfunction. One should be cautious when using amlodipine to cure patients with liver cirrhosis.


Medical uses

Amlodipine is mainly used to treat primary hypertension and other forms of arterial hypertension. Amlodipine can be prescribed as initial treatment for myocardial ischemia caused by a permanent obstruction (stable angina) or coronary artery spasms (Prinzmetal's angina or variant angina pectoris). It may also work well in cases when the presence of a vasospastic (vasoconstrictive) agent is possible.


Adverse effects

Amlodipine is easily tolerated. Clinical placebo trials, involving patients with hypertension and angina, showed that the most common side effects: headache, edema, fatigue, nausea, flushing and dizziness. Any characteristic of clinically significant abnormalities on laboratory tests in the test amlodipine were noted. The trials didnt reveal any discrepancies in the results of laboratory tests.



Although elderly patients may have a higher concentration of amlodipine in plasma, its half-life remains unchanged. Amlodipine is equally well tolerated by both elderly and younger patients. Therefore, a regular drug therapy is recommended.

In patients with renal failure 10% of amlodipine is recovered in urine in unchanged form, as inactive metabolites. Changes in plasma concentrations of amlodipine are affected by the degree of renal failure. To treat such patients regular doses of amlodipine can be used. Amlodipine cannot be eliminated during dialysis. The half-life of amlodipine is increased in patients with impaired liver function. The recommended dose for such cases has not been established. Therefore, additional safety measures should be taken.


Pregnancy and breast-feeding

Safety level of amlodipine administration during pregnancy and lactation has not yet been established. Pregnant animal studies show no signs of amlodipines toxicity except childbirth delay and labor increase in rats at a dose 50 times as high as the maximum recommended human dose. Thus, the usage during pregnancy is recommended only in cases where the benefits a mother and a child may get outweigh the potential risks.



There are no document supported cases of amlodipine overdose. Since the absorption of amlodipine is slow, gastric lavage might be carried out in some cases. Available data suggest that a strong overdose can cause excessive peripheral vasodilation, which can result in replacement and prolonged systemic hypotension. Clinically significant hypotension caused by amlodipine overdose requires active measures to be taken to support the cardiovascular system, including the monitoring of cardiac and respiratory function and limb lifting. Particular attention should be paid to maintaining blood volume and the amount of urine. Vasopressors can be used to restore vascular tone and blood pressure, provided there are no contraindications. Since amlodipine is largely protein bound, dialysis is unlikely to be of any help.




Amlodipine can be safely used in combination with thiazide diuretics, beta-blockers, ACE inhibitors, long-acting nitrates, sublingual nitroglycerin, NSAIDs, antibiotics, and oral hypoglycemic drugs. Additional research has shown that the simultaneous use of amlodipine and digoxin neither alters the level of digoxin in serum nor renal excretion of digoxin, and administration of cimetidine does not affect the pharmacokinetics of amlodipine. In vitro studies indicate that amlodipine has no effect on protein binding of such drugs as digoxin, phenytoin, warfarin, and indomethacin.



The usual starting dose for hypertension and angina pectoris is 5 mg one time per day. This dose may be increased to 10 mg, depending on an individual patient response.