Selective calcium channel blockers with mainly vascular effects; Dihydropyridine derivatives - ATC code: C 08 CA 01

amlodipine besilate

Each tablet contains Amlodipine besilate equivalent to 10 mg of amlodipine.

Tablet White or almost white, flat, bevelled edges, round tablet debossed with "C" on one side and "59" on the other side.

Essential hypertension.

Chronic stable and vasospastic angina pectoris.

For oral use.

The tablets should be taken with a glass of liquid (e.g. a glass of water) with or without food.

In adults

For the treatment of hypertension and angina pectoris, the starting dose is 5 mg once daily. If the desired therapeutic effect cannot be achieved within 2-4 weeks, the dose can be increased to a maximum of 10 mg daily (given as a single dose) depending on the individual response of the patient. Amlodipine can be used as monotherapy or in combination with anti-anginal medication in patients suffering from angina pectoris.

Patients with renal impairment

The normal dosage is recommended. Amlodipine is not dialyzable. Amlodipine should be administered with particular caution to patients undergoing dialysis.

Patients with hepatic impairment

In patients with hepatic impairment, no dosage regimen has been defined, therefore amlodipine should be administered with caution

Children with hypertension from 6 years to 17 years of age

The recommended antihypertensive oral dose in pediatric patients ages 6-17 years is 2.5 mg once daily as a starting dose, up-titrated to 5 mg once daily if blood pressure goal is not achieved after 4 weeks. Doses in excess of 5 mg daily have not been studied in pediatric patients. The effect of amlodipine on blood pressure in patients less than 6 years of age is not known

The 2.5 mg dose cannot be obtained with Amlodipine 5 mg tablets as these tablets are not manufactured to break into two equal halves.

For elderly patients, the normal dose is recommended; however, caution is advised when the dose is increased.

Amlodipine is contraindicated in patients with:

- hypersensitivity to amlodipine, other dihydropyridines or any of the excipients

- severe hypotension

- shock (including cardiogenic shock)

- obstruction of the outflow tract of the left ventricle (e.g. high grade aortic stenosis)

- haemodynamically unstable heart failure after acute myocardial infarction

The safety and efficacy of amlodipine in hypertensive crisis has not been established.

Patients with cardiac failure:

Patients with heart failure should be treated with caution. In a long-term, placebo controlled study in patients with severe heart failure (NYHA class III and IV) the reported incidence of pulmonary oedema was higher in the amlodipine treated group than in the placebo group, but this was not associated with worsening of the heart failure.

Use in patients with impaired hepatic function:

The half life of amlodipine is prolonged in patients with impaired liver function; dosage recommendations have not been established. Amlodipine should therefore be administered with caution in these patients.

Use in elderly patients

In elderly patients, caution is advised when the dosage is increased.

Use in renal failure

Amlodipine may be used in such patients at normal doses. Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment. Amlodipine is not dialyzable

Effects of other medicinal products on amlodipine

CYP3A4 inhibitors: With concomitant use with the CYP3A4 inhibitor erythromycin in young patients and diltiazem in elderly patients respectively the plasma concentration of amlodipine increased by 22% and 50 % respectively. However, the clinical relevance of this finding is uncertain. It cannot be ruled out that strong inhibitors of CYP3A4 (e.g. ketoconazole, itraconazole, ritonavir) 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. The concomitant use of CYP3A4 inducers (e.g. rifampicin, hypericum perforatum) may give a lower plasma concentration of amlodipine. Amlodipine should be used with caution together with CYP3A4 inducers.

In clinical interaction studies grapefruit juice, cimetidine, aluminium/ magnesium (antacid) and sildenafil did not affect the pharmacokinetics of amlodipine.

Effects of amlodipine on other medicinal products

The blood pressure lowering effects of amlodipine adds to the blood pressure-lowering effects of other antihypertensive agents.

In clinical interaction studies, amlodipine did not affect the pharmacokinetics of atorvastatin, digoxin, ethanol (alcohol), warfarin or cyclosporin.

There is no effect of amlodipine on laboratory parameters.

The following undesirable effects have been observed and reported during treatment with amlodipine with the following frequencies: Very common (1/10); common (1/100 to <1/10); uncommon (1/1,000 to 1/100); rare (1/10,000 to 1/1,000); very rare (1/10,000).

*mostly consistent with cholestatis

Aurobindo Pharma Ltd

POM- Prescription Only Medicine

23 March 2012