LOPICARD Amlodipine Besilate 10mg Tablet 20's

Indications/Uses

Treatment of hypertension. Treatment and prophylaxis of chronic stable angina pectoris. Treatment of confirmed or suspected vasopastic angina (Prinzmetal's or Variant Angina).
Lopicard may be used alone or in combination with other antianginal or antihypertensive agents.

Dosage/Direction for Use

Hypertension and Angina: Initial Dose: 5 mg once daily which may be increased to a maximum dose of 10 mg depending on the individual patient's response. No dose adjustment of Lopicard is required upon concomitant administration of thiazide, diuretics, β-blockers and ACE inhibitors.
Elderly >65 years: Initial Dose: 5 mg once daily. If required, increasing the dose should be done gradually and with caution.
Hepatic impairment: Dosage requirements have not been established in patients with impaired hepatic function. Therefore, the dosage should be carefully and gradually adjusted depending on the patient's tolerance and response. A lower starting dose of 2.5 mg once daily should be considered.

Administration

May be taken with or without food.

Contraindications

Patients with known sensitivity to dihydropyridines, amlodipine or any other components of Lopicard.
Amlodipine should not be used in cardiogenic shock, clinically significant aortic stenosis, unstable angina (excluding Prinzmetal's angina).
Patients with severe hypotension (<90 mm Hg systolic).
During pregnancy and lactation. Not recommended for use in children.

Special Precautions

General: The safety and efficacy of amlodipine in hypertensive crisis has not been established.
Hypotension: Careful monitoring of blood pressure is recommended, especially in patients with a history of cerebrovascular insufficiency and those taking medications known to lower blood pressure.
Peripheral Edema: Care should be taken to differentiate this peripheral edema from the effects of increasing left ventricular dysfunction.
Hepatic Impairment: When amlodipine is used in hepatically impaired patients, the dosage should be carefully and gradually adjusted depending on the patient's tolerance and response.

Use In Pregnancy & Lactation

Lopicard is contraindicated during pregnancy and lactation.

Adverse Reactions

Amlodipine therapy is generally well tolerated at doses of up to 10 mg/day. Most of the reported reactions are of mild to moderate severity and are related to the drug's vasodilator effect on the periphery. Headache and edema are reported most frequently. Dizziness, flushing and palpitations also occur and appear to be dose-related. Other adverse reactions that have been reported and do not appear to be dose-related include fatigue, nausea/vomiting, abdominal pain and drowsiness.

Drug Interactions

Cytochrome P-450 System: Dihydropyridine calcium-channel blockers undergo biotransformation by the cytochrome P-450 system, mainly via CYP3A4 isoenzyme. Co-administration of amlodipine with other drugs which follow the same route of biotransformation may result in altered bioavailability of amlodipine or these drugs.
Dosages of similarly metabolized drugs, particularly those of low therapeutic ratio, and especially in patients with renal and/or hepatic impairment, may require adjustment when starting or stopping concomitantly administered amlodipine to maintain optimum therapeutic blood levels.
Beta-Blockers: When β-adrenergic receptor blocking drugs are administered concomitantly with amlodipine, patients should be carefully monitored since blood pressure lowering effect of β-blockers may be augmented by amlodipine's reduction in peripheral vascular resistance.
Grapefruit Juice: Published data indicates that through inhibition of cytochrome P-450 system, grapefruit juice can increase plasma levels and augment pharmacodynamic effects of some dihydropyridine calcium-channel blockers.

Storage

Store below 30°C. Protect from sunlight and moisture.
Shelf-Life: 24 months.

Action

Pharmacology: Amlodipine is a calcium ion influx inhibitor (slow channel blocker or calcium ion antagonist) and inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle.
Mechanism of Action: The mechanism of the antihypertensive action of amlodipine is due to a direct relaxant effect on vascular smooth muscle. The precise mechanism by which amlodipine relieves angina has not been fully determined but amlodipine reduces total ischemic burden by the following 2 actions:
Amlodipine dilates peripheral arterioles and thus, reduces the total peripheral resistance against which the heart works. Since the heart rate remains stable, this unloading of the heart reduces myocardial energy consumption and oxygen requirements.
The mechanism of action of amlodipine also probably involves dilatation of the main coronary arteries and coronary arterioles, both in normal and ischemic regions. This dilatation increases myocardial oxygen delivery in patients with coronary artery spasm.
Pharmacokinetics: Absorption: Oral administration of therapeutic doses of amlodipine produces peak plasma concentrations between 6-12 hrs. Absolute bioavailability has been estimated to be between 64-80%. The bioavailability of amlodipine when administered alone is not altered by the presence of food.
Distribution: Approximately 97.5% of the circulating amlodipine drug is bound to plasma proteins in hypertensive patients. The volume of distribution is approximately 21 L/kg. Steady-state plasma levels of amlodipine are reached after 7-8 days of consecutive daily dosing.
Metabolism: Amlodipine is extensively (90%) converted to inactive metabolites via hepatic metabolism.
Excretion: Elimination from the plasma is biphasic with a terminal t_½ of about 35-50 hrs, 10% of the parent amlodipine compound and 60% of the metabolites of amlodipine are excreted in the urine.
Special Populations: Elderly: In elderly hypertensive patients there was a decrease in clearance of amlodipine from plasma as compared to young volunteers with a resulting increase in the AUC of about 60%.
Hepatic Insufficiency: Following single oral administration of 5 mg amlodipine, patients with chronic mild to moderate hepatic insufficiency showed about 40% increase in AUC of amlodipine as compared to normal volunteers.

MedsGo Class

Calcium Antagonists / Anti-Anginal Drugs