Amlodipine Besilate

Amlodipine Besilate is a dihydropyridine calcium channel blocker with a long duration of action, used for the treatment of hypertension and angina pectoris. It influences myocardial cells, cells within the specialized conducting system of the heart, and cells of vascular smooth muscle.

Administration of amlodipine results primarily in vasodilation, with reduced peripheral resistance, blood pressure and afterload, increased coronary blood flow and a reflex increase in heart rate. This in turn results in an increase in myocardial oxygen supply and cardiac output.

Common side effects include fatigue, ankle swelling, sleepiness, dizziness, flushing, headache, palpitations, and abdominal pain.

• Essential hypertension - alone or in combination with other antihypertensive agents
• Chronic stable angina pectoris - alone or in combination with other antianginal agents
• Vasospastic angina (Prinzmetal's or variant angina) - as monotherapy or in combination with other antianginal drugs

Amlodipine Besilate is a dihydropyridine calcium-channel blocker with a long duration of action, used for the treatment of hypertension and angina pectoris. Amlodipine influences the myocardial cells, the cells within the specialized conducting system of the heart, and the cells of vascular smooth muscle.

Administration of amlodipine results primarily in vasodilation, with reduced peripheral resistance, blood pressure and afterload, increased coronary blood flow and a reflex increase in heart rate. This in turn results in an increase in myocardial oxygen supply and cardiac output.

Amlodipine inhibits calcium ion entry into slow channels or select voltage-sensitive channels of vascular smooth muscle and myocardium during depolarization, producing coronary vasodilation. It relaxes peripheral and coronary vascular smooth muscle, reducing blood pressure and increasing myocardial oxygen delivery in patients with vasospastic angina.

Hypertension: 5 mg once daily (maximum 10 mg). Elderly and hepatic impairment patients may start with 2.5 mg once daily.

Angina (Chronic stable or Vasospastic): 5-10 mg daily (lower dose for elderly and hepatic impairment). Most patients require 10 mg.

Pediatric (6-17 years - hypertension): 2.5 mg once daily initial, up to 5 mg once daily after 4 weeks. Efficacy in children <6 years not established.

Hepatic Impairment: Severe hepatic impairment: start with 2.5 mg once daily and titrate slowly.

Renal Impairment: No dose adjustment needed (amlodipine is not dialyzable).

Take this medicine in the dose and duration as advised by your doctor. Swallow the tablet whole - do not chew, crush or break. May be taken at any time of the day, with or without food, but take at a fixed time.

If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.

• Fatigue
• Ankle swelling
• Sleepiness
• Dizziness
• Flushing
• Headache
• Nausea
• Palpitations
• Edema
• Abdominal pain
• Increased micturition frequency
• Lethargy
• Eye pain
• Mental depression

Rare: Increased angina, excessive hypotension, cerebral or myocardial ischemia, transient blindness, rash, fever, liver function abnormalities

Serious Precautions:

• Patients with severe obstructive coronary artery disease may develop increased angina or MI when starting calcium channel blocker therapy or increasing dose
• Caution in severe aortic stenosis, hepatic impairment
• Caution in severe left ventricular dysfunction, sick-sinus syndrome, hypertrophic cardiomyopathy
• Heart failure patients may have increased risk of pulmonary edema
• Caution during pregnancy - animal studies have shown fetal risk
• Blood pressure may drop suddenly - rise slowly from sitting or lying position
• Caution while driving or operating machinery - may cause dizziness

• Hypersensitivity to dihydropyridine derivatives
• Severe hypotension
• Cardiogenic shock
• Left ventricular outflow tract obstruction (e.g., severe aortic stenosis)
• Unstable angina (other than acute MI)

• Beta-blockers: Avoid combination in patients with severe left ventricular dysfunction
• Digoxin: No significant interaction
• Cimetidine: No significant interaction
• Warfarin: No significant alteration in prothrombin time
• Other antihypertensives: Additive effects may occur

[CAUTION] Caution with alcohol consumption. Alcohol may enhance the blood pressure lowering effect.

[CONSULT YOUR DOCTOR] Amlodipine may be unsafe during pregnancy (Category C). Animal studies have shown harmful effects on the developing baby. Use only if potential benefit justifies the risk.

[SAFE IF PRESCRIBED] It is unknown whether amlodipine is excreted in human milk. Caution is advised during breastfeeding.

Pediatric (6-17 years): 2.5 mg once daily initial, up to 5 mg once daily. Efficacy in children under 6 years not established.

Elderly patients should start with lower dose (2.5 mg). Dose increases should be done with care.

Renal Impairment: No dose adjustment needed. Amlodipine is not dialyzable.

Hepatic Impairment: Mild-moderate impairment: start with lower dose. Severe impairment: start with 2.5 mg once daily and titrate slowly.

Symptoms: Excessive peripheral vasodilation, reflex tachycardia, severe and prolonged systemic hypotension, shock (may be fatal).

Management: Cardiovascular support (monitoring cardiac and respiratory function, elevation of extremities, monitoring fluid volume and urine output). Vasoconstrictors may be used. IV calcium gluconate may help reverse calcium channel blockade. Gastric lavage may be helpful. Dialysis is not effective as amlodipine is highly protein-bound.

Keep out of reach of children. Store in a cool and dry place, protected from light.

Amlodipine Besilate (C₂₀H₂₅ClN₂O₅·C₆H₆O₃S)