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Amlodipine

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Generic Name of Amlodipine - Learn More

Amlodipine

Amlodipine Precaution - What You Need to Know

Amlodipine is a calcium channel blocker used primarily to treat hypertension and angina. While it is generally well-tolerated, certain precautions must be taken, particularly in individuals with pre-existing cardiovascular conditions. It should be used with caution in patients with severe aortic stenosis, as it can exacerbate symptoms by reducing afterload and potentially impairing coronary perfusion.

For individuals with liver impairment, amlodipine may need to be used at a reduced dose, as hepatic metabolism significantly influences its clearance. Close monitoring is recommended for these patients, especially for signs of hypotension, as amlodipine can cause a significant decrease in blood pressure, especially following the first dose. In elderly individuals, the initial dose should be on the lower end of the dosing spectrum due to the potential for increased sensitivity to the drug, which may result in a heightened risk of orthostatic hypotension.

During pregnancy, amlodipine falls under Category C, meaning that while animal studies have shown some adverse effects, there is insufficient data in humans. It should be used during pregnancy only when the potential benefits outweigh the risks. Amlodipine is excreted in breast milk, but no adverse effects on nursing infants have been documented, making it generally safe for breastfeeding women.

Amlodipine Indication - Uses and Benefits

Amlodipine is indicated primarily for the treatment of hypertension (high blood pressure) and chronic stable angina, including variant (Prinzmetal’s) angina. It works by inhibiting the influx of calcium ions into vascular smooth muscle and cardiac muscle, leading to vasodilation and a reduction in peripheral vascular resistance, which lowers blood pressure. This effect also makes amlodipine effective in relieving symptoms of angina by increasing blood flow to the heart.

In addition to its primary uses, amlodipine is sometimes used off-label for the management of conditions like Raynaud’s phenomenon and certain types of arrhythmias, although these indications are less common. Evidence supporting the use of amlodipine in these off-label situations is limited but suggests benefits in improving circulation and reducing vascular spasms in some cases.

Amlodipine may also be prescribed as part of combination therapy with other antihypertensive medications, including ACE inhibitors, diuretics, or beta-blockers, for patients whose hypertension is not controlled by a single medication. It is also used as a first-line treatment for hypertension in certain populations, especially in elderly patients and those with a history of coronary artery disease.

Amlodipine Contraindications - Important Warnings

Amlodipine is contraindicated in patients with a known hypersensitivity to the drug or any of its components. It should not be used in patients with severe hypotension, as the drug’s vasodilatory effects can further reduce blood pressure and lead to symptoms such as dizziness, fainting, and shock. It is also contraindicated in patients with cardiogenic shock, as amlodipine can exacerbate the condition by lowering blood pressure and reducing myocardial perfusion.

In patients with severe aortic stenosis, amlodipine should be avoided, as it may impair coronary perfusion and worsen symptoms of heart failure due to the drug’s afterload-reducing properties. Additionally, it should not be used in conjunction with other medications that excessively lower blood pressure or in patients with severe liver disease unless the risks are carefully considered and closely monitored.

During pregnancy, particularly in the first trimester, the safety of amlodipine has not been well-established, so it should only be prescribed when absolutely necessary. Similarly, it is not recommended during breastfeeding without careful assessment of the risk-benefit ratio.

Amlodipine Side Effects - What to Expect

The most common side effects of amlodipine include peripheral edema (swelling of the ankles and feet), dizziness, and headache. Peripheral edema occurs due to the vasodilation effects of the drug, which can lead to fluid retention. This side effect can be bothersome but is generally manageable and often resolves with dose adjustment or the use of diuretics in combination.

Other side effects include palpitations, flushing, and fatigue. In some patients, amlodipine can cause gastrointestinal symptoms such as nausea and abdominal discomfort. Less commonly, it may lead to sleep disturbances or mood changes, including depression.

In rare cases, amlodipine may cause more severe side effects, including hypotension, severe dizziness, or fainting, particularly after the first dose. These effects are usually transient and resolve with dose adjustment. Serious cardiovascular effects such as tachycardia, bradycardia, or heart block have been reported, though these are rare.

In very rare cases, amlodipine has been associated with allergic reactions, including skin rash, pruritus, or swelling of the face or throat, which could indicate anaphylaxis. Immediate medical attention is necessary if these symptoms occur.

Amlodipine Pregnancy Category ID - Safety Information

3

Amlodipine Mode of Action - How It Works

Amlodipine works by inhibiting the influx of calcium ions into vascular smooth muscle and cardiac muscle cells through voltage-gated calcium channels. By blocking calcium entry, amlodipine causes smooth muscle relaxation, leading to vasodilation, particularly in the peripheral vasculature. This reduction in vascular resistance lowers blood pressure, which is beneficial in the treatment of hypertension.

In addition to its effects on the vasculature, amlodipine’s action on the coronary arteries helps increase myocardial oxygen supply, which can be beneficial in the management of angina. The reduction in afterload also reduces the workload on the heart, which can help improve exercise tolerance and reduce symptoms of angina.

Amlodipine’s long half-life allows for once-daily dosing, making it convenient for patients. It does not have significant negative effects on heart rate or conduction, which distinguishes it from other calcium channel blockers, such as verapamil or diltiazem, making it a preferred option in many hypertensive and angina patients.

Amlodipine Drug Interactions - What to Avoid

Amlodipine can interact with several medications, which may alter its effectiveness or lead to adverse effects. When used in combination with other antihypertensive agents, such as ACE inhibitors, beta-blockers, or diuretics, the blood pressure-lowering effects may be enhanced, which can increase the risk of hypotension, especially after the first dose of amlodipine. Therefore, careful monitoring of blood pressure is essential, particularly when starting or adjusting therapy.

Amlodipine may also interact with cytochrome P450 3A4 inhibitors, such as ketoconazole, itraconazole, and certain HIV protease inhibitors, leading to increased amlodipine plasma concentrations and a higher risk of adverse cardiovascular events like hypotension. Conversely, drugs that induce CYP3A4, such as rifampin and St. John's Wort, may reduce amlodipine’s effectiveness by increasing its metabolism.

In patients taking cyclosporine, a common immunosuppressant, the use of amlodipine can lead to increased levels of cyclosporine in the blood, which can increase the risk of nephrotoxicity. The combination of amlodipine and simvastatin (a commonly prescribed statin) should be used cautiously, as high doses of simvastatin may increase the risk of muscle-related side effects.

Alcohol and grapefruit juice should be avoided in excessive amounts, as they can potentiate amlodipine’s blood pressure-lowering effects, leading to increased risk of dizziness and orthostatic hypotension.

Amlodipine Adult Dose - Recommended Dosage

For hypertension, the usual starting dose of amlodipine is 5 mg once daily. This dose may be increased to 10 mg once daily based on the patient’s response to treatment. The maximum recommended dose is 10 mg per day, which can be taken at any time of day, with or without food.

For the treatment of chronic stable angina, the starting dose is also typically 5 mg once daily, with the dose titrated to a maximum of 10 mg per day. Amlodipine is often used in combination with other medications, such as nitrates or beta-blockers, to achieve optimal control of angina.

Amlodipine Child Dose - Dosage for Children

Amlodipine is approved for use in pediatric patients for the treatment of hypertension. The usual starting dose for children aged 6 to 17 years is 2.5 mg once daily, with a maximum dose of 5 mg once daily. For children who are unable to achieve blood pressure control with lower doses, the dose may be increased up to 5 mg daily, but the response should be carefully monitored. Amlodipine is generally not recommended for children under 6 years of age due to insufficient data on its safety and efficacy in this population.

Amlodipine Renal Dose - Dosage for Kidney Conditions

Amlodipine does not require significant dose adjustment in patients with mild to moderate renal impairment. However, in individuals with severe renal impairment (creatinine clearance < 30 mL/min), the use of amlodipine should be approached with caution, as these patients may be more sensitive to the effects of the drug. Lower starting doses of 2.5 mg per day may be considered in these patients, with gradual dose escalation while closely monitoring for any signs of hypotension.

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