Active Substance: Amlodipine (as besilate).
Overview
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This medicine contains an important and useful components, as it consists of
Amlodipine (as besilate)is available in the market in concentration
Amlodipine
- **Heart Failure**: Caution is required when using amlodipine in patients with heart failure, as it may cause or worsen symptoms, particularly in those with severe conditions. Regular monitoring is essential. - **Liver Dysfunction**: Amlodipine is metabolized in the liver. In patients with hepatic impairment, the drug may accumulate, leading to an increased risk of side effects. Dose reduction or monitoring of liver function is recommended. - **Pregnancy and Breastfeeding**: Amlodipine is categorized as a pregnancy category C drug, meaning its use should be avoided during pregnancy unless absolutely necessary. It passes into breast milk, so caution should be exercised when prescribed to breastfeeding mothers. - **Elderly Patients**: Elderly patients may be more sensitive to amlodipine's effects, particularly hypotension and dizziness. A lower initial dose may be considered to reduce the risk of adverse events. - **Hypotension**: Amlodipine may cause or exacerbate hypotension, especially in patients who are volume-depleted or those on other antihypertensive medications. Blood pressure should be carefully monitored. - **Renal Impairment**: Patients with renal impairment may require dose adjustments or closer monitoring as amlodipine’s clearance may be reduced in such cases.
- **Hypertension**: Amlodipine is primarily used in the management of hypertension. It helps to lower blood pressure by relaxing the blood vessels, making it easier for the heart to pump blood. - **Angina Pectoris**: Amlodipine is indicated for the treatment of angina, both stable and variant types (Prinzmetal's angina). It works by dilating coronary arteries, improving blood flow to the heart, and reducing the frequency of angina attacks. - **Coronary Artery Disease (CAD)**: Amlodipine is used to treat CAD, either alone or in combination with other therapies, to improve exercise tolerance and reduce chest pain. - **Chronic Stable Angina**: Amlodipine is effective in preventing chest pain associated with chronic stable angina by decreasing the heart's workload and oxygen demand. - **Off-label Uses**: Amlodipine is sometimes used for conditions such as Raynaud's phenomenon, certain types of arrhythmias, and diabetic nephropathy in combination with other treatments.
- **Hypersensitivity**: Amlodipine is contraindicated in patients with a known hypersensitivity to amlodipine, dihydropyridines, or any other components of the formulation due to the risk of severe allergic reactions. - **Severe Hypotension**: Amlodipine should not be used in patients with severe hypotension or shock, as it may worsen these conditions. - **Aortic Stenosis**: In patients with severe aortic stenosis, amlodipine may cause further complications, as it could reduce cardiac output and exacerbate the condition. - **Acute Myocardial Infarction (MI)**: Amlodipine should be avoided immediately after a heart attack in patients with cardiogenic shock, as it may cause an adverse effect on the heart's ability to pump blood. - **Pregnancy Category C**: Amlodipine should not be used during pregnancy unless the potential benefits outweigh the risks. It is contraindicated in the third trimester due to the risk of adverse effects on fetal development.
- **Common Side Effects**: - Headache - Swelling of the ankles or feet (edema) - Dizziness - Fatigue - Flushing - Palpitations - **Serious Side Effects**: - Severe hypotension - Chest pain or pressure - Shortness of breath - Tachycardia or bradycardia - Liver toxicity (jaundice, dark urine, abdominal pain) - Swelling of the gums - **Cardiovascular Effects**: Amlodipine can cause bradycardia, palpitations, or worsening angina in some patients, particularly when used in higher doses or in combination with other blood pressure-lowering drugs. - **Peripheral Edema**: One of the more common side effects of amlodipine is peripheral edema, which is usually dose-dependent and can be particularly bothersome for patients. - **Gastrointestinal Disturbances**: Some patients may experience nausea, constipation, or abdominal discomfort. - **Skin Reactions**: Rash, pruritus, or skin irritation may occur, especially in patients with sensitivity to calcium channel blockers. - **Allergic Reactions**: Though rare, severe allergic reactions like anaphylaxis or angioedema can occur and require immediate medical attention.
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- **Calcium Channel Blockade**: Amlodipine works by inhibiting the entry of calcium ions into vascular smooth muscle and cardiac muscle cells via the L-type calcium channels. This results in relaxation and dilation of blood vessels, leading to reduced vascular resistance and lower blood pressure. - **Vasodilation**: The drug primarily causes vasodilation in the peripheral vasculature, which decreases blood pressure and reduces the heart's workload. It is especially effective in the treatment of hypertension and angina. - **Coronary Artery Dilation**: In patients with angina, amlodipine dilates the coronary arteries, improving oxygen delivery to the heart muscle and reducing ischemic chest pain. - **Reduced Cardiac Workload**: By lowering systemic vascular resistance, amlodipine decreases the heart’s workload, which can help prevent further heart damage in patients with heart failure or coronary artery disease. - **Smooth Muscle Relaxation**: Amlodipine relaxes smooth muscle, leading to the dilation of arteries and a decrease in both preload and afterload, which helps to reduce the heart’s oxygen demand.
- **Other Antihypertensive Agents**: Combining amlodipine with other antihypertensive drugs such as ACE inhibitors, beta-blockers, or diuretics can lead to an additive blood pressure-lowering effect, which may increase the risk of hypotension. Careful monitoring is advised. - **CYP3A4 Inhibitors**: Amlodipine is metabolized by the CYP3A4 enzyme. Drugs that inhibit this enzyme (e.g., ketoconazole, grapefruit juice) may increase amlodipine concentrations, leading to an increased risk of side effects, including hypotension and peripheral edema. - **CYP3A4 Inducers**: Drugs that induce CYP3A4 (e.g., rifampin, carbamazepine) may reduce the efficacy of amlodipine by decreasing its plasma levels. Dose adjustments may be necessary. - **Lithium**: Concurrent use of amlodipine with lithium may increase the risk of lithium toxicity, particularly in patients with renal dysfunction. - **Digoxin**: The combination of amlodipine and digoxin can increase the risk of bradycardia and other cardiac arrhythmias, especially in susceptible individuals. - **Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)**: Chronic use of NSAIDs in conjunction with amlodipine may decrease the antihypertensive effects of amlodipine, potentially leading to poor blood pressure control. - **Alcohol**: Alcohol can exacerbate amlodipine’s blood pressure-lowering effects, leading to an increased risk of dizziness, lightheadedness, and fainting.
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- **Hypertension**: The typical starting dose is 5 mg once daily, which can be increased to a maximum of 10 mg once daily, depending on the patient’s response to therapy and the control of blood pressure. - **Angina**: For the management of stable angina or vasospastic angina, the usual dose is 5 mg once daily, which may be increased to 10 mg once daily as needed to control symptoms. - **Coronary Artery Disease**: In patients with CAD, amlodipine is often combined with other medications such as beta-blockers or ACE inhibitors, with a typical dose of 5 mg to 10 mg once daily. - **Dosing Adjustments**: For patients with hepatic impairment or elderly patients, a lower initial dose of 2.5 mg per day may be considered, with gradual increases as tolerated.
- **Children 6-17 years old**: The usual starting dose for children is 2.5 mg to 5 mg once daily, with the maximum recommended dose being 5 mg to 10 mg once daily, depending on the child’s weight and response to treatment. - **Children under 6 years**: Amlodipine has not been studied extensively in children under the age of 6, so it is not recommended for use in this age group without a healthcare provider’s supervision.
- **Renal Impairment**: No dose adjustment is required for patients with mild to moderate renal impairment, as amlodipine is not significantly excreted unchanged by the kidneys. However, caution should be used in patients with severe renal impairment. - **Hemodialysis**: Amlodipine is not significantly removed by hemodialysis, so no dose adjustment is necessary in patients undergoing dialysis.
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