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Amlodipine


In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345. Precautions Before taking amlodipine, tell your doctor or pharmacist if you are allergic to it; or to other dihydropyridine calcium channel blockers (such as nisoldipine, nifedipine) or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.




amlodipine



Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details. Images amlodipine 10 mg tablet


Amlodipine is used alone or in combination with other medications to treat high blood pressure in adults and children 6 years and older. It is also used to treat certain types of angina (chest pain) and coronary artery disease (narrowing of the blood vessels that supply blood to the heart). Amlodipine is in a class of medications called calcium channel blockers. It lowers blood pressure by relaxing the blood vessels so the heart does not have to pump as hard. It controls chest pain by increasing the supply of blood to the heart. If taken regularly, amlodipine controls chest pain, but it does not stop chest pain once it starts. Your doctor may prescribe a different medication to take when you have chest pain.


Amlodipine comes as a tablet and an suspension (liquid) to take by mouth. It is usually taken once a day. To help you remember to take amlodipine, take it around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take amlodipine exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.


Amlodipine helps to control high blood pressure, angina, and coronary artery disease, but does not cure these conditions. Continue to take amlodipine even if you feel well. Do not stop taking amlodipine without talking to your doctor.


Swelling from amlodipine is a common, but often troublesome side effect of amlodipine with 5% to 9% of people stopping amlodipine because of it. If you develop swelling with amlodipine, tell your doctor right away because they may be able to change your blood pressure medications slightly to help reduce the swelling. Swelling caused by amlodipine does not usually respond to treatment with diuretics (such as furosemide) because it is caused by changes in capillary pressure that result in leakage into the spaces between capillaries (called the interstitial area) rather than water retention.


Weight gain has been reported by some people taking amlodipine but this is not a common side effect and some people have also reported weight loss. Weight gain with amlodipine may also be a symptom of edema, which is when you retain fluid, which may be particularly noticeable around your ankles or lower legs. The risk of edema is greater in women compared with men and in those people taking a higher dosage of amlodipine, and edema is usually noticed as weight gain.


If you are being treated for high blood pressure, keep using amlodipine even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.


Tell your doctor if you are pregnant or plan to become pregnant. It is not known whether amlodipine will harm an unborn baby. However, having high blood pressure during pregnancy may cause complications such as diabetes or eclampsia (dangerously high blood pressure that can lead to medical problems in both mother and baby). The benefit of treating hypertension may outweigh any risks to the baby.


Take amlodipine exactly as prescribed by your doctor. Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use this medicine in larger or smaller amounts or for longer than recommended.


If you are being treated for high blood pressure, keep using amlodipine even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medicine for the rest of your life.


In rare cases, when you first start taking amlodipine, your angina may get worse or you could have a heart attack. Seek emergency medical attention or call your doctor right away if you have symptoms such as: chest pain or pressure, pain spreading to your jaw or shoulder, nausea, sweating.


This list is not complete. Other drugs may interact with amlodipine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.


Swelling from amlodipine is a common, but often troublesome side effect of amlodipine with 5% to 9% of people stopping amlodipine because of it. If you develop swelling with amlodipine, tell your doctor right away because they may be able to change your blood pressure medications slightly to help reduce the swelling. Swelling caused by amlodipine does not usually respond to treatment with diuretics (such as furosemide) because it is caused by changes in capillary pressure that result in leakage into the spaces between capillaries (called the interstitial area) rather than water retention. Continue reading


Weight gain has been reported by some people taking amlodipine but this is not a common side effect and some people have also reported weight loss. Weight gain with amlodipine may also be a symptom of edema, which is when you retain fluid, which may be particularly noticeable around your ankles or lower legs. The risk of edema is greater in women compared with men and in those people taking a higher dosage of amlodipine, and edema is usually noticed as weight gain. Continue reading


Other situations occur, however, where amlodipine generally should not be used. In patients with cardiogenic shock, where the heart's ventricles are not able to pump enough blood, calcium channel blockers exacerbate the situation by preventing the flow of calcium ions into cardiac cells, which is required for the heart to pump.[20] While use in patients with aortic stenosis (narrowing of the aorta where it meets the left ventricle) since it does not inhibit the ventricle's function is generally safe, it can still cause collapse in cases of severe stenosis.[21] In unstable angina (excluding variant angina), amlodipine can cause a reflex increase in cardiac contractility (how hard the ventricles squeeze) and heart rate, which together increase the demand for oxygen by the heart itself.[22] Patients with severe hypotension can have their low blood pressure exacerbated, and patients in heart failure can get pulmonary edema. Those with impaired liver function are unable to metabolize amlodipine to its full extent, giving it a longer half-life than typical.[7][6]


Some common dose-dependent adverse effects of amlodipine include vasodilatory effects, peripheral edema, dizziness, palpitations, and flushing.[7][24] Peripheral edema (fluid accumulation in the tissues) occurs at rate of 10.8% at a 10-mg dose (versus 0.6% for placebos), and is three times more likely in women than in men.[7] It causes more dilation in the arterioles and precapillary vessels than the postcapillary vessels and venules. The increased dilation allows for more blood, which is unable to push through to the relatively constricted postcapillary venules and vessels; the pressure causes much of the plasma to move into the interstitial space.[25] Amlodipine-association edema can be avoided by adding ACE inhibitors or angiotensin II receptor antagonist.[10] Of the other dose-dependent side effects, palpitations (4.5% at 10 mg vs. 0.6% in placebos) and flushing (2.6% vs. 0%) occurred more often in women; dizziness (3.4% vs. 1.5%) had no sex bias.[7]


Although rare,[29] amlodipine overdose toxicity can result in widening of blood vessels, severe low blood pressure, and fast heart rate.[30] Toxicity is generally managed with fluid replacement[31] monitoring ECG results, vital signs, respiratory system function, glucose levels, kidney function, electrolyte levels, and urine output. Vasopressors are also administered when low blood pressure is not alleviated by fluid resuscitation.[7][30]


Several drugs interact with amlodipine to increase its levels in the body. CYP3A inhibitors, by nature of inhibiting the enzyme that metabolizes amlodipine, CYP3A4, are one such class of drugs. Others include the calcium-channel blocker diltiazem, the antibiotic clarithromycin, and possibly some antifungals.[7] Amlodipine causes several drugs to increase in levels, including cyclosporine, simvastatin, and tacrolimus (the increase in the last one being more likely in people with CYP3A5*3 genetic polymorphisms).[32] When more than 20 mg of simvastatin, a lipid-lowering agent, are given with amlodipine, the risk of myopathy increases.[33] Giving amlodipine with Viagra increases the risk of hypotension.[7][10]


Amlodipine ends up significantly reducing total vascular resistance without decreasing cardiac output expressed by pressure-rate product and cardiac contractability in comparison with verapamil, a non-dihydropyridine.[37] In turn, following treatment lasting a month, with amlodipine, cardiac output is significantly enhanced.[37] Unlike verapamil which has efficacy in moderation of emotional arousal and reduces cardiac load without lowering cardiac output demands, amlodipine increases the cardiac output response concomitantly with increased functional cardiac load.[37]


Amlodipine has been studied in healthy volunteers following oral administration of 14C-labelled drug.[45] Amlodipine is well absorbed by the oral route with a mean oral bioavailability around 60%; the half-life of amlodipine is about 30 h to 50 h, and steady-state plasma concentrations are achieved after 7 to 8 days of daily dosing. In the blood it has high plasma protein binding of 97.5%.[35] Its long half-life and high bioavailability are largely in part of its high pKa (8.6); it is ionized at physiological pH, and thus can strongly attract proteins.[7] It is slowly metabolized in the liver by CYP3A4, with its amine group being oxidized and its side ester chain being hydrolyzed, resulting in an inactive pyridine metabolite.[46] Renal elimination is the major route of excretion with about 60% of an administered dose recovered in urine, largely as inactive pyridine metabolites. However, renal impairment does not significantly influence amlodipine elimination.[47] 20-25% of the drug is excreted in the faeces.[48] 041b061a72


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