The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects can be detected in vitro but such effects have not been seen in intact animals at therapeutic doses.
Serum calcium concentration is not affected by Amlodipine. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. The precise mechanisms by which Amlodipine relieves angina have not been fully delineated, but are thought to include the following: In patients with exertional angina, Amlodipine besylate reduces the total peripheral resistance afterload against which the heart works and reduces the rate pressure product, and thus myocardial oxygen demand, at any given level of exercise.
Amlodipine besylate has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium epinephrine, serotonin, and thromboxane A2 analog in experimental animal models and in human coronary vessels in vitro.
This inhibition of coronary spasm is responsible for the effectiveness of Amlodipine besylate in vasospastic Prinzmetal's or variant angina. Following administration of therapeutic doses to patients with hypertension, Amlodipine besylate produces vasodilation resulting in a reduction of supine and standing blood pressures.
These decreases in blood pressure are not accompanied by a significant change in heart rate or plasma catecholamine levels with chronic dosing. Although the acute intravenous administration of Amlodipine decreases arterial blood pressure and increases heart rate in hemodynamic studies of patients with chronic stable angina, chronic oral administration of Amlodipine in clinical trials did not lead to clinically significant changes in heart rate or blood pressures in normotensive patients with angina.
With chronic once daily oral administration, antihypertensive effectiveness is maintained for at least 24 hours. Plasma concentrations correlate with effect in both young and elderly patients.
In hypertensive patients with normal renal function, therapeutic doses of Amlodipine besylate resulted in a decrease in renal vascular resistance and an increase in glomerular filtration rate and effective renal plasma flow without change in filtration fraction or proteinuria.
In hemodynamic studies, Amlodipine besylate has not been associated with a negative inotropic effect when administered in the therapeutic dose range to intact animals and man, even when co-administered with beta-blockers to man.
Similar findings, however, have been observed in normal or well-compensated patients with heart failure with agents possessing significant negative inotropic effects. Amlodipine besylate does not change sinoatrial nodal function or atrioventricular conduction in intact animals or man.
In patients with chronic stable angina, intravenous administration of 10 mg did not significantly alter A-H and H-V conduction and sinus node recovery time after pacing. Similar results were obtained in patients receiving Amlodipine besylate and concomitant beta-blockers.
In clinical studies in which Amlodipine besylate was administered in combination with beta-blockers to patients with either hypertension or angina, no adverse effects on electrocardiographic parameters were observed. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells.
Negative inotropic effects can be detected in vitro but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine.
Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. The precise mechanisms by which amlodipine relieves angina have not been fully delineated, but are thought to include the following: Exertional Angina In patients with exertional angina, NORVASC reduces the total peripheral resistance afterload against which the heart works and reduces the rate pressure product, and thus myocardial oxygen demand, at any given level of exercise.
Vasospastic Angina NORVASC has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium epinephrine , serotonin , and thromboxane A2 analog in experimental animal models and in human coronary vessels in vitro. Pharmacodynamics Hemodynamics Following administration of therapeutic doses to patients with hypertension , NORVASC produces vasodilation resulting in a reduction of supine and standing blood pressures.
These decreases in blood pressure are not accompanied by a significant change in heart rate or plasma catecholamine levels with chronic dosing. Although the acute intravenous administration of amlodipine decreases arterial blood pressure and increases heart rate in hemodynamic studies of patients with chronic stable angina, chronic oral administration of amlodipine in clinical trials did not lead to clinically significant changes in heart rate or blood pressures in normotensive patients with angina.
With chronic once daily oral administration, antihypertensive effectiveness is maintained for at least 24 hours. Plasma concentrations correlate with effect in both young and elderly patients. In hypertensive patients with normal renal function, therapeutic doses of NORVASC resulted in a decrease in renal vascular resistance and an increase in glomerular filtration rate and effective renal plasma flow without change in filtration fraction or proteinuria.
In hemodynamic studies, NORVASC has not been associated with a negative inotropic effect when administered in the therapeutic dose range to intact animals and man, even when co-administered with beta-blockers to man. Similar findings, however, have been observed in normal or well-compensated patients with heart failure with agents possessing significant negative inotropic effects.
Somnolence, dizziness, headache Uncommon 0. Hypertonia, peripheral neuropathy , ataxia, migraine , amnesia, parosmia Frequency not reported: Extrapyramidal syndrome, postural dizziness, vertigo [ Ref ] Headache occurred commonly during clinical trials, especially at the beginning of treatment.
Extrapyramidal syndrome may be associated with this drug. Abdominal pain , nausea Uncommon 0. Vomiting, dyspepsia , altered bowel habits including diarrhea and constipation , dry mouth Very rare less than 0. Pancreatitis , gastritis , gingival hyperplasia, loose stools Frequency not reported: With amlodipine besylate tablets there were more reports of pulmonary edema. There may be new information. This information does not replace talking with your doctor. If you have any questions about amlodipine besylate tablets, ask your doctor.
Your doctor will know if amlodipine besylate tablets are right for you. What are amlodipine besylate tablets? Amlodipine besylate tablets are a type of medicine known as a calcium channel blocker CCB. It is used to treat high blood pressure hypertension and a type of chest pain called angina. It can be used by itself or with other medicines to treat these conditions.
High Blood Pressure hypertension High blood pressure comes from blood pushing too hard against your blood vessels. Amlodipine besylate tablets relaxes your blood vessels, which lets your blood flow more easily and helps lower your blood pressure. Drugs that lower blood pressure lower your risk of having a stroke or heart attack. Angina Angina is a pain or discomfort that keeps coming back when part of your heart does not get enough blood.
Angina feels like a pressing or squeezing pain, usually in your chest under the breastbone. Sometimes you can feel it in your shoulders, arms, neck, jaws, or back.
Amlodipine besylate tablets can relieve this pain. Who should not use amlodipine besylate tablets? Do not use amlodipine besylate tablets if you are allergic to amlodipine the active ingredient in amlodipine , or to the inactive ingredients. Your doctor or pharmacist can give you a list of these ingredients. What should I tell my doctor before taking amlodipine besylate tablets? Tell your doctor about any prescription and non-prescription medicines you are taking, including natural or herbal remedies.
Tell your doctor if you: Get up slowly and steady yourself to prevent a fall. Drinking alcohol can further lower your blood pressure and may increase certain side effects of amlodipine.
What other drugs will affect amlodipine Norvasc? Tell your doctor about all other medicines you use, especially: This list is not complete and other drugs may interact with amlodipine. Tell your doctor about all medications you use.
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