Is amlodipine a vasodilator
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Amlodipine as a Vasodilator: Mechanisms and Clinical Implications
Introduction to Amlodipine and Vasodilation
Amlodipine is a dihydropyridine calcium channel blocker widely recognized for its potent vasodilatory effects. It achieves vasodilation by inhibiting calcium influx through 'slow' channels in peripheral vascular and coronary smooth muscle cells, leading to significant dilation in these vascular beds 1. This mechanism underpins its efficacy in treating conditions such as hypertension and angina pectoris.
Mechanisms of Vasodilation
Calcium Channel Blockade
Amlodipine's primary mechanism involves blocking L-type calcium channels, which reduces calcium influx into vascular smooth muscle cells. This action decreases vascular resistance and leads to vasodilation 16. The drug's slow association and dissociation with calcium channels contribute to its prolonged duration of action, making it effective for once-daily dosing 6.
Nitric Oxide and cGMP Pathways
In addition to calcium channel blockade, amlodipine stimulates the release of nitric oxide (NO), which further enhances vasodilation. NO activates guanylate cyclase, increasing cyclic guanosine monophosphate (cGMP) production, which relaxes vascular smooth muscle 3. This dual mechanism of action underscores amlodipine's potent vasodilatory properties.
Clinical Evidence of Vasodilatory Effects
Hypertension Management
Clinical studies have demonstrated that amlodipine effectively reduces blood pressure in hypertensive patients. It increases arterial compliance and reduces mean blood pressure significantly compared to placebo 2. These effects are consistent across various patient populations, including those with mild to moderate hypertension 19.
Angina Pectoris
Amlodipine is also effective in managing angina pectoris. It improves blood flow in coronary arteries, reducing the frequency and severity of angina attacks 17. Its vasodilatory action helps alleviate the symptoms of chronic stable angina and vasospastic angina, providing significant relief to patients.
Pulmonary Hypertension
Emerging evidence suggests that amlodipine can produce acute pulmonary vasodilation in patients with pulmonary hypertension. Studies have shown that it decreases mean pulmonary artery pressure and pulmonary vascular resistance, indicating its potential utility in this condition 5.
Adverse Effects Related to Vasodilation
While amlodipine is generally well-tolerated, its vasodilatory effects can lead to adverse events such as peripheral edema, flushing, and headaches. These side effects are typically mild to moderate and do not outweigh the therapeutic benefits for most patients 19.
Conclusion
Amlodipine is a potent vasodilator with a well-established role in the management of hypertension and angina pectoris. Its dual mechanism of action, involving calcium channel blockade and NO-mediated vasodilation, makes it highly effective in reducing vascular resistance and improving blood flow. Despite some vasodilatory side effects, amlodipine remains a valuable therapeutic option for cardiovascular disease management. Further research may expand its use in conditions like pulmonary hypertension, highlighting its versatility as a vasodilator.
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Most relevant research papers on this topic
Amlodipine
Amlodipine is an effective and well-tolerated alternative to other cardiovascular agents for treating essential hypertension and chronic stable angina pectoris.
Highly CitedAmlodipine induces a flow and pressure-independent vasoactive effect on the brachial artery in hypertension.
Amlodipine reduces mean blood pressure and increases arterial compliance in hypertensive men, but does not significantly affect flow-dependent vasodilation.
RCTMethylene blue in the treatment of refractory shock from an amlodipine overdose.
Methylene blue effectively treats refractory shock in patients with amlodipine toxicity by inhibiting guanylate cyclase and scavenging nitric oxide.
Case ReportArterial vasodilator effects of the dihydropyridine calcium antagonist amlodipine alone and in combination with verapamil in systemic hypertension.
Amlodipine alone and combined with verapamil significantly increase arterial blood flow in patients with primary hypertension, potentially due to interactions between distinct calcium antagonists at distinct binding sites.
Non-RCTAcute pulmonary vasodilatory properties of amlodipine in humans with pulmonary hypertension.
Oral amlodipine can produce acute pulmonary vasodilatation in patients with pulmonary hypertension, potentially benefiting primary pulmonary hypertension treatment.
Non-RCTPharmacologic profile of amlodipine.
Amlodipine is a potent calcium antagonist and effective oral antihypertensive agent with natriuretic properties, making it a potential first-line treatment for hypertension.
Non-RCT
Animal StudyHighly CitedAmlodipine: a new calcium antagonist
Amlodipine is an effective and well-tolerated treatment for hypertension and angina, offering advantages over other calcium antagonists in patients with systolic dysfunction-related congestive heart failure.
Novel Vascular Biology of Third-Generation L-Type Calcium Channel Antagonists: Ancillary Actions of Amlodipine
Amlodipine, a third-generation calcium channel blocker, has pharmacologic actions distinct from L-type calcium channel blockade, potentially contributing to its beneficial effects in treating vascular diseases.
Highly CitedAmlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease.
Amlodipine effectively lowers mild to moderately elevated blood pressure and relieves angina symptoms, offering potential for patients with angina pectoris and congestive heart failure.
Highly CitedVasodilation in patients with calcium channel blocker poisoning treated with high-dose insulin: a comparison of amlodipine versus non-dihydropyridines
Amlodipine-poisoned patients treated with high-dose insulin require more vasopressors, higher doses of epinephrine, and more often receive rescue methylene blue than similarly treated patients with non-dihydropyridine CCB poisoning.
Observational Study