Fenoldopam Mesylate: A Comprehensive Overview
Fenoldopam Mesylate, marketed under trade names such as Corlopam, is a peripheral
dopamine-1 receptor agonist with potent vasodilatory properties. This medication was developed primarily to manage severe
hypertension, especially in emergency settings. The drug has been an appealing option for clinicians due to its unique mechanism of action and its ability to provide rapid blood pressure control while preserving renal function. Fenoldopam has been extensively researched and utilized by institutions across the globe, including prominent hospitals and research organizations that prioritize cardiovascular health. It has been approved by the FDA for short-term (up to 48 hours) management of severe hypertension and is a crucial tool in the therapeutic arsenal against hypertensive emergencies.
The primary target of Fenoldopam Mesylate is the D1-like dopaminergic receptors located in the arteries and renal arterioles. By activating these receptors, Fenoldopam induces vasodilation, which leads to a significant reduction in blood pressure. It offers the dual benefit of improving renal blood flow and increasing sodium excretion, which is particularly advantageous in patients with compromised kidney function. The research on Fenoldopam's efficacy and safety continues to evolve, with numerous clinical trials and studies emphasizing its potential benefits and applications in various hypertensive crises.
Fenoldopam Mesylate Mechanism of Action
The mechanism of action of Fenoldopam Mesylate revolves around its selective agonism of D1-like dopamine receptors. These receptors are found in vascular smooth muscle and the renal tubules. When Fenoldopam binds to these receptors, it stimulates
adenylate cyclase, leading to an increase in cyclic AMP (cAMP) levels. This biochemical cascade results in the relaxation of vascular smooth muscle cells, thereby causing vasodilation.
One of the remarkable features of Fenoldopam's mechanism is its ability to dilate both peripheral and renal arteries. This dual action not only reduces systemic vascular resistance but also enhances renal perfusion. The increase in renal blood flow boosts diuresis and natriuresis (excretion of sodium in the urine), which can be particularly beneficial in hypertensive patients with
edema or those at risk of
acute kidney injury. Unlike many other antihypertensive agents, Fenoldopam does not cause a significant increase in heart rate, making it a safer option for patients with cardiovascular risks.
How to Use Fenoldopam Mesylate
Fenoldopam Mesylate is administered intravenously, which allows for rapid onset of action and precise titration to achieve the desired blood pressure reduction. The drug is typically initiated at a dose of 0.1 to 0.3 micrograms per kilogram per minute and can be titrated upwards based on the patient’s response. The dose can be increased every 15 minutes if needed, with a typical maximum dose being around 1.6 micrograms per kilogram per minute. The infusion should be prepared and administered using an infusion pump to ensure accurate dosing.
The onset of action of Fenoldopam is swift, usually within 5 minutes of starting the infusion, which makes it highly effective in emergency settings where rapid blood pressure control is crucial. The duration of its effects is also relatively short, allowing for quick adjustments in therapy based on continuous blood pressure monitoring. Fenoldopam is primarily used in inpatient settings such as intensive care units, where patients can be closely monitored for efficacy and side effects. It’s also important to note that the drug should be titrated off rather than abruptly discontinued to avoid rebound hypertension.
What is Fenoldopam Mesylate Side Effects
Like all medications, Fenoldopam Mesylate comes with a range of potential side effects. The most common adverse effects include
headache,
flushing,
dizziness, and
nausea. These side effects are generally related to the vasodilatory action of the drug and are often transient. However, some patients may experience more severe reactions such as
hypotension (an excessively low blood pressure),
tachycardia (increased heart rate), and reflex tachycardia, although these are less common.
Fenoldopam is contraindicated in patients with known hypersensitivity to the drug or any of its components. Caution is advised when using Fenoldopam in patients with
glaucoma or
high intraocular pressure, as the drug can increase intraocular pressure. For patients with severe cardiovascular conditions or those who are volume-depleted, careful monitoring is required to avoid exacerbating these conditions. Additionally, due to its effects on renal blood flow and diuresis, there is a potential risk of electrolyte imbalances, particularly
hypokalemia (low potassium levels), which should be monitored during treatment.
What Other Drugs Will Affect Fenoldopam Mesylate
Fenoldopam Mesylate, like many medications, can interact with other drugs, potentially altering its efficacy or increasing the risk of adverse effects. One important consideration is the use of other antihypertensive agents. While combining Fenoldopam with other antihypertensives can be beneficial for achieving optimal blood pressure control, it also increases the risk of excessive hypotension. Therefore, such combinations should be managed carefully with close monitoring of blood pressure.
Nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce the antihypertensive effects of Fenoldopam due to their potential to cause sodium and water retention. Concurrent use of medications that can increase intraocular pressure, such as corticosteroids, should be approached with caution, especially in patients with or at risk for glaucoma. Additionally, certain diuretics and electrolyte-altering drugs may exacerbate the risk of hypokalemia when used with Fenoldopam, necessitating regular monitoring of serum electrolytes.
In conclusion, Fenoldopam Mesylate is a potent and fast-acting medication used primarily for the management of severe hypertension in emergency situations. Its unique mechanism of action, which includes vasodilation and improved renal perfusion, makes it a valuable option in the therapeutic landscape. However, like all medications, it requires careful administration and monitoring to mitigate potential side effects and drug interactions. With ongoing research and clinical experience, Fenoldopam continues to play a crucial role in the management of hypertensive crises and in improving patient outcomes.
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