Corlopam

Uses

Corlopam is a dopamine D1 receptor agonist used for the short term management of hypertension.

For the in-hospital, short-term (up to 48 hours) management of severe hypertension when rapid, but quickly reversible, emergency reduction of blood pressure is clinically indicated, including malignant hypertension with deteriorating end-organ function.

Corlopam is also used to associated treatment for these conditions: Malignant Hypertension, Severe Hypertension

How Corlopam works

Corlopam is a rapid-acting vasodilator. It is an agonist for D₁-like dopamine receptors and binds with moderate affinity to α₂-adrenoceptors. It has no significant affinity for D₂-like receptors, α₁ and β-adrenoceptors, 5_HT1 and 5_HT2 receptors, or muscarinic receptors. Corlopam is a racemic mixture with the R-isomer responsible for the biological activity. The R-isomer has approximately 250-fold higher affinity for D₁-like receptors than does the S-isomer. In non-clinical studies, fenoldopam had no agonist effect on presynaptic D₂-like dopamine receptors, or α or β -adrenoceptors, nor did it affect angiotensin-converting enzyme activity. Corlopam may increase norepinephrine plasma concentration.

Toxicity

The most likely reaction of overdose would be excessive hypotension which should be treated with drug discontinuation and appropriate supportive measures.

Food Interaction

• Take on an empty stomach. Orally administered fenoldopam should be taken in a fasted state for optimal absorption.

Corlopam Alcohol interaction

[Moderate]

Many psychotherapeutic and CNS-active agents (e.g., anxiolytics, sedatives, hypnotics, antidepressants, antipsychotics, opioids, alcohol, muscle relaxants) exhibit hypotensive effects, especially during initiation of therapy and dose escalation.

Coadministration with antihypertensives and other hypotensive agents, in particular vasodilators and alpha-blockers, may result in additive effects on blood pressure and orthostasis.

Caution and close monitoring for development of hypotension is advised during coadministration of these agents.

Some authorities recommend avoiding alcohol in patients receiving vasodilating antihypertensive drugs.

Patients should be advised to avoid rising abruptly from a sitting or recumbent position and to notify their physician if they experience dizziness, lightheadedness, syncope, orthostasis, or tachycardia.

Corlopam Drug Interaction

Moderate: diltiazem, diltiazem, losartan, losartanUnknown: amoxicillin / clavulanate, amoxicillin / clavulanate, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, cyclophosphamide, cyclophosphamide, meperidine, meperidine, glucose, glucose, fentanyl, fentanyl, heparin, heparin, sodium iodide, sodium iodide

Corlopam Disease Interaction

Major: congestive heart failure, glaucoma, hypokalemia, hypotension, tachycardia

Half Life

The elimination half-life is about 5 minutes in mild to moderate hypertensives, with little difference between the R (active) and S isomers.

Elimination Route

Radiolabeled studies show that about 90% of infused fenoldopam is eliminated in urine, 10% in feces. Elimination is largely by conjugation, without participation of cytochrome P-450 enzymes. Only 4% of the administered dose is excreted unchanged.

Innovators Monograph

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