What Is Esaxeron 5 mg Indications and Uses?

Esaxeron 5 mg (Esaxerenone) is indicated- For the treatment of patients with essential hypertension by lowering both systolic and diastolic blood pressure. Patients with moderate renal impairment, type 2 diabetes mellitus and albuminuria.

Pharmacology (Source, Chemical and Physical Composition) Of Esaxeron 5 mg

Esaxeron 5 mg (Esaxerenone) is a novel, non-steroidal, highly selective mineralocorticoid receptor (MR) antagonist. Esaxerenone selectively binds to the mineralocorticoid receptor, blocking the effects of aldosterone and thereby reducing sodium reabsorption in the renal tubules, leading to a decrease in blood pressure. Unlike some other MR antagonists, Esaxerenone does not exhibit significant binding to other steroid hormone receptors such as the glucocorticoid, progesterone, or androgen receptors, which contributes to its improved selectivity and safety profile.

Dosage And Administration of Esaxeron 5 mg

The recommended starting and standard dose of Esaxeron 5 mg (Esaxerenone) for adults is 2.5 mg taken orally once daily. If blood pressure is not adequately controlled, the dose may be increased to a maximum of 5 mg once daily. For patients with moderate renal impairment (eGFR ≥30 to <60 mL/min/1.73 m²), diabetic patients with albuminuria or proteinuria, or those at higher risk of hyperkalemia, treatment should be initiated at a lower dose of 1.25 mg once daily. After at least 4 weeks, the dose may be increased to 2.5 mg once daily based on serum potassium levels and blood pressure response. Further increase to 5 mg may be considered if blood pressure remains uncontrolled. Serum potassium levels should be monitored within 2 weeks after initiation or dose adjustment and periodically thereafter. Safety and effectiveness in pediatric patients have not been established.

Drug Interactions of Esaxeron 5 mg

Concomitant use with potent CYP3A4 inhibitors (e.g., itraconazole) may increase Esaxeron 5 mg (Esaxerenone) exposure, raising the risk of hyperkalemia. Concomitant use with potent CYP3A4 inducers (e.g., rifampicin) may decrease Esaxeron exposure and reduce its antihypertensive effect. Midazolam exposure is increased by Esaxeron due to CYP3A4 inhibition. Concomitant use with ACE inhibitors, ARBs, or other drugs that increase serum potassium requires caution and frequent monitoring. Esaxeron may slightly increase digoxin levels. No significant interaction was observed with amlodipine.

Side Effects of Esaxeron 5 mg

Increased Blood Potassium Nasopharyngitis Upper Respiratory Tract Infections Headache and Back Pain.

Precautions And Warnings for Esaxeron 5 mg

Hyperkalemia is a significant risk during treatment with Esaxeron 5 mg (Esaxerenone). Serum potassium should be measured before initiation, within 2 weeks after starting or adjusting the dose, and periodically thereafter. Caution is required in patients at higher risk of hyperkalemia, including those with moderate renal impairment, diabetic patients with albuminuria or proteinuria, the elderly, and patients concurrently using drugs that increase potassium levels (e.g., ACE inhibitors, ARBs). Dose reduction or discontinuation should be considered if serum potassium exceeds 5.0 mEq/L. The treatment should be discontinued immediately if serum potassium reaches ≥6.0 mEq/L. Blood pressure and renal function should also be monitored regularly. Caution is advised when administering to patients with severe hepatic impairment.

Use During Pregnancy and Lactation

Esaxeron 5 mg (Esaxerenone) should be avoided during pregnancy. There are no adequate and well-controlled studies of Esaxerenone in pregnant women. Animal studies have shown reduced fetal weight and other reproductive effects at high doses. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Treatment should be discontinued if pregnancy is confirmed. It is not known whether Esaxerenone is excreted in human milk. Animal studies indicate excretion of Esaxerenone in milk. Breastfeeding is not recommended during treatment considering the potential risk to the infant.

Storage Conditions of It

Do not store above 30ºC temperature. Keep away from light and wet place. Keep out of reach of children. Pack Image: Esaxeron 5 mg Tablet Thanks for using MedEx! How would you rate your experience so far?