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Finerenone is prescribed to lower the risk of sustained declines in estimated glomerular filtration rate (eGFR), end-stage kidney disease, cardiovascular death, nonfatal myocardial infarction, and heart failure hospitalizations in adults with chronic kidney disease (CKD) related to type 2 diabetes (T2D).
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✅ Description:
Finerenone is a nonsteroidal mineralocorticoid receptor (MR) antagonist that selectively targets MR, which is activated by aldosterone and cortisol and influences gene expression. By blocking MR-mediated sodium reabsorption and MR overactivation in tissues like the kidneys, heart, and blood vessels, Finerenone helps to counteract fibrosis and inflammation. It has high potency and selectivity for MR, with minimal interaction with other steroid receptors. When used, Finerenone has been shown to reduce systolic blood pressure by 3 mmHg and diastolic blood pressure by 1-2 mmHg. The drug does not prolong the QT interval even at doses up to four times the maximum recommended amount. After oral administration, Finerenone is fully absorbed but has a 44% absolute bioavailability. Peak plasma levels are reached within 0.5 to 1.25 hours. Finerenone’s exposure increases with dose, reaching a steady state in about 2 days. It has a volume of distribution of 52.6 L and is 92% bound to plasma proteins. Its half-life is approximately 2 to 3 hours, and it is primarily metabolized by CYP3A4 with about 80% of the dose excreted in the urine.
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✔️ Composition
✔️ Dosage & Administration
- Starting Dosage: Begin with 10 mg or 20 mg orally once daily, depending on eGFR and serum potassium levels. After 4 weeks, adjust to the target dose of 20 mg once daily, considering eGFR and serum potassium.
- eGFR ≥60 mL/min/1.73 m²: Start with 20 mg once daily.
- eGFR 25 to <60 mL/min/1.73 m²: Start with 10 mg once daily.
- eGFR <25 mL/min/1.73 m²: Not recommended.
- Administration: Tablets can be taken with or without food. For patients who cannot swallow tablets, they can be crushed and mixed with water or soft foods.
✔️ Side Effect
- Common adverse reactions (≥ 1% of patients) include hyperkalemia, hypotension, and hyponatremia.
✔️ Monitoring and Dose Adjustment
- Measure serum potassium 4 weeks after starting treatment or adjusting the dose, and adjust accordingly. If potassium levels are >4.8 to 5.0 mEq/L, consider additional monitoring and dosage adjustments based on clinical judgment.
- For missed doses, take them as soon as possible on the same day, or skip it if it is too late, then continue with the next dose as scheduled.
✔️ Interactions
- Strong CYP3A4 Inhibitors: Avoid using Finerenone with strong CYP3A4 inhibitors due to increased exposure and risk of adverse reactions. Grapefruit and grapefruit juice should also be avoided.
- Moderate and Weak CYP3A4 Inhibitors: Concomitant use may increase Finerenone exposure. Monitor serum potassium and adjust the dose as necessary.
- Strong and Moderate CYP3A4 Inducers: Avoid these as they may reduce Finerenone efficacy by decreasing exposure.
✔️ Contraindications
- Strong CYP3A4 Inhibitors: Avoid use.
- Adrenal Insufficiency: Contraindicated in patients with this condition.
✔️ Use in Special Populations
- Pediatric: Safety and efficacy not established in those under 18.
- Geriatric: No differences in safety or efficacy were observed in older patients. No dose adjustment is needed.
- Hepatic Impairment: Avoid severe hepatic impairment. No dosage adjustment for mild to moderate impairment, but consider additional monitoring.
✔️ Overdose Effects
- Symptoms: Primarily hyperkalemia. Discontinue Finerenone and initiate standard hyperkalemia treatment. Hemodialysis is unlikely to be effective.
✔️ Pregnancy & Lactation
- Pregnancy: Insufficient data on risks. Animal studies show developmental toxicity at high exposures. Use only if needed.
- Lactation: No data on human milk. Animal studies suggest that Finerenone is present in milk and may affect infants. Avoid breastfeeding during treatment and for 1 day after.
✔️ Precautions & Warnings
- Hyperkalemia: Monitor serum potassium and eGFR before starting and during treatment. Avoid initiating if potassium >5.0 mEq/L and adjust doses as needed.
✔️ Storage Conditions
- Store below 30°C, away from light and moisture. Keep out of reach of children.
✔️ Disposal
Discard any unused, expired medicine properly. Do not flush the medicine.
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