finerenone

Therapeutic Classification: none assigned

Pharmacologic Classification: mineralocorticoid receptor antagonists non steroidal

Indications ⬆ ⬇

REMS

Chronic kidney disease (CKD) associated with type 2 diabetes.

Action ⬆ ⬇

Acts as a nonsteroidal, selective antagonist of the mineralocorticoid receptor, which results in reduction in sodium reabsorption and a reduction in fibrosis and inflammation in the heart, blood vessels, and kidneys.

Therapeutic effects:

Reduction in the risk of a sustained eGFR decline, end-stage kidney disease, cardiovascular death, nonfatal MI, and hospitalization for HF in CKD associated with type 2 diabetes.

Pharmacokinetics ⬆ ⬇

Absorption: 44% absorbed following oral administration.

Distribution: Widely distributed to tissues.

Protein Binding: 92%.

Metabolism/Excretion: Primarily metabolized in the liver via the CYP3A4 isoenzyme, and to a lesser extent by the CYP2C8 isoenzyme to inactive metabolites. Primarily excreted in the urine (80%) as metabolites, with 20% being excreted in feces.

Half-Life: 2–3 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	30 min–1.25 hr	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Concurrent use of strong CYP3A4 inhibitors;
Adrenal insufficiency;
Hyperkalemia (serum potassium >5 mEq/L);
eGFR <25 mL/min/m²;
Severe hepatic impairment;
Lactation: Lactation.

Use Cautiously in:

Renal impairment (↑ risk of hyperkalemia) (adjust dose);
Moderate hepatic impairment;
OB: Safety not established in pregnancy;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension

F and E: hyperkalemia, hyponatremia

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors may significantly ↑ levels and risk of hyperkalemia; concurrent use contraindicated.
Moderate CYP3A4 inhibitors, including erythromycin or weak CYP3A4 inhibitors, including amiodarone, may ↑ levels and risk of hyperkalemia; closely monitor serum potassium levels after initiation of or after dosage adjustment of either the CYP3A4 inhibitor or finerenone.
Strong CYP3A4 inducers, including rifampin, or moderate CYP3A4 inducers, including efavirenz, may ↓ levels and effectiveness; avoid concurrent use.
Use with ACE inhibitors, NSAIDs, potassium supplements, angiotensin II receptor antagonists, potassium-sparing diuretics, angiotensin converting enzyme inhibitors, or cyclosporine↑ risk of hyperkalemia.

Drug-Food:

Grapefruit juice or grapefruit may ↑ levels and risk of hyperkalemia; avoid concomitant use.

Route/Dosage ⬆ ⬇

PO (Adults ): 20 mg once daily.

Renal Impairment

PO (Adults ): eGFR 25–<60 mL/min/m²: 10 mg once daily; after 4 wk, may ↑ to 20 mg once daily if serum potassium ≤4.8 mEq/L.

Availability ⬆ ⬇

Tablets: 10 mg; 20 mg

Assessment ⬆ ⬇

Monitor for signs and symptoms of hyperkalemia (fatigue, muscle weakness, paresthesia, confusion, dyspnea, cardiac arrhythmias) during therapy. If symptoms occur, confirm with serum potassium.

Lab Test Considerations:

Measure serum potassium levels and eGFR before starting therapy. Do not start therapy if serum potassium is >5.0 mEq/L.
- Measure serum potassium 4 wk after starting therapy and adjust dose. If serum potassium is ≤4.8 mEq/L, ↑ dose to 20 mg, if at 10 mg/day or maintain 20 mg/day dose. If serum potassium levels are >4.8 to 5.5 mEq/L, maintain current 10 mg/day or 20 mg/day dose. If serum potassium is >5.5 mEq/L, hold finerenone dose. If at 10 mg/day dose, consider restarting at 10 mg/day once serum potassium is ≤5.0 mEq/L. If at 20 mg/day dose, restart at 10 mg/day when serum potassium is ≤5.0 mEq/L. Monitor serum potassium 4 weeks after a dose adjustment and throughout treatment, and adjust the dose as needed.

Implementation ⬆ ⬇

PO: For patients unable to swallow tablets whole, tablets may be crushed and mixed with water or soft foods (applesauce) immediately before use.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take finerenone as directed. Take missed dose as soon as remembered, but only on same day. Do not double doses.
Advise patients to consult with health care professional before using potassium supplements or salt substitutes containing potassium.
Caution patient to avoid grapefruit and grapefruit juice during therapy; may increase the plasma concentration of finerenone.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during and for 1 day after last dose.
Emphasize the importance of regular lab test to monitor potassium levels.

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Pronunciation ⬇

Classifications ⬆ ⬇