finerenone

General

Pronunciation:
fin-er-e-none


Trade Name(s)

  • Kerendia

Ther. Class.

none assigned

Pharm. Class.

mineralocorticoid receptor antagonists non steroidal

Indications

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 Effect(s):

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 and 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)

ROUTEONSETPEAKDURATION
POrapid30 min–1.25 hrunknown

Contraindication/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.

Adverse Reactions/Side Effects

CV: hypotension

F and E: hyperkalemia, hyponatremia

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

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 concurrent 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 >5.0 mEq/L.

  • Measure serum potassium 4 wk after starting therapy and adjust dose. If serum potassium ≤4.8 mEq/L, ↑ dose to 20 mg/day if at 10 mg/day or maintain 20 mg/day dose. If serum potassium >4.8–5.5 mEq/L, maintain current 10 mg/day or 20 mg/day dose. If serum potassium >5.5 mEq/L, hold finerenone dose; if at 10 mg/day dose, consider restarting at 10 mg/day once serum potassium ≤5.0 mEq/L; if at 20 mg/day dose, restart at 10 mg/day when serum potassium ≤5.0 mEq/L. Monitor serum potassium 4 wk 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

  • Explain the purpose and side effects of finerenone. Instruct patient to take as directed. Take missed dose as soon as remembered, but only on same day. Do not double doses. Advise patient to read  Patient Information  before starting and with each Rx refill in case of changes.
  • Emphasize the importance of regular lab tests to monitor potassium levels.
  • 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. 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.
  • Rep:   Advise women of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy and for 1 day after last dose.

Evaluation/Desired Outcomes

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