finerenone

General

Pronunciation:
fin-er-e-none

Trade Name(s)

  • Kerendia

Ther. Class.
none assigned

Pharm. Class.
mineralocorticoid receptor antagonists non steroidal

Indications

To reduce the risk of sustained eGFR decline, end-stage kidney disease, cardiovascular death, nonfatal myocardial infarction, and hospitalization for heart failure in patients with chronic kidney disease 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 myocardial infarction, and hospitalization for heart failure in chronic kidney disease associated with type 2 diabetes.

Pharmacokinetics

Absorption: 44% absorbed following oral administration.

Distribution: Widely distributed to extravascular 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 is 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 estimated glomerular filtration rate (eGFR) before starting therapy. Do not start therapy if serum potassium is > 5.0 mEq/L.

  • Measure serum potassium 4 wks after starting therapy and adjust dose. If serum potassium is ≤4.8 mEq/L, increase 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.

Evaluation/Desired Outcomes

Reduction of the risk of sustained eGFR decline, end-stage kidney disease, cardiovascular death, nonfatal myocardial infarction, and hospitalization for heart failure in adult patients with chronic kidney disease (CKD) associated with type 2 diabetes

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