Finerenone role in chronic Kidney disease

I.Overview

• Finerenone is an potent , Selective,MineraloCorticosteroid receptor antagonist or MRA 
• The drug blocks the overactivation of MineraloCorticosteroid receptors (MR) in kidneys.
• This overactive protein in chronic Kidney disease patients  can cause inflammation,cell injury ,fibrosis which eventually is end up in causing irreversible damage to kidneys 
• So,the drug Finerenone comes into action by targeting and blocking the MR activity .
• Finerenone belongs to Non -steroidal group of drugs ,where  steroidal drugs include spironolactone ,Eplerenone 
• Finerenone is a novel medications with therapeutic interventions beyond the limit unlike Eplerenone and spironolactone by not only  glycemic control and inhibition of RAAS 
• Finerenone is a passive antagonist which works by inhibiting cofactor binding in absence of aldosterone. more over,finerenone is bulky drug

Pharmacokinetics

• The urinary excretion is minimal with very short half life 
• No active metabolites involved 
• Due to its higher tissue distribution and signaling properties considered when compare with steroidal MineraloCorticosteroid antagonists
• Mode of administration is orally ,sometimes for patients who are unable to swallow can be crushed and mixed with the soft foods or water as alternative

II.Uses of finerenone

Almost 40_45% of diabetic patients associated with chronic kidney disease leading to kidney failure or end up with potential cardiovascular diseases 

So ,the finerenone is used in those patients to further prevent the progression of the disease 

• It is used to reduce risk of decline in kidney function
• Kidney failure 
• Cardiovascular death
• Non fatal heart attacks or 
• Hospitalization for heart failures in adults with CKD associated with type 2 diabetic mellitus
• Finerenone plays crucial role in maintaining blood pressure,extracellular fluid volume and also helps is decreased protein in urine in Diabetic Kidney disease patients 

III.Dosage in Chronic kidney disease patients 

The dosage of finerenone is based on the eGFR and serum potassium levels 

• It is recommended for eGFR greater than 25mL/min/m² or serum potassium greater than 4.8 mEq/L to  5.0m EQ/L

• It is not recommended  in patients with eGFR less than 25 mL/min/1.73 m2 and serum potassium is greater than 5 mEq/L.

Renal dosage adjustments

     Initial dosage:

• For eGFR  greater than 60 mL/min/1.73m² 

             Initial dosage should be 20 mg daily  

• For eGFR greater than 25mL/min/1.73m² to 59mL/min/1.73m²

             Dosage includes 10 mg of finerenone daily 

Dosage adjustments 

• If serum potassium remains less than or equal to 4.8mEq/L , Dosage can be titrated from 10 mg daily to 20 mg daily which is a maximum dosage

• If serum potassium is exceeds 5.5mEq/L , finerenone must be hold and cannot be restarted until the serum potassium levels drops less than or equal to 5.0mEq/L

• Following the finerenone initiation careful regular monitoring of serum potassium levels and eGFR should be done for every 4 weeks ,because there are still chances of elevation

For dialysis patients

• The dosage recommendations are still under research but the  drug is highly bound to plasma proteins; 
• So the efficient removal via hemodialysis is unlikely 

IV.Dose in general population 

Usually recommended dosage is 20 mg / day ,no dose adjustments requires 

Patient advice:

• If a dose is missed, take it as soon as you remember but only on the same day, otherwise skip the missed dose and take the next dose as scheduled.
• Periodic monitoring of serum potassium levels is necessary; consult a physician before using potassium supplements or salt substitutes containing potassium.

V.Side effects

The side effects are quite manageable but few need medical attention.These includes majorly 

• Hyperkalemia 
• Hypotension
• Hyponatremia 

Few other side effects which are less common and they include 

• Nausea, vomiting
• Confusion
• Tiredness
• Weakness in legs 
• Tingling sensation of legs ,hands 
• Confusion
• Headache 
• Stomach pain
• Blurred vision
• Muscle cramps 
• Decreased urine output
• Sweating 
• Irregular heart beat 
• Edema 
• Dizziness,syncope 
• Pruritus 
• Anemia 

Note :

• Should not consider in children of age Less than 18 and pregnant women where there are evidences of embryo fetal toxicity and teratogenicity at materno toxic doses

•  Breastfeeding is not recommended during usage  of  finerenone and for 1 day after treatment. It should be discontinued 

VI.Major drug reactions

• Should avoid in patients receiving stimulus treatment strong CYP3A4 inhibitors and those who are suffering with adrenal insufficiency 

• Food interaction might happen on consumption of grapefruit juice due to presence of  high levels of potassium may lead to hyperkalemia which further causes   kidney failure, paralysis ,cardiac arrest and death

• Finerenone should also be avoided in patients suffering from severe liver  impairment.

• Should be avoided in patients on captopril,  cyclosporine, Eplerenone, dexamethasone, erythromycin,fluconazole,losartan , phenytoin ,ramipril,telmisartan,verapamil etc 

VII.Brands available in India 

• This novel invented drug named  finerenone is available with brand name as  kerendia ™ by Bayer Zydus Pharma in 2022 

Frequently asked questions ?