Oral Chronic kidney disease associated with type 2 diabetes mellitus
Adult: To reduce the risk of sustained eGFR decline, ESRD, CV death, non-fatal MI, and hospitalisation for heart failure in cases with albuminuria, in addition to standard of care: Recommended target dose: 20 mg once daily. eGFR 25-59 mL/min/1.73 m2: Initially, 10 mg once daily; may increase after 4 weeks to 20 mg once daily based on eGFR and serum K thresholds. eGFR ≥60 mL/min/1.73 m2: Initially, 20 mg once daily. Do not initiate treatment if eGFR is <25 mL/min/1.73 m2 or serum K is >5 mmol/L. Dose adjustment or interruption may be required according to eGFR and serum K thresholds (refer to detailed product guidelines).
Hepatic Impairment
Severe (Child-Pugh class C): Avoid use.
Administration
May be taken with or without food. Swallow whole. For patients w/ swallowing difficulties, tab may be crushed and mixed w/ water or soft foods (e.g. applesauce). Take immediately.
Contraindications
Adrenal insufficiency. Concomitant use with strong CYP3A4 inhibitors.
Special Precautions
Patient with risk factors for hyperkalaemia (e.g. low eGFR, higher baseline K levels, previous episodes of hyperkalaemia). Moderate hepatic impairment (Child-Pugh class B); avoid use in severe hepatic impairment (Child-Pugh class C). Pregnancy and lactation.
Adverse Reactions
Significant: Hyperkalaemia. Investigations: Decreased GFR. Metabolism and nutrition disorders: Hyponatraemia. Skin and subcutaneous tissue disorders: Pruritus. Vascular disorders: Hypotension.
Monitoring Parameters
Measure serum K (at baseline, 4 weeks after initiation of therapy or dosage adjustments, and periodically during therapy), eGFR (at baseline and periodically during therapy), and LFT.
Drug Interactions
Moderate CYP3A4 inhibitors (e.g. erythromycin, verapamil) or weak CYP3A4 inhibitors (e.g. amiodarone, fluvoxamine) may increase finerenone exposure. Increased risk of hyperkalaemia with drugs that increase serum K including K supplements, K-sparing diuretics (e.g. amiloride, triamterene), other mineralocorticoid receptor antagonists (e.g. eplerenone, esaxerenone, spironolactone, canrenone), trimethoprim or trimethoprim + sulfamethoxazole. Strong CYP3A4 inducers (e.g. carbamazepine, phenytoin, phenobarbital, rifampicin) or moderate CYP3A4 inducers (e.g. efavirenz) may decrease the plasma concentration of finerenone. Potentially Fatal: Strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, cobicistat, clarithromycin, telithromycin, ritonavir, nelfinavir, nefazodone) significantly increase finerenone exposure, which may increase the risk of adverse reactions.
Food Interaction
Concomitant intake of grapefruit or grapefruit juice significantly increases the plasma concentration of finerenone; avoid concomitant intake. May reduce plasma concentration with St. John's wort.
Action
Description: Mechanism of Action: Finerenone is a nonsteroidal, selective antagonist of the mineralocorticoid receptor (MR), which is activated by cortisol and aldosterone and regulates gene transcription. It blocks MR-mediated Na reabsorption and decreases MR overactivation in both epithelial (e.g. kidney) and nonepithelial (e.g. blood vessels, heart) tissues, thereby reducing inflammation and fibrosis. Pharmacokinetics: Absorption: Almost completely absorbed. Bioavailability: 44%. Time to peak plasma concentration: 0.5-1.25 hours. Distribution: Plasma protein binding: 92%, mainly to albumin. Metabolism: Metabolised in the liver mainly by CYP3A4 (90%) and to a lesser extent by CYP2C8 (10%) into 4 major inactive metabolites. Excretion: Mainly via urine (approx 80%; <1% as unchanged drug); faeces (approx 20%; <0.2% as unchanged drug). Elimination half-life: Approx 2-3 hours.
Chemical Structure
Finerenone Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 60150535, Finerenone. https://pubchem.ncbi.nlm.nih.gov/compound/Finerenone. Accessed Feb. 27, 2023.
C03DA05 - finerenone ; Belongs to the class of aldosterone antagonists. Used as potassium-sparing diuretics.
References
Anon. Finerenone. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/01/2023.Anon. Finerenone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/01/2023.Buckingham R (ed). Finerenone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/01/2023.Joint Formulary Committee. Finerenone. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/01/2023.Kerendia 20 mg Film Coated Tablets (Bayer plc). MHRA. https://products.mhra.gov.uk. Accessed 04/01/2023.Kerendia Tablet, Film Coated (Bayer Healthcare Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/01/2023.Kerendia Tablets (Bayer HealthCare Limited [HK]). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 16/02/2023.
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