Inhibitors of CYP450 3A4 -
Do not use with drugs described as strong inhibitors of CYP3A4

Use with ACE inhibitors-
 Eplerenone 200mg combined with ACE  inhibitors enalapril 10mg increased frequency
  of hyperkalemia than on enalapril alone

Lithium-
Drug interaction study of eplerenone with Lithium has not been conducted

Lithium toxicity has been reported in patients receiving lithium concomittantly with
diuretics and ACE inhibitors.

Monitor serum lithium levels frequently if eplerenone is coadministered with lithium

NSAIDs- drug interaction  study with eplerenone not conducted.
Adminstration of other potassium sparing antihypertensives with NSAIDs  has been
shown to reduce anti-hypertensive effects in some patients and result in severe hyperkalemia
in patients with impaired renal function

When eplerenone and NSAIDs are used concomittantly observe patients to detremine whether
the desired effect on blood pressure is obtained

Congestive heart failure

Hypertension

Frequently incidence of adverse reactions-
Hyperkalemia (3.4% ), increased creatinine (2.4%),

Others-
Dizziness, (3%)
Abdominal pain ( 1%),diarrhea ( 2%)
Albuminuria 1%
Hypercholesterolemia  (1% ) Hypertriglyceridemia  (1%)

 

Serum potassium greater than 5.5 mEq/L  at initiation

Creatinine clearance less than or equal to 30mL/min

Concomittant use with following potent CYP3A4 inhibitors-
Clarithromycin, itraconazole, ketoconazole, nefazodone, nelfinavir, rotonavir, and troleandomycin

Do not use eplerenone with other drugs noted to be potent  CYP3A4 inhibitors-

Special precautions-
Hyperkalemia-
Principal risk of Eplerenone is hyperkalemia.
Hyperkalemia cause serious sometimes fatal arrhythmias.
Minimise hyperkalemia by proper patient selection , avoidance of certain concomittant
treatments, and perodic monitoring until effect of eplerenone is established

Renal function impairment-
Eplerenone is contraindicated  in patients with serum potassium greater than 5.5mEq/L
at initiation  and/ or creatinine clearance less than or equal to 30mL/min

Pregnancy-
No adeaquate and well controlled studies on pregnant women
Use only if required

Lactation-
Because of potential adverse reaction to breast-feeding infant, decide based on importance
of the drug to the mother

Children-
Safety and efficacy of eplerenone have not been established

 

Congestive heart failure

Hypertension

Recommended dosage is 25mg once daily and titrate to the target dosage of 50mg once daily
preferably within  4 weeks as tolerated by the patient

Administer Eplerenone with or without food

1. Inform patients using eplerenone not to use potassium supplements , salt substitutes
  containing potassium  or cotraindicated without consulting their doctors.

Pharmacology-

Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldersterone a component renin-angiotensin -alderstrone system RAAS Aldersterone binds to mineralocorticoid receptors in both epithelial eg.kidney and non-epithelial (eg. heart , blood vessels, brain ) tissues and increases blood pressure through induction of sodiun reabsorption and possibly other mechanisms.

Pharmcokinetics-

Absorption - not affected by food Following oral administration, mean peak plasma concentrations are reached in approximately 12.5 hours

Eplerenone is metabolised primarily via CYP3A4. steady state is reached within 2 days

The elimination half-life of epleronone is approximately 4 to 6 hours

Administer Eplerenone with or without food

Pregnancy-

No adeaquate and well controlled studies on pregnant women made Use only if required

Lactation-

Because of potential adverse reaction to breast-feeding infant, decide based on importance of the drug to the mother

Children-

Safety and efficacy of eplerenone have not been established