Names and pronunciation
(ep-ler-ee′known) Inspra
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Individual generic drug information
Extracted information for eplerenone only.
(ep-ler-ee′known) Inspra
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Func. class.: Antihypertensive
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Chem. class.: Selective aldosterone receptor antagonist
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Do not confuse: Inspra/Spiriva
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ACTION: Binds to mineralocorticoid receptor and blocks the binding of aldo- sterone, a component of the renin- angiotensin-aldosterone system (RAAS)
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USES: Hypertension, alone or in com- bination with thiazide diuretics, HF, post-MI
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Extracted information for eplerenone only.
CONTRAINDICATIONS: Hyper- sensitivity; increased serum creatinine >2 mg/dL (male), >1.8 mg/dL (female); potassium >5.5 mEq/L, type 2 diabetes with microalbuminuria, hepatic disease, CCr <30 mL/min; CCr <50 mL/min in hypertension Precautions: Pregnancy, breastfeed- ing, children, geriatric patients, impaired renal/hepatic function, hyperkalemia
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SIDE EFFECTS CNS: Headache, dizziness, fatigue CV: Angina, MI GI: Increased GGT, diarrhea, abdominal pain, increased ALT GU: Gynecomastia, mastodynia (males), abnormal vaginal bleeding META: Hyperkalemia, hyponatremia, hypercholesteremia, hypertriglyceride- mia, increased uric acid RESP: Cough
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INTERACTIONS Increase: hyperkalemia—ACE inhibi- tors, angiotensin II antagonists, NSAIDs, potassium supplements, potassium- sparing diuretics; do not use together Increase: serum levels of lithium; moni- tor lithium level Increase: eplerenone levels—erythro- mycin, fluconazole, verapamil; reduce dose of eplerenone Increase: levels of eplerenone—CYP3A4 inhibitors (ketoconazole, itraconazole, saqui- navir, clarithromycin, imatinib, nelfinavir, nefazodone, ritonavir, troleandomycin); do not use concurrently or reduce dose of eplerenone Decrease: antihypertensive effect—NSAIDs Drug/Herb Decrease: antihypertensive effect— ephedra, St. John’s wort Drug/Food • Grapefruit, grapefruit juice—increase product level by 25% • Do not use salt substitutes containing potassium Drug/Lab Test Increase: BUN, creatinine, potassium, cho- lesterol, lipids, uric acid, ALT, BUN, GGT Decrease: sodium
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Extracted information for eplerenone only.
DOSAGE AND ROUTES Hypertension • Adult: PO 50 mg/day initially, may in- crease to 50 mg bid after 4 wk, max 100 mg/day; 25 mg/day max if patient is tak- ing CYP3A4 inhibitors HF or post-MI • Adult: PO 25 mg/day initially, may in- crease to 50 mg/day max after 4 wk Renal dose • Adult: PO CCr <30 mL/min: contrain- dicated; CCr <50 mL/min for HTN: contra- indicated; CCr 30-49 mL/min for HF: 25 mg every other day, max 25 mg daily Dosage adjustments for those receiving moderate CYP3A4 inhibitors • Potassium level <5 mEq/L, increase from 25 mg every other day to 25 mg daily, or increase dose from 25 mg daily to 50 mg daily; potassium level 5 to 5.4 mEq/L no adjustment; potassium level 5.5 to 5.9 mEq/L, decrease dose from 50 mg to E 25 mg, or decrease dose from 25 mg daily to 25 mg every other day; if dose was 25 mg every other day, withhold dose; if potassium is >6 mEq/L, withhold; may restart drug at 25 mg every other day when potassium level is <5.5 mEq/L
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Available forms: Tablets 25, 50 mg
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Administer: • Without regard to food • Do not use salt substitutes containing potassium • Store in tight container at ≤86°F (30°C)
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Extracted information for eplerenone only.
Assess: • Hypertension: B/P at peak/trough level of product, orthostatic hypotension, syn- cope when used with diuretic; monitor lithium level in those also taking lithium; those on CYP3A4 inhibitor should moni- tor potassium at baseline, within first wk, at 1 mo, and more often in diabetes, re- nal disease • Renal studies: protein, BUN, creati- nine; LFTs, uric acid may be increased; contraindicated in CCr <30 mL/min • Potassium levels; hyperkalemia may occur • Pregnancy/breastfeeding: use in pregnancy only if clearly needed; may be excreted in breast milk; do not breastfeed
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Evaluate: • Therapeutic response: decreased B/P
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Not to discontinue product abruptly • Not to use OTC products (cough, cold, allergy) unless directed by prescriber; not to use salt substitutes containing potassium without consulting pre- scriber • To comply with dosage schedule, even if feeling better • That product may cause dizziness, fainting, light headedness; may occur during first few days of therapy • How to take B/P and about normal readings for age group HIGH ALERT
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Extracted information for eplerenone only.
PHARMACOKINETICS Peak 11/2 hr; serum protein binding 50%; half-life 4-6 hr; metabolized in liver by CYP3A4; excreted in urine <5%, feces
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Filter the extracted dose blocks for this individual drug.
Hypertension
• Adult: PO 50 mg/day initially, may in- crease to 50 mg bid after 4 wk, max 100 mg/day; 25 mg/day max if patient is tak- ing CYP3A4 inhibitors HF or post-MI
Candidate age grouping · source page 483
Hypertension
• Adult: PO 25 mg/day initially, may in- crease to 50 mg/day max after 4 wk Renal dose
Candidate age grouping · source page 483
Hypertension
• Adult: PO CCr <30 mL/min: contrain- dicated; CCr <50 mL/min for HTN: contra- indicated; CCr 30-49 mL/min for HF: 25 mg every other day, max 25 mg daily Dosage adjustments for those receiving moderate CYP3A4 inhibitors
Candidate age grouping · source page 483
Hypertension
• Potassium level <5 mEq/L, increase from 25 mg every other day to 25 mg daily, or increase dose from 25 mg daily to 50 mg daily; potassium level 5 to 5.4 mEq/L no adjustment; potassium level 5.5 to 5.9 mEq/L, decrease dose from 50 mg to E 25 mg, or decrease dose from 25 mg daily to 25 mg every other day; if dose was 25 mg every other day, withhold dose; if potassium is >6 mEq/L, withhold; may restart drug at 25 mg every other day when potassium level is <5.5 mEq/L
Candidate age grouping · source page 483