enalapril/felodipine (Discontinued)

Brand and Other Names:Lexxel
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

enalapril/felodipine

tablet

  • 5mg/5mg

LEXXEL (enalapril maleate-felodipine ER) is a combination product, consisting of an outer layer of enalapril maleate surrounding a core tablet of an extended-release felodipine formulation

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Hypertension

Not indicated for initial therapy

Usual dose: enalapril maleate 5 mg/felodipine 5 mg PO qD

Increase to enalapril maleate 10 mg/felodipine 10 mg PO qD if needed after 1-2 week

If control remains unsatisfactory, consider addition of thiazide diuretic

Renal Impairment

Use caution in patients with impaired renal function

Other Information

When LEXXEL is taken with food, the peak concentration of felodipine is almost doubled, and the trough (24-hour) concentration is approximately halved

Felodipine component of LEXXEL has not been shown to be bioequivalent to the available extended-release felodipine

<18 years: Safety/efficacy not established

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Interactions

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and enalapril/felodipine

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            Adverse Effects

            1-10%

            Enalapril

            • Chest pain
            • Cough
            • Dizziness
            • Headache
            • Hypotension
            • Rash

            Felodipine

            • Cough
            • Dizziness
            • Headache
            • Flushing
            • Palpitations
            • Peripheral edema

            Frequency Not Defined

            Enalapril

            • Asthenia
            • Hyperkalemia
            • Nausea
            • Vomiting

            Felodipine

            • Gingival hyperplasia
            • Rash
            • Tachycardia
            • Upper respiratory infection
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            Warnings

            Black Box Warnings

            Enalapril: Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death

            Contraindications

            Hypersensitivity to either component or sulfonamides

            History of angioedema

            Hereditary or idiopathic angioedema

            Bilateral renal artery stenosis

            Pregnancy (2nd and 3rd trimesters): significant risk of fetal and neonatal morbidity and mortality

            Cautions

            CHF, aortic stenosis, hypotension (initially or after dose increases)

            Persistent progressive dermatologic reactions

            Exacerbation of angina (during initiation of treatment, after dose increase, or withdrawal of beta blocker)

            Liver impairment

            Avoid taking with grapefruit juice

            Heart failure or compromised ventricular function

            Excessive hypotension if concomitant diuretics, hypovolemia, hyponatremia

            Risk of hyperkalemia, especially in patients with renal impairment, DM or those taking concomitant K+-elevating drugs

            Aheresis (LDL) with dextran sulfate

            Hypertrophic cardiomyopathy, collagen vascular disease, hemodialysis with high flux membrane, renal or arotic stenosis

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            Pregnancy & Lactation

            Pregnancy Category: C (1st trimester); D (2nd & 3rd trimester)

            Lactation: excreted in breast milk, use caution

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Half-Life

            enalapril: parent drug 1.3 hr, active metabolite (enalaprilat) 11 hr

            felodipine: 10-16 hr

            Absorption

            enalapril 60% bioavailability

            felodipine 20% bioavailability

            Onset

            enalapril: initial 1-4 hr, peak 8-18 hr

            felodipine: 2-5 hr

            Duration

            enalapril: 12-24 hr

            felodipine: 24 hr

            Peak Plasma Time

            enalapril: 1 hr

            felodipine: 2-5 hr

            Protein Bound

            enalapril: 50-60%

            felodipine: 99%

            Metabolism

            enalapril: liver (70%)

            enalapril undergoes hepatic biotransformation to enalaprilat within 4 hr

            felodipine: hepatic P450 enzyme CYP3A4

            Metabolites: enalaprilat (active)

            felodipine: pyridine analog (inactive)

            Clearance

            enalapril: renal 158 mL/min

            felodipine: 823 mL/min

            Excretion

            felodipine: urine 37% feces 10%

            Dialyzable

            enalapril HD: yes

            felodipine HD: no

            Mechanism of Action

            Lexxel is a fixed-combination tablet that combines an angiotensin-converting enzyme (ACE) inhibitor, enalapril, and a calcium channel blocker, felodipine

            Enalapril is a prodrug hydrolyzed in vivo to enalaprilat; enalaprilat prevents conversion of angiotensin I to angiotensin II (a potent vasoconstrictor) through competitive inhibition of angiotensin coverting enzyme (ACE) resulting in decreased plasma angiotensin II concentrations and consequently, blood pressure may be reduced in part through decreased vasoconstriction, increase renin activity, and decrease aldosterone secretion

            Felodipine, a channel blocker: inhibits transmembrane influx of extracellular Ca ions across myocardial and vascular smooth muscle cell membranes, without changing serum calcium concentrations, resulting in inhibition of cardiac and vascular smooth muscle contraction, thereby dilating main coronary and systemic arteries

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