Enoxolone, also known as glycyrrhetinic acid, is a naturally occurring compound derived from licorice root (Glycyrrhiza glabra) and has been studied for its anti-inflammatory, antiviral, and hepatoprotective properties. Its history includes early research into its medicinal effects in traditional herbal medicine, followed by modern pharmacological studies that characterized its biological activities. Enoxolone has been investigated for potential therapeutic applications in liver diseases, viral infections, and inflammatory conditions. While generally considered safe in moderate doses, excessive use can lead to side effects such as hypertension and hypokalemia due to its mineralocorticoid-like activity. Research into Enoxolone continues, particularly for its role in developing novel treatments and combination therapies targeting viral and inflammatory diseases.
BRAND NAMES
Enoxolone, also known as glycyrrhetinic acid, is a compound derived from licorice root, often studied for anti-inflammatory, antiviral, and hepatoprotective properties
MECHANISM OF ACTION
Enoxolone, also known as glycyrrhetinic acid, exerts its pharmacological effects primarily by inhibiting the enzyme 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), which normally converts active cortisol into inactive cortisone in mineralocorticoid-sensitive tissues such as the kidney.
PHARMACODYNAMICS
Enoxolone, the active metabolite of glycyrrhizin, exerts its pharmacological effects through multiple mechanisms. Its primary action is the inhibition of 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), which prevents the conversion of cortisol to inactive cortisone in mineralocorticoid-sensitive tissues, allowing cortisol to activate mineralocorticoid receptors.
ADMINISTRATION
Enoxolone is most commonly administered orally in the form of glycyrrhizin-containing preparations, such as tablets, capsules, syrups, or extracts, because the free acid itself is poorly absorbed.
DOSAGE AND STRENGTH
Enoxolone is typically administered orally in the form of glycyrrhizin-containing preparations, as the free compound is poorly absorbed. For adults, the usual oral dosage ranges from 25 to 150 mg of glycyrrhizin per dose, taken one to three times daily, with a recommended maximum daily intake of 100 mg to minimize the risk of sodium retention, hypokalemia, and hypertension.
DRUG INTERACTIONS
Enoxolone can interact with several drugs due to its mineralocorticoid-like effects and impact on electrolyte balance. Concomitant use with potassium-wasting diuretics or systemic corticosteroids may increase the risk of hypokalemia, edema, and hypertension.
CONTRAINDICATIONS
Enoxolone is contraindicated in individuals with severe hypertension, heart failure, or significant edema, as its mineralocorticoid-like effects can worsen fluid retention and increase blood pressure.
SIDE EFFECTS
Enoxolone is primarily absorbed after the oral ingestion of glycyrrhizin-containing foods or supplements, such as licorice root. Its absorption can be slightly affected by food intake, but no major dietary restrictions are typically required.
TOXICITY
Enoxolone toxicity is primarily related to its mineralocorticoid-like effects, which can lead to pseudoaldosteronism. This manifests as hypertension, sodium and water retention, hypokalemia, edema, and, in severe cases, cardiac arrhythmias.
