Active ingredient: Fludrocortisone - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Anti-inflammatory Agents
• Adrenergic Agents

Dosage Forms

• Tablet

Brands / Synonyms

9 .Alpha. Ff; 9 Alpha Ff; 9 alpha-Fludrocortisone; 9 alpha-Fluorocortisol; 9.Alpha.-Fluorocortisol; 9.Alpha.-Fluorohydrocortisone; Alflorone; Astonin-H; F-COL; F-Cortef; Florinef; Fludrocortisona [Inn-Spanish]; Fludrocortisone; Fludrocortisone Acetate; Fludrocortisonum [Inn-Latin]; Fludrocortone; Fludrone; Fludronef; Fluodrocortisone; Fluohydrisone; Fluohydrocortisone; Fluorocortisol; Fluorocortisone; ZK5

Indications

For partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing adrenogenital syndrome.

Pharmacology

Fludrocortisone is a synthetic adrenocortical steroid possessing very potent mineralocorticoid properties and high glucocorticoid activity. It is indicated as partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison’s disease and for the treatment of salt-losing adrenogenital syndrome. The physiologic action of fludrocortisone acetate is similar to that of hydrocortisone. However, the effects of fludrocortisone acetate, particularly on electrolyte balance, but also on carbohydrate metabolism, are considerably heightened and prolonged. Mineralocorticoids act on the distal tubules of the kidney to enhance the reabsorption of sodium ions from the tubular fluid into the plasma; they increase the urinary excretion of both potassium and hydrogen ions.

Mechanism of Action

Fludrocortisone binds the mineralocorticoid receptor (aldosterone receptor). This binding (or activation of the mineralocorticoid receptor by fludrocortisone) in turn causes an increase in ion and water transport and thus raises extracellular fluid volume and blood pressure and lowers potassium levels.

Absorption

Not Available

Toxicity

Effects of overexposure include irritation, cardiac edema, increased blood volume, hypertension, cardiac arrhythmias, enlargement of the heart, headaches, and weakness of the extremities.

Biotrnasformation / Drug Metabolism

Hepatic, some renal.

Contraindications

Corticosteroids are contraindicated in patients with systemic fungal infections and in those with a history of possible or known hypersensitivity to these agents.

Drug Interactions

When administered concurrently, the following drugs may interact with adrenal corticosteroids.

Amphotericin B or potassium-depleting diuretics (benzothiadiazines and related drugs, ethacrynic acid and furosemide)óenhanced hypokalemia. Check serum potassium levels at frequent intervals; use potassium supplements if necessary .

Digitalis glycosidesóenhanced possibility of arrhythmias or digitalis toxicity associated with hypokalemia. Monitor serum potassium levels; use potassium supplements if necessary.

Oral anticoagulantsódecreased prothrombin time response. Monitor prothrombin levels and adjust anticoagulant dosage accordingly.

Antidiabetic drugs (oral agents and insulin)ódiminished antidiabetic effect. Monitor for symptoms of hyperglycemia; adjust dosage of antidiabetic drug upward if necessary.

Aspirinóincreased ulcerogenic effect; decreased pharmacologic effect of aspirin. Rarely salicylate toxicity may occur in patients who discontinue steroids after concurrent high-dose aspirin therapy. Monitor salicylate levels or the therapeutic effect for which aspirin is given; adjust salicylate dosage accordingly if effect is altered.

Barbiturates, phenytoin, or rifampinóincreased metabolic clearance of fludrocortisone acetate because of the induction of hepatic enzymes. Observe the patient for possible diminished effect of steroid and increase the steroid dosage accordingly.

Anabolic steroids (particularly C-17 alkylated androgens such as oxymetholone, methandrostenolone, norethandrolone, and similar compounds)óenhanced tendency toward edema. Use caution when giving these drugs together, especially in patients with hepatic or cardiac disease.

Vaccinesóneurological complications and lack of antibody response .

Estrogenóincreased levels of corticosteroid-binding globulin, thereby increasing the bound (inactive) fraction; this effect is at least balanced by decreased metabolism of corticosteroids. When estrogen therapy is initiated, a reduction in corticosteroid dosage may be required, and increased amounts may be required when estrogen is terminated.

Corticosteroids may affect the nitrobluetetrazolium test for bacterial infection and produce false-negative results.