Florinef Acetate

Generic Name: Fludrocortisone Acetate
Class: Adrenals
ATC Class: H02AA02
VA Class: HS502
CAS Number: 514-36-3

Introduction

Synthetic corticosteroid; very potent mineralocorticoid activity.a b

Uses for Florinef Acetate

Used for oral mineralocorticoid replacement therapy; use is contraindicated in all conditions except those that require a high degree of mineralocorticoid activity.b

Adrenocortical Insufficiency

Partial replacement therapy, in combination with hydrocortisone or cortisone, for treatment of primary and secondary adrenocortical insufficiency in Addison’s disease after electrolyte balance has been restored.a b

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Hydrocortisone or cortisone (in conjunction with liberal salt intake) usually is the corticosteroid of choice for replacement therapy; concomitant administration of fludrocortisone may be required in some patients.

Adrenogenital Syndrome

Treatment of salt-losing congenital adrenogenital syndrome after electrolyte balance has been restored.a b

Postural Hypotension

Has been used with some success to increase SBP and DBP in patients with severe, chronic postural hypotension (e.g., secondary to autonomic dysfunction, levodopa therapy) that does not respond adequately to nondrug therapy.b

Florinef Acetate Dosage and Administration

General

  • Dosage depends on the severity of the disease and patient response.a b

  • Titrate dosage to the lowest effective level.a Gradually reduce dosage when possible.a

  • Patients should be continually monitored for signs that indicate dosage adjustment is necessary (e.g., remissions or exacerbations of the disease, stress [surgery, infection, trauma]).a b

Administration

Oral Administration

Administer orally.a b

Manufacturer makes no specific recommendations regarding administration with meals.a

Dosage

Available as fludrocortisone acetate; dosage expressed in terms of the salt.a

Adults

Adrenocortical Insufficiency
Oral

Usually, 0.1 mg daily; dosage may range from 0.1 mg 3 times weekly to 0.2 mg daily.a b

If hypertension occurs, reduce dosage to 0.05 mg daily.a b

Administer concomitantly with cortisone (10–37.5 mg daily in divided doses) or hydrocortisone (10–30 mg daily in divided doses).a b

Adrenogenital Syndrome
Oral

0.1–0.2 mg daily.a b

Postural Hypotension
Oral

0.1–0.4 mg daily has been given to diabetic patients with postural hypotension.b

0.05–0.2 mg daily has been given to patients with postural hypotension secondary to levodopa therapy.b

Prescribing Limits

Adults

Adrenocortical Insufficiency
Oral

Maximum 0.2 mg daily.a b

Adrenogenital Syndrome
Oral

Maximum 0.2 mg daily.a b

Special Populations

Hepatic Impairment

No special population dosage recommendations at this time.a

Renal Impairment

No special population dosage recommendations at this time.a

Geriatric Patients

Careful dosage selection recommended due to possible age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.a

Cautions for Florinef Acetate

Contraindications

  • Systemic fungal infections.a

  • Known hypersensitivity to fludrocortisone or any ingredient in the formulation.a

Warnings/Precautions

Warnings

Adrenocortical Insufficiency

When given in supraphysiologic doses for prolonged periods, glucocorticoids may cause decreased secretion of endogenous corticosteroids by suppressing pituitary release of corticotropin (secondary adrenocortical insufficiency).a c

The degree and duration of adrenocortical insufficiency is highly variable among patients and depends on the dose, frequency and time of administration, and duration of glucocorticoid therapy.c

Withdraw fludrocortisone gradually following long-term therapy with pharmacologic dosages.a c

Adrenal suppression may persist up to 12 months in patients who receive large dosages for prolonged periods.a c

Until recovery occurs, signs and symptoms of adrenal insufficiency may develop if subjected to stress (e.g., infection, surgery, trauma), and replacement therapy may be required.a

Immunosuppression

Increased susceptibility to infections secondary to glucocorticoid-induced immunosuppression.a Certain infections (e.g., varicella [chickenpox], measles) can have a more serious or even fatal outcome in such patients.a (See Increased Susceptibility to Infection under Warnings.)

Administration of live virus vaccines, including smallpox, is contraindicated in patients receiving immunosuppressive dosages of glucocorticoids.a If inactivated viral or bacterial vaccines are administered to such patients, the expected serum antibody response may not be obtained.a

Increased Susceptibility to Infection

Glucocorticoids, especially in large doses, increase susceptibility to and mask symptoms of infection.a

Infections with any pathogen, including viral, bacterial, fungal, protozoan, or helminthic infections in any organ system, may be associated with glucocorticoids alone or in combination with other immunosuppressive agents.a c

Infections may be mild, but they can be severe or fatal, and localized infections may disseminate.c

Do not use, except in life-threatening situations, in patients with viral infections or bacterial infections not controlled by anti-infectives.c

Some infections (e.g., varicella [chickenpox], measles) can have a more serious or even fatal outcome, particularly in children.a c

Children and any adult who are not likely to have been exposed to varicella or measles should avoid exposure to these infections while receiving glucocorticoids.a

If exposure to varicella or measles occurs in susceptible patients, treat appropriately (e.g., VZIG, IG, acyclovir).a

Fatal outcome (e.g., in those developing hemorrhagic varicella) may not always be avoided even if appropriate therapy is initiated aggressively.c

Can reactivate tuberculosis.a Include chemoprophylaxis in patients with a history of active tuberculosis undergoing prolonged glucocorticoid therapy.a Observe closely for evidence of reactivation.a Restrict use in active tuberculosis to those with fulminating or disseminated tuberculosis in which glucocorticoids are used in conjunction with appropriate chemoprophylaxis.a

Fluid and Electrolyte Disturbances

Marked sodium retention with resultant edema, potassium loss, and elevation of BP may occur with small doses of fludrocortisone.a Edema and CHF (in susceptible patients) may occur.a

During long-term therapy, perform periodic electrolyte evaluations.a c

Dietary salt restriction is advisable, and potassium supplementation may be necessary.a

Increased calcium excretion and possible hypocalcemia.a

Ocular Effects

Prolonged use may result in posterior subcapsular cataracts, exophthalmos, and/or increased IOP which may result in glaucoma or may occasionally damage the optic nerve.a c

May enhance the establishment of secondary fungal and viral infections of the eye.a

Use with caution in patients with active ocular herpes simplex infections for fear of corneal perforation.a

General Precautions

Monitoring

During therapy, perform periodic electrolyte and BP evaluations.a (See Fluid and Electrolyte Disturbances under Cautions.)

Endocrine and Metabolic Effects

Administration over a prolonged period may produce various endocrine disorders, including hypercorticism (cushingoid state) or menstrual difficulties; decrease glucose tolerance; produce hyperglycemia; or aggravate or precipitate diabetes mellitus.a c

If glucocorticoid therapy is required in patients with diabetes mellitus, changes in insulin or oral antidiabetic agent dosage or diet may be necessary.b

Exaggerated response to glucocorticoids in hypothyroidism.a

Musculoskeletal Effects

Muscle weakness, loss of muscle mass, osteoporosis, vertebral compression fractures, aseptic necrosis of femoral or humeral heads, or pathologic fractures of long bones may occur during prolonged therapy with glucocorticoids.a c These adverse effects may be especially serious in geriatric or debilitated patients.c

Use with caution in patients with osteoporosis or myasthenia gravis.a

Nervous System Effects

May precipitate mental disturbances ranging from euphoria, insomnia, mood swings, depression and anxiety, and personality changes to frank psychoses.a Use may aggravate emotional instability or psychotic tendencies.a

GI Effects

Corticosteroids should be used with caution in patients with diverticulitis, nonspecific ulcerative colitis (if there is a probability of impending perforation, abscess, or other pyogenic infection), recent intestinal anastomoses, or active or latent peptic ulcer.a

Specific Populations

Pregnancy

Category C.a

Lactation

Glucocorticoids are distributed into milk.a Caution if used in nursing women.a

Pediatric Use

Safety and efficacy not established.a

With long-term use, may delay growth and maturation in children and adolescents.c Monitor carefully the growth and development of pediatric patients receiving prolonged corticosteroid therapy.c Titrate dosage to the lowest effective level.c

Geriatric Use

With prolonged therapy, muscle wasting, muscle pain or weakness, delayed wound healing, and atrophy of the protein matrix of the bone resulting in osteoporosis, vertebral compression fractures, aseptic necrosis of femoral or humeral heads, or pathologic fractures of long bones may occur.a c May be especially serious in geriatric or debilitated patients.a c

Use with caution due to greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy observed in the elderly.a

Hepatic Impairment

Exaggerated glucocorticoid response in patients with cirrhosis.a

Renal Impairment

Use with caution in patients with renal insufficiency.a

Common Adverse Effects

Hypertension, edema, cardiac enlargement, CHF, potassium loss, hypokalemic alkalosis.a

Interactions for Florinef Acetate

Specific Drugs

Drug

Interaction

Comments

Amphotericin B

Increased hypokalemiaa

Monitor serum potassium concentrations frequently; potassium supplementation may be necessarya

Anabolic steroids

Increased risk of edemaa

Use concurrently with caution, particularly in patients with hepatic or cardiac diseasea

Anticoagulants, oral

Decreased PTa

Monitor PT;a may require dosage adjustment of anticoagulanta

Antidiabetic therapy

Increased blood glucose concentrations in diabetes mellitusa

May require dosage adjustment of concurrent insulin and/or oral hypoglycemic agentsa

Aspirin

Increased risk of GI ulcerationa

Decreased serum salicylate concentrations;c when corticosteroids are discontinued, serum salicylate concentration may increase possibly resulting in salicylate intoxicationa

Observe patients receiving both drugs closely for adverse effects of either drug;b monitoring salicylate concentrations may be requireda

May be necessary to increase salicylate dosage when corticosteroids are administered concurrently or decrease salicylate dosage when corticosteroids are discontinueda

Use concomitantly with caution in patients with hypoprothrombinemiaa

Barbiturates

Increased metabolic clearance of fludrocortisone a

Increased dosage of fludrocortisone may be necessarya

Digitalis

Hypokalemia may increase risk of arrhythmias or digitalis toxicitya

Monitor serum potassium concentrations requently; administer potassium supplementation as requireda

Diuretics, potassium-depleting

Increased hypokalemiaa

Monitor serum potassium concentrations frequently; potassium supplementation may be necessary a

Estrogens

Increased levels of corticosteroid-binding globulin result in increased bound (inactive) fractiona

Decreased metabolism of corticosteroida

May be necessary to decrease corticosteroid dosage when estrogen is initiated or increase corticosteroid dosage when estrogen is discontinueda

NSAIAs

Increased risk of GI ulceration

Use concurrently with cautionc

Phenytoin

Increased metabolic clearance of fludrocortisonea

Increased dosage of fludrocortisone may be necessarya

Rifampin

Increased metabolic clearance of fludrocortisonea

Increased dosage of fludrocortisone may be necessarya

Vaccines and toxoids

May cause a diminished response to toxoids and live or inactivated vaccines

Can aggravate neurologic reactions to some vaccines (supraphysiologic dosages)

Live virus vaccines (i.e., smallpox vaccine) not recommended in individuals receiving fludrocortisonea

Generally, defer routine administration of vaccines or toxoids until corticosteroid therapy is discontinueda

May undertake immunization procedures in patients receiving nonimmunosuppressive doses of glucocorticoids or in patients receiving glucocorticoids as replacement therapy (e.g., Addison’s disease)c

Florinef Acetate Pharmacokinetics

Absorption

Bioavailability

Readily absorbed after oral administration.c

Distribution

Extent

Most corticosteroids are rapidly removed from the blood and distributed to muscles, liver, skin, intestines, and kidneys.c Corticosteroids cross the placenta and are distributed into milk.a

Elimination

Metabolism

Metabolized in most tissues, but primarily in the liver, to biologically inactive compounds.a

Half-life

Plasma half-life is ≥3.5 hours.a Biologic half-life is 18–36 hours.a

Stability

Storage

Oral

Tablets

Room temperature; avoid excessive heat.a

Actions

  • Exhibits very potent mineralocorticoid activitya b and high glucocorticoid activity.a

  • Acts on the distal tubules of the kidney to enhance reabsorption of sodium; also increases urinary excretion of potassium and hydrogen ions.a

  • Small doses produce marked sodium retention and increased potassium excretion.a

  • Large doses inhibit thymic activity; suppress pituitary release of corticotropin (thus inhibiting adrenal cortex secretion of endogenous corticosteroids); promote deposition of liver glycogen; and may induce negative nitrogen balance if protein intake is inadequate.a

Advice to Patients

  • Importance of notifying a clinician of any infections, signs of infections (e.g., fever, sore throat, pain during urination, muscle aches), or injuries that develop during therapy or within 12 months after therapy is discontinued.a

  • Importance of carrying identification cards listing the diseases being treated, the glucocorticoid regimen, and the name and telephone number of the clinician.a

  • In immunosuppressed patients, importance of avoiding exposure to certain infections (e.g., chickenpox, measles) and of obtaining medical advice if such exposure occurs.a

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.a

  • Importance of regular follow-up visits and of promptly notifying clinician of dizziness, severe or continuing headaches, swelling of feet or lower legs, or unusual weight gain.a

  • Importance of taking medication only as directed, taking a missed dose as soon as possible, and not doubling the next dose.a

  • Importance of keeping medication out of reach of children.a

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.a

  • Importance of informing patients of other important precautionary information. (See Cautions.)a

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Fludrocortisone Acetate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

0.1 mg

Florinef Acetate (scored)

Monarch

Fludrocortisone Acetate Tablets (scored)

Barr, Global

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Fludrocortisone Acetate 0.1MG Tablets (GLOBAL PHARMACEUTICAL CORP): 30/$24.99 or 90/$63.97

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions June 1, 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

a. Monarch Pharmaceuticals. Florinef (fludrocortisone acetate) tablets prescribing information. Bristol, TN; 2003 Jul.

b. AHFS drug information 2006. McEvoy GK, ed. Fludrocortisone. Bethesda, MD: American Society of Health-System Pharmacists; 2006: 2997-98

c. AHFS drug information 2006. McEvoy GK, ed. Corticosteroids general statement. Bethesda, MD: American Society of Health-System Pharmacists; 2006:2974-87.

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