Cortisone acetate is a glucocorticoid. Gluco-corticoids are adrenocortical steroids, both naturally occurring and synthetic, which are readily absorbed from the gastrointestinal tract. Cortisone acetate is a white to practically white, odorless, crystalline powder. It is insoluble in water; freely soluble in chloroform; soluble in dioxane; sparingly soluble in acetone; slightly soluble in alcohol.

The chemical name for cortisone acetate is pregn-4-ene-3,11,20-trione, 21-(acetyloxy)-17-hydroxy and the molecular weight is 402.49. The structural formula is represented below:

Cortisone Acetate Tablets are available in 2 strengths: 5 mg or 10 mg. Inactive ingredients: calcium stearate, corn starch, lactose, mineral oil, sorbic acid, sucrose.

Last updated on RxList: 1/6/2005

Cortisone acetate is indicated in the following conditions:

1.Endocrine Disorders

Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the first choice; synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy mineralocor-ticoid supplementation is of particular importance)

Congenital adrenal hyperplasia

Hypercalcemia associated with cancer

Nonsuppurative thyroiditis

2.Rheumatic Disorders

As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in: Psoriatic arthritis Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy)

Ankylosing spondylitis

Post-traumatic osteoarthritis

Acute and subacute bursitis

Synovitis of osteoarthritis

Acute nonspecific tenosynovitis

Epicondylitis Acute gouty arthritis

3.Collagen Diseases

During an exacerbation or as maintenance therapy in selected cases of:

Systemic lupus erythematosus

Acute rheumatic carditis

Systemic dermatomyositis (polymyositis)

4.Dermatologic Diseases

Pemphigus

Exfoliative dermatitis

Bullous dermatitis herpetiformis

Mycosis fungoides Severe erythema multiforme (Stevens-Johnson syndrome)

Severe psoriasis

Severe seborrheic dermatitis

5.Allergic States

Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment.

Seasonal or perennial allergic rhinitis

Contact dermatitis

Atopic dermatitis

Serum sickness

Drug hypersensitivity reactions

Bronchial asthma

6.Ophthalmic Diseases

Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as:

Allergic conjunctivitis

Anterior segment inflammation

Keratitis

Allergic corneal marginal ulcers

Diffuse posterior uveitis and choroiditis

Herpes zoster ophthalmicus

Iritis and iridocyclitis

Optic neuritis

Chorioretinitis

Sympathetic ophthalmia

7.Respiratory Diseases

Symptomatic sarcoidosis

Loeffler’s syndrome not manageable by other means

Fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy

Berylliosis

Aspiration pneumonitis

8.Hematologic Disorders

Idiopathic thrombocytopenic purpura in adults

Acquired (autoimmune) hemolytic anemia

Secondary thrombocytopenia in adults

Erythroblastopenia (RBC anemia)

Congenital (erythroid) hypoplastic anemia

9.Neoplastic Diseases

For palliative management of:

Leukemias and lymphomas in adults

Acute leukemia of childhood

10.Edematous States

To induce a diuresis or remission of protein-uria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus

11.Gastrointestinal Diseases

To tide the patient over a critical period of the disease in: Ulcerative colitis Regional enteritis

12.Miscellaneous

Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculous chemotherapy

Trichinosis with neurologic or myocardial involvement

The initial dosage of cortisone acetate may vary from 25 to 300 mg per day depending on the specific disease entity being treated. In situations of less severity, lower doses will generally suffice; while in selected patients higher initial doses may be required. The initial dosage should be maintained or adjusted until a satisfactory response is noted. If after a reasonable period of time there is a lack of satisfactory clinical response, cortisone acetate should be discontinued and the patient transferred to other appropriate therapy. IT SHOULD BE EMPHASIZED THAT DOSAGE REQUIREMENTS ARE VARIABLE AND MUST BE INDIVIDUALIZED ON THE BASIS OF THE DISEASE UNDER TREATMENT AND THE RESPONSE OF THE PATIENT. After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage which will maintain an adequate clinical response is reached. It should be kept in mind that constant monitoring is needed in regard to drug dosage. Included in the situations which may make dosage adjustments necessary are changes in clinical status secondary to remissions or exacerbations in the disease process, the patient’s individual drug responsiveness, and the effect of patient exposure to stressful situations not directly related to the disease entity under treatment; in this latter situation it may be necessary to increase the dosage of cortisone acetate for a period of time consistent with the patient’s condition. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.

Cortisone Acetate Tablets, USP are available in the following strengths and package sizes:

5 mg

(white, round, scored, imprinted UPJOHN 15)

Bottles of 50 …………………………………………….. NDC 0009-0015-01

10 mg

(white, round, scored, imprinted UPJOHN 23)

Bottles of 100 …………………………………………….. NDC 0009-0023-01

Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP].

Pharmacia & Upjohn Company

A subsidiary of Pharmacia Corporation Kalamazoo, MI 49001, USA, Revised February 2002, 810 931 813 692851

Last updated on RxList: 1/6/2005

Fluid and electrolyte disturbances

Sodium retention

Potassium loss

Fluid retention

Hypokalemic alkalosis

Congestive heart failure in susceptible patients

Hypertension

Musculoskeletal

Muscle weakness

Vertebral compression fractures

Steroid myopathy

Aseptic necrosis of femoral and humeral heads

Loss of muscle mass

Osteoporosis

Tendon rupture, particularly of the Achilles tendon

Pathologic fracture of long bones

Gastrointestinal

Peptic ulcer with possible perforation and hemorrhage

Abdominal distention

Ulcerative esophagitis

Pancreatitis

Increases in alanine transaminase (ALT, SGPT), aspartate transaminase (AST, SGOT) and alkaline phosphatase have been observed following corticosteroid treatment. These changes are usually small, not associated with any clinical syndrome and are reversible upon discontinuation.

Dermatologic

Impaired wound healing

Facial erythema

Thin fragile skin

Increased sweating

Petechiae and ecchymoses

May suppress reactions to skin tests

Neurological

Increased intracranial pressure with papil-ledema (pseudotumor cerebri) usually after treatment

Convulsions

Vertigo

Headache

Endocrine

Menstrual irregularities

Suppression of growth in children

Development of Cushingoid state

Decreased carbohydrate tolerance

Secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery or illness

Manifestations of latent diabetes mellitus Increased requirements for insulin or oral hypoglycemic agents in diabetics

Ophthalmic

Posterior subcapsular cataracts Glaucoma

Increased intraocular pressure Exophthalmos

Metabolic

Negative nitrogen balance due to protein catabolism

The pharmacokinetic interactions listed below are potentially clinically important. Drugs that induce hepatic enzymes such as phenobarbital, phenytoin and rifampin may increase the clearance of corticosteroids and may require increases in corticosteroid dose to achieve the desired response. Drugs such as troleandomycin and ketoconazole may inhibit the metabolism of corticosteroids and thus decrease their clearance. Therefore, the dose of corticosteroid should be titrated to avoid steroid toxicity. Corticosteroids may increase the clearance of chronic high dose aspirin. This could lead to decreased salicylate serum levels or increase the risk of salicylate toxicity when corticosteroid is withdrawn. Aspirin should be used cautiously in conjunction with cortico-steroids in patients suffering from hypopro-thrombinemia. The effect of corticosteroids on oral anticoagulants is variable. There are reports of enhanced as well as diminished effects of anticoagulants when given concurrently with corticosteroids. Therefore, coagulation indices should be monitored to maintain the desired anticoagulant effect.

Last updated on RxList: 1/6/2005

In patients on corticosteroid therapy subjected to unusual stress, increased dosage of rapidly acting corticosteroids before, during, and after the stressful situation is indicated.

Corticosteroids may mask some signs of infection, and new infections may appear during their use. Infections with any pathogen including viral, bacterial, fungal, protozoan or helminthic infections, in any location of the body, may be associated with the use of corti-costeroids alone or in combination with other immunosuppressive agents that affect cellular immunity, humoral immunity, or neutrophil function.¹

These infections may be mild, but can be severe and at times fatal. With increasing doses of corticosteroids, the rate of occurrence of infectious complications increases.² There may be decreased resistance and inability to localize infection when corticosteroids are used.

Prolonged use of corticosteroids may produce posterior subcapsular cataracts, glaucoma with possible damage to the optic nerves, and may enhance the establishment of secondary ocular infections due to fungi or viruses.

Usage in pregnancy: Since adequate human reproduction studies have not been done with corticosteroids, the use of these drugs in pregnancy, nursing mothers or women of childbearing potential requires that the possible benefits of the drug be weighed against the potential hazards to the mother and embryo or fetus. Infants born of mothers who have received substantial doses of corticosteroids during pregnancy, should be carefully observed for signs of hypoadrenalism.

Average and large doses of hydrocortisone or cortisone can cause elevation of blood pressure, salt and water retention, and increased excretion of potassium. These effects are less likely to occur with the synthetic derivatives except when used in large doses. Dietary salt restriction and potassium supplementation may be necessary. All corticosteroids increase calcium excretion.

Administration of live or live, attenuated vaccines is contraindicated in patients receiving immunosuppressive doses of corticosteroids. Killed or inactivated vaccines may be administered to patients receiving immunosuppressive doses of corticosteroids; however, the response to such vaccines may be diminished. Indicated immunization procedures may be undertaken in patients receiving nonimmuno-suppressive doses of corticosteroids.

The use of cortisone acetate in active tuberculosis should be restricted to those cases of fulminating or disseminated tuberculosis in which the corticosteroid is used for the management of the disease in conjunction with an appropriate antituberculous regimen.

If corticosteroids are indicated in patients with latent tuberculosis or tuberculin reactivity, close observation is necessary as reactivation of the disease may occur. During prolonged corticosteroid therapy, these patients should receive chemoprophylaxis.

Persons who are on drugs which suppress the immune system are more susceptible to infections than healthy individuals. Chicken pox and measles, for example, can have a more serious or even fatal course in non-immune children or adults on corticosteroids. In such children or adults who have not had these diseases, particular care should be taken to avoid exposure. How the dose, route and duration of corticosteroid administration affects the risk of developing a disseminated infection is not known. The contribution of the underlying disease and/or prior corticosteroid treatment to the risk is also not known. If exposed to chicken pox, prophylaxis with varicella zoster immune globulin (VZIG) may be indicated. If exposed to measles, prophylaxis with pooled intramuscular immunoglobulin (IG) may be indicated. (See the respective package inserts for complete VZIG and IG prescribing information.) If chicken pox develops, treatment with antiviral agents may be considered. Similarly, corticosteroids should be used with great care in patients with known or suspected Strongyloides (threadworm) infestation. In such patients, corticosteroid-induced immunosuppression may lead to Strongyloides hyperinfection and dissemination with widespread larval migration, often accompanied by severe enterocolitis and potentially fatal gram-negative septicemia.

General Precautions

Drug-induced secondary adrenocortical insufficiency may be minimized by gradual reduction of dosage. This type of relative insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralo-corticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently.

There is an enhanced effect of corticosteroids on patients with hypothyroidism and in those with cirrhosis.

Corticosteroids should be used cautiously in patients with ocular herpes simplex because of possible corneal perforation.

The lowest possible dose of corticosteroid should be used to control the condition under treatment, and when reduction in dosage is possible, the reduction should be gradual.

Psychic derangements may appear when corticosteroids are used, ranging from euphoria, insomnia, mood swings, personality changes, and severe depression, to frank psychotic manifestations. Also, existing emotional instability or psychotic tendencies may be aggravated by corticosteroids.

Steroids should be used with caution in nonspecific ulcerative colitis, if there is a probability of impending perforation, abscess or other pyogenic infection; diverticulitis; fresh intestinal anastomoses, active or latent peptic ulcer; renal insufficiency; hypertension; osteoporosis; and myasthenia gravis.

Growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.

Kaposi’s sarcoma has been reported to occur in patients receiving corticosteroid therapy. Discontinuation of corticosteroids may result in clinical remission.

Information for Patients

Persons who are on immunosuppressant doses of corticosteroids should be warned to avoid exposure to chicken pox or measles. Patients should also be advised that if they are exposed, medical advice should be sought without delay.

REFERENCES

¹ Fekety R. Infections associated with cortico-steroids and immunosuppressive therapy. In: Gorbach SL, Bartlett JG, Blacklow NR, eds.

Infectious Diseases. Philadelphia: WBSaunders Company 1992:1050-1.

² Stuck AE, Minder CE, Frey FJ. Risk of infectious complications in patients taking glucocor-ticoids. Rev Infect Dis 1989:11(6):954-63.

Last updated on RxList: 1/6/2005

Systemic fungal infections and known hypersensitivity to components.

Last updated on RxList: 1/6/2005

ACTIONS

Naturally occurring glucocorticoids (hydrocor-tisone and cortisone), which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states. Their synthetic analogs are primarily used for their potent anti-inflammatory effects in disorders of many organ systems.

Glucocorticoids cause profound and varied metabolic effects. In addition, they modify the body’s immune responses to diverse stimuli.

Last updated on RxList: 1/6/2005

Persons who are on immunosuppressant doses of corticosteroids should be warned to avoid exposure to chicken pox or measles. Patients should also be advised that if they are exposed, medical advice should be sought without delay.

Last updated on RxList: 1/6/2005

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

CORTISONE - ORAL

(KOR-ti-sone)

USES: Cortisone is a corticosteroid hormone (glucocorticoid). It decreases your body's natural defensive response and reduces symptoms such as swelling and allergic-type reactions.

This medication is used to treat conditions such as arthritis, blood/hormone/immune system disorders, allergic reactions, certain skin and eye conditions, breathing problems, and certain cancers.

HOW TO USE: Take this medication by mouth with food or milk to prevent stomach upset. If you take this medication once daily, take it in the morning before 9 AM. If you are taking this medication every other day or on another schedule besides a daily one, it may help to mark your calendar with a reminder.

The dosage and length of treatment are based on your medical condition and response to therapy. Use this medication regularly in order to get the most benefit from it. To help you remember, take it at the same time(s) each day. It is important to continue taking this medication even if you feel well. Follow the dosing schedule carefully, and take this medication exactly as prescribed.

Do not stop taking this medication without consulting your doctor. Some conditions may become worse when this drug is suddenly stopped. Your dose may need to be gradually decreased.

Inform your doctor if your condition persists or worsens.

SIDE EFFECTS: Stomach upset, headache, dizziness, menstrual changes (e.g., delayed/irregular/absent periods), trouble sleeping, increased appetite, or weight gain may occur.

If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: black stools, bone/joint pain, easy bruising/bleeding, fast/pounding/irregular heartbeat, increased thirst/urination, mental/mood changes (e.g., depression, mood swings, agitation), muscle pain, persistent weight gain, puffy face, slow wound healing, seizures, signs of infection (e.g., fever, persistent sore throat), stomach/abdominal pain, swelling of the ankles/feet, thinning skin, trouble breathing, unusual hair growth, unusual skin growths, vision changes, vomit that looks like coffee grounds, weakness.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking cortisone, tell your doctor or pharmacist if you are allergic to it; or to other corticosteroids (e.g., prednisone); or if you have any other allergies.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: untreated active fungal infections.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: bleeding problems, history of blood clots, brittle bones (osteoporosis), diabetes, eye diseases (e.g., cataracts, glaucoma, herpes infection of the eye), heart problems (e.g., congestive heart failure), high blood pressure, other infections (e.g., tuberculosis, herpes), kidney disease, liver problems (e.g., cirrhosis), mental/mood conditions (e.g., psychosis, anxiety, depression), low blood minerals (e.g., low potassium or calcium), stomach/intestinal problems (e.g., ulcer, ulcerative colitis, diverticulitis), underactive thyroid (hypothyroidism).

This medication may mask signs of infection or put you at greater risk of developing very serious infections. Report any injuries or signs of infection (e.g., persistent sore throat/fever/cough, pain during urination, muscle aches) that occur during treatment.

If you have been taking this medication for a long time, your body may not make enough natural hormones while you are under physical stress (e.g., due to infection, surgery, injury). Your dose may need to be adjusted. If you have stopped taking this drug within the past 12 months, you may need to start taking it again if your body is under physical stress. Consult your doctor for more details.

Before having surgery, tell your doctor or dentist that you are using this medication or have taken it within the last 12 months.

Do not have immunizations, vaccinations or skin tests unless specifically directed by your doctor. Live vaccines may cause serious complications (e.g., infection) if given while you are taking this medication. Avoid contact with people who have recently received oral polio vaccine or flu vaccine inhaled through the nose.

Avoid contact with people who have chickenpox or measles unless you have previously had these diseases (e.g., in childhood). If you are exposed to one of these infections and you have not previously had it, seek immediate medical attention.

If you have a history of ulcers or take large doses of aspirin or other arthritis medication, limit alcoholic beverages while taking this medication to decrease the risk of stomach/intestinal bleeding.

If you have diabetes, this drug may make it harder to control your blood sugar levels. Monitor your blood sugar levels regularly and inform your doctor of the results. Your medicine, exercise plan, or diet may need to be adjusted.

This drug may make you dizzy; use caution while engaging in activities requiring alertness such as driving or using machinery. Limit alcoholic beverages.

Caution is advised when using this drug for long periods in children. This medication may temporarily slow down a child's rate of growth, but it will probably not affect final adult height. Monitor your child's height periodically.

This medication should be used only when clearly needed during pregnancy. There have been rare reports of harm to the unborn baby. Discuss the risks and benefits with your doctor. Infants born to mothers who have been using this medication for an extended time may have low levels of corticosteroid hormone. Tell your doctor immediately if you notice symptoms such as persistent nausea/vomiting, severe diarrhea, or weakness in your newborn.

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first.

This drug should not be used with the following medications because very serious interactions may occur: live vaccines, natalizumab.

If you are currently using either of the medications listed above, tell your doctor or pharmacist before starting cortisone.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially: aldesleukin, large doses of aspirin and aspirin-like drugs (salicylates), birth control pills, "blood thinners" (e.g., warfarin), bupropion, diabetes medications, estrogen hormone replacement, mifepristone, nonsteroidal anti-inflammatory drugs (NSAIDs such as indomethacin, ibuprofen), drugs affecting liver enzymes that remove cortisone from your body (such as azole antifungals including ketoconazole, barbiturates including phenobarbital, macrolide antibiotics including erythromycin, rifamycins including rifampin, certain anti-seizure medications including phenytoin), drugs that may cause potassium loss (e.g., amphotericin B, "water pills" such as hydrochlorothiazide or furosemide).

Check all prescription and nonprescription medicine labels carefully since many medications contain pain relievers/fever reducers (NSAIDs such as aspirin, ibuprofen, or naproxen) that may increase the risk of stomach bleeding. Low-dose aspirin, as prescribed by your doctor for specific medical reasons such as heart attack or stroke prevention (usually at dosages of 81-325 milligrams per day), should be continued. Consult your doctor or pharmacist for more details.

This medication may interfere with certain laboratory tests, possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly.

NOTES: Do not share this medication with others.

If this medication is used for an extended time, laboratory and/or medical tests (e.g., blood sugar/mineral levels, blood pressure, eye exams) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

Lifestyle changes that may help reduce the risk of brittle bones (osteoporosis) while taking this drug for an extended time include doing weight-bearing exercise, stopping smoking, getting enough calcium and vitamin D, and limiting alcohol. Discuss with your doctor lifestyle changes that might benefit you.

If you take this medication for long-term treatment, wear or carry identification stating that you are using it. (See also Medical Alert section.)

MISSED DOSE: If you are taking this medication once daily and miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

Ask your doctor ahead of time what you should do if you miss a dose while taking this medication every other day or on another schedule besides a daily one.

STORAGE: Store the US product at room temperature between 68-77 degrees F (20-25 degrees C) away from light and moisture.

Store the Canadian product at room temperature between 59-86 degrees F (15-30 degrees C) away from light and moisture.

Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For enrollment information call MedicAlert at 1-800-854-1166 (USA) or 1-800-668-1507 (Canada).

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.