Dexamethasone Intensol

Description

DESCRIPTION Dexamethasone Tablets, USP are available for oral administration containing either 0.5 mg, 0.75 mg, 1 mg, 1.5 mg, 2 mg, 4 mg or 6 mg of dexamethasone, USP. Each tablet contains the following inactive ingredients: lactose monohydrate, magnesium stearate, starch, sugar, D&C Yellow #10 (0.5 mg and 4 mg), FD&C Blue #1 (0.75 mg and 1.5 mg), FD&C Green #3 (4 mg and 6 mg), FD&C Red #3 (1.5 mg), FD&C Red #40 (1.5 mg), FD&C Yellow #6 (0.5 mg and 4 mg) and Yellow Iron Oxide (1 mg). Dexamethasone Oral Solution, USP is formulated for oral administration containing 0.5 mg per 5 mL of dexamethasone, USP. The cherry brandy flavored oral solution contains the following inactive ingredients: anhydrous citric acid, cherry brandy flavor, disodium edetate, glycerin, methylparaben, propylene glycol, propylparaben, sorbitol solution and water. Dexamethasone Oral Solution, USP Intensol ™ (Concentrate) is formulated for oral administration containing 1 mg per mL of dexamethasone, USP. In addition, the oral solution contains the following inactive ingredients: alcohol 30% v/v, anhydrous citric acid, benzoic acid, disodium edetate, propylene glycol and water. Dexamethasone, a synthetic adrenocortical steroid, is a white to practically white, odorless, crystalline powder. It is stable in air. It is practically insoluble in water. The empirical formula is C 22 H 29 FO 5 . The molecular weight is 392.46. It is designated chemically as 9-fluoro-11β,17,21-trihydroxy-16α-methylpregna-1,4-diene,3,20-dione and the structural formula is: Chemical Structure

What Is Dexamethasone Intensol Used For?

INDICATIONS AND USAGE Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment in asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, perennial or seasonal allergic rhinitis, and serum sickness. Dermatologic Diseases Bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus, and severe erythema multiforme (Stevens-Johnson syndrome). Endocrine Disorders Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the drug of choice; may be used in conjunction with synthetic mineralocorticoid analogs where applicable; in infancy mineralocorticoid supplementation is of particular importance), congenital adrenal hyperplasia, hypercalcemia associated with cancer, and nonsuppurative thyroiditis. Gastrointestinal Diseases To tide the patient over a critical period of the disease in regional enteritis and ulcerative colitis. Hematologic Disorders Acquired (autoimmune) hemolytic anemia, congenital (erythroid) hypoplastic anemia (Diamond-Blackfan anemia), idiopathic thrombocytopenic purpura in adults, pure red cell aplasia, and selected cases of secondary thrombocytopenia. Miscellaneous Diagnostic testing of adrenocortical hyperfunction, trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used with appropriate antituberculous chemotherapy. Neoplastic Diseases For the palliative management of leukemias and lymphomas. Nervous System Acute exacerbations of multiple sclerosis, cerebral edema associated with primary or metastatic brain tumor, craniotomy, or head injury. Ophthalmic Diseases Sympathetic ophthalmia, temporal arteritis, uveitis, and ocular inflammatory conditions unresponsive to topical corticosteroids. Renal Diseases To induce a diuresis or remission of proteinuria in idiopathic nephrotic syndrome or that due to lupus erythematosus. Respiratory Diseases Berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis. Rheumatic Disorders As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in acute gouty arthritis, acute rheumatic carditis, ankylosing spondylitis, psoriatic arthritis, rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy). For the treatment of dermatomyositis, polymyositis, and systemic lupus erythematosus.

Dosage and Administration

DOSAGE AND ADMINISTRATION For Oral Administration The initial dosage varies from 0.75 mg to 9 mg a day depending on the disease being treated. 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 that maintains an adequate clinical response is reached. 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 the corticosteroid 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. In the treatment of acute exacerbations of multiple sclerosis, daily doses of 30 mg of dexamethasone for a week followed by 4 mg to 12 mg every other day for one month have been shown to be effective (see PRECAUTIONS: Neuro-Psychiatric ). In pediatric patients, the initial dose of dexamethasone may vary depending on the specific disease entity being treated. The range of initial doses is 0.02 mg to 0.3 mg/kg/day in three or four divided doses (0.6 mg to 9 mg/m 2 bsa/day). For the purpose of comparison, the following is the equivalent milligram dosage of the various corticosteroids: Cortisone, 25 mg Triamcinolone, 4 mg Hydrocortisone, 20 mg Paramethasone, 2 mg Prednisolone, 5 mg Betamethasone, 0.75 mg Prednisone, 5 mg Dexamethasone, 0.75 mg Methylprednisolone, 4 mg These dose relationships apply only to oral or intravenous administration of these compounds. When these substances or their derivatives are injected intramuscularly or into joint spaces, their relative properties may be greatly altered. In acute, self-limited allergic disorders or acute exacerbations of chronic allergic disorders, the following dosage schedule combining parenteral and oral therapy is suggested: Dexamethasone sodium phosphate injection, 4 mg per mL First Day: 1 or 2 mL, intramuscularly Dexamethasone tablets, 0.75 mg Second Day: 4 tablets in two divided doses Third Day: 4 tablets in two divided doses Fourth Day: 2 tablets in two divided doses Fifth Day: 1 tablet Sixth Day: 1 tablet Seventh Day: No treatment Eighth Day: Follow-up visit This schedule is designed to ensure adequate therapy during acute episodes, while minimizing the risk of overdosage in chronic cases. In cerebral edema , dexamethasone sodium phosphate injection is generally administered initially in a dosage of 10 mg intravenously followed by 4 mg every six hours...

Side Effects (Adverse Reactions)

ADVERSE REACTIONS (Listed alphabetically, under each subsection) The following adverse reactions have been reported with dexamethasone or other corticosteroids: Allergic Reactions Anaphylactoid reaction, anaphylaxis, angioedema. Cardiovascular Bradycardia, cardiac arrest, cardiac arrhythmias, cardiac enlargement, circulatory collapse, congestive heart failure, fat embolism, hypertension, hypertrophic cardiomyopathy in premature infants, myocardial rupture following recent myocardial infarction (see WARNINGS: Cardio-Renal ), edema, pulmonary edema, syncope, tachycardia, thromboembolism, thrombophlebitis, vasculitis. Dermatologic Acne, allergic dermatitis, dry scaly skin, ecchymoses and petechiae, erythema, impaired wound healing, increased sweating, rash, striae, suppression of reactions to skin tests, thin fragile skin, thinning scalp hair, urticaria. Endocrine Decreased carbohydrate and glucose tolerance, development of cushingoid state, hyperglycemia, glycosuria, hirsutism, hypertrichosis, increased requirements for insulin or oral hypoglycemic agents in diabetes, manifestations of latent diabetes mellitus, menstrual irregularities, secondary adrenocortical and pituitary unresponsiveness (particularly in times of stress, as in trauma, surgery, or illness), suppression of growth in pediatric patients. Fluid and Electrolyte Disturbances Congestive heart failure in susceptible patients, fluid retention, hypokalemic alkalosis, potassium loss, sodium retention, tumor lysis syndrome. Gastrointestinal Abdominal distention, elevation in serum liver enzyme levels (usually reversible upon discontinuation), hepatomegaly, increased appetite, nausea, pancreatitis, peptic ulcer with possible perforation and hemorrhage, perforation of the small and large intestine (particularly in patients with inflammatory bowel disease), ulcerative esophagitis. Metabolic Negative nitrogen balance due to protein catabolism. Musculoskeletal Aseptic necrosis of femoral and humeral heads, loss of muscle mass, muscle weakness, osteoporosis, pathologic fracture of long bones, steroid myopathy, tendon rupture, vertebral compression fractures. Neurological/Psychiatric Convulsions, depression, emotional instability, euphoria, headache, increased intracranial pressure with papilledema (pseudotumor cerebri) usually following discontinuation of treatment, insomnia, mood swings, neuritis, neuropathy, paresthesia, personality changes, psychic disorders, vertigo. Ophthalmic Exophthalmos, glaucoma, increased intraocular pressure, posterior subcapsular cataracts, vision blurred. Other Abnormal fat deposits, decreased resistance to infection, hiccups, increased or decreased motility and number of spermatozoa, malaise, moon face, weight gain.

Drug Interactions

Drug Interactions Aminoglutethimide : Aminoglutethimide may diminish adrenal suppression by corticosteroids. Amphotericin B injection and potassium-depleting agents : When corticosteroids are administered concomitantly with potassium-depleting agents (e.g., amphotericin B, diuretics), patients should be observed closely for development of hypokalemia. In addition, there have been cases reported in which concomitant use of amphotericin B and hydrocortisone was followed by cardiac enlargement and congestive heart failure. Antibiotics : Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance (see Drug Interactions: CYP 3A4 Inducers , CYP 3A4 Inhibitors , and CYP 3A4 Substrates ). Anticholinesterases : Concomitant use of anticholinesterase agents and corticosteroids may produce severe weakness in patients with myasthenia gravis. If possible, anticholinesterase agents should be withdrawn at least 24 hours before initiating corticosteroid therapy. Anticoagulants, oral : Co-administration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports. Therefore, coagulation indices should be monitored frequently to maintain the desired anticoagulant effect. Antidiabetics : Because corticosteroids may increase blood glucose concentrations, dosage adjustments of antidiabetic agents may be required. Antitubercular drugs : Serum concentrations of isoniazid may be decreased. Cholestyramine : Cholestyramine may increase the clearance of corticosteroids. Cyclosporine : Increased activity of both cyclosporine and corticosteroids may occur when the two are used concurrently. Convulsions have been reported with this concurrent use. Dexamethasone suppression test (DST) : False-negative results in the dexamethasone suppression test (DST) in patients being treated with indomethacin have been reported. Thus, results of the DST should be interpreted with caution in these patients. Digitalis glycosides : Patients on digitalis glycosides may be at increased risk of arrhythmias due to hypokalemia. Ephedrine : Ephedrine may enhance the metabolic clearance of corticosteroids, resulting in decreased blood levels and lessened physiologic activity, thus requiring an increase in corticosteroid dosage. Estrogens, including oral contraceptives : Estrogens may decrease the hepatic metabolism of certain corticosteroids, thereby increasing their effect. CYP 3A4 Inducers: Dexamethasone is metabolized by CYP 3A4. Drugs which induce cytochrome P450 3A4 (CYP 3A4) enzyme activity (e.g., barbiturates, phenytoin, carbamazepine, rifampin) may enhance the metabolism of corticosteroids and require that the dosage of the corticosteroid be increased. CYP 3A4 Inhibitors: Concomitant administration of dexamethasone with erythromycin, a moderate CYP 3A4 inhibitor, has the potential to result in increased plasma concentrations of dexamethasone. Ketoconazole, a strong CYP3A4...

Contraindications

CONTRAINDICATIONS Systemic fungal infections (see WARNINGS: Fungal Infections ) and in patients who are hypersensitive to any components of these products.

Pregnancy and Breastfeeding

Pregnancy Teratogenic Effects: Corticosteroids have been shown to be teratogenic in many species when given in doses equivalent to the human dose. Animal studies in which corticosteroids have been given to pregnant mice, rats, and rabbits have yielded an increased incidence of cleft palate in the offspring. There are no adequate and well-controlled studies in pregnant women. Corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Infants born to mothers who have received substantial doses of corticosteroids during pregnancy should be carefully observed for signs of hypoadrenalism.

Nursing Mothers Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from corticosteroids, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Overdosage

OVERDOSAGE Treatment of overdosage is by supportive and symptomatic therapy. In the case of acute overdosage, according to the patient's condition, supportive therapy may include gastric lavage or emesis.

How Supplied

HOW SUPPLIED Dexamethasone Tablets, USP 0.5 mg tablets are supplied as a light yellow, flat tablet with beveled edges, scored on one side and product identification “54 299” debossed on the other side. NDC 0054-8179-25: 10x10 Unit-Dose NDC 0054-4179-25: Bottle of 100 Tablets 0.75 mg tablets are supplied as a pale blue, flat tablet with beveled edges, scored on one side and product identification “54 960” debossed on the other side. NDC 0054-8180-25: 10x10 Unit-Dose NDC 0054-4180-25: Bottle of 100 Tablets 1 mg tablets are supplied as a yellow, flat tablet with beveled edges, scored on one side and product identification “54 489” debossed on the other side. NDC 0054-8174-25: 10x10 Unit-Dose NDC 0054-4181-25: Bottle of 100 Tablets 1.5 mg tablets are supplied as a pink, flat tablet with beveled edges, scored on one side and product identification “54 943” debossed on the other side. NDC 0054-8181-25: 10x10 Unit-Dose NDC 0054-4182-25: Bottle of 100 Tablets 2 mg tablets are supplied as a white, flat tablet with beveled edges, scored on one side and product identification “54 662” debossed on the other side. NDC 0054-8176-25: 10x10 Unit-Dose NDC 0054-4183-25: Bottle of 100 Tablets 4 mg tablets are supplied as a green, flat tablet with beveled edges, scored on one side and product identification “54 892” debossed on the other side. NDC 0054-8175-25: 10x10 Unit-Dose NDC 0054-4184-25: Bottle of 100 Tablets 6 mg tablets are supplied as an aqua, flat tablet with beveled edges, scored on one side and product identification “54 769” debossed on the other side. NDC 0054-8183-25: 10x10 Unit-Dose NDC 0054-4186-25: Bottle of 100 Tablets Store and Dispense Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Dispense in a tight light-resistant, child-resistant container as defined in the USP/NF. Dexamethasone Oral Solution, USP 0.5 mg per 5 mL oral solution is supplied as a (cherry brandy flavored) clear colorless solution. NDC 0054-3177-57: Bottle of 240 mL NDC...