cortisone

Cortisone is a synthetic corticosteroid prodrug that is converted into cortisol in the body. Cortisol is a natural steroid hormone produced in the cortex region of the adrenal glands, hence known as a corticosteroid.

Cortisone is an anti-inflammatory and immunosuppressive drug used to control or reduce inflammation caused by a wide variety of conditions. Cortisone is also used to treat chronic adrenal insufficiency and to supplement inadequate natural cortisol production.

Cortisone inhibits pro-inflammatory signals and promotes anti-inflammatory signals. Cortisone binds to glucocorticoid receptors, protein molecules on cell membranes and activates multiple processes that help reduce inflammation, including:

• Controls the rate of protein synthesis
• Inhibits release of proinflammatory substances
• Prevents migration and aggregation of polymorphonuclear leukocytes (PMN), types of white cells such as neutrophils, eosinophils and basophils that release inflammatory substances
• Reduces capillary permeability to prevent the leakage of inflammatory cells and proteins (cytokines) into the inflammation site
• Prevents migration of fibroblasts, cells that form extracellular matrix, the supportive structure of tissue, and prevents scar tissue formation

Cortisone is administered as oral tablets to treat both adult and pediatric patients with conditions that include the following:

• Severe allergic states: Bronchial asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, perennial or seasonal allergic rhinitis, and serum sickness
• Dermatologic diseases: Severe psoriasis, severe seborrheic dermatitis, bullous dermatitis herpetiformis, exfoliative dermatitis, mycosis fungoides, pemphigus, and severe erythema multiforme (Stevens-Johnson syndrome)
• Endocrine disorders: Primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, hypercalcemia associated with cancer, and nonsuppurative thyroiditis
• Gastrointestinal conditions: Acute episodes of regional enteritis and ulcerative colitis
• Blood disorders: Acquired (autoimmune) hemolytic anemia, congenital (erythroid) hypoplastic anemia, red blood cell anemia (erythroblastopenia), immune thrombocytopenia and secondary thrombocytopenia in adults
• Cancers: Palliative management of leukemias and lymphomas in adults and acute leukemia of childhood
• Ophthalmic conditions: Severe, acute, and chronic allergies and inflammations involving the eye such as allergic conjunctivitis, allergic corneal marginal ulcers, anterior segment inflammation, chorioretinitis, diffuse posterior uveitis and choroiditis, keratitis, herpes zoster ophthalmicus, iritis and iridocyclitis, optic neuritis, and sympathetic ophthalmia
• Rheumatic disorders: As adjunctive therapy for short-term to tide over an acute episode in acute gouty arthritis, acute and subacute bursitis, acute nonspecific tenosynovitis, ankylosing spondylitis, epicondylitis, posttraumatic osteoarthritis, psoriatic arthritis, rheumatoid arthritis (RA), including juvenile RA, and synovitis of osteoarthritis; and as maintenance therapy or during an exacerbation in select case of acute rheumatic carditis, systemic dermatomyositis (polymyositis), and systemic lupus erythematosus
• Respiratory diseases: Aspiration pneumonitis, berylliosis, fulminating or disseminated pulmonary tuberculosis used concurrently with appropriate antituberculosis chemotherapy, Loeffler syndrome not manageable by other means, symptomatic sarcoidosis
• Kidney diseases: To promote urination and remission of protein in urine (proteinuria) associated with idiopathic nephrotic syndrome or lupus erythematosus
• Others: Tuberculous meningitis with subarachnoid block or impending block used concurrently with appropriate antituberculous chemotherapy, and trichinosis with neurologic or myocardial involvement

• Do not prescribe to patients with hypersensitivity to any of the components in the cortisone formulation.
• Do not use cortisone in patients with systemic fungal infection.
• Cortisone is not intended for intravenous use.
• Use the lowest possible dose to control the condition, particularly in elderly patients, and when dosage can be reduced, reduce gradually.
• Corticosteroids can cause suppression of hypothalamic-pituitary-adrenal axis, and potential for adrenal insufficiency after discontinuation, lasting for months. Institute corticosteroid replacement therapy in situations of stress during that period.
• Discontinuation of cortisone can cause withdrawal symptoms including fever, myalgia, arthralgia, and malaise even in patients without adrenal insufficiency. Withdraw with gradual tapering of dose.
• Patients on corticosteroid therapy subjected to unusual stress may require increased dosage of rapid-acting corticosteroids before, during, and after the stressful situation.
• Prolonged use of corticosteroids suppresses the immune system and may increase the risk of secondary infection, activate latent infections, mask acute infection, prolong or exacerbate viral infections, or limit response to killed or inactivated vaccines. Patients should be advised to avoid exposure to chickenpox or measles.
• Patients receiving immunosuppressive doses of corticosteroids should not take live or live, attenuated vaccines.
• Do not use corticosteroids for cerebral malaria or viral hepatitis.
• Amebiasis should be ruled out in patients who have recently traveled to tropical climates or those who have unexplained diarrhea, before initiation of cortisone.
• Use of cortisone in active tuberculosis should be restricted to cases of fulminating or disseminated tuberculosis (TB) in which it is used in conjunction with an appropriate antituberculous regimen. Patients with latent TB should be closely monitored.
• Prolonged use of corticosteroid can lead to cataracts, glaucoma, ocular inflammation and secondary eye infections.
• Cortisone can elevate blood pressure, cause water and sodium retention and increase excretion of potassium and calcium. Patients may require dietary salt restriction and potassium and calcium supplementation.
• Use cortisone with caution in patients with heart failure and/or hypertension.
• Use with caution in patients who have had a recent myocardial infarction. Rupture of left ventricular wall has been reported with corticosteroid use.
• Use with caution in patients with diabetes, corticosteroids can cause hyperglycemia.
• Prolonged use of corticosteroids is associated with development of Kaposi sarcoma, consider discontinuing therapy.
• Corticosteroid use is associated with psychiatric disturbances and exacerbation of pre-existing psychiatric conditions.
• Corticosteroids may cause mood and behavioral disturbances, caution the patient, family and caregivers.
• Acute myopathy has been reported with high-dose corticosteroids given concomitantly with neuromuscular blocking agents or in patients with neuromuscular transmission disorders. it may involve ocular and/or respiratory muscles, monitor creatine kinase.
• Use with caution in myasthenia gravis, may exacerbate symptoms.
• High doses and/or long-term use of corticosteroids have been known to increase bone loss and osteoporotic fractures, use with caution in patients with osteoporosis.
• Use cortisone with caution in gastrointestinal disease because of perforation risk.
• Use with caution in patients with ocular herpes simplex because of possible corneal perforation.
• Use with caution in kidney or liver function impairment, may cause fluid retention.
• Use with caution in patients with a history of seizure disorder, seizures have been reported with adrenal crisis.
• Changes in thyroid status may necessitate dosage adjustments.
• Do not use in the management of head injury, increased mortality has been reported in patients receiving high-dose intravenous methylprednisolone to manage head injuries.
• Corticosteroids may slow down growth and development in pediatric patients, monitor growth regularly.

Common side effects of cortisone include:

• Nausea
• Indigestion
• Reduced intestinal carbohydrate absorption
• Intestinal perforation
• Increased appetite
• Weight gain
• Fluid retention
• Sodium retention
• Reduced serum potassium (hypokalemia)
• Increased alkalinity of body fluids due to hypokalemia (hypokalemic alkalosis)
• Negative nitrogen balance
• Male pattern growth in women (hirsutism)
• Menstrual disorders
• Heart failure in susceptible patients
• Heart muscle (myocardial) rupture after recent heart attack (myocardial infarction)
• Blood clot block in blood vessel (thromboembolism)
• Tiny spots on skin due to bleeding under the skin (petechiae)
• Hives (urticaria)
• Thinning (atrophy) of skin
• Bruising of skin (ecchymosis)
• Redness of skin (erythema)
• Allergic dermatitis
• Excessive sweating (diaphoresis)
• Hypersensitivity reactions
• Swelling under the skin and mucous membranes (angioedema)
• Impaired wound healing
• Bulging eyes (exophthalmos)
• Cataract
• Nosebleed (epistaxis)
• Headache
• Increased intracranial pressure
• Feeling unwell (malaise)
• Vertigo
• Seizure
• Psychosis
• Joint pain (arthralgia)
• Steroid-induced muscle disease (myopathy)
• Tendon rupture
• Asymmetric muscle wasting in lower limbs (amyotrophy)
• Long bone fracture
• Aseptic tissue death (necrosis) of femoral or humeral head

Less common side effects of cortisone include:

• High blood pressure (hypertension)
• Blood clot in vein (venous thrombosis)
• Rapid and irregular heart rate in the atria (atrial fibrillation)
• Abdominal distension
• Peptic ulcer
• Ulcerative inflammation of the esophagus (esophagitis)
• Inflammation of the pancreas (pancreatitis)
• Agitation
• Anxiety
• Distractibility
• Euphoria
• Fear
• Hypomania
• Irritability
• Mood swings
• Lethargy
• Pressured speech
• Restlessness
• Tearfulness
• Brittle bones (osteoporosis)
• Vertebral compression fractures
• Glaucoma, an eye condition with high intraocular pressure that damages the optic nerve
• High blood sugar levels (hyperglycemia)
• Prediabetes
• Onset or exacerbation of diabetes mellitus
• Adrenal suppression
• Development of Cushing syndrome and cushingoid features such as:
  • Moon face
  • Abnormal fat deposits
  • Weight gain around the midsection and upper back
• Abnormally elevated blood fat levels (dyslipidemia)
• Redistribution of body fat
• Growth retardation in children

Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:

• Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
• Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
• Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
• Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

Tablets

• 5 mg
• 10 mg
• 25 mg

Adult:

Anti-inflammatory/Immunosuppressive

• 2.5 mg/kg/day orally divided every 8 hours or 25-300 mg/day orally each day or divided every 12 hours
• 1-5 mg/kg intramuscularly each day

Physiologic Replacement

• 0.5-0.75 mg/kg/day orally divided every 8 hours or 25-35 mg/day
• 0.25-0.35 mg/kg intramuscularly each day

Pediatric:

Anti-inflammatory/Immunosuppressive

• 2.5 mg-10 mg/kg/day orally or 20-300 mg/m2/day orally divided every 6-8 hours

Physiologic Replacement

• 0.5-0.75 mg/kg/day orally or 20-25 mg/sq.meter/day orally divided every 8 hours

Overdose

• There is insufficient data on acute cortisone overdose. Chronic high doses because of prolonged therapy can cause many conditions including hypertension, hyperlipidemia, hyperglycemia, osteoporosis, electrolyte disturbances, immune suppression, and susceptibility to infections.
• Cortisone overdose treatment includes adjusting the dosage or discontinuing cortisone, as well as initiating symptomatic and supportive treatment.

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

• Severe interactions of cortisone include:
  • mifepristone
• Cortisone has serious interactions with at least 73 different drugs.
• Cortisone has moderate interactions with at least 232 different drugs.
• Cortisone has minor interactions with at least 121 different drugs.

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

• There are no adequate and well-controlled studies of cortisone use in pregnant women. There is some suggestion (not fully substantiated) of slightly increased cleft palate risk if corticosteroids are used in pregnancy.
• Use cortisone during pregnancy only if the benefits to the mother outweigh potential fetal risks. Monitor infants born to mothers who have received substantial doses of cortisone during pregnancy for signs of hypoadrenalism.
• Cortisone is present in breast milk and may suppress growth, interfere with natural (endogenous) corticosteroid production, or cause other untoward effects in the breastfed infant. Breastfeeding should be avoided while on cortisone treatment.

• Take cortisone exactly as prescribed, do not take higher or more frequent doses.
• Do not take live or live, attenuated vaccines while receiving cortisone treatment.
• Corticosteroids can increase susceptibility to infections. Take precautions to avoid exposure to infections.
• Report to your physician if you develop infections or severe allergic reactions.
• Corticosteroids may cause mood and behavioral disturbances, notify your physician if you notice any unexplained mood or behavioral changes.
• Store safely out of reach of children.
• In case of overdose, contact your physician or Poison Control.