Cortisone: how is it used? Side Effects and Warnings

Index

  • Introduction: what is it?
  • Dosage: how is it used and how does it work?
  • Warnings and Precautions
  • Interactions and side effects
  • Pregnancy and breastfeeding

Questions and answers

Introduction: what is it?

Cortisone is a natural hormone belonging to the class of corticosteroids , substances with a structural formula closely related to corticosterone. Corticosteroids and adrenaline are hormones released into the blood by the adrenal glands in stressful situations. Glucocorticoids are adrenocortical steroids, which can be found both naturally and synthetic, and which are readily absorbed from the gastrointestinal tract. They raise blood pressure and prepare the body for the fight or flight reaction. Cortisone is the inactive precursor of the cortisol molecule , the active form of cortisone, also called hydrocortisone.

Cortisone is used in thetreatment of various ailments . Cortisones are anti – inflammatory and immunosuppressive drugs , with a structure similar to endogenous corticosteroids. The latter are synthesized by the adrenal glands starting from cholesterol and are divided into two categories: that of mineralocorticoids and that of glucocorticoids (depending on whether the action mainly affects the balance of sugars or salts and liquids ).

The synthetic steroids have a similar structure to those endogenousand as such they are characterized by the presence of a chemical structure similar to that of cholesterol and steroid hormones. It is possible to intervene on the basic structure by making substitutions at the level of the carbon atoms to increase its anti-inflammatory power and reduce the side effects on metabolism.

The corticosteroids bind to specific protein receptors in target tissues and regulate the ‘ expression of genes that are sensitive to the presence of corticosteroids, by modulating the levels and types of proteins synthesized by the various target tissues. Many of the effectsof corticosteroids are not immediate but only become evident after several hours . In fact, in the clinical setting, it is often necessary to wait a certain time before the beneficial effects of therapy with corticosteroids occur.

Corticosteroids have several effects , including a modulation of the metabolism of carbohydrates , proteins and lipids . They intervene in maintaining the balance of fluids and electrolytes , as well as in preserving the normal function of the cardiovascular system , the immune system , kidneys ,skeletal , endocrine and nervous system muscles . Furthermore, corticosteroids allow the body to resist stress-generating and harmful stimuli, as well as adapt to changes in the surrounding environment. In the absence of adequate secretion of corticosteroids by the adrenal glands, any stresses such as infections, trauma and exposure to extreme temperatures can be fatal .

The therapeutic indications of cortisone when used as a drug are quite numerous. Just to cite a few examples, cortisones are classically used in the presence of arthritis, joint pain and inflammation, dermatitis, allergic reactions, asthma, rhinitis, systemic lupus erythematosus, chronic autoimmune hepatitis and inflammatory bowel diseases. However, their use remains palliative , that is, intended to alleviate the symptoms of a disease without removing the cause.

More specifically, the indications for the use of corticosterone are as follows:

  • Conditions of rheumatological interest as adjunctive therapy for short-term administration (to help the patient overcome an acute episode or exacerbation) in rheumatoid arthritis(special cases may require low-dose maintenance therapy), acute non-specific tenosynovitis, acute bursitis and subacute, acute gouty arthritis.
  • Collagen diseases : during an exacerbation or as maintenance therapy in particular cases of systemic lupus erythematosus, acute rheumatic carditis.
  • Dermatological affections : pemphigus.
  • Allergic forms : to control severe or debilitating allergic conditions that cannot be treated conventionally such as bronchial asthma, contact dermatitis, atopic dermatitis.
  • Ophthalmic diseases: chronic and acute severe inflammatory and allergic processes involving the eye and its appendages.
  • Neoplasms (palliative purposes only): leukemia and lymphomas in adults, acute leukemia in childhood.
  • Conditions that require hormone replacement therapy , including Addison’s disease, acute adrenal insufficiency, Waterhouse-Friderichsen syndrome, postoperative adrenal insufficiency.
  • Gastrointestinal diseases : as an adjuvant in the treatment of ulcerative colitis, intractable sprue, regional enteritis.

In cortisone it is available as tablets containing 25 mg cortisone acetate. It is sold in pharmacies after presentation of the medical prescription.

Dosage: how is it used and how does it work?

Cortisone inhibits the formation of chemicals responsible for the inflammatory reaction , such as prostaglandins and histamine, some of the substances produced and released by our body as a reaction to the onset of an infection or the attack of any external agent.

The dosage of cortisone does not depend so much on the specific diagnosis as on the severity , prognosis , foreseeable duration of the disease and the individual response . The posologies described below can serve as guidance to the physician, but should be adapted to the individual patient based on the opinion of thedoctor .

The tablets should be administered in 2-4 divided doses per day . The first dose is taken during or after breakfast . Further administrations may be necessary in case of particularly intense manifestations of inflammation with nocturnal accentuation. The treatment with cortisone can not be stopped suddenly , the initial dosage as well as the reduction must be agreed with your doctor and must be performed so much more gradual and slow as further prove the dose and duration of treatment.

Primary chronic polyarthritis, chronic asthma , chronic diseases and other chronic forms usually non-lethal:

  • attack dose : 80-100 mg per day until satisfactory response is obtained; usually for 1 to 2 weeks.
  • maintenance dose : gradually reduce the attack dose by 5-15 mg every 4-5 days until the minimum suitable daily maintenance dose is reached: usually 50-75 mg.

Severe seasonal asthma, acute circumscribed ocular diseases and other circumscribed morbid forms :

  • first day : 200-300 mg; second day : 100-200 mg; third day : 100 mg.
  • Thereafter, gradually reduce the dosage and finally discontinue. In the infectious processes of the eye, associate an adequate antibiotic therapy .

Acute articular rheumatism and other acute morbid forms that are progressing or with a fatal evolution or leading to permanent organic damage :

  • attack dose : first day, up to 400 mg; thereafter 200 mg per day until a satisfactory response is obtained.
  • maintenance dose : gradually reduce to 100 mg or less per day until remission seems likely; resume treatment in the event of a relapse.

Disseminated lupus erythematosus , pemphigus and other prolonged or usually fatal diseases :

  • attack dose : first day 400 mg or more; then 200 mg or more per day until satisfactory response is obtained.
  • maintenance dose : gradually reduce to 100 mg or less per day. Continue indefinitely or until remission seems likely. Afterwards, gradually discontinue; however, resume treatment in case of relapses.

Asthmatic status, Waterhouse-Friederichsen syndrome , laryngeal edema, acute episodes of disseminated lupus erythematosus and other acute life-threatening conditions:

  • In the first few days : 300-450 mg or more, then reduce to maintenance dosage or discontinue.

Addison’s disease or adrenalectomy :

  • 10-20 mg or sometimes more , per day combining 4-6 g of sodium chloride or 1-3 mg of deoxycorticosterone acetate.
  • In the event of a crisis , surgery, or other major stressful state, 100-300 mg or more per day until the unusual stress is overcome and normal nutrition is resumed.

Warnings and Precautions

The use of cortisone is contraindicated in patients suffering from tuberculosis , gastro-duodenal ulcer , psychosis , systemic mycotic infections , ocular herpes simplex , recent intestinal anastomosis or hypersensitivity to this drug. Although tuberculosis, recent intestinal anastomoses and herpes simplex of the eye are almost absolute contraindications, the use of cortisone acetate is justified if the patient suffers from a potentially fatal or potentially fatal disease.make him lose his sight , and that he is susceptible to therapy with this hormone.

It is advisable to always use the minimum dosage of cortisone necessary for the control of the disease, implementing a gradual reduction in dosage as soon as possible. Medium or high dosages of hydrocortisone or cortisone can cause increased blood pressure , water and salt retention , or excessive potassium depletion . Such effects are less likely to occur with synthetic cortisone derivatives unless they are used in high dosages. You may need to adopt alow salt regime and an additional potassium intake . All corticosteroids increase calcium excretion. During prolonged therapy it may be appropriate to adopt an anti- ulcer regimen including an antacid, as a precaution.

In patients under corticosteroid therapy exposed to considerable stress, an increase in the dosage of fast-acting corticosteroids is indicated , before, during and after the stressful situation. Always consult a doctor before taking cortisone. A possible adrenal insufficiency secondary induced by the drug can be reduced to a minimum through a gradual reduction of the doseof cortisone. However, this type of relative insufficiency may persist for a few months after discontinuation of therapy. In any stressful situation that occurs during this period, it is therefore advisable to resume hormone therapy .

If the patient is already on steroid treatment , an increase in dosage may be necessary. Since mineralocorticoid secretion may be inadequate, concomitant administration of a mineralocorticoid is advisable . After long-term therapy, discontinuation of corticosteroids could cause a syndrome characterized by fever, myalgia, arthralgia, and feeling unwell. This can also happen in patients without evidence of adrenal insufficiency. Patients should not be vaccinated against smallpox

during corticosteroid therapy . Other procedures involving the immune system should not be implemented in patients treated with corticosteroids, especially at high doses, given the danger of a lack of antibody response. However, immunization of patients who are taking corticosteroids as replacement therapy, for example for Addison’s disease, can be done. In the presence of hypoprothrombinaemia l ‘ acetylsalicylic acid it should be used with caution

during corticosteroid therapy. The use of cortisone acetate tablets in current tuberculosis should be limited to cases of fulminant or disseminated tuberculosis in which the corticosteroid is used to treat the disease in combination with an appropriate antituberculous regimen. When corticosteroids are indicated in patients with latent tuberculosis or with a positive response to tuberculin, close monitoring is required , as reactivation of the disease may occur. During prolonged corticosteroid therapy, these patients should undergo chemoprophylaxis .

the steroidsshould be used with caution in the presence of: Nonspecific ulcerative colitis with the possibility of perforation, abscesses or other pyogenic infections ; diverticulitis ; recent intestinal anastomosis ; active or latent peptic ulcer ; kidney failure ; hypertension ; osteoporosis ; myasthenia gravis . Cases of systemic emboli of adipose tissue have been described as possible complications from overdosing of cortisone. The corticosteroid should be used with caution in patients with herpes simplex ophthalmic, given the possible risk of corneal perforation . In hyperthyroid and cirrhotic patients the effects of corticosteroids are more marked. In some patients, steroids can increase or decrease sperm motility and sperm count .

Diphenildantoin, ephedrine, phenobarbital, rifampicin, can induce an increase in the metabolism and clearance of corticosteroids; consequently it may be necessary to increase the dosage of the steroid. The corticosteroids may mask certain symptoms of the infection and during their use may manifest itself superimposed infections. During corticosteroid therapy, a reduced resistance to infections and a tendency, on the part of infectious processes, not to localize can be observed. Psychic alterations

may occur during treatment with corticosteroids , ranging from symptoms of euphoria, insomnia, mood swings , personality changes , severe depression , to actual psychotic manifestations . When present, psychic instability and psychotic tendencies can be aggravated by corticosteroids. Prolonged use of corticosteroids can causeposterior sub-capsular cataract , glaucoma with possible damage to the optic nerves and can favor the onset of secondary ocular infections due to fungi or viruses.

Children and adolescents undergoing prolonged corticosteroid therapy should be closely monitored for growth and development.
The prothrombin time should be checked frequently in patients receiving corticosteroids and coumarin anticoagulants at the same time, since in some cases it is seen that corticosteroids have altered the response to anticoagulants. Some studies have shown that the effect produced by adding corticosteroids is the inhibition of the response to coumarin compounds.

When corticosteroids are co-administered with diuretics that cause potassium loss , it should be strictly monitored for hypokalaemia in patients .

For those who carry out sports activities : the use of the drug without therapeutic need constitutes doping and can in any case determine positive anti-doping tests.

There are no data on overdose in humans.

Interactions and side effects

Cortisone has various metabolic effects and its co-administration with other drugs could cause drug interactions that must be carefully considered.

  • Co-administration of thiazide diuretics and corticosteroids can cause severe potassium depletion . The interaction is clinically relevant, therefore co-administration of thiazide diuretics and corticosteroids is not recommended. Potassium depletion is relevant for natural corticosteroids, such as cortisone and hydrocortisone , and for fludrocortisone . Corticotropin (ACTH) and tetracosactrin(a synthetic polypeptide) instead stimulate the secretion of corticosteroids from the adrenal cortex and can therefore indirectly cause the loss of potassium. Synthetic corticosteroids (glucocorticoids, including betamethasone, dexamethasone, prednisolone, prednisone and triamcinolone) have a less pronounced effect on potassium depletion and are therefore less likely to cause problems.
  • The use of corticosteroids causes decreased exposure to salicylic acid(aspirin), with the risk of compromising the antiplatelet effect of low doses of aspirin. Furthermore, plasma concentrations of salicylates may increase after discontinuation of corticosteroid therapy, with the risk of occurrence of salicylate toxicity. Concomitant use of corticosteroids and high dose aspirin (> 325 mg / day) may increase the risk of gastrointestinal bleeding and ulceration. In case of concomitant use of corticosteroids and aspirin at anti-inflammatory dosages it is advisable to consider the use of a gastroprotector. The therapeutic effect of salicylic acid, when co-administered with corticosteroids may be diminished, while monitoring for signs of salicylate toxicity after discontinuation of corticosteroid therapy is advised.
  • Carbamazepine . Co-administration may cause a reduction in serum corticosteroid levels , with the risk of decreased therapeutic response. Monitor the response to the corticosteroid and increase the dose if necessary.
  • Phenytoin can reduce the serum levels of corticosteroids and thus compromise the therapeutic response. Both increased and decreased phenytoin levels have been reported with concomitant use. Close monitoring of the response to corticosteroids and, if necessary, an increase in their dosage is recommended. It is recommended to monitor phenytoin serum levels.
  • Phenobarbital and primidone can alter the therapeutic response to corticosteroids. In case of concomitant use with phenobarbital or primidone, careful monitoring of the response to corticosteroids is recommended. The dose of corticosteroids may need to be adjusted. Instead of phenobarbital, consider using oxcarbazepine, lamotrigine or gabapentine, which are less likely to interact. Decreased plasma levels of corticosteroids may occur during concomitant use . Concomitant use may impair corticosteroid therapy. In case of concomitant use, corticosteroid doses should be increased. However, it is difficult to predict how much the dose should be increased.
  • The Somatropin induces a modest reduction of serum cortisol levels in patients with growth hormone deficiency treated with replacement therapy for adrenal. Corticosteroid doses may possibly need to be increased in conjunction with somatropin administration. Furthermore, corticosteroid replacement therapy may attenuate the effects promoted by somatropin.
  • The corticosteroids and immunosuppressants may interfere with the efficacy and pharmacodynamics pembrolizumab . The use of systemic corticosteroids and immunosuppressants should be avoided prior to initiation of therapy with pembrolizumab. These drugs can be given after initiation of therapy if needed to treat immune-related adverse drug reactions.
  • Cortisone causes hypokalemia (or hypokalemia), increasing the possibility of torsades de pointes. Therefore, concomitant use with vemurafenib, known to prolong the QT interval , should be very well monitored to avoid any torsades de pointes which could be fatal to the patient. Cases have also been reported in which the same treatment with vemurafenib has caused hypokalaemia: this condition could therefore be aggravated if cortisone is used concomitantly. Concomitant use is not recommended. If strictly necessary, blood potassium concentration should be monitored closely.
  • Concomitant use with warfarin may increase the risk of gastrointestinal bleeding , especially in patients with previous bleeding episodes. An increase in the levels of the International Normalized Ratio (INR) is possible. It is advisable to intensify the monitoring of INR, even if this is not sufficient to determine the risk of bleeding. Monitor hemoglobinemia to allow early detection of any gastrointestinal bleeding. Consider using a gastroprotector (e.g. lansoprazole or pantoprazole).

Cortisones are also metabolized by the liver, as is the case with ethanol (alcohol) . Therefore, in case of cortisone intake it is advisable to limit the use of alcoholic beverages as much as possible and to periodically perform blood chemistry tests to evaluate liver function : AST, ALT, gamma GT, CPK, bilirubinemia.

In case of cortisone intake it is necessary to pay attention to sun exposure . In fact, cortisone can be responsible for reactions to the sun’s rays which can be divided into toxic and allergic . It is therefore advisable to replace this hormone during the summer months with other types of remediesor products with similar action to cortisone. Phototoxic reactions (the most frequent ones) depend on both the duration of exposure to the sun and the amount of drug used. The interaction of cortisone with the sun’s rays causes a chemical reaction that causes damage to the skin tissues , while at the same time causing the formation of free radicals. Photoallergic reactions occur in predisposed subjects within 24 or 48 hours. Sunlight interacts with the drug on the skin itself, giving symptoms of a sunburn or irritation .

Other side effects that can develop are:

  • Water and electrolyte disturbances : sodium retention, fluid retention, congestive heart failure in predisposed patients, potassium loss resulting in hypokalaemic alkalosis. Hypertension with congestive heart failure.
  • Musculoskeletal disorders : steroid myopathy, hypotrophy of muscle masses, osteoporosis with possible pathological fractures of the long bones, tendon ruptures, aseptic necrosis of the femoral head and humerus.
  • Gastrointestinal disorders : ulcerative esophagitis, pancreatitis, peptic ulcer with possible perforation and haemorrhage, perforation of the small and large intestine, particularly in patients with inflammatory intestinal pathology, abdominal distension.
  • Dermatological disorders : difficult healing, skin dystrophies, petechiae and ecchymosis, erythema, skin reactions and tests, other skin reactions, such as allergic dermatitis, urticaria, angioneurotic edema can be suppressed .
  • Neurological disorders : convulsions, increased intracranial pressure with papilledema (pseudotumor of the brain) usually after treatment, dizziness, headache.
  • Endocrine disorders : menstrual irregularities. Development of cushingoid syndrome.
  • Growth arrest in children . Lack of adrenocortical and pituitary response particularly under stress, such as trauma, surgery and morbid conditions.
  • Reduced tolerance to carbohydrates . Manifestations of latent diabetes mellitus. Need to increase insulin or oral hypoglycemic dosages in diabetics.
  • Eye disorders : posterior subcapsular cataracts, increased intraocular pressure, glaucoma, exophthalmos.
  • Metabolic disorders : negative nitrogen balance due to protein catabolism.
  • Others : Hypersensitivity. Thromboembolism. Weight gain. Increased appetite. Nausea. Malaise.

Pregnancy and breastfeeding

Adequate studies on corticosteroids in relation to human reproduction are not yet available, the use of these drugs in pregnant women , in nursing mothers or in women of childbearing age requires that the possible risks and benefits derived from the drug for the mother and fetus. The babies born to mothers who are pregnant have been treated with substantial doses of corticosteroids should be subjected to strict controls acts to ascertain any signs of the posurrenalismo .

Corticosteroids can pass into breast milk and could impede growth , interfere with the production of endogenous corticosteroids, or cause other side effects. The women taking pharmacologic doses of corticosteroids should not breastfeed .

Notes (validity, storage conditions)

The tablets are valid for 5 years when unopened. No special precautions are necessary for conservation .

Questions and answers

WHAT IS CORTISONE USED FOR?

Cortisone is used in the treatment of various ailments. Cortisones are anti-inflammatory and immunosuppressive drugs, with a structure similar to endogenous corticosteroids. Cortisone is a hormone used against all types of body inflammation and is used to reduce swelling, redness, itching and allergic reactions.

IS WEIGHT GAIN AMONG THE SIDE EFFECTS OF CORTISONE?

In the case of prolonged therapy, cortisone may cause weight gain as it can increase appetite and fluid retention. In these cases a controlled diet is useful, with the possible combination of diuretics.

HOW LONG CAN YOU TAKE CORTISONE?

The duration of treatment may vary in the individual patient and depends on the severity of the disease. Duration, dosage and suspension of treatment must always be agreed with the attending physician.

ARE CORTISONE AND HYDROCORTISONE THE SAME THING?

Hydrocortisone, also called cortisol, is the active form of cortisone.

WHAT ARE THE DIFFERENCES BETWEEN CORTISONE AND BENTELAN?

Bentelan is a drug containing betamethasone, a steroid anti-inflammatory, belonging to the class of long-acting glucocorticoids. It is therefore a drug that belongs to the same pharmacological category as cortisone, but with a longer duration of anti-inflammatory action. Cortisone, however, has a greater mineralocorticoid activity.

 

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