Corticosteroids

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Corticosteroids are steroid hormones that are either produced by the body or are man-made.

Systemic corticosteroids refer to corticosteroids that are given orally or by injection and distribute throughout the body. It does not include corticosteroids used in the eyes, ears, or nose, on the skin or that are inhaled, although small amounts of these corticosteroids can be absorbed into the body.

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Naturally occurring corticosteroids, hydrocortisone (Cortef) and cortisone, are produced by the outer portion of the adrenal gland known as the cortex (hence the name, corticosteroid). Corticosteroids are classified as either:

  1. glucocorticoids (anti-inflammatory) which suppress inflammation and immunity and assist in the breakdown of fatscarbohydrates, and proteins, or as
  2. mineralocorticoids (salt retaining) that regulate the balance of salt and water in the body.

Synthetic corticosteroids mimic the actions of naturally occurring corticosteroids and may be used to replace corticosteroids in people with adrenal glands that are unable to produce adequate amounts of corticosteroids, however, they more often are used in higher-than-replacement doses to treat diseases of immunity, inflammation or salt and water balance.

Examples of synthetic corticosteroids include:

  • bethamethasone, (Celestone)
  • prednisone (Prednisone Intensol)
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Some glucocorticoids also in addition to their anti-inflammatory actions have salt retaining properties but they are used mostly for their anti-inflammatory effects. Fludrocortisone (Florinef), a synthetic mineralocorticoid has strong salt retaining effects with significant anti-inflammatory actions, and is used mostly for it’s salt retaining capabilities.

What are some examples of systemic (oral and injectable) corticosteroids?

The following is a list of the systemic (oral and injectable) corticosteroids that are available in the United States:

Glucocorticoids:

  • hydrocortisone (Cortef)
  • cortisone
  • ethamethasoneb (Celestone)
  • prednisone (Prednisone Intensol)
  • prednisolone (Orapred, Prelone)
  • triamcinolone (Aristospan Intra-Articular, Aristospan Intralesional, Kenalog) Methylprednisolone (Medrol, Depo-Medrol, Solu-Medrol)
  • dexamethasone (Dexamethasone Intensol, DexPak 10 Day, DexPak 13 Day, DexPak 6 Day)

Mineralocorticoid:

  • Fludrocortisone (Florinef)

http://www.medicinenet.com/corticosteroids-oral/article.htm

For what conditions are systemic corticosteroids used?

Corticosteroids belonging to the glucocorticoid class influence the body system in several ways, but they are used mostly for their strong anti-inflammatory effects and in conditions that are related to the immune system function such as:

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Glucocorticoid corticosteroids are used to treat systemic lupussevere psoriasisleukemialymphomas, idiopathic thrombocytopenic purpura, and autoimmune hemolytic anemia. These corticosteroids also are used to suppress the immune system and prevent rejection in people who have undergone organ transplant as well as many other conditions.

Fludrocortisone (Florinef), a potent systemic oral mineralocorticoid corticosteroid is used to treat Addison’s disease and diseases that cause salt loss as in congenital adrenal hyperplasia. It also is used commonly to treat conditions of low blood pressure (hypotension) although this is not a Food and Drug Administration (FDA) approved indication.

Are there any differences among the different types of systemic corticosteroids?

Corticosteroids differ in their relative amount of anti-inflammatory and mineralocorticoid potency and they are used according to these effects. Among the systemic (oral and injectable) corticosteroids, fludrocortisone (Florinef) has the most significant mineralocorticoid (salt retaining) actions and is best used for this effect despite it’s strong anti-inflammatory action.

Other systemically available corticosteroids have mostly glucocorticoid effects, and are used for their anti-inflammatory activities. Examples of these include the naturally occurring hydrocortisone (Cortef) and cortisone, and the synthetic corticosteroids including:

  • bethamethasone (Celestone)
  • prednisone (Prednisone Intensol)
  • prednisolone (Orapred, Prelone)
  • triamcinolone (Aristospan Intra-Articular, Aristospan Intralesional, Kenalog)
  • methylprednisolone((Medrol, Depo-Medrol, Solu-Medrol)
  • dexamethasone (Dexamethasone Intensol, DexPak 10 Day, DexPak 13 Day, DexPak 6 Day).

Among all glucocorticoids, prednisone is not effective in the body unless it is converted to prednisolone by enzymes in theliver. For this reason prednisone may not be very effective in people with liver disease because of a reduction in their ability to convert prednisone to prednisolone.  

http://www.medicinenet.com/corticosteroids-oral/page2.htm

With which drugs do systemic (oral and injectable) corticosteroids interact?

Certain drugs such as troleandomycin (TAO), erythromycin (Ery-Tab, EryPed 200), and clarithromycin (Biaxin) and ketoconazole (Nizoral) can reduce the ability of the liver to metabolize (breakdown) corticosteroids and this may lead to an increase in the levels and side effects of corticosteroids in the body. On the other hand, phenobarbital, ephedrine, phenytoin (Dilantin), and rifampin (Rifadin, Rimactane) may reduce the blood levels of corticosteroids by increasing the breakdown of corticosteroids by the liver. This may necessitate an increase of corticosteroid dose when they are used in combination with these drugs.

Estrogens have been shown to increase the effects of corticosteroids possibly by decreasing their breakdown by the liver.

Corticosteroid effects on warfarin (Coumadin) can vary; therefore when taking warfarin (Coumadin) along with corticosteroids, there may be increased need for monitoring coagulation levels more closely.

Low blood potassium (hypokalemia) and a higher chance of heart failure can result from combining corticosteroids with drugs that reduce potassium in the blood (for example, diuretics, amphotericin B).

Anticholinesterase drugs (for example, physostigmine) may cause severe weakness in some patients with myasthenia gravis when prescribed with corticosteroids.

Corticosteroids can increase blood glucose, so close monitoring of blood sugar and higher doses of diabetes medications may be needed.

Cholestyramine (Questran, Questran Light) can decrease the absorption of oral corticosteroids from the stomach and this could reduce the blood levels of corticosteroids

http://www.medicinenet.com/corticosteroids-oral/page3.htm

Side effects

Glucocorticoids may sound like miracle drugs, but they do have side effects. Some of these side effects can be very damaging. This is why these drugs aren’t prescribed for long-term use.

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These drugs can:

  • increase your blood sugar level, which can trigger temporary and possibly long-term diabetes
  • suppress your body’s ability to absorb calcium, which can lead to osteoporosis
  • increase your cholesterol and triglyceride levels
  • increase your risk of ulcers and gastritis
  • delay wound healing, which requires a certain amount of inflammation
  • suppress your immune system and make you more prone to infections

Long-term use of glucocorticoids can cause a loss of muscle tissue. It can also result in Cushing’s syndrome, which can lead to:

  • a fatty hump between your shoulders
  • round face
  • weight gain
  • pink stretch marks
  • weakened bones
  • diabetes
  • high blood pressure
  • thin skin
  • slow healing
  • acne
  • irregular menstrual cycles
  • decreased libido
  • fatigue
  • depression

If you have used glucocorticoids for more than a few weeks, your doctor will most likely taper your dosage slowly rather than have you stop taking it all at once. This helps to prevent withdrawal effects. Your body naturally makes glucocorticoids, but when you start taking them as medication, your body reacts by making less of it on its own. When you stop taking glucocorticoids, your body needs time to start making more of its own at normal levels again.

http://www.healthline.com/health/glucocorticoids#overview1

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