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dexamethasone

 
Dictionary: dex·a·meth·a·sone   (dĕk'sə-mĕth'ə-sōn', -zōn') pronunciation
n.
A synthetic glucocorticoid used primarily in the treatment of inflammatory disorders.

[dexa- (blend of DECA-HEXA-) + METH(YL) + probably alteration of (CORTI)SONE.]


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Oncology Encyclopedia: Dexamethasone
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Key Terms: Addison's disease, Elute, Glucocorticoid, Hyperglycemia, Induction therapy, Palliation.

Definition

Dexamethasone is a synthetic glucocorticoid. Its naturally occuring counterparts are hydrocortisone and cortisone. Although the drug is used in a variety of ways, in general, it reduces inflammation and depresses the immune system. Dexamethasone may also be called by its brand name, Decadron.

Purpose

Dexamethasone is used in the treatment of many disorders. For example, it may be used:

  • as replacement therapy in the treatment of Addison's disease
  • in the management of various inflammatory disorders, such as rheumatoid arthritis
  • to coat drug-eluting stents, which are devices used in treating coronary artery disease to reduce the chance that previously clogged arteries will become blocked again
  • in managing such allergic disorders as asthma
  • as induction therapy prior to stem cell transplantation

Patients with ulcerative colitis may benefit from dexamethasone therapy, as might those with exacerbations of multiple sclerosis. Such blood disorders as thrombocytopenic purpura or erythroblastopenia, may also be managed with dexamethasone.

Dexamethasone is often prescribed to patients with cancer. In some cases, the drug is part of the drug treatment for the disease, and in other cases it is used to manage side effects caused by the treatment or the cancer itself. For example, dexamethasone may be given to treat nausea and vomiting associated with chemotherapy.

Dexamethasone may be used to decrease abnormally high levels of potassium that develop in association with cancer. In some cases, it may be used as palliation in leukemia or lymphoma. Because of its antiinflammatory properties, dexamethasone may help reduce swelling in the brain caused by a brain tumor. It may also help prevent hypersensitivity reactions associated with drugs like paclitaxel. Dexamethasone is also commonly used to treat nausea associated with chemotherapy. It is particularly useful with the drug cisplatin, which frequently causes nausea and vomiting.

In non-Hodgkin's lymphoma (NHL), dexamethasone is part of a drug regimen known as DHAP. Here, dexamethasone is given with chemotherapy drugs called cisplatin and cytarabine. Also in treating NHL, dexamethasone may be used in a regimen caled "m-BACOD," which also includes the administration of methotrexate, leucovorin, bleomycin, doxorubicin, cyclophosphamide, and vincristine. Dexamethasone may also be helpful in patients with multiple myeloma. In the EDAP regimen, dexamethasone is given with etoposide, cytosine arabinoside (cytarabine), and cisplatin; in VAD, it is given with vincristine and doxorubicin.

Description

Patients should not stop taking dexamethasone without first consulting their physician. When dexamethasone treatment stops, it must be gradually reduced over time before it can be completely discontinued. Sudden withdrawal of glucocorticoids may result in adrenal insufficiency.

When possible, the drug should be taken before nine A.M. to imitate the time that the body's corticosteroid levels are typically at their highest. A child taking dexamethasone will be carefully monitored to ensure the drug is not affecting his or her growth. Patients taking large doses of dexamethasone should try to take the drug with meals. Antacids may be recommended between meals to reduce gastrointestinal effects and to prevent peptic ulcer.

Recommended Dosage

Dexamethasone is available in oral, intravenous (IV), topical, ophthalmic, or inhaled form. In cancer patients, the oral and IV routes are used most frequently. The pill is available in several color-coded dosages [0.25 milligrams (mg), 0.5mg, 0.75mg, 1.5mg, 4mg, and 6mg]. Dexamethasone should be given very slowly by the IV route.

Dosages to treat disease are highly individualized, but generally start at 0.75 to 9.0 mg per day. The lowest therapeutic dose should be given, though amounts given may need to be increased during times of stress. Dosages of medications may be changed based on factors specific to the individual. The following dosages are general guidelines for dexamethasone when it is used in conjunction with chemotherapy agents:

  • DHAP. Forty milligrams of dexamethasone is given in pill or IV form per day for the first four days of treatment, followed by cisplatin and cytarabine.
  • M-BACOD. Six milligrams per meter square (mg/m2) of dexamethasone is given as a pill on the first five days of treatment.
  • EDAP. Forty milligrams of dexamethasone is given in pill form on the first four days of treatment. It is given again on days 9-12, and 17-20.

When used to prevent or manage nausea or vomiting associated with chemotherapy, dexamethasone is given in the following dosages: 4–20 mg IV every 4–6 hours. Alternatively, a one-time dose of 10–20 mg may be given IV. When pills are preferred, 4–8 mg of dexamethasone may be given four times, every four hours. When used to prevent hypersensitivity reactions in paclitaxel treatment, 20mg should be given orally twelve and six hours before treatment begins.

Precautions

Dexamethasone should be used cautiously in patients with kidney or liver problems, hypothyroidism, high blood pressure, or a history of heart attack. Patients with diabetes mellitus should monitor blood sugar levels carefully, as hyperglycemia may result. If changes occur, patients should notify their doctors immediately. Sudden cessation of dexamethasone therapy is dangerous for patients on therapy for longer than two weeks. The drug should be gradually withdrawn under a physician's guidance.

Side Effects

Adverse effects vary widely, and depend on the dosage and route of the drug. Certain drugs may result in decreased blood levels, and therefore render dexamethasone less effective. Patients taking the following drugs should be carefully monitored for decreased levels of dexamethasone: phenytoin, phenobarbitol, ephedrine, and rifampin. Conversely, some drugs, such as troleandomycin, may increase blood levels of dexamethasone.

Because of its immunosuppressive properties, dexamethasone may decrease the signs and symptoms of infection. Depending on the amount of drug being administered, patients may consider taking measure to prevent infection by avoiding crowded areas and washing their hands frequently. Patients should inform their doctor if they notice a fever, sore throat, or cuts or abrasions that don't heal. Laboratory tests may also be affected—false negative results may occur in the nitroblu-tetrazolium test for bacterial infections.

Glucocorticoids, such as hydrocortisone, tend to make the body retain salt. Although dexamethasone's salt-retaining properties are not as severe as hydrocortisone's, salt retention may result in fluid and electrolyte imbalances. Patients at risk may experience high blood pressure or even congestive heart failure. Weight gain or swelling may indicate salt and fluid retention.

Other adverse effects may include headache, dizziness, insomnia, increased appetite, mood swings, menstrual changes, muscle weakness, acne and/or sweating. Depression may be worsened with dexamethasone use. Some men experience changes in the motility and number of their sperm with steroid treatment. Patients should talk to their doctors about any unusual symptoms they experience. In cancer patients, increased appetite may actually be beneficial.

Dexamethasone crosses the placenta and is excreted in breast milk. If a pregnant woman is taking large doses of the drug, her newborn should be monitored for evidence of hypoadrenalism. Optimally, breast-feeding should be avoided. There is some concern that dexamethasone, in large quantities, suppresses growth or disrupts the baby's normal corticosteroid production.

Interactions

Patients should discuss all their medications, prescription and non-prescription, with their doctor. If dexamethasone is administered in amounts that suppress the immune system, live vaccines, such as small pox, should not be administered. Dexamethasone may alter the effect of anticoagulant drugs. Frequent laboratory tests should be performed to monitor blood levels. If dexamethasone is given with diuretics, potassium levels may be abnormally low, and should be frequently monotired. Doctors may recommend that patients on long-term therapy follow a potassium-rich diet.

Resources

Books

Wilson, Billie A., Margaret T. Shannon, and Carolyn L. Stang. Nurses Drug Guide 2000. Stamford, CT: Appleton & Lange, 2000.

Periodicals

Hesketh, P. J. "New Treatment Options for Chemotherapy-Induced Nausea and Vomiting." Supportive Care in Cancer 12 (August 2004): 550–554.

Kumar, S., M. Q. Lacy, A. Dispenzieri, et al. "Single-Agent Dexamethasone for Pre-Stem Cell Transplant Induction Therapy for Multiple Myeloma." Bone Marrow Transplantation 34 (September 2004): 485–490.

Liu, X., I. de Scheerder, and W. Desmet. "Dexamethasone-Eluting Stent: An Anti-Inflammatory Approach to Inhibit Coronary Restenosis." Expert Review of Cardiovascular Therapy 2 (September 2004): 653–660.

Organizations

American Society of Health-System Pharmacists (ASHP). 7272 Wisconsin Avenue, Bethesda, MD 20814. (301) 657-3000. .

United States Food and Drug Administration (FDA). 5600 Fishers Lane, Rockville, MD 20857-0001. (888) INFOFDA. .

—Tamara Brown, R.N.; Rebecca J. Frey, PhD

Drug Info: Dexamethasone
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Brand names: AK-Dex®Cortastat®Cortastat® L.A.Cortidex™Cortidex™ L.A.Dalalone D.P®Dalalone L.A®Dalalone®Deca 4™Deca L.A. 8™Decadron®Decadron-LA®Dexacort® PH TurbinaireDexacort® RespihalerDexone L.A.®DexPak™ TaperPakMaxidex®Ocu-Dex®Primethasone™Primethasone™ L ARobadex™ LASolurex™

Chemical formula:



Dexamethasone ear solution

What is dexamethasone ear solution?

DEXAMETHASONE (Decadron®) is a corticosteroid. It helps to reduce swelling, redness, itching, and allergic reactions. Dexamethasone treats inflammatory conditions of the outer ear. Generic dexamethasone ear solution is not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• history of middle ear infections
• infection; fungal, viral, tubercular or other bacterial
• perforated ear drum
• an unusual or allergic reaction to dexamethasone, corticosteroids, other medicines, foods, dyes, or preservatives

How should I use this medicine?

Dexamethasone ear solution is for use in the ear only. Do not take by mouth. Follow the directions on the prescription label. Wash hands before and after use. Lie on your side or tilt head so that ear is up. Pull the earlobe up and back (adults), or down and back (children), and drop in the prescribed number of drops (usually 4—5 drops); avoid touching the ear with the dropper tip. Keep head tilted for about 5 minutes or insert a soft cotton gauze 'wick' in the ear to prevent the medication from running out. Replace the cotton at least once a day. Do not use more often than directed.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What drug(s) may interact with dexamethasone?

It is unlikely that when dexamethasone is used in the ear it will interact with medicines taken by mouth. However, tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking dexamethasone?

Check with your prescriber or health care professional if your condition has not improved after 2 or 3 days. Check with your prescriber or health care professional before using dexamethasone for any future ear problems.

What side effects may I notice from using dexamethasone?

If dexamethasone is used for long periods of time other serious side effects may develop. Report any other unusual effects to your prescriber or health care professional as soon as you can.

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• burning or stinging in the ear

Where can I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F); do not freeze. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Veterinary Dictionary: dexamethasone
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A synthetic glucocorticoid used primarily as an anti-inflammatory agent in various conditions, including autoimmune diseases, hypersensitivity reactions and shock; it is also used in a screening test for the diagnosis of cushing's syndrome, and for the termination of pregnancy in cattle.

  • d. suppression test — the determination of blood cortisol levels before and after administration of dexamethasone assists in diagnosing Cushing's syndrome and identifying the cause, depending on the protocol and dose used. Dexamethasone suppresses pituitary secretion of ACTH in normal animals and therefore the blood level of cortisol is decreased; low doses do not suppress cortisol levels in dogs with pituitary-dependent Cushing's syndrome, high doses do. Cortisol production by functional adrenal tumors is not affected by dexamethasone.
Wikipedia: Dexamethasone
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Dexamethasone
Systematic (IUPAC) name
(8S,9R,10S,11S,13S,14S,16R,17R)-9-Fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one
Identifiers
CAS number 50-02-2
ATC code A01AC02 C05AA09, D07AB19, H02AB02, R01AD03, S01BA01, S02BA06, S03BA01
PubChem 5743
DrugBank APRD00674
ChemSpider 5541
Chemical data
Formula C22H29FO5 
Mol. mass 392.461 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 80-90%
Protein binding 70%
Metabolism hepatic
Half life 36-54 hours
Excretion renal
Therapeutic considerations
Pregnancy cat.

C(US)

Legal status

Prescription only

Routes Oral, IV, IM, SC and IO
 Yes check.svgY(what is this?)  (verify)

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid hormones. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of hydrocortisone and 4-5 times of prednisone.

Contents

Therapeutic use

Anti-inflammatory

Dexamethasone is used to treat many inflammatory and autoimmune conditions, such as rheumatoid arthritis.

It is also given in small amounts (usually 5-6 tablets) before and/or after some forms of dental surgery, such as the extraction of the wisdom teeth, an operation which often leaves the patient with puffy, swollen cheeks.

It is injected into the heel when treating plantar fasciitis, sometimes in conjunction with triamcinolone acetonide.

It is useful to counteract allergic anaphylactic shock, if given in high doses. It is present in certain eye drops – particularly post-eye surgery drops – and as a nasal spray (trade name Dexacort).

Dexamethasone is used in transvenous screw-in cardiac pacing leads to minimize the inflammatory response of the myocardium. The steroid is released into the myocardium as soon as the screw is extended and can play a significant role in minimizing the acute pacing threshold due to the reduction of inflammatory response. The typical quantity present in a lead tip is less than 1.0 mg.

Dexamethasone is often administered before antibiotics in cases of bacterial meningitis. It then acts to reduce the inflammatory response of the body to the bacteria killed by the antibiotics (bacterial death releases pro-inflammatory mediators that can cause a response which is harmful to the patient), thus improving prognosis and outcome.[1]

Oncologic uses

In oncology, it is given to cancer patients undergoing chemotherapy, to counteract certain side-effects of their antitumor treatment. Dexamethasone can augment the antiemetic effect of 5-HT3 receptor antagonists like ondansetron. Dexamethasone is also used in certain hematological malignancies, especially in the treatment of multiple myeloma, in which dexamethasone is given alone or together with thalidomide (thal-dex) or a combination of Adriamycin (doxorubicin) and vincristine (VAD). In brain tumours (primary or metastatic), dexamethasone is used to counteract the development of edema, which could eventually compress other brain structures. Dexamethasone is also given in cord compression where a tumor is compressing the spinal cord.

Endocrine

Dexamethasone can be used in the context of congenital adrenal hyperplasia, to prevent virilisation of a female fetus. If one or both parents are carriers of mutations to the CYP21 (CYP21A2) gene, the mother may start dexamethasone treatment within 7 weeks of conception. At the 12th week, a chorionic villus sample will determine whether the fetus is male (in which case the dexamethasone is stopped) or female. Subsequent DNA analysis can then reveal whether the female fetus is a carrier of the mutation, in which case dexamethasone treatment must continue until birth. The side-effects for the mother can be severe and the long-term impact on the child is not clear.

In adrenal insufficiency and Addison's disease, dexamethasone is prescribed when the person doesn't respond well to prednisone or methylprednisone.

Obstetrics

Dexamethasone may be given to women at risk of delivering prematurely in order to promote maturation of the fetus' lungs. This has been associated with low birth weight, although not with increased rates of neonatal death.[2]

High altitude illnesses

Dexamethasone is used in the treatment of high altitude cerebral edema as well as pulmonary edema. It is commonly carried on mountain climbing expeditions to help climbers deal with altitude sickness.[3][4]

Diagnostic use

Dexamethasone is also used in a diagnostic context, namely in its property to suppress the natural pituitary-adrenal axis. Patients presenting with clinical signs of glucocorticoid excess (Cushing's syndrome) are generally diagnosed by a 24-hour urine collection for cortisol or by a dexamethasone suppression test. During the latter, the response of the body to a high dose of glucocorticoids is monitored. Various forms are performed. In the most common form, a patient takes a nighttime dose of either 1 or 4 mg of dexamethasone, and the serum cortisol levels are measured in the morning. If the levels are relatively high (over 5 µg/dL or 150 nmol/L), then the test is positive and the patient has an autonomous source of either cortisol or ACTH, indicating Cushing's syndrome where the tumor does not have a feedback mechanism. If ACTH levels are lowered by at least 50%, this would indicate Cushing's Disease, since the pituitary adenoma has a feedback mechanism that has been reset to a higher level of cortisol. Longer versions rely on urine collections on oral dexamethasone over various days.

Veterinary use

Combined with marbofloxacin and clotrimazole, dexamethasone is available under the name Aurizon , CAS number 115550-35-1, and used to treat difficult ear infections, especially in dogs. It can also be combined with Trichlormethiazide to treat horses with swelling of distal limbs and general bruising.[5]

Contraindications

Some of these contraindications are relative:

Side effects

If dexamethasone is given orally or by injection (parenteral) over a period of more than a few days, side-effects common to systemic glucocorticoids may occur. These may include:

  • Stomach upset, increased sensitivity to stomach acid to the point of ulceration of esophagus, stomach, and duodenum
  • Increased appetite leading to significant weight gain
  • A latent diabetes mellitus often becomes manifest. Glucose intolerance is worsened in patients with preexisting diabetes.
  • Immunsuppressant action, particularly if given together with other immunosuppressants such as ciclosporine. Bacterial, viral, and fungal disease may progress more easily and can become life-threatening. Fever as a warning symptom is often suppressed.
  • Psychiatric disturbances, including personality changes, irritability, euphoria, mania
  • Osteoporosis under long term treatment, pathologic fractures (e.g., hip)
  • Muscle atrophy, negative protein balance (catabolism)
  • Elevated liver enzymes, fatty liver degeneration (usually reversible)
  • Cushingoid (syndrome resembling hyperactive adrenal cortex with increase in adiposity, hypertension, bone demineralization, etc.)
  • Depression of the adrenal gland is usually seen, if more than 1.5 mg daily are given for more than three weeks to a month.
  • Hypertension, fluid and sodium retention, edema, worsening of heart insufficiency (due to mineral corticoid activity)
  • Dependence with withdrawal syndrome is frequently seen.
  • Increased intraocular pressure, certain types of glaucoma, cataract (serious clouding of eye lenses)
  • 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.
  • Allergic reactions (though infrequently): Anaphylactoid reaction, anaphylaxis, angioedema.

Other side-effects have been noted, and should cause concern if they are more than mild.

The short time treatment for allergic reaction, shock, and diagnostic purposes usually does not cause serious side effects.

Interactions

  • NSAIDs and alcohol: increased risk of gastrointestinal ulceration
  • Mineralocorticoids: increased risk of hypertension, edema and heart problems
  • Oral antidiabetic drugs and insulin: antidiabetic therapy may have to be adjusted

Other interactions (with certain antibiotics, estrogens, ephedrine, digoxin) are known.

Dosage

  • Shock: 4 to 8 mg intravenously initially, repeat if necessary to a total dose of 24 mg.
  • Autoimmune diseases and inflammations: longterm therapy with 0.5 to 1.5 mg oral per day. Avoid more than 1.5 mg daily, because serious side effects are more frequently encountered with higher doses.
  • Adjuvant to or part of chemotherapy: individual schedule
  • Diagnostic purposes: special schedule

Sports doping

In 2005, Polish cross country skier Justyna Kowalczyk was disqualified from the Under 23 (U23) OPA (Alpine nations) Intercontinential Competition in Germany and issued a 2-year suspension for her doping offenses on dexamethasone.[6] This was eventually reduced to one year during 2005 and later rescinded by the Court of Arbitration for Sport in December 2005.[7] She would later earn a bronze in the women's 30 km freestyle mass start at the 2006 Winter Olympics in Turin.

References

  1. ^ van de Beek D, de Gans J, McIntyre P, Prasad K (2007). "Corticosteroids for acute bacterial meningitis". Cochrane Database Syst Rev (1): CD004405. doi:10.1002/14651858.CD004405.pub2. PMID 17253505. http://mrw.interscience.wiley.com/cochrane/clsysrev/articles/CD004405/frame.html. 
  2. ^ Bloom SL, Sheffield JS, McIntire DD, Leveno KJ (2001). "Antenatal dexamethasone and decreased birth weight" ([dead link]Scholar search). Obstet Gynecol 97 (4): 485–90. doi:10.1016/S0029-7844(00)01206-0. PMID 11275014. http://www.greenjournal.org/cgi/content/full/97/4/485. 
  3. ^ Cymerman, A; Rock, PB. Medical Problems in High Mountain Environments. A Handbook for Medical Officers. USARIEM-TN94-2. US Army Research Inst. of Environmental Medicine Thermal and Mountain Medicine Division Technical Report. http://archive.rubicon-foundation.org/7976. Retrieved 2009-03-05. 
  4. ^ COMMENTS AND RESPONSES Reducing the Incidence of High-Altitude Pulmonary Edema Annals of Internal Medicine PDF
  5. ^ "Trichlormethiazide and Dexamethasone for veterinary use". Wedgewood Pharmacy. http://www.wedgewoodpharmacy.com/monographs/trichlormethiazide.asp. Retrieved 2008-01-23. 
  6. ^ June 13, 2005 FIS Doping Control statement on Kowalcyzk (Digitized version). - Accessed July 30, 2006
  7. ^ December 14, 2005 FIS Newsflash on her overturned suspension (Digitized version). - Accessed July 30, 2006

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Copyrights:

Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Oncology Encyclopedia. Gale Encyclopedia of Cancer. Copyright © 2006 by The Gale Group, Inc. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Dexamethasone" Read more