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Dexamethasone

 

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Dexamethasone



 
 
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid
Steroid

A steroid is a terpenoid lipid characterized by a carbon skeleton with four fused rings, generally arranged in a 6-6-6-5 fashion.Steroids vary by the functional groups attached to these rings and the oxidation state of the rings....
 hormone
Hormone

Hormones are chemicals released by cells that affect cells in other parts of the body. Only a small amount of hormone is required to alter cell metabolism....
s. It acts as an anti-inflammatory
Anti-inflammatory

Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids which affect the brain....
 and immunosuppressant
Immunosuppressive drug

Immunosuppressive drugs or immunosuppressive agents are medication that inhibit or prevent activity of the immune system. They are used in immunosuppression to:...
. Its potency is about 20-30 times that of hydrocortisone and 4-5 times of prednisone
Prednisone

Prednisone is a synthetic corticosteroid drug that is usually taken orally but can be delivered by intramuscular injection and can be used for a number of different conditions....
.

methasone is used to treat many inflammatory
Inflammation

Inflammation is the complex biological response of Blood vessel tissues to harmful stimuli, such as pathogens, damaged cells, or irritants. It is a protective attempt by the organism to remove the injurious stimuli as well as initiate the healing process for the tissue....
 and autoimmune
Autoimmune disease

Autoimmune diseases arise from an overactive immune response of the body against substances and tissues normally present in the body. In other words, the body attacks its own cells....
 conditions, e.g., rheumatoid arthritis
Rheumatoid arthritis

Rheumatoid arthritis is a chronic, systemic disease inflammation that may affect many tissues and organs, but principally attacks the joints producing a inflammatory synovitis that often progresses to destruction of the articular cartilage and ankylosis of the joints....
.

It is also given in small amounts (usually 5-6 tablets) before and/or after some forms of dental surgery
Dental surgery

Dental surgery is any of a number of medical procedures which involve artificially modifying the dentition....
, 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
Plantar fasciitis

Plantar fasciitis is a painful Inflammation condition of the foot caused by excessive wear to the plantar fascia that supports the arches of the foot or by biomechanical faults that cause abnormal pronation....
, sometimes in conjunction with triamcinolone acetonide
Triamcinolone acetonide

Triamcinolone acetonide is a more potent type of triamcinolone, being about 8 times as effective as prednisone. Triamcinolone acetonide should not be used by those with tuberculosis or untreated fungal, bacterial, viral or herpes infections without consulting a doctor first....
.

It is useful to counteract allergic anaphylactic shock, if given in high doses.






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Encyclopedia


Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid
Steroid

A steroid is a terpenoid lipid characterized by a carbon skeleton with four fused rings, generally arranged in a 6-6-6-5 fashion.Steroids vary by the functional groups attached to these rings and the oxidation state of the rings....
 hormone
Hormone

Hormones are chemicals released by cells that affect cells in other parts of the body. Only a small amount of hormone is required to alter cell metabolism....
s. It acts as an anti-inflammatory
Anti-inflammatory

Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids which affect the brain....
 and immunosuppressant
Immunosuppressive drug

Immunosuppressive drugs or immunosuppressive agents are medication that inhibit or prevent activity of the immune system. They are used in immunosuppression to:...
. Its potency is about 20-30 times that of hydrocortisone and 4-5 times of prednisone
Prednisone

Prednisone is a synthetic corticosteroid drug that is usually taken orally but can be delivered by intramuscular injection and can be used for a number of different conditions....
.

Therapeutic use


Anti-inflammatory

Dexamethasone is used to treat many inflammatory
Inflammation

Inflammation is the complex biological response of Blood vessel tissues to harmful stimuli, such as pathogens, damaged cells, or irritants. It is a protective attempt by the organism to remove the injurious stimuli as well as initiate the healing process for the tissue....
 and autoimmune
Autoimmune disease

Autoimmune diseases arise from an overactive immune response of the body against substances and tissues normally present in the body. In other words, the body attacks its own cells....
 conditions, e.g., rheumatoid arthritis
Rheumatoid arthritis

Rheumatoid arthritis is a chronic, systemic disease inflammation that may affect many tissues and organs, but principally attacks the joints producing a inflammatory synovitis that often progresses to destruction of the articular cartilage and ankylosis of the joints....
.

It is also given in small amounts (usually 5-6 tablets) before and/or after some forms of dental surgery
Dental surgery

Dental surgery is any of a number of medical procedures which involve artificially modifying the dentition....
, 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
Plantar fasciitis

Plantar fasciitis is a painful Inflammation condition of the foot caused by excessive wear to the plantar fascia that supports the arches of the foot or by biomechanical faults that cause abnormal pronation....
, sometimes in conjunction with triamcinolone acetonide
Triamcinolone acetonide

Triamcinolone acetonide is a more potent type of triamcinolone, being about 8 times as effective as prednisone. Triamcinolone acetonide should not be used by those with tuberculosis or untreated fungal, bacterial, viral or herpes infections without consulting a doctor first....
.

It is useful to counteract allergic anaphylactic shock, if given in high doses. It is present in certain eye drop
Eye drop

Eye drops are saline -containing drops used as a Vector to administer medication in the eye. Depending on the condition being treated, they may contain steroids , antihistamines, sympathomimetics, Beta blockers, parasympathomimetics , parasympatholytics , prostaglandins, non-steroidal anti-inflammatory drugs or topical anesthetics....
s and as a nasal spray
Nasal spray

Nasal sprays, or nasal mists, are used for the nasal delivery of a drug or drugs, either locally to generally alleviate cold or allergy symptoms such as nasal congestion or systemically, see nasal administration....
 (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.

Oncologic uses

In oncology, it is given to cancer
Cancer

Cancer is a class of diseases in which a group of cell display uncontrolled growth , invasion , and sometimes metastasis . These three malignant properties of cancers differentiate them from benign tumors, which are self-limited, do not invade or metastasize....
 patients undergoing chemotherapy
Chemotherapy

Chemotherapy, in its most general sense, refers to treatment of disease by chemicals that kill cells, specifically those of micro-organisms or cancer....
, to counteract certain side-effects
Adverse drug reaction

An adverse drug reaction or adverse drug event is an expression that describes the unwanted, negative consequences associated with the use of given medications....
 of their antitumor treatment. Dexamethasone can augment the antiemetic
Antiemetic

An antiemetic is a medication that is effective against vomiting and nausea. Anti-emetics are typically used to treat motion sickness and the Adverse effect of opioid analgesics, general anaesthetics and chemotherapy directed against cancer....
 effect of 5-HT3 receptor antagonists
5-HT3 antagonist

The 5-HT3 antagonists are a class of medications which act as receptor antagonists at the 5-HT3 receptor , a subtype of serotonin 5-HT receptor found in terminals of the vagus nerve and in certain areas of the brain....
 like ondansetron
Ondansetron

Ondansetron or GlaxoSmithKline's Zofran is a serotonin 5-HT3 antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy....
. Dexamethasone is also used in certain hematological malignancies
Hematological malignancy

Hematological malignancies are the types of cancer that affect blood, bone marrow, and lymph nodes. As the three are intimately connected through the immune system, a disease affecting one of the three will often affect the others as well: although lymphoma is technically a disease of the lymph nodes, it often spreads to the bone marrow, affe...
, especially in the treatment of multiple myeloma
Multiple myeloma

Multiple myeloma is a cancer of plasma cells. These immune system cells are formed in bone marrow, are numerous in lymphatics and produce antibody....
, in which dexamethasone is given alone or together with thalidomide
Thalidomide

Thalidomide is a sedative-hypnotic, and multiple myeloma medication. The drug is a potent Teratology in rabbits and primates including humans: this means that severe birth defects may result if the drug is taken during pregnancy....
 (thal-dex) or a combination of Adriamycin (doxorubicin) and vincristine
Vincristine

Vincristine , also known as leurocristine, is a vinca alkaloid from the Catharanthus roseus , formerly Vinca rosea and hence its name....
 (VAD). In brain tumours (primary or metastatic), dexamethasone is used to counteract the development of edema
Edema

File:Oedema.jpgEdema or Oedema , formerly known as dropsy or hydropsy, is an abnormal accumulation of fluid beneath the skin, or in one or more cavities of the body....
, 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
Congenital adrenal hyperplasia

Congenital adrenal hyperplasia refers to any of several autosomal recessive diseases resulting from mutations of genes for enzymes mediating the biochemical steps of production of cortisol from cholesterol by the adrenal glands ....
, to prevent virilisation of a female fetus. If one or both parents are carriers of mutations to the CYP21A gene, the mother may start dexamethasone treatment within 7 weeks of conception. At the 12th week, a chorionic villus sample
Chorionic villus sampling

Chorionic villus sampling is a form of prenatal diagnosis to determine chromosomal abnormalities or genetic disorders in the fetus. It entails getting a sample of the chorionic villus and testing it....
 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
Respiratory system

A respiratory system?s function is to allow gas exchange. The space between the alveoli and the capillaries, the anatomy or structure of the exchange system, and the precise physiological uses of the exchanged gases vary depending on the organism....
 of the fetus' lungs. This has been associated with low birth weight
Low Birth Weight

Low Birth Weight is the third album by Piano Magic....
, although not with increased rates of neonatal death.

High altitude illnesses

Dexamethasone is used in the treatment of high altitude cerebral edema
High altitude cerebral edema

High altitude cerebral edema is a severe form of altitude sickness. HACE is the result of swelling of brain tissue from fluid leakage. Symptoms can include headache, loss of coordination , weakness, and decreasing levels of consciousness including disorientation, loss of memory, hallucinations, irrational behavior, and coma....
 as well as pulmonary edema. It is commonly carried on mountain climbing expeditions to help climbers deal with altitude sickness.

Diagnostic use

Dexamethasone is also used in a diagnostic context, namely in its property to suppress the natural pituitary-adrenal axis
Hypothalamic-pituitary-adrenal axis

The hypothalamic-pituitary-adrenal axis , also known as thelimbic-hypothalamic-pituitary-adrenal axis , is a complex set of direct influences and feedback interactions among the hypothalamus , the pituitary gland , and the adrenal glands ....
. Patients presenting with clinical signs of glucocorticoid excess (Cushing's syndrome
Cushing's syndrome

Cushing's syndrome is a hormone disorder caused by high levels of cortisol in the blood. This can be caused by taking glucocorticoid drugs, or by tumors that produce cortisol or adrenocorticotropic hormone ....
) are generally diagnosed by a 24-hour urine collection for cortisol or by a dexamethasone suppression test
Dexamethasone suppression test

The dexamethasone suppression test is designed to diagnosis and differentiate among the various types of Cushing's syndrome and other hypercortisol states....
. 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
Cortisol

Cortisol is a corticosteroid hormone or glucocorticoid produced by the adrenal cortex, that is part of the adrenal gland . It is usually referred to as the "stress hormone" as it is involved in response to stress and anxiety, controlled by Corticotropin-releasing hormone....
 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
Pituitary adenoma

Pituitary adenomas are tumors that occur in the pituitary gland, and account for about 10% of intracranial neoplasia. They often remain undiagnosed, and small pituitary tumors have an estimated prevalence of 16.7% ....
 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
Marbofloxacin

Marbofloxacin is a potent antibiotic of the fluoroquinolone group. It is used in veterinary medicine under the trade names Marbocyl and Zeniquin....
 and clotrimazole
Clotrimazole

Clotrimazole is an antifungal medication commonly used in the treatment of fungal infections of both humans and animals such as candidiasis and ringworm....
, 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
Trichlormethiazide

Trichlormethiazide is a diuretic with properties similar to those of hydrochlorothiazide. It is usually administered for the treatment of oedema and hypertension....
 to treat horses with swelling of distal limbs and general bruising.

Contraindications

Some of these contraindications are relative:
  • Existing gastrointestinal ulceration
    Peptic ulcer

    A peptic ulcer, also known as ulcus pepticum, PUD or peptic ulcer disease, is an ulcer of an area of the gastrointestinal tract that is usually acidic and thus extremely painful....
  • Cushing's syndrome
  • Severe forms of heart insufficiency
  • Severe hypertension
    Hypertension

    Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
  • Uncontrolled diabetes mellitus
    Diabetes mellitus

    Diabetes mellitus , often referred to simply as diabetes , is a syndrome of disordered metabolism, usually due to a combination of genetic disorder and environmental causes, resulting in abnormally high blood sugar levels ....
  • Systemic tuberculosis
    Tuberculosis

    Tuberculosis is a common and often deadly infectious disease caused by mycobacterium, mainly Mycobacterium tuberculosis . Tuberculosis usually attacks the lungs but can also affect the central nervous system, the lymphatic system, the circulatory system, the genitourinary system, the gastrointestinal system, bones, joints, and even the...
  • Severe systemic viral, bacterial, and fungal infections
  • Preexisting wide angle glaucoma
    Glaucoma

    Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....
  • Osteoporosis
    Osteoporosis

    Osteoporosis is a disease of bone that leads to an increased risk of bone fracture. In osteoporosis the bone mineral density is reduced, bone microarchitecture is disrupted, and the amount and variety of collagen proteins in bone is altered....


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
    Anaphylaxis

    Anaphylaxis is an acute Circulatory system and very severe Type I hypersensitivity allergy reaction in humans and other mammals. The term comes from the Greek words a?a ana and f??a??? phylaxis ....
    , angioedema
    Angioedema

    Angioedema is the rapid swelling of the dermis, subcutaneous tissue, mucosa and submucosal tissues. It is very similar to urticaria, but urticaria occurs in the upper dermis....
    . (Highly unlikely, since dexamethasone is given to prevent anaphylactoid reactions.)


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
Poland

Poland , officially the Republic of Poland , is a country in Central Europe. Poland is bordered by Germany to the west; the Czech Republic and Slovakia to the south; Ukraine, Belarus and Lithuania to the east; and the Baltic Sea and Kaliningrad Oblast, a Russian Enclave and exclave, to the north....
 cross country skier Justyna Kowalczyk
Justyna Kowalczyk

Justyna Kowalczyk is a Poland cross country skier who has been competing since 2000. She won the bronze medal in the 30 km freestyle at the 2006 Olympic Winter Games in Turin, becoming the first Pole to medal in cross country skiing at the Winter Olympics....
 was disqualified from the Under 23 (U23) OPA (Alpine nations) Intercontinential Competition in Germany
Germany

Germany , officially the Federal Republic of Germany , is a country in Central Europe. It is bordered to the north by the North Sea, Denmark, and the Baltic Sea; to the east by Poland and the Czech Republic; to the south by Austria and Switzerland; and to the west by France, Luxembourg, Belgium, and the Netherlands....
 and issued a 2-year suspension for her doping offenses on dexamethasone. This was eventually reduced to one year during 2005 and later rescinded by the Court of Arbitration for Sport
Court of Arbitration for Sport

The Court of Arbitration for Sport is an international arbitration body set up to settle disputes related to sports. Its headquarters are in Lausanne; there are additional courts located in New York City and Sydney, with ad-hoc courts created in Olympics host cities as required....
 in December 2005. She would later earn a bronze in the women's 30 km freestyle mass start at the 2006 Winter Olympics
2006 Winter Olympics

The 2006 Winter Olympics, officially known as the XX Olympic Winter Games, were a winter multi-sport event which was celebrated in Turin, Italy from February 10, 2006, through February 26, 2006....
 in Turin
Turín

Tur?n is a municipality in the Ahuachap?n Department Departments of El Salvador of El Salvador....
.

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