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Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs that has anti-inflammatory and immunosuppressant effects. It is 25 times more potent than cortisol in its glucocorticoid effect, while having minimal mineralocorticoid effect.
It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system
Endocrine
Dexamethasone is the treatment for the very rare disorder of glucocorticoid resistance.
In adrenal insufficiency and Addison's disease, dexamethasone is prescribed when the patient does not respond well to prednisone or methylprednisolone.
It can be used in congenital adrenal hyperplasia in older adolescents and adults in order to suppress ACTH production. It is typically given at night.
Pregnancy
Dexamethasone may be given to women at risk of delivering prematurely to promote maturation of the fetus' lungs. This has been associated with low birth weight, although not with increased rates of neonatal death.
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.
Synthesis
To synthesize dexamethasone, 16β-methylprednisolone acetate is dehydrated to the 9,11-dehydro derivative. This is then reacted with a source of hypobromite, such as basic N-bromosuccinimide, to form the 9α-bromo-11β-hydrin derivative, which is then ring-closed to an epoxide. A ring-opening reaction with hydrogen fluoride in tetrahydrofuran gives dexamethasone.
Nonmedical use
Dexamethasone is given in legal Bangladeshi brothels to prostitutes not yet of legal age, causing weight gain aimed at making them appear healthier and older to customers and police.
Rare instances of anaphylactoid reactions have occurred in patients receiving corticosteroid therapy (see ADVERSE REACTIONS).
Increased dosage of rapidly acting corticosteroids is indicated in patients on corticosteroid therapy subjected to any unusual stress before, during, and after the stressful situation.
Cardio-Renal
Average and large doses of corticosteroids can cause elevation of blood pressure, sodium and water retention, and increased excretion of potassium. These effects are less likely to occur with the synthetic derivatives except when used in large doses. Dietary salt restriction and potassium supplementation may be necessary. All corticosteroids increase calcium excretion.
Literature reports suggest an apparent association between use of corticosteroids and left ventricular free wall rupture after a recent myocardial infarc-tion;therefore, therapy with corticosteroids should be used with great caution in these patients.
Medical use
Anti-inflammatory
Dexamethasone is used to treat many inflammatory and autoimmune conditions, such as rheumatoid arthritis and bronchospasm. Idiopathic thrombocytopenic purpura, decreased numbers of platelets due to an immune problem, responds to 40 mg daily for four days; it may be administered in 14-day cycles. It is unclear whether dexamethasone in this condition is significantly better than other glucocorticoids.
It is also given in small amounts 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 after eye surgery– and as a nasal spray (trade name Dexacort), and certain ear drops (Sofradex, when combined with an antibiotic and an antifungal)
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:
Acne; clumsiness; dizziness; facial flushing; feeling of whirling motion; general body discomfort; headache; increased appetite; increased sweating; nausea; nervousness; pain, swelling, or redness at the injection site; sleeplessness; upset stomach.
Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); black, tarry stools; changes in body fat; changes in menstrual periods; changes in skin color; chest pain; easy bruising or bleeding; mental or mood changes (eg, depression); muscle pain, weakness, or wasting; swelling of feet or legs; seizures; severe nausea or vomiting; sudden severe dizziness or headache; symptoms of infection (eg, fever, chills, sore throat); tendon or bone pain; thinning of the skin; unusual skin sensation; unusual weight gain; vision changes or other eye problems; vomit that looks like coffee grounds.
Dexamethasone should be used with caution in patients with active tuberculosis infection of respiratory tract or in untreated fungal, bacterial or systemic viral infections. Corticosteroids should only be used systemically with great caution in the presence of congestive heart failure (CHF), recent myocardial infraction (MI), hypertension, diabetes mellitus, epilepsy, glaucoma, hypothyroidism, liver failure, osteoprosis, peptic ulceration or renal impairment. Children may be at increase risk of some adverse effects, corticosteroid cause growth retardation and prolonged use is rarely justified. Passive immunization is recommended to non-immune patients who do come in contact with chickenpox or measles. Live vaccine should not be given to patients receiving high dose systemic corticosteroid therapy nor for atleast 3 months afterwards, killed vaccine or toxoids may be given, although the response may be attenuated. During prolong treatment with corticosteroids, patients should be examined regularly, sodium intake may need to be reduced and calcium and potassium supplement may be necessary.
General
The lowest possible dose of corticosteroids should be used to control the condition under treatment. When reduction in dosage is possible, the reduction should be gradual.
Since complications of treatment with corticosteroids are dependent on the size of the dose and the duration of treatment, a risk/benefit decision must be made in each individual case as to dose and duration of treatment and as to whether daily or intermittent therapy should be used.
Kaposi's sarcoma has been reported to occur in patients receiving corticosteroid therapy, most often for chronic conditions. Discontinuation of corticos-teroids may result in clinical improvement.
Cardio-Renal
As sodium retention with resultant edema and potassium loss may occur in patients receiving corticosteroids, these agents should be used with caution in patients with congestive heart failure, hypertension, or renal insufficiency.
Endocrine
Drug-induced secondary adrenocortical insufficiency may be minimized by gradual reduction of dosage. This type of relative insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently.
Drug Interactions
Aminoglutethimide
Aminoglutethimide may diminish adrenal suppression by corticosteroids.
Amphotericin B injection and potassium-depleting agents
When corticosteroids are administered concomitantly with potassium-depleting agents (e.g., amphotericin B, diuretics), patients should be observed closely for development of hypokalemia. In addition, there have been cases reported in which concomitant use of amphotericin B and hydrocortisone was followed by cardiac enlargement and congestive heart failure.
Antibiotics
Macrolide antibiotics have been reported to cause a significant decrease in corticosteroid clearance (see Drug Interactions, Hepatic Enzyme lnducers, Inhibitors and Substrates).
Anticholinesterases
Concomitant use of anticholinesterase agents and corticosteroids may produce severe weakness in patients with myasthenia gravis. If possible, anticholinesterase agents should be withdrawn at least 24 hours before initiating corticosteroid therapy.
Anticoagulants, oral
Co-administration of corticosteroids and warfarin usually results in inhibition of response to warfarin, although there have been some conflicting reports. Therefore, coagulation indices should be monitored frequently to maintain the desired anticoagulant effect.
Antidiabetics
Because corticosteroids may increase blood glucose concentrations, dosage adjustments of antidiabetic agents may be required.
Antitubercular drugs
Serum concentrations of isoniazid may be decreased.
Cholestyramine
Cholestyramine may increase the clearance of corticosteroids
Cyclosporine
Increased activity of both cyclosporine and corticosteroids may occur when the two are used concurrently. Convulsions have been reported with this concurrent use.
Dexamethasone suppression test (DST)
False-negative results in the dexamethasone suppression test (DST) in patients being treated with indomethacin have been reported. Thus, results of the DST should be interpreted with caution in these patients.
OVERDOSAGE
Treatment of overdosage is by supportive and symptomatic therapy. In the case of acute overdosage, according to the patient’s condition, supportive therapy may include gastric lavage or emesis.
DOSAGE AND ADMINISTRATION
For oral administration: The initial dosage of dexamethasone varies from 0.75 to 9 mg a day depending on the disease being treated.
It Should Be Emphasized That Dosage Requirements Are Variable And Must Be Individualized On The Basis Of The Disease Under Treatment And The Response Of The Patient.
After a favorable response is noted, the proper maintenance dosage should be determined by decreasing the initial drug dosage in small decrements at appropriate time intervals until the lowest dosage that maintains an adequate clinical response is reached.
Situations which may make dosage adjustments necessary are changes in clinical status secondary to remissions or exacerbations in the disease process, the patient’s individual drug responsiveness, and the effect of patient exposure to stressful situations not directly related to the disease entity under treatment. In this latter situation it may be necessary to increase the dosage of the corticosteroid for a period of time consistent with the patient’s condition. If after long-term therapy the drug is to be stopped, it is recommended that it be withdrawn gradually rather than abruptly.
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