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All about: Dexamethasone

Big Image Pronouncation: (DEX-uh-METH-uh-sone)
Class: Topical corticosteroid, Glucocorticoid, Corticosteroid

Trade Names:
Dexamethasone
- Tablets 0.5 mg
- Tablets 0.75 mg
- Tablets 1 mg
- Tablets 1.5 mg
- Tablets 2 mg
- Tablets 4 mg
- Tablets 6 mg
- Elixir 0.5 mg per 5 mL
- Solution, oral 0.5 mg per 5 mL

Trade Names:
Dexamethasone Intensol
- Concentrate, oral 1 mg/mL

Trade Names:
Maxidex
- Suspension, ophthalmic 0.1%

Dexamethasone Sodium Phosphate

Trade Names:
Dexamethasone Sodium Phosphate
- Injection 4 mg/mL
- Injection 10 mg/mL

Trade Names:
Dexasol
- Solution, ophthalmic 0.1%

PMS-Dexamethasone (Canada)
ratio-Dexamethasone (Canada)

Mechanism of Action

Pharmacology

Synthetic long-acting glucocorticoid that depresses formation, release and activity of endogenous mediators of inflammation including prostaglandins, kinins, histamine, liposomal enzymes and complement system. Also modifies body's immune response.

Pharmacokinetics

Metabolism

Metabolized in the liver by CYP3A4.

Elimination

The t ½ 1.8 to 3.5 h.

Onset

Rapid (injection).

Duration

Short (injection).

Indications and Usage

Testing of adrenal cortical hyperfunction; management of allergic and inflammatory ophthalmic processes, allergic states, cerebral edema associated with primary or metastatic brain tumor, collagen diseases, craniotomy or head injury, dermatologic diseases, edematous states (caused by nephrotic syndrome), GI diseases, hematologic disorders, multiple sclerosis, neoplastic diseases, primary or secondary adrenal cortex insufficiency, respiratory diseases, rheumatic disorders, trichinosis with neurologic or myocardial involvement, tuberculous meningitis.

Intralesional administration

Treatment for such conditions as alopecia areata, discoid lupus erythematosus, keloids, psoriatic plaques.

Intra-articular or soft tissue administration

Short-term adjunctive treatment for such conditions as synovitis of osteoarthritis, rheumatoid arthritis, acute gouty arthritis, posttraumatic osteoarthritis.

Ophthalmic

Treatment of steroid-responsive inflammatory conditions of palpebral and bulbar conjunctiva, lid, cornea, and anterior segment of globe.

Contraindications

Systemic fungal infections; IM use in idiopathic thrombocytopenic purpura; administration of live virus vaccines; topical monotherapy in primary bacterial infections; intranasal use in untreated localized infections involving nasal mucosa; ophthalmic use in acute superficial herpes simplex keratitis, fungal diseases of ocular structures, vaccinia, varicella, and ocular tuberculosis.

Dosage and Administration

All dosages shown are for adults unless indicated otherwise.

Dexamethasone
Initial dose

PO 0.75 to 9 mg/day.

Suppression Tests Cushing syndrome

PO 1 mg at 11 PM or 0.5 mg every 6 h for 48 h.

To distinguish Cushing syndrome-caused pituitary ACTH excess from other causes

PO 2 mg every 6 h for 48 h.

Acute Mountain Sickness

PO 4 mg every 6 h.

Antiemetic

PO 16 to 20 mg.

Diagnosis of Depression

PO 1 mg.

Hirsutism

PO 0.5 to 1 mg/day.

Ophthalmic solution

Instill 1 to 2 drops into conjunctival sac 4 to 6 times daily.

Dexamethasone Sodium Phosphate
Systemic

IV/IM 0.5 to 9 mg/day.

Cerebral Edema

IV 10 mg, then IM 4 mg every 6 h until max response.

Brain Tumors

IV/IM 2 mg 2 to 3 times daily.

Unresponsive shock

IV 1 to 6 mg/kg as single injection; or 40 mg followed by repeated IV injections every 2 to 6 h.

Bacterial meningitis

IV 0.15 mg/kg every 6 h.

Bronchopulmonary dysplasia in preterm infants

IV 0.5 mg/kg.

Intra-Articular, Intralesional, or Soft Tissue

Large joints 2 to 4 mg; small joints 0.8 to 1 mg; bursae 2 to 3 mg; tendon sheaths 0.4 to 1 mg; soft tissue infiltration 2 to 6 mg; ganglia 1 to 2 mg.

Ophthalmic solution

Instill 1 to 2 drops into conjunctival sac every 1 h during day and every 2 h during night.

Storage/Stability

Refer to package insert for directions on how to store particular form of dexamethasone.

Drug Interactions

Aminoglutethimide

May decrease dexamethasone-induced adrenal suppression.

Anticholinesterases

May antagonize anticholinesterase effects in myasthenia gravis.

Anticoagulants, oral

May alter anticoagulant dose requirements.

Barbiturates

May decrease effects of dexamethasone.

Hydantoins

May increase Cl and decrease therapeutic efficacy of dexamethasone.

Rifampin

May increase Cl and decrease therapeutic efficacy of dexamethasone.

Salicylates

May reduce serum levels and efficacy of salicylates.

Troleandomycin

May increase dexamethasone effects.

Laboratory Test Interactions

May cause increased urine glucose and serum cholesterol; decreased serum levels of potassium, T 3 and T 4 ; decreased uptake of thyroid 131 I; false-negative nitroblue-tetrazolium test; altered brain scan results; suppression of skin test reactions.

Adverse Reactions

Cardiovascular

Cardiac arrhythmias or ECG changes, CHF, hypertension, myocardial rupture, necrotizing angiitis, syncopal episodes, thromboembolism or fat embolism, thrombophlebitis.

CNS

Headache, increased intracranial pressure with papilledema (pseudotumor cerebri), neuritis, paresthesias, psychosis, seizures, vertigo.

Dermatologic

Acneiform eruptions, allergic contact dermatitis, allergic dermatitis, angioneurotic edema, burning, cracking and tightening of skin, dryness, erythema, erythema, folliculitis, hirsutism, hyperpigmentation or hypopigmentation, hypertrichosis, pruritus, impaired wound healing, irritation, itching, lupus erythematosus-like lesions, miliaria, perineal irritation, perioral dermatitis, secondary infections, skin atrophy, stinging, striae, subcutaneous fat atrophy, striae, telangiectasia (topical), thin fragile skin, petechiae and ecchymoses, urticaria.

EENT

Posterior subcapsular cataracts; increased IOP; glaucoma; exophthalmos. Dry mouth; throat irritation; hoarseness; dysphonia; coughing (oral inhalation). Nasal irritation; burning; stinging; dryness; epistaxis or bloody mucus; rebound congestion; sneezing, rhinorrhea; anosmia; loss of sense of taste; throat discomfort (intranasal). Glaucoma with optic nerve damage; visual acuity and field defects; posterior subcapsular cataract formation; secondary ocular infections; transient stinging or burning (ophthalmic).

GI

Abdominal distension, bowel perforation, increased appetite and weight gain, nausea, pancreatitis, peptic ulcer with perforation and hemorrhage, ulcerative esophagitis, vomiting.

Genitourinary

Increased or decreased number and motility of spermatozoa.

Hematologic

Leukocytosis.

Metabolic

Hypocalcemia, hypokalemia, hypokalemic alkalosis, metabolic alkalosis, sodium and fluid retention.

Respiratory

Wheezing (oral inhalation).

Miscellaneous

Aggravation or masking of infections, endocrine abnormalities (eg, menstrual irregularities, cushingoid state, growth suppression in children sweating, decreased carbohydrate tolerance, hyperglycemia, glycosuria, increased insulin or sulfonylurea requirements in diabetics, anaphylactoid or hypersensitivity reactions), facial flushing (intra-articular), fatigue, hypersensitivity, infection, insomnia, leukocytosis, malaise, musculoskeletal effects (eg, weakness, myopathy, muscle mass loss, osteoporosis, spontaneous fractures), osteonecrosis, postinjection flare, skin atrophy, tendon rupture, topical use may theoretically produce adverse reactions seen with systemic use because of absorption.

Precautions

Pregnancy

Pregnancy category undetermined (systemic use); Category C (topical uses).

Lactation

Excreted in breast milk.

Children

May be more susceptible to adverse reactions from topical use than are adults. Observe growth and development of infants and children on prolonged therapy.

Elderly

May require lower doses.

Renal Function

Use cautiously; monitor renal function.

Sulfite Sensitivity

Some products may contain sodium bisulfite, which may cause allergic-type reactions in some individuals.

Adrenal suppression

Prolonged therapy may lead to hypothalamic-pituitary-adrenal suppression.

Fluid and electrolyte balance

Can cause elevated BP, salt and water retention, and increased potassium and calcium excretion. Dietary salt restriction and potassium supplementation may be needed.

Hepatitis

May be harmful in chronic active hepatitis positive for hepatitis B surface antigen.

Infections

May mask signs of infection. May decrease host-defense mechanisms to prevent dissemination of infection.

Ocular effects

Use systemically with caution in ocular herpes simplex because of possible corneal perforation.

Ophthalmic use

Prolonged use may result in glaucoma or other complications.

Peptic ulcer

May contribute to peptic ulceration, especially in large doses.

Stress

Increased dosage of rapidly acting corticosteroid may be needed before, during and after stressful situations.

Withdrawal

Abrupt discontinuation may result in adrenal insufficiency. Discontinue gradually.

Overdosage

Symptoms

Acne, anorexia, arthralgia, central obesity, diabetes, dizziness, dyspnea, ecchymoses, electrolyte and fluid imbalance (chronic cushingoid changes), fainting, fever, hirsutism, hyperlipidemia, hypertension, hypoglycemia (acute overdose), infection, malaise, moonface, myalgia, myopathy, nausea, orthostatic hypotension, osteoporosis, peptic ulcer, sexual dysfunction, skin desquamation, striae.

Patient Information

  • Caution patient that stopping drug abruptly is dangerous and may cause adrenal insufficiency.
  • Explain rationale for tapering off medication when that time comes.
  • Teach patient or family procedures for correctly administering specific form of drug (eg, ophthalmic).
  • Caution patient against receiving immunizations while drug is being taken.
  • Advise patient on long-term therapy to carry medication identification card or to wear bracelet. In case of emergency, this information is important for treatment.
  • Instruct patient to avoid people with infections, particularly respiratory.
  • Teach patient to take oral forms with meals or snacks if GI irritation occurs.
  • Review guidelines for missed doses of particular product with patient.
  • Teach patient on long-term therapy how to keep a weight record.
  • Instruct patient to inform other health care providers if taking a steroid.
  • Review signs of infection and remind patient that fever, swelling, and redness may be masked in infection.
  • Review possible adverse reactions of dexamethasone with patient and to report these to health care provider.

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