Mechanism of action
Corticosteroid (long acting).
Binds to intracellular glucocorticoid receptor and changes gene expression which leads to decrease of leukocyte migration, suppression of inflammatory mediators and inhibition of macrophages and antigen presenting cells (APCs).
Indications and dose
Pharmacokinetics
Onset of action: rapid
Duration of action: 36–54 hours
Half-life of elimination: 4 hours
Metabolism: Hepatic, Kidneys
Elimination: Kidneys
Directions for administration
Parenteral dose is usually one-third to one half the oral dose.
Take tablet with or after food to prevent irritation to the gastrointestinal tract.
Relative potency
Hydrocortisone 1x
Predniso(lo)ne 4x
Methylprednisolone 4-5x
Dexamethasone 30x
Medicinal forms
Tablets – 1 mg, 2 mg, 4 mg, 8 mg, 20 mg, 40 mg
Solution for injection/infusion
- 1 vial = 2 ml (8 mg)
Side-effects
Endocrine:
- cushingoid faces, hirsutism, weight gain, menstrual irregularity
Immunosuppressive:
- increased susceptibility to infections
- suppression of clinical symptoms and signs
Musculoskeletal:
- osteoporosis
- tendon rupture
- myopathy
Fluid and electrolyte disturbance:
- sodium and water retention
- hypokalaemic alkalosis
- hypertension
Neuropsychiatric:
- wide range of psychiatric reactions
Opthalmic:
- increased intra-ocular pressure
Gastrointestinal:
- dyspepsia
- peptic ulceration, haemorrhage
- acute pancreatitis
Dermatological
- impaired healing, skin atrophy, bruising, acne, striae
General:
- leucocytosis
- thromboembolism
- hypersensitivity (anaphylaxis, angioedema)
Withdrawal:
- acute adrenal insufficiency, hypotension, death
- fever, myalgia, arthralgia, loss of weight
References
