Corticosteroids

• What are corticosteroids?


  Corticosteroids are a class of steroid hormones produced in the adrenal cortex.
• What types of corticosteroids are included in this class?


  Corticosteroids include natural glucocorticoids and mineralocorticoids, and their synthetic analogues.
• From what are steroids synthesized in the adrenal cortex?


  Steroids are synthesized from cholesterol in adrenal cortical cells.
• How many zones is the adrenal cortex divided into?


  The adrenal cortex is divided into three zones.
• What is produced in the zona glomerulosa?


  Mineralocorticoids such as aldosterone are produced in the zona glomerulosa.
• What is the function of aldosterone?

  Aldosterone regulates sodium and water balance.
• What is produced in the zona fasciculata?


  Glucocorticoids such as hydrocortisone are produced in the zona fasciculata.
• What are the functions of glucocorticoids?


  Glucocorticoids regulate carbohydrate and protein metabolism and Na+ & H2O balance.
• What is produced in the zona reticularis?


  The zona reticularis is involved in the biosynthesis of androgens.
• How many carbon atoms do corticosteroids have?


  Corticosteroids have 21 carbon atoms.
• What are the two classes of steroids synthesized by the adrenal cortex?


  The two classes are corticosteroids and androgens.
• What are the classifications of steroids?

  • Mineralocorticoids (e.g., Cortisone, Fludrocortisone)
  • Glucocorticoids (e.g., Betamethasone, Methylprednisolone)
  • Sex Steroids (e.g., Estrogen, Progestins)
• How do steroids exert their action in the body?

  Steroids bind to transcortin in blood and then to cytoplasmic receptor proteins.
• What happens after glucocorticoids bind to their receptor proteins?


  Structural changes occur in the receptor-steroid complex, leading to migration into the nucleus.
• What is the role of glucocorticoid response elements?


  They bind to the steroid complex on chromatin, leading to gene suppression.
• What contributes to the anti-inflammatory and immunosuppressive action of glucocorticoids?


  Gene inhibition contributes to their anti-inflammatory and immunosuppressive action.
• What are the pharmacologic actions of glucocorticoids on metabolism?


  • Carbohydrates: Increase gluconeogenesis and peripheral glucose utilization.
  • Protein: Decrease conversion of AAs to proteins, increase muscle wasting.
  • Fat: Promote lipolysis, causing moon face.
• How do glucocorticoids affect mineral metabolism?


  They impair calcium absorption from the gut.
• What cardiovascular effects do glucocorticoids have?


  They increase the incidence of clots and blood pressure.
• What effects do glucocorticoids have on skeletal muscles?


  They cause weakness in cases of hypo and hypercorticism.
• What central nervous system effects can glucocorticoids precipitate?


  They can precipitate seizures in epileptic patients and cause euphoria and hostility.
• How do glucocorticoids affect gastric secretion?


  They increase the secretion of gastric acid and pepsin.
• What is the effect of glucocorticoids on the inflammatory and allergy response?


  They decrease the production of inflammatory cells and reduce allergic response.
• How do glucocorticoids affect the hemopoietic system?


  They increase the number of RBCs and platelets but decrease lymphocytes, eosinophils, and basophils.
• What is the effect of glucocorticoids on the inflammatory response?


  They reduce phagocytic activity.
• How do glucocorticoids affect immunologic and allergic responses?


  They suppress all types of allergic phenomena and hypersensitization.
• What is the absorption route for corticosteroids?


  Corticosteroids are effective via the oral route and act rapidly by IV/IM.
• What is the bioavailability of synthetic corticosteroids?


  The oral bioavailability of synthetic corticosteroids is high.
• What is the plasma protein binding percentage for corticosteroids?


  Plasma protein binding is 90%.
• How are corticosteroids metabolized?


  Corticosteroids are metabolized by hepatic microsomal enzymes.
• How are corticosteroids excreted from the body?


  Corticosteroids are excreted in urine.
• How are corticosteroids distributed in the body?


  Corticosteroids are widely distributed in the body.
• What are the categories and doses of glucocorticoids based on their duration of action?


  • Short Acting (t1/2 <12h): Hydrocortisone (20mg), Cortisone (25mg)
  • Intermediate Acting (t1/2 12 – 36 h): Prednisolone (5mg), Methylprednisolone (4mg), Triamcinolone (4mg)
  • Long Acting (t1/2 > 36 h): Paramethasone (2mg), Dexamethasone (0.75mg), Betamethasone (0.75mg)
• What are the doses of mineralocorticoids?

  • Desoxycortisone: 2.5mg
  • Fludrocortisone: 0.2mg
  • Aldosterone: dosage varies
• What are the indications for corticosteroid therapy?


  • Replacement therapy for adrenal insufficiency
  • Arthritis
  • Severe allergic reactions
  • Autoimmune diseases
  • Bronchial asthma
  • Infective diseases
  • Eye and skin inflammatory diseases
  • Intestinal diseases
  • Cerebral edema
  • Malignancies
  • Organ transplantation
  • Septic shock
  • Thyroid storm
  • Addison's disease
  • Adrenogenital syndrome
• What are the adverse effects of mineralocorticoids?


  Adverse effects include Na and water retention, edema, hypokalemic alkalosis, and hypertension.
• What are the adverse effects of glucocorticoids?


  Adverse effects include Cushing habitus, hyperglycemia, myopathy, susceptibility to infections, peptic ulceration, osteoporosis, glaucoma, growth retardation, and fetal abnormalities.
• What are the absolute contraindications for corticosteroid use?


  • Hypersensitivity
  • Cushing syndrome
• What are the relative contraindications for corticosteroid use?


  • Peptic ulcer
  • Diabetes mellitus and hypertension
  • Viral and fungal infections
  • Tuberculosis
  • Osteoporosis
  • Psychosis
  • Epilepsy
  • Congestive heart failure
  • Renal failure
• Where are androgens secreted from?


  Androgens are secreted by the testes.