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Adrenocorticosteroids & Adrenocortical Antagonists. By S. Bohlooli, PhD School of Medicine, Ardabil University of Medical Sciences. ADRENOCORTICOSTEROIDS. THE NATURALLY OCCURRING GLUCOCORTICOIDS SYNTHETIC CORTICOSTEROIDS. THE NATURALLY OCCURRING GLUCOCORTICOIDS; CORTISOL (HYDROCORTISONE).

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adrenocorticosteroids adrenocortical antagonists

Adrenocorticosteroids & Adrenocortical Antagonists

By

S. Bohlooli, PhD

School of Medicine, Ardabil University of Medical Sciences

adrenocorticosteroids
ADRENOCORTICOSTEROIDS
  • THE NATURALLY OCCURRING GLUCOCORTICOIDS
  • SYNTHETIC CORTICOSTEROIDS
the naturally occurring glucocorticoids cortisol hydrocortisone
THE NATURALLY OCCURRING GLUCOCORTICOIDS; CORTISOL (HYDROCORTISONE)
  • Pharmacodynamics
    • MECHANISM OF ACTION
    • PHYSIOLOGIC EFFECTS
    • METABOLIC EFFECTS
    • CATABOLIC AND ANTIANABOLIC EFFECTS
    • ANTI-INFLAMMATORY AND IMMUNOSUPPRESSIVE EFFECTS
    • OTHER EFFECTS
metabolic effect
Metabolic effect
  • Gluconeogensis
  • Muscle protein catablism
  • Lipolysis
  • Lipogenesis
  • Increase in insulin release
  • Decrease in glucose uptake in muscle
catabolic effect
Catabolic effect
  • Muscle protein catabolism
  • Wasting of
    • Lymphoid
    • connective tissue
    • Fat
    • Skin
  • Steoporesis
  • Growth inhibition in children
immunosuppressive effects
Immunosuppressive effects
  • Inhibit cell-mediated immunologic functions
  • Lymphotoxic
  • Important in the therapy of hematologic cancers
anti inflammatory effects
Anti-inflammatory effects
  • Dramatic effect of distribution and function of leukocyte
    • Increase neutrophils
    • Decrease lymphoctes, eosinophils, basophils, monocytes
    • Inhibition of leukocyte migration
  • Inhibition of PLA2
  • Decreased production of COX2
  • Decrease in IL2, IL3, and PAF
other effects
Other effects
  • Need for normal excretion of water load
  • Effect of CNS:
    • Low level: depression
    • High level: behavioral changes
  • Large doses: stimulation of gastric acid secretion and peptic ulcer
clinical pharmacology
Clinical Pharmacology
  • DIAGNOSIS AND TREATMENT OF DISTURBED ADRENAL FUNCTION
    • Adrenocortical insufficiency
      • Chronic (Addison\'s disease)
      • Acute
    • Adrenocortical hypo- and hyperfunction
      • Congenital adrenal hyperplasia
      • Cushing\'s syndrome
      • Aldosteronism
    • Use of glucocorticoids for diagnostic purposes
  • CORTICOSTEROIDS AND STIMULATION OF LUNG MATURATION IN THE FETUS
  • CORTICOSTEROIDS AND NONADRENAL DISORDERS
corticosteroids and nonadrenal disorders
CORTICOSTEROIDS AND NONADRENAL DISORDERS
  • Many disorders respond to coticosteroids
  • Inflammatory or immunologic diseases:
    • Asthma, organ transplant rejection, collagen disease
  • Hematopoietic cancers
  • Neurolgic disorders
  • Chemotherapy induced vomiting
  • Hypercalcemia
  • Mountain sickness
  • Hasten maturation of the fetal lungs
toxicity
Toxicity
  • METABOLIC EFFECTS
    • Growth inhibition, diabetes, muscle wasting, salt retention, psychosis,
  • OTHER COMPLICATIONS
    • Peptic ulcer,
    • masking of bacterial and fungal disease clinical finding
    • acute psychosis ,growth retardation
  • ADRENAL SUPPRESSION
contraindications cautions
Contraindications & Cautions
  • SPECIAL PRECAUTIONS
    • monitored carefully for the development of :
      • hyperglycemia, glycosuria, sodium retention with edema
      • hypertension, hypokalemia, peptic ulcer, osteoporosis, and hidden infections
contraindications
CONTRAINDICATIONS
  • Great caution in patients with:
      • Peptic ulcer
      • Heart disease or hypertension with heart failure
      • Psychoses
      • Diabetes
      • Osteoporosis
      • Glaucoma
antagonists of adrenocortical agents
ANTAGONISTS OF ADRENOCORTICAL AGENTS
  • SYNTHESIS INHIBITORS
    • Metyrapone
    • Aminoglutethimide
    • Ketoconazole
    • Trilostane
  • GLUCOCORTICOID ANTAGONISTS
    • Mifepristone (RU 486)
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