Glucocorticoids

TYPES:
  • Glucocorticoids are:
  1. Cortisol
  2. Corticosterone
  3. Cortisone.
GLUCOCORTICOID DRUGS:
  1. Beclomethasone
  2. Budesonide
  3. Cortisone(least)
  4. Prednisone
  5. Hydrocortisone(maximum effect)
  • Intermediate acting:
  1. Methylprednisolone
  2. Prednisolone
  3. Triamcinolone
  • Long acting:
  1. Betamethasone(most potent)
  2. Dexamethasone
SOURCE OF SECRETION:
  • Secreted mainly by zonafasciculataof adrenal cortex.
  • A small quantity of glucocorticoids is also secreted by zonareticularis.
  • Intracellular receptors are used by glucocorticoid
  • Pregnenolone is Common precursor of mineralocorticoid, glucocorticoids and sex steroids
  • Chemical process involved in conversion of progesterone to glucocorticoids is Hydroxylation
ACTION:
  • On Carbohydrate Metabolism
  1. Glucocorticoids increase the blood glucose level by two ways:
  2. By promoting gluconeogenesis in liver from amino acids
  3. By inhibiting the uptake and utilization of glucose by peripheral cells
  • On Protein Metabolism
  1. Glucocorticoids promote the catabolism of proteins Leading to:
  2. Decrease in cellular proteins
  3. Increase in plasma level of amino acids
  4. Increase in protein content in liver.
  • On Fat Metabolism
  1. Actions on fats are:
  2. Mobilization of fatty acids from adipose tissue
  3. Increasing the utilization of fat for energy.
  4. It leads to the formation of a large amount of ketone bodies
  5. On Water Metabolism
  6. Glucocorticoids play an important role in the maintenance of water balance, by accelerating excretion of water.
  • On Mineral Metabolism
  1. Glucocorticoids enhance the retention of sodium and to lesser extent, increase the excretion of potassium.
  2. Glucocorticoids decrease the blood calcium by inhibiting its absorption from intestine and increasing the excretion through urine
  • On Bone
  1. Glucocorticoids stimulate the bone resorption (osteoclastic activity) and inhibit bone formation and mineralization (osteoblastic activity)causing osteoporosis On Muscles
  2. Glucocorticoids increase the catabolism of proteins in muscle.
  • On Blood Cells
  1. Destruction of eosinophils in reticuloendothelial cells
  2. Decrease the number of basophils and lymphocytes and increase the number of circulating neutrophils, RBCs and platelets.
  • On Vascular Response
  1. Presence of glucocorticoids is essential for the constrictor action of adrenaline and noradrenaline
  • On CNS:
  1. Insufficiency of these hormones causes personality changes like irritability and lack of concentration.
  2. Sensitivity to olfactory and taste stimuli increases in adrenal insufficiency.
  • Permissive Action of Glucocorticoids:
  1. Calorigenic effect of glucagon
  2. Lipolytic effect of catecholamines
  3. Vascular effects of catecholamines
  4. Bronchodilator effect of catecholamines
  • On Resistance to Stress:
  1. The increase in glucocorticoid level is very essential for survival during stress conditions, as it offers high resistance to the body against stress. Anti-Inflammatory Effects:
  2. Glucocorticoids prevent the inflammatory changes by ↑ Lipocortin
  3. Anti-allergic Actions
USES:
  • Autoimmune disorders
  1. Multiple sclerosis
  2. Rheumatoid arthritis:Suppression of inflammation
  3. Inflammatory bowel disease
  4. Ulcerative colitis
  5. Psoriasis
  6. Eczema
  7. Allergies and asthma
  • Adrenal insufficiency:
  1. In adrenal insufficiency body can’t produce enough cortisol.
  2. This can be a result of a condition such as Addison’s disease or surgical removal of your adrenal glands.
  3. Glucocorticoids can be used to replace cortisol that your body can no longer make.
  • Heart failure
  1. Short-term use (less than 7 days) of glucocorticoids can help treat heart failure by increasing your body’s ability to respond to certain diuretics.
  •  Cancer
  1. Glucocorticoids can be used in cancer therapy to reduce some of the side effects of chemotherapy. 
  2. They may also be used to kill some cancer cells in some cancers, including:
  • Acute lymphoblastic leukemia
  • Chronic lymphoblastic leukemia
  • Hodgkin lymphoma
  • Non-Hodgkin lymphoma
  • Multiple myeloma
  • Preterm Labour help in reducing 
  1. Respiratory distress syndrome, 
  2. Intraventricular hemorrhage, 
  3. Necrotising enterocolitis
  • Induction of thymic involution, Production of surfactant by type II alveolar cells & Functional hypothalamopituitary axis depends on production of maternal or fetal glucocorticoid Skin conditions
  • Skin conditions ranging from eczema to poison ivy are treated with glucocorticoids. 
Surgery
  1. Glucocorticoids may be used during sensitive neurosurgeries. 
  2. They reduce inflammation in delicate tissues. 
  3. They are also administered right after an organ transplant to help prevent the immune system from rejecting the donor organ.
SIDE EFFECTS:
  • Increase blood sugar level, which can trigger temporary and possibly long-term diabetes
  • Suppress body’s ability to absorb calcium, which can lead to osteoporosis
  • Increase cholesterol and triglyceride levels
  • Increase risk of ulcers and gastritis
  • Oral candidiasis can occur as a side effect of inhaled glucocorticoids in bronchial asthma
  • Delay wound healing, which requires a certain amount of inflammation
  • Suppress immune system and make more prone to infections
  1. Long-term use:
  2. Fatty hump between shoulders
  3. Round face
  4. Weight gain
  5. Pink stretch marks
  6. Weakened bones
  7. Diabetes
  8. High blood pressure
  9. Thin skin
  10. Slow healing
  11. Acne
  12. Irregular menstrual cycles
  13. Decreased libido
  14. Fatigue
  15. Depression
Exam Question
  • Drug causing hyperglycemia is Glucocorticoid
  • Glucocorticoids causes Muscle wasting, Diabetes mellitus, Osteoporosis,Peptic ulceration, Cataracts
  • Induction of thymic involution, Production of surfactant by type II alveolar cells & Functional hypothalamopituitary axis depends on production of maternal or fetal glucocorticoid Glucocorticoids given to a case of Preterm Labour help in reducing Respiratory distress syndrome, Intraventricular hemorrhage, Necrotising enterocolitis Stress-induced hyperglycemia is due to Glucocorticoids
  • Oral candidiasis can occur as a side effect of inhaled glucocorticoids in bronchial asthma
  • Glucocorticoids act in inflammation by ↑ Lipocortin
  • Cortisone has least glucocorticoid activity
  • Compared to hydrocortisone, maximum glucocorticoid activity is seen in Hydrocortisone
  • Short acting glucocorticoid is Hydrocortisone
  • Longest acting glucocorticoids is Dexamethasone
  • The primary goal of glucocorticoid treatment in rheumatoid arthritis is Suppression of inflammation and improvement in functional capacity
  • Glucocorticoids drug produce neutrophilia
  • Betamethasone is the most potent glucocorticoid
  • Glucocorticoids induces apoptosis in a cell 
  • Pregnenolone is Common precursor of mineralocorticoid, glucocorticoids and sex steroids
  • Intracellular receptors are used by glucocorticoid
  • Chemical process involved in conversion of progesterone to glucocorticoids is Hydroxylation
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