Introduction
Table of Contents
Steroidal hormones produced in the adrenal cortex mainly it is involved in the regulation of physiological activity, such as:
- Immune response
- Carbohydrate metabolism
- Regulation of inflammation
- Protein metabolism
- Regulation of blood electrolyte level.
Types of Corticosteroids:
1. Glucocorticoid
2. Mineralocorticoid
1. Glucocorticoid
- Dexamethasone
- Prednisolone
- Fludrocortisone
Function
- Glucocorticoids are used in the treatment of joint pain and inflammation, dermatitis, allergic reaction, asthma, Hepatitis, ulcerative colitis.
- Used in the treatment of Addison’s disease.
- Topical formulations are used for skin infection, asthma, and laryngitis.
Side Effects:
- Anxiety, depression, psychosis.
- Hyperglycemia.
- Osteoporosis.
- Retinopathy.
Biosynthesis
Pharmacological Action:
Carbohydrate and Protein Metabolism:
- It promotes glycogen deposition in the liver.
- It promote gluconeogenesis.
- Induce protein break down.
- Increases uric acid excretion.
Fat Metabolism:
- Glucocorticoids induce lipolysis due to glucagon, growth hormone, adrenaline, and thyroxine.
- Break down of triglyceride enhanced by cAMP.
- Loses fat deposited over face, neck, and shoulder producing ‘moon face’, ‘fish mouth’ and ‘buffalo hump’.
Calcium Metabolism:
- It enhances the renal excretion of calcium.
- Results loss of Ca++ from bone, leading to negative calcium balance.
Cardiovascular System:
- Maintain myocardial contractility.
- It producing minor hypertension.
Skeletal Muscle:
- Enhances muscular activity.
- Excess glucocorticoid action leads to muscle wasting and myopathy.
CNS:
- Produces euphoria, insomnia, anxiety
Stomach:
- It increases gastric acid and pepsin secretion.
Blood and Lymphoid Tissue:
- Destruction of lymphoid tissue.
- Increasing the no. of RBC by inhibiting hemolysis.
- Decrease the no. of circulating lymphocytes, monocytes, basophils, eosinophils.
Effect on Immune Response:
- Blocks the synthesis of cytokines.
- Block the action of cytokines.
- Increasing the expression of a gene coding for an enzyme that degrades inflammatory mediators.
Hydrocortisone (Cortisol):
- Mainly used for the treatment of ulcerative colitis and hormone replacement therapy.
Prednisolone:
- It is 4 times more potent than hydrocortisone and more selective. Act as anti-inflammatory, anti-allergic, and used for the treatment of autoimmune disease.
Dexamethasone:
- Potent and selective glucocorticoid. It is used for the allergic and inflammatory condition, which is long-acting.
2. Mineralocorticoid
- Aldosterone is the prototype that produces mineralocorticoid effects.
- By acting on the distal tubule aldosterone enhances the absorption of Na+.
- A similar effect occurs in the colon, sweat gland, and salivary gland.
- Deficiency of mineralocorticoid action leads to hyponatremia, hyperkalemia, acidosis.
- Hyperaldosterinism results in positive Na+ balance increased plasma Na, hypokalaemia, alkalosis.
ACTH Inhibitors:
- Aminoglutethimide: Which stop/inhibit the conversion of cholesterol to pregnenolone. Used in the treatment of adrenocortical cancer.
- Metyrapone: 11 beta-hydroxylase enzyme inhibitor – used in Cushing’s syndrome and test of pituitary efficiency.
- Mifepristone: Progesterone antagonist.
- Ketoconazole: Inhibit the synthesis of all hormones in the testes and adrenal cortex, used in the treatment of Cushing’s syndrome and hirsutism in females.
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