Corticosteroids

Introduction

Steroidal hormones produced in the adrenal cortex mainly it is involved in the regulation of physiological activity, such as:

1. Immune response
2. Carbohydrate metabolism
3. Regulation of inflammation
4. Protein metabolism
5. 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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