Glucocorticoids

Classification:

1.Natural		Cortisol(t½:1-1.5hr) Hydrocortisone
2.Synthetic	[A]Short acting (8-12 hours)	Prednisolone Prednisone Methyl-prednisolone
	[B]Intermediate acting (12-36 hours)	Flu-prednisolone Paramethasone Triamcinolone
	[C]Long acting (36-72 hours)	Dexamethasone Betamethasone Beclomethasone

Mechanism of action/ Prednisolone/Dexamethasone/Glucocorticoids::

Glucocorticoids

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Enter into the cell

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Bind with specific protein in the cytoplasm

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Steroid receptor complex

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The complex enters into the nucleus

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Binds with (GRE)glucocorticoid receptor element of specific gene

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Transcription reaction

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mRNA in the cytoplasm

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Synthesis of new protein

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New protein is responsible for various effects of steriod.

Adverse effect /Prednisolone/Dexamethasone/ Glucocorticoids:

1)      Cushing’s syndrome.

2)      Avascular necrosis of bone.

3)      Insomnia.

4)      Diabetic mellitus.

5)      Glucoma.

6)      Increased intra-cranial pressure.

7)      Fever.

8)      Nausea,dizzines,weight.

Indications/Prednisolone/Dexamethasone/Glucocorticoids:         

1)      Allergic reaction:

·         Asthma.

·         Allergic rhinitis.

·         Urticaria.

·         Anphylactic shock.

2)      Bone and joint disease:

·         Arthritis.

·         Bursitis.

·         Sinuvitis.

3)      Collagen vascular disease:

·         SLE.

·         Rheumatoid arthritis.

4)      Dermatological diseases:

·         Atopic dermatitis.

·         Contact dermatitis.

·         Seborrheic dermatitis.

5)      Eye disease:

·         Acute uveitis.

·         Choroiditis.

·         Optic neuritis.

6)      Joint disease.

7)      Kidney disease:nephrotic syndrome.

8)      Lung disease:

·         Bronchial asthma.

·         Infant respiratory distress.

·         Aspiraton pneumonia.

9)      Neurological disorders:

·         Cerebral oedema.

·         Multiple sclerosis.

10)  Sub-acute thyroiditis.

Contraindication:

1)      Cushing syndrome(absolute contraindication)

2)      Peptic ulcer.

3)      DM.

4)      Infection.

5)      Osteoporosis.

6)      HTN.

7)      CCF.

8)      Children(because glucocorticoids cause growth reterdation).

9)      Psychosis.

10)  Glaucoma.

11)  Epilepsy.

12)  TB.

13)  Renal dysfunction.

14)  Thrombo-embolism.

Difference between Prednisolone & Ketoprofen:

Trait	Prednisolone	Ketoprofen
1.Type	Steroidal anti-inflammatory	Non-steroidal anti-inflammatory
2.M/A	Inhibit phospholipase A2→No arachidonic acid synthesis from member phospholipids→ so no PG,LT→ anti-  inflammatory action	Inhibit cycloxygenase→No PG synthesis from arachidonic acid→So no mediators of inflammation→Anti-inflammatory action
3.Adverse effects	Cushing syndrome, Insomnia,DM,Avascular necrosis of bone.	PUD,Headache,Dizziness, Neutropenia.