Glucocorticoids

Glucocorticoids

1. GLUCOCORTICOIDS ADRENOCORTICAL STEROIDS OPTOM FASLU MUHAMMED

2. SYNTHESIS Adrenal gland is the important endocrine gland of human body. The steroidal hormone secreted from the adrenal gland have glucocorticoid and mineralocorticoid activities. Glucocorticoids are synthesized in the adrenal cortex They elicit their function by stimulating /inhibiting some protein synthesis

3. Mechanism of action at cellular level Corticosteroids penetrate cells-bind to high affinity cytoplasmic receptor protein a structural change occurs at receptor complex –allows it migration to nucleus and binding to specific site on chromatin transcription of specific site of mRNA regulation of protein synthesis In many tissues overall effect is inhibition of protein synthesis.

4. EXAMPLES Hydrocortisone Prednisolone Methylprednisolone Triamcinolone Dexamethazone Betamethazone paramethasone

5. GENERAL PRINCIPLES OF STEROID THERAPY Steroids are powerful drugs. they have potential to cause improvement in many severe disease as well as produce adverse effect if not used properly. Single dose is not harmful: can be used to tide over mortal crisis even when benefit is not certain Short courses are not likely to be harmful in the absence of contraindications : starting dose can be high in severe illness. Long term use is potentially hazardous: keep the dose to minimum, which is found to by trial and error method. No abrupt withdrawal after a corticoid has been given for >2 to 3 weeks : may precipitate adrenal insufficiency. Infection or any stress during therapy-increase the dose

6. Topical preparations Betamethasone sodium phosphate solution, 0.1% Hydrocortisone acetate solution, 1% and ointment ,25% Prednisolone acetate suspension , 0.125%, 1% Prednisolone sodium phosphate solution 0.125%, 1.00% Dexamethasone sodium phosphate solution and ointment 0.05%, 0.1%

7. Systemic preparations Hydrocortisone injection ; vial contain 100 mg hydrocortisone IM/IV Prednisolone tabs 5, 10, 20 mg Betamethasone tabs 0.5 mg and inj 4 mg/ml in 2 ml vial. Dexamethasone tabs 0.5 mg and inj 4 mg/ml in 2 ml vial.

8. Ophthalmic uses of corticosteroids Conjunctival diseases: vernal conjunctivitis , Phlyctenulosis Scleral diseases: episcleritis , sceleritis Uveitis Retrobulbar neuritis To prevent rejection of corneal graft. Prophylactic use against proliferative vitreoretinopathy . Harada’s disease. Graves orbitopathy

9. Non ophthalmic indications Skin diseases Bronchial asthma Malignancies Organ transplantation Cerebral edema

10. Routes of administration of corticosteroids in eye TOPICAL -as eye drops or ointments- dexamethasone , betamethasone , prednisolone Medroxy progesterone – used for alkali burns of cornea RETROBULBAR AND PERIOCULAR ROUTE Suspensions are used to sustain its effect for 4-8 weeks Considerable concentration are achieved in vitreous, optic nerve and uveal tract.

11. INTRA-VITREAL ROUTE Used in endophthalmitis and in prophylaxis of proliferative vitreo retinopathy. SYSTEMIC ROUTE Generally indicated in those ocular conditions which are actually a part of systemic autoimmune disorders.

12. Contraindications of steroid application Diabetes mellitus Hypertension Peptic ulcer Pregnancy Renal failure Epilepsy Psychiatric problem

13. Ocular side effects Cataract Glaucoma Diffuse retinal pigment Susceptibility to infection Delay in corneal wound healing.

14. Systemic side effects GI tract- peptic ulcer Immunity-increase infection CVS- hypertension CNS-psychosis Endocrine system- hyperglycaemia