GLUCOCORTICOIDSADRENOCORTICAL STEROIDS

OPTOM FASLU MUHAMMED

SYNTHESISAdrenal 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

Mechanism of action at cellular levelCorticosteroids 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.

EXAMPLESHydrocortisonePrednisoloneMethylprednisoloneTriamcinoloneDexamethazoneBetamethazoneparamethasone

GENERAL PRINCIPLES OF STEROID THERAPYSteroids 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

Topical preparationsBetamethasone 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%

Systemic preparationsHydrocortisone injection ; vial contain 100

mg hydrocortisone IM/IVPrednisolone tabs 5, 10, 20 mgBetamethasone 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.

Ophthalmic uses of corticosteroidsConjunctival diseases: vernal conjunctivitis ,

PhlyctenulosisScleral diseases: episcleritis, sceleritisUveitisRetrobulbar neuritisTo prevent rejection of corneal graft.Prophylactic use against proliferative

vitreoretinopathy.Harada’s disease.Graves orbitopathy

Non ophthalmic indicationsSkin diseasesBronchial asthmaMalignanciesOrgan transplantationCerebral edema

Routes of administration of corticosteroids in eyeTOPICAL-as eye drops or ointments- dexamethasone,

betamethasone, prednisoloneMedroxy progesterone – used for alkali burns

of corneaRETROBULBAR AND PERIOCULAR ROUTESuspensions are used to sustain its effect for

4-8 weeksConsiderable concentration are achieved in

vitreous, optic nerve and uveal tract.

INTRA-VITREAL ROUTEUsed in endophthalmitis and in prophylaxis of

proliferative vitreo retinopathy.SYSTEMIC ROUTEGenerally indicated in those ocular conditions

which are actually a part of systemic autoimmune disorders.

Contraindications of steroid applicationDiabetes mellitusHypertensionPeptic ulcerPregnancyRenal failureEpilepsyPsychiatric problem

Ocular side effectsCataractGlaucomaDiffuse retinal pigmentSusceptibility to infectionDelay in corneal wound healing.

Systemic side effectsGI tract- peptic ulcerImmunity-increase infectionCVS- hypertensionCNS-psychosisEndocrine system- hyperglycaemia