2.Corticosteroids

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Corticosteroids

Dr.S.A.F.Kurukulasuriya


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Contents History

Introduction Biosynthesis

Classes of steroids

Types of steroids Actions of steroids

Pharmacokinetics of steroids


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Contents contd Indications for steroids

Side effects of steroids Precautions/ Contraindications

Acute adrenocortical insufficiency


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History Tadeusz Reichestein and colleagues were

awarded the Nobel Prize for in 1950 for

their work on the hormones of the adrenal

cortex.Cortisone was isolated by them.


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Introduction A class of steroid hormones produced in the

adrenal cortex.

Involved in the

1. stress response

2. immune response

3.

Regulation of inflammation4. Carbohydrate and protein metabolism

5. Blood electrolyte levels

6. Behavior


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Cholesterol

Pregnenolone

Progesterone

11-deoxycorticosterone

Corticosterone

18-hydroxy-corticosterone

Aldosterone Corticosterone


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Classes of corticosteroids 4 classes based on chemical structure

1. Group A-Hydrocortisone,Hydrocortisone

acetate

2. Group B-Triamcenelone acetonide, Budesonide

3. Group C-Betamethasone,Dexamethasone,

4. Group D-Hydrocortisone 17-butyrate,Betamethasone


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Types of corticosteroids Topical-skin,eye,mucous membranes

Inhaled-Treat nasal

mucosa,sinuses,bronci,lungs

Oral-prednisone,prednisolone

Systemic-intravenously


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Actions of hydrocortisone1. Mineralocorticoid effects

2. Glucocorticoid effects


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Mineralocorticoid effects Increased retention of sodium by the renal

tubule

Increased excretion of potassium in the

urine


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Glucocorticoid effects Carbohydrate metabolism-Increased

gluconeogenisis,Hyperglycaemia,

Glycosuria

Protein metabolism-negative nitrogen

balance with muscle wasting,

Osteoporosis, delayed wound healing.

Fat deposition increased


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Glucocorticoid effects contd Inflammatory response depressed-

Neutrophil and macrophage function

depressed

Allergic response suppressed

Anti vitamin D action

Reduction of hypercalcaemia

Urinary calcium excretion increased


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Hydrocortisone The principal naturally occurring steroid

Oral /I.V. /intra-articularly

The I.V. form is given for rapid effect in

emergency (deficiency,allergy or

inflammatory disease)

Tablet strength 20 mg


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Prednisolone Biologically active

Mainly anti-inflammatory(glucocorticoid)

Little sodium retaining activity


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Triamcinolone Fluorinated corticosteroid

No mineralocorticoid activity

May cause muscle wasting, anorexia,

depression


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Fludrocortisone Great sodium retaining effect

Little anti-inflammatory action

To replace aldosterone where the adrenal

cortex is destroyed(Addisons disease)

Used in autonomic neuropathy-forvolume expansion


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Beclomethasone and budesonide For bronchial asthma-inhalation route

Most of the inhaled dose is swallowed.

Can give a very low systemic plasma

concentration.


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Pharmacokinetics of steroids Topical steroids(skin,lungs,joints) can

cause enough absorption to cause systemic

side effects. In the blood 5% of the steroids are carried

free(active form).The rest is bound to

transcortin. Hence steroid dose should be reduced in

low albumin states and liver disease.


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Indications for use of steroids Acute severe asthma

Exfoliative dermatitis and pemphigus

SLE,Polymyalgia rheumatica,giant cell

arteritis,dermatomyositis

Acquired haemolytic anaemia Severe allergic reactions

Organ transplant rejection


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Indications contd.. Rheumatoid arthritis

Ulcerative colitis and proctitis

Crohns disease

Nephrotic syndrome


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Reducing hypothalamo/pituitary/adrenalsuppression

Single daily doseearly morning

Alternative day schedules

Short courses

Mega doses far apart


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Short courses



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Side effects of steroid treatmentUsually followprolonged administration

Cushings syndrome

Diabetes mellitus

Proximal myopathy

Osteoporosis Avascular necrosis of bone

Spread of infection and atypical features


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Side effects of steroids contd Peptic ulcer and haemorrhage

Pancreatitis

Depression,psychosis,insomnia

Posterior subcapsular lens cataract,

glaucoma Growth retardation in children-esp. if

treatment exceeds 6 months.


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Short courses



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Precautions / chronic steroid therapy Use the minimum dose to get the desired effect

Patient education

1. Carry a card containing details of therapy

2. What to do if they intercurrent illness or other

severe stress-double the dose & tell the doctor

3. What to do if they miss a dose- take the dose assoon as possible

Vomiting-may require parentral administration


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Precautions contd Surgery-hydrocortisone 100-200 mg i.m./

i.v.with premedication and repeated 6 hrly

for 24-72 hrs.

Minor operations-hydrocortisone 20 mg

by mouth before and after surgery.


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Cautions Used only for serious reasons in patients with

1. Diabetes

2. Mental disorder

3. Peptic ulcer disease

4. Tuberculosis

5. Epilepsy

6. Hypertention/heart failure


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Contraindications Topical corticosteroids in eye inflammation

due to herpes virus

Florinated steroids in diabetes


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Acute adrenocortical insufficiency Also known as addisonian crisis

A MEDICAL EMERGENCY

100 mg of hydrocortisone on suspicion

Infusion of 0.9% NaCl & second 100 mg of

hydrocortisone added to first litre.

Hydrocortisone 50-100 mg given every 6 hrs Initiate oral dose of steroids

Treat cause

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2.Corticosteroids