Anti-inflammatory Drugs Flashcards
What is corticosteroids?
Hormones -includes glucocorticoids and mineralocorticoids
Where are corticosteroids produced?
In the adrenal cortex which a small organ on top of each kidney
Which hormone from the pituitary gland regulates corticosteroids?
Adrenocorticotrophic hormone- ACTH
What is an example of a glucocorticoid?
Cortisol which maintains normal levels of blood glucose and promotes injury recovery
What is an example of a mineralocorticoids ?
Aldosterone which controls sodium balance in the body and influence blood pressure
Therapeutically, what is glucocorticoid used to treat?
Inflammation
What are the two pharmacological actions of glucocorticoid?
1) Anti-inflammatory and immunosuppressive by reducing the activity of inflammatory mediators
2) Metabolic effects on carbs and fats
How does glucocorticoids reduce the activity of inflammatory mediators?
The steroid- receptor in the cytoplasm which when bound to its receptor moves to the nucleus to bind to glucocorticoid response elements which affects the transcription to synthesis inflammatory mediators
- The steroid binds to steroid receptor in the cytoplasm
- The new complex moves to the nuc
- The complex will bind to glucocorticoid response elements and inhibit the transcription of enzymes that produce inflammatory mediators
What enzyme can a corticosteroid inhibit?
Phospholipase A2- a key enzyme in the arachidonic acid pathway
What does phospholipase A2 convert phospholipids into?
Arachidonic acid which then gets metabolised to generate inflammatory mediators
Name the four therapeutic uses of corticosteroids.
1) Anti-inflammatory effects (eczema, rheumatic disease)
2) Replacement therapy for diseases of the adrenal gland (if they have low levels of corticosteroid levels)
3) Chemotherapy
4) Immunosuppression- post transplantation
What is the function of corticosteroids?
Reduce inflammation and suppress the immune system
What are some adverse side effects of corticosteroids?
- Impaired glucose tolerance (can develop diabetes)
- Osteoporosis - brittle bones
- Cushings syndrome
-Immuno-suppression
What does the adverse side effects of corticosteroid use depend on?
Dosage an duration of the treatment
What is Cushings Syndrome ?
When the adrenal gland makes too much cortisol hormone
What are indications to use ophthalmic corticosteroids?
-Used to treat sight threatening diseases such as anterior uveitis or vernal conjunctivitis
- Post-operative inflammation
- Intravitreal steroids used to treat macular oedema (following retinal vein occlusion)
How do you decide which ophthalmic corticosteroid you would prescribe?
Whether it is penetrating or intraocular or whether it is more on the ocular surface so non-penetrating
Why is prednisolone acetate more penetrating that prednisolone sodium phosphate?
It is more lipid soluble whereas prednisolone sodium phosphate contains charge groups so cannot penetrate as readily