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
What are two examples of a high potency ophthalmic corticosteroid?
Prednisolone acetate and dexamethasone
Name five ophthalmic corticosteroid
1) Betamethsone
2) Dexamethsone
3) Fluorometholone
4) Loteprednol
5) Prednisolone
What are some adverse ophthalmic side effects of corticosteroids usage?
- Increased risk of a posteriori sub-capsular cataract- 4% cataracts account of it, dosage dependent
- Raised IOPs which can lead to steroid glaucoma (acute response)
Are NSAIDs available topically for ophthalmic use?
Yes
Why are eicodanoids important in the inflammatory response?
They are your prostaglandins and leukotrienes which have an effect on vasodilation, increase IOPs, and reduces pupil size, macular oedema–> DUE TO inhibition of cyclo-oxygenase
What are indication to ophthalmically use NSAIDs?
- Reduce intra operative and post operative ocular inflammation
- Reduce post-operative ocular inflammation
- Reduction of pain after following corneal trauma
- Allergic conjunctivitis
- Episcleritis (not licensed)
Name the five topical NSAIDs available for topical use
1) Diclofenac sodium (Voltarol)–> licenced for pain and seasonal conjunctivitis
2) Flurbiprofen (Ocufen)
3) Ketorolac trometamol (Acular)
4) Nepafenac (Nevanac)
5) Bromfenac (Yellow)
Trade name is in brackets
What is ciclosporin?
Immunosuppressant medication and works by inhibiting release of cytokines from T-lymphocytes and therefore suppresses the cell-mediated immune response, can treat dry eye in keratitis or severe vernal keratoconjunctivitis
What does Verkazia treat?
Severe vernal keratoconjunctivitis
What does Ikervis treat?
Dry eye in severe keratitis
Describe the role of mast cells in ocular allergy
- Antigen crosses conjunctiva
- being taken up by an APC
- APC presents the antigen to T-helper cells which leads to production of cytokines and interleukins to induces b cell to produce antibodies
-IgE antibodies are produced to bind to surface of mast cells by cross linking –> leads to calcium influx - Degranulation of mast cell due to calcium influx
- Preformed histamine mediators and newly formed prostaglandin mediators are released
- Px becomes symptomatic by the itching, epiphora
Name the five types of anti-allergy drugs
1) Anti-histamines
2) Mast cell stabilisers
3) Corticosteroids
4) NASIDs
5) Vasoconstrictors
Name an OTC systemic antihistamine
Cetirizine, diphenhydramine (sedative side effects)
What is an issue with diphenhydramine?
Sedative side effects
What eye allergies do topical antihistamines treat ?
SAC and PAC
What is special about the newer drugs to treat eye allegries?
They contain both anti-histamines and mast cell stabilisers (dual-acting agents)
Name the five topical antihistamines and say whether they are P or POM
- Antazoline (P)
- Azelastine (POM) - dual acting
- Epinastine (POM) - dual acting
- Ketoifen (POM) - dual acting
- Olopatadine (POM)- dual acting
Can non-independent prescribing optometrists prescribe POM medicines?
No
What is an issue with antazoline?
Contains a vasoconstrictor so not licenced for children under 12 and cautions with cardiovascular issues
How do mast cell stabilisers work?
Block calcium influx into mast cell membrane so mast cell degranulation cannot take place; mast cells become stabilised
What is a disadvantage of MCS?
They will take up to 2 weeks to reach full potential so not instant symptomatic relief
What are three mast cell stabilizers (one is discontinued )
- sodium cromoglicate - opticrom (GSL/P/POM)
- Lodoxamide (POM)
-Neodocromil sodium (POM)- DISCONTINUED
What is an NSAID used to treat SAC?
Diclofenac sodium (POM)- give instant relief
What type of agonists are vasoconstrictors?
Alpha-receptor agonists as the alpha receptors are responsible for vasoconstriction so adrenergic receptors are stimulated and BV are constricted
What type of drug is a vasoconstrictor?
Sympathomimetic drug
Are vasoconstrictors advised to treat allergic eye disease?
No
Name the three types of vasoconstrictors
- Xylometazoline ( Otrivine Antistin)
- Naphazoline (Murine, Optrex clear eyes)
- Phenylephrine (not in the UK though)
