7. Clinical Anti-inflammatories Flashcards
Name the 7 anti-inflammatories in Australia.
• Astringents
• Anti-histamines
• Mast cell stabilisers
• Dual action MCS/ AH
• NSAIDS
• Corticosteriods
• Calcineurin/ T cell inhibitor
What are the 3 different formulations of topical anti-inflammatories? What makes them different?
• Multi-use eyedrops - perserved, usually with BAK → AH, MCS, MCS/AH, NSAIDs
• Single use eyedrops - non-preserved → lubricants, phenylephrine, ketotifen, flubiprofen, prednisolone phosphate
• Ointments - non-preserved, typically used for skin conditions areound the ocular areas → lubricants, hydrocortisone
What are the indications for ocular lubricants?
For mild, non-specific inflmamation; mild ocular surface irritation (SPK), dry eye, neurotrophic keratitis; adjunct in severe inflammation
What are the indication for astingents?
Mucoid discharge in allergic surface disease. Not used commonly in Australia.
What are the indications for anti-histamines, mast cell stabiliser and dual action MCS/ AH?
MCS and AH usedful in eye disease with type I hypersensitivity (allergy)
Anti-histamines are H1 antagonists → will not reudce redness, effective at reducing itching
MCS takes times to control symptoms (reduce release of histamines), therefore should add topical steroids to control intial symptoms.
What are the properties and indications for NSAIDS?
NSAIDS are anti-inflammatory, anti-pyretic and analgesic. They are used in mild/ moderate allergic eye disease (seasonal allergic conjunctivits) and other surface inflammation
e.g. episcleritis; intra-operative inhibition of miosis; post-operative inflammation (cystoid macular oedema)/ analgeia; post refractive surgery (photophobia/ pain)
What are the indicaitons for corticosteroids?
Moderate to severe ocular surface inflammation; HSV and HZO keratitis (not epithelial), anterior uveitis; endophthalmitis (intravitreal). Any inflammation with type IV hypersensitivity component may require steriods.
What are the indications for cyclosporine?
• Corneal graft
• Uveitis
• Scelritis
• Vernal keratoconjunctivitis
• Dry eyes
Steroids/ ...
block ...
activity, which inhibits ...
synthesis. Steroids also decrease ...
production, which decrease ...
, prevent ...
, and also deregulate ...
expression. Steroids also inhibit inflammaton, wihch therefore inhibits ...
, decrease ...
and ...
. In appearance, this can reduce ...
. The use of steriods can ...
.
Steroids/ glucocorticoids
block phospholipase A2
activity, which inhibits prostaglandin
synthesis. Steroids also decrease inflammatory cytokine
production, which decrease cellular response and macrophage activation
, prevent mast cell degranulation
, and also deregulate cellular DNA
expression. Steroids also inhibit inflammaton, wihch therefore inhibits vasodilation
, decrease vascular permeability
and scar formation
. In appearance, this can reduce redness of the eyes
. The use of steriods can suppress adrenal secretions of steriods
.
What are the treatment goals of steroids? How should we go abouts with the management?
Goal of using steroids is to rapidly control inflammation in order to minimse complications with the disease and also with the use of steroids. This is to prevent structral changes, scarring, and functional changes to the tissues. Short term or long term adverse effects can occur with steroids. Steroids should only used in short term in order to prevent or reduce side effects and withdrawal symptoms.
What are the possible complcations of inflammation? Give examples of diseases that can lead to the complication.
Inflammation may cause cell and tissue loss, such as bacterial keratitis and necrotic HSV keratitis. It can also cause scarring and loss of function, such as microbial keratitis, stromal HSV keratitis, synechiae in anteiror uveitis. It can lead to collateral ocular surface disturbance, such as giant papillary conjunctivitis and vernal keratoconjunctivitis.
What are the possible steroid adverse effects with short term to medium term doses? (5 points)
• IOP spike
• Secondary/ reactivation of infection (fungal, protozoa, viral)
• Masking clinical signs (can misjudge infection progress and delay recovery)
• Delayed wound healing (block tissue contraction, prevent scar formation)
• Transient discomfort
What are the possible steroid adverse effects with long term doses? (3 points)
• IOP rise leading to steriod-induced glaucoma
• Posterior subcapsular cataract
• Systemic effects: weight gain, adrenal insufficiency, gernealised edema, Cushing syndrome, osteopenia, gastritis, avascular necrosis of femur head, excess body hair growth, premature closure of bony epiphysis etc.
Rank the steroid potency in terms of drug type. [low to high]
Hydrocortisone → Flurometholone → Prednisolone
Rank the steroid potency in terms of formulation. [low to high]. Why does changing formulation matter?
Sodium phosphate < Alcohol < < Acetate.
Changing the solubility and penetrance of steriods in order to suit where the drug should act.
E.g. Fluorometholone has poor corneal penetration itself, therefore good for surface diseases;
Adding acetate to fluorometholone (Fluorometholone acetate) allows for high corneal penetration, allowing high activity at the anterior chamber.