wk8: AED - Anti-inflammatories [DG] Flashcards
What are the 7 categories of anti-inflammatories in Australia? Provide an example for each category
Astringents - zinc sulphate Anti-histamines - levocabastine MCS - sodium cromoglycate Dual action MCS/AH - olopatadine NSAIDS - diclofenac Corticosteroids - fluoromethalone Calcineurin/T-cell inhibitor - cyclosporine (not available in aus.)
How do astringents work?
break down mucus production, reduce leakiness
How long do MCSs take to start working? Knowing this, what do we clinicians like to do?
2-4 week period. So we like to use dual action MCS/Anti-histamines like patanol or zatadin 2 x day
List the topical multi-use (preserved) eye drops available in Australia (5)
all anti-histamines all MCSs all dual action MCS/AHs all NSAIDS all corticosteroids (except prednisolone phosphate)
List the topical single-use (non-preserved) eye drops available in Australia (5)
most lubricant bases phenylephrine (in albalon relief) ketotifen (zatiden single dose) flurbiprofen (in ocufen) prednisolone phosphate (minims)
List the topical eye ointments available in Australia (2)
lubricants (but as paraffin)
hydrocortisone
How do topical steroid formulations differ? (2)
different potencies
different corneal penetration
What type of inflammation is low potency, low penetration steroids good for? Why?
ok for mild surface inflammation (minimises chances of steroid-induced pressure rise)
When are high potency, high penetrative steroids essential? If they are required, what should you write on the Rx?
for anterior uveitis. If this level of steroid is required, write ACETATE on the Rx
Which has the greater corneal penetrance: alcohol based steroids or acetate based steroids?
acetate based steroids
What is the treatment goal for inflammation?
Rapid control of inflammation to minimize complications (drug and disease)
What is a “loading dose”?
an initial higher dose of a drug that may be given at the beginning of a course of treatment before dropping down to a lower maintenance dose.
Is a loading dose always required for steroid use?
Some argue for some argue against it. Though you honestly don’t have to reach therapeutic window as fast as antibiotics (because you don’t have to deal with exponentially dividing bacteria). Darryl Guest - “I don’t think loading dose matters too much for steroids”
Do you use a loading dose for antibiotics? And if so, do you finish the course early or go through the entire course of antibiotics?
Yes. Still go through the whole course
How does steroid potency differ from antibiotic potency?
Different steroids vary in potency. Different antibiotics don’t vary in potency because potency is determined by what you are trying to kill
What are the 3 levels of lists on the OBA website for optometry drugs
- Drugs you are allowed to use
- TGA list - what’s available
- PBS list - what’s subsidised
Name 6-8 anti-inflammatories found in the OBA
Cyclosporin Dexamethasone Diclofenac Fluoromethalone Flurbiprofen Hydrocortisone Ketorolac Prednisolone
For a steroid to have an adequate effect in the anterior chamber, what 2 things will it need?
Needs both potency and penetration
Describe the following drugs for their potency, penetration and capacity to raise IOP (when in ant. chamber):
- Hydrocortisone alcohol
- Hydrocortisone acetate
- Flouromethalone alcohol
Potency Penetr. IOP
Hy.Al v. low - ++
Hy.Ac low ++ ++
Fl. Al. mid - +++
Describe the following drugs for their potency, penetration and capacity to raise IOP (when in ant. chamber):
- prednisolone phosphate
- fluorometholone acetate
- prednisolone acetate
- dexamethasone alcohol
poten. pen. IOP Pr.Ph mid + +++ Fl.Ac high ++ +++ Pr.Ac. high +++ ++++ D.Al high ++ ++++
How do acetates, alcohols and phosphate steroids compare in terms of penetration? Rank them from highest penetrance to lowest
acetate»_space; alcohol > phosphate
What are the 2 main side effects of steroid use? Give an example of a patient where one of these side effects won’t be a concern
increase in IOP
increase risk of steroid cataract
- note: patients who have already had cataract surgery and are wearing IOLs will not have to worry about the cataract side effect
As a general guideline for anti-inflammatory usage:
- What should ocular lubricants be used for? (4)
mild ocular surface irritation (inc. SPK)
dry eye
neurotrophic keratitis
adjunct in severe inflammation
As a general guideline for anti-inflammatory usage:
- What should astringents be used for? (1)
- what is a limitation of astringents? (1)
mucoid discharge in allergic surface disease
but not as readily available as other options
As a general guideline for anti-inflammatory usage:
- What should anti-histamines be used for? (1)
- What should MCSs be used for? (1)
- What should dual action MCS/AH be used for?(1)
All 3 of these are used for allergic eye disease (type 1 hypersensitivity)
As a general guideline for anti-inflammatory usage:
- What should NSAIDs be used for? (5)
mild/moderate allergic eye disease
other surface inflammation (e.g. epicleritis)
intra-operative inhibition of miosis
post-operative inflammation/analgesia
“my main use is cystic oedema associated with cataract surgery” - Darryl Guest
As a general guideline for anti-inflammatory usage:
- What should corticosteroids be used for? (4)
all types of moderate-severe ocular surface inflammation
HSV and HZO keratitis (NOT epithelial)
anterior uveitis
endophthalmitis (intravitreal)
As a general guideline for anti-inflammatory usage:
- what should cyclosporine be used for? (5)
corneal graft uveitis scleritis VKC dry eye
As a general guideline for anti-inflammatory usage, How safe are the following drugs in pregnancy?
- Astringents
- Anti-histamines
- MCSs
Astringents: safe
Anti-histamines: avoid (probably ok in kids)
MCS: cromoglycate safe, lodoxaimde uncertain (both safe lactation/kids)
As a general guideline for anti-inflammatory usage, How safe are the following drugs in pregnancy?
- dual action MCS/AH
- NSAIDs
- Cyclosporin
dual action: same as antihistamines (avoid preg, lac. kids ok)
NSAIDs: caution/not recommended (safe in lactation/kids)
Cyclosporin: caution/not reccommended (contraind. in lac)
Are steroids safe in pregnancy? Explain
Controversial. Differing opinions from different studies. Manufacturers say no so they don’t get sued. But in some cases benefits may outweigh risks
You have a pregnant patient with iritis and are considering steroids but they are pregnant. What should you do to best manage this patient? (2)
Be up to date with literature (literature surrounding this may change)
Engage in conversation with px
When given multiple drops of steroids, how long should the time gap be between the drops?
Minimum 5 minutes
In regards to prednisolone:
- describe its characteristics (2)
Ketone based
highly efficacious
In regards to prednisolone:
- what is different about its acetate form? (1.5)
acetate form is a suspension, so you’ll have to shake the bottle
In regards to prednisolone:
- What do we use it for? (2)
significant inflammation
uveitis mx
How strong are fluoromethalones?
moderate strength
What are the 2 forms of fluoromethalones?
Alcohol form = FML and Flucon
Acetate form = Flarex
How does the effect of fluorometholones compare to pred forte? (2)
Less of an IOP spike but less effective than pred forte.
How does steroid anti-inflammatory treatment change based on whether the inflammation is at the iris/ciliary body or deeper than the iris/ciliary body? (4)
At iris/cil.body: topical therapy may be appropriate; better penetrance or more frequent admin may be needed for therapeutic dose
Deeper (or not controlled by topical): oral or intraocular/sub conj./sub-Tenon’ injection may be required
List the short-medium term dose potential side effects of steroids (5)
IOP spike secondary/reactivation of infection masking clinical signs delayed wound healing transient discomfort
What type of infections are likely to reinfect if using steroids for short-medium term? (3)
zosta type infections
simplex infections
pseudomonas
**so basically don’t use steroids for these
Is delayed wound healing from steroid use a big deal?
not particularly. May only slow 15-20% and the benefits often outweigh this downside
List the potential side effects from long term dose steroids (2)
IOP rise
Cataract - mainly posterior subcapsular
What percentage of patients get cataracts after 12 months of steroid use? What about 24 months?
12 months: 33%
24 months: 52%
What would you consider a critical IOP rise in a young person after short term steroid use? Why?
Start to worry at about 28-30 IOP. Because at this IOP we start to risk central retinal vein occlusion. If diastolic blood pressure in the eye is lower than IOP, the blood won’t flow, hence occlusion.
(note: blood pressure in the eye is different from rest of body)
List the different actions of glucocorticoids (5)
Block phospholipase A2 activity – decrease infl. cytokine prod.
Decrease cellular response and macrophages
Prevent mast cell degranulation
Deregulate cellular DNA expression
Suppress adrenal secretions of steroids (takes one week)
How ong do adrenal secretions of steroids take to come back when glucocorticoids are removed?
about 3-5 weeks
What is the average drop size of a topical steroid compared to our tear volume? Knowing this, how much of the drop is lost on administration?
avg. drop size = 50ul
tear vol = 30ul
So like 30ul of the drop is lost. I.e. most of the drop is lost immediately
When administering prednisolone (in a rabbit study), what percentage of the prednisolone can you expect to reach the cornea? aqueous?
Cornea - 1.7%
Aqueuous - 0.1%
Why suppress inflammation? (4)
May lead to cell/tissue loss (e.g. bacterial keratitis, necrotic hsv keratitis)
May lead to scarring + loss of function (e.g. microbial keratitis, stromal hsv keratitis, synechiae in ant. uveitis)
May lead to collateral ocular surface disturbance (e.g. GPC, VKC)
Improved px comfort, improved surgical outcome
What are the potential ocular downsides to anti-inflammatory steroids? (5)
cataract glaucoma HSV fungal/acanhamoebal potentiation accelerated tissue loss (MMPs)
What are the potential systemic downsides to anti-inflammatory steroids? (3.5)
Cushing’s syndrome (obesity, gastric ulcers, osteoporosis skin changes)
What are the potential downsides of NSAIDs? (2)
stromal lysis from diclofenac
increased risk of post refractive surgery infections
What are the indications for anti-inflammatory prophylaxis? (2)
very few:
- pre-operative (e.g. px H/O uveitis about to undergo intraocular sx)
- Mx of Px with H/O seasonal allergic eye disease
Do short term/low dose steroids require tapering?
No
What level of dose of steroid should you use?
Dose should be sufficient to control inflammation and continue as long as necessary. Appropriate dose must be re-evaluated at regular intervals
How much can you decrease marked corneal inflammation by with 18 hours of intense steroid application?
50-70%
Should we taper long-term/high dosage steroids?
Yes we should
Why should we taper steroids? (1)
To give the body time to adjust and produce more natural cortisol again to prevent rebound inflammation
(b/c while delivering synthetic steroid, the body starts producing less cortisol because it doesn’t need it)
What does “pulse-dose” mean?
usually assoc. with systemic admin - high dose short bursts produce quicker therapeutic effect with shorter-lived side effects
What does “pulse-dose” mean in the context of topical administration?
usually involves delivery at greatly increased frequency than rapid withdrawal (with no or limited taper)
What is pulse-dose topical administration of steroids typically used for? (1.5)
allergic/contact conjunctivitis
What must you NOT use pulse-dose topical administration of steroids for? (2)
uveitis or HZO
Biologically, what does ocular pulse-dosing achieve? (4)
increases bioavailability
achieves faster inflammatory control
minimal rebound effect
reduces duration side effects
Provide 5 examples for conditions that lend to pulse dosing
non-specific ocular surface dry eye help symptoms in adenoviral SAC GPC
How can you usually manage type 1 allergic eye disease?
MCS and AH
How can you manage type IV delayed hypersensitivity responses? (1)
Need steroid
Is a steroid necessary to tx toxicity?
it might be