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Flashcards in ophthalmic drugs: anti-inflammatory drugs Deck (106):

which type go optometrists can only supply corticosteroids

optometrists with a independent prescribing qualification


what is the lowest prescribed ophthalmic drug in the UK



what is the highest prescribed ophthalmic drug in the UK

Glaucoma treatments


what type of compound is corticosteroids

a naturally occurring compound: hormones


what are corticosteroid hormones produced by

the adrenal cortex


name 2 types of corticosteroid hormones/chemicals produced by the adrenal cortex

- glucocorticoids
- mineralocorticoids


what are the levels of corticosteroid hormones such as glucocorticoids and mineralocorticoids regulated by

by hormones also such as the adrenocorticotrophic hormone ACTH from the pituitary gland


what is the properties of the glucocorticoids (type of corticosteroid) and give an example of a glucocorticoid that does this

maintains normal levels of blood glucose and promotes recovery from injury - so has important anti-inflammatory properties

e.g. hydrocortisone


what is the properties of the mineralocorticoids (type of corticosteroid) and give an example of a mineralocorticoid that does this

they affect (control electrolytes) the Na+ balance causing Na+ reuptake and water retention, and so influence blood pressure

e.g. aldosterone


why are corticosteroids used by athletes

because they promote recovery in injury


what are the two main pharmacological actions of glucocorticoids

- anti-inflammatory and immunosuppressive effects
- metabolic effects in carbohydrates, proteins and fat


what are the anti-inflammatory and immunosuppressive effects of glucocorticoids done through and name 3 examples

reduction in the activity of inflammatory mediators
e.g. eicosenoids, platelet-activating factor and interleukins


what type of formulation is topical corticosteroids available as

a highly insoluble substance, so doesn't dissolve in water, therefore is a emulsion which needs to be shaken before use


where is the receptor for corticosteroids found

it is found within the cytoplasm of the cell
(as opposed to being on the cell surface)


why is a corticosteroid able to get inside the cell cytoplasm in order to reach its receptor

because it is lipophilic and therefore insoluble
so it is able to pass through the cell membrane in order to encounter its receptor


state the process of how corticosteroids influences the secretion of anti-inflammatory proteins

- the corticosteroid passes through the cell membrane to bind to its receptor in the cytoplasm
- the receptor-steroid complex is translocated to the nucleus
- this is where it influences the secretion of anti-inflammatory proteins


where are phospholipids found

in all plasma membranes


how do steroid block inflammatory mediators and name an example

by the corticosteroid inhibiting the synthesis of the inflammatory mediator: Eicosanoid, which then blocks/inhibits the enzyme phospholipase A2


what do phospholipids turn into under the the action of the phospholipase A2 enzyme and what pathway does this substance enter

arachidonic acid
which enters the inflammatory pathway


what is the 2 enzymes that arachidonic acid is converted into, and therefore what do these 2 enzymes form

converted into: cyclo-oxygenase and lipoxygenase
they form inflammatory mediators and therefore induces inflammation

we block these enzymes in order to inhibit inflammation


what drug blocks cyclo-oxygenase and enzymes in order to inhibit inflammation and formation of inflammatory mediators



which inflammatory mediator forming enzyme do NSAIDs still have and therefore what is there still a production of

- lipo-oxygenase
- still get the production of leukotrienes

e.g. ibuprofen


which inflammatory mediator forming enzyme do NSAIDs block



list the 4 therapeutic uses of systemic corticosteroids

- anti-inflammatory effects (systemic or topical) e.g. asthma, eczema, inflammatory bowel disease or rheumatic disease

- replacement therapy for diseases of the adrenal gland

- chemotherapy e.g. acute leukaemia/hodgkin lymphoma

- immunosuppression e.g. post transplantation


adverse effects of corticosteroids are _________ and can be _________

adverse effects of corticosteroids are common and can be severe


what 2 things are the adverse effects of corticosteroids dependent on

- dose
- duration of treatment


list 4 adverse effects of corticosteroids

- impaired glucose tolerance/metabolism, so that blood glucose levels goes up and in extreme cases can cause diabetes mellitus
- osteoporosis = brittle bones
- cushings syndrome
- immune suppression


what must you take in addition to corticosteroids in order to avoid osteoporosis

calcium supplements


what implications does the adverse effects of corticosteroids, of immune suppression have

it reduces the body's ability to defend against pathogens, therefore opens up the body to opportunistic infections


name 2 indications for ophthalmic corticosteroids

- treatment of acute and chronic inflammation e.g. anterior uveitis, vernal conjunctivitis
- to reduce post operative inflammation


there is no official _________ hierarchy for topical ________ ____________

there is no official potency hierarchy for topical ocular glucocorticoids


other than upon its strength, what 2 other things does the efficacy of a particular glucocorticoid preparation depend upon

- the salt used e.g. prednisolone acetate reduces inflammation more effectively than prednisolone sodium phosphate
- the integrity of the cornea, the drug will penetrate the eye better in the cornea is abraded


name the 2 variations of prednisolone

- prednisolone acetate
- prednisolone sodium phosphate


which form of prednisolone will you use if treating ocular surface inflammation and which form of prednisolone will you use if treating a more deeper seated inflammation and state why

- ocular surface inflammation: use prednisolone sodium phosphate.
as it has a charged component which impairs it'd ability to transit through the cornea, this is based on the fact that the cornea is healthy and the ocular surface is intact

- deeper seated inflammation: use prednisolone acetate.
as it is more lipophilic and therefore penetrates more readily than prednisolone sodium phosphate.


what correlation is their with the potency of a corticosteroid

adverse reactions


name the 2 corticosteroids which is used when inflammation is more severe

- prednisolone acetate
- dexamethasone
= strong steroids


name the 2 corticosteroids which is used when inflammation is less severe or when glucocorticoid side effects need to be minimal e.g. in the presence of a viral infection

- prednisolone sodium phosphate 0.05% or 0.1%
- hydrocortisone
= weak unpenetrating steroids


list 6 available preparations of ophthalmic corticosteroids with their trade name

- Betamethasone: Betnesol
- Dexamethasone: Maxidex
- Fluormetholone: FML
- Loteprednol Etabonate: Lotemax
- Prednisolone: Predsol, Pred Forte
- Rimexolone: vexol


name 3 corticosteroids that are combined with antibiotics

- Betnosol N
- Maxitrol
- Tobradex

however this is not prescribed often as it is not a good idea to combine corticosteroids with antibiotics


what is a NICE approved treatment for retinal venous occlusions

intravitreal corticosteroids
e.g. Ozurdex intravitreal implant for macula oedema following retinal venous occlusions


what can be 2 side effects of intravitreal corticosteroids used to treat retinal venous occlusions and how is this tackled

cataract and raised IOP causing glaucoma
but the drug is beneficial as it prevents the patient from becoming blind from RVO, therefore need to remove the cataract and treat the glaucoma


what is an adverse reaction of prolonged use of steroids

an increased risk of posterior sub capsular cataract


what does the risk of developing posterior sub capsular cataract from corticosteroid use depend on

the dose and duration
e.g. taking a high dose for >1 year


how many % of cataracts does corticosteroids account for

approx 4%


what is an acute adverse reaction from short term use of ophthalmic steroids

raised IOP
from topical or inhaled systemic steroids (not always eyedrops)


can an acute raised IOP from short term use of steroids be avoided and why

because you can't tell ahead of time which patients will respond with a raised IOP
there is no characteristic that will tell you ahead of time


what do NSAIDs provide

a mild to moderate anti-inflammatory potency without the side effects of corticosteroids


whats do NSAIDs prevent

the formation of a family of compounds called eicosanoids


give an example of when are NSAIDs used

either given just before or just after a surgery


what are eicosanoids the important mediators of

the inflammatory response


what are the 2 principle eicosanoids

- prostaglandins
- leukotrienes


list 4 ocular effects of eicosanoids

- vasodilation
- increased IOP
- miosis
- macular oedema


what is the anti-inflammatory action of NSAIDs primarily due to

the inhibition of the enzyme cyclo-oxygenase (COX)


list the 5 indications of ophthalmic NSAIDs

- Reduction of intra-operative and post-operative ocular inflammation
- Reduction of post-operative pain
- Reduction of pain following corneal trauma
- Allergic conjunctivitis
- Episcleritis (off license)


what is not a licensed indication of ophthalmic NSAIDs even though it is still used for that purpose



list 5 ophthalmic NSAIDs

- Diclofenac sodium
- Flurbiprofen
- Ketorolac trometamol
- Nepafenac
- Bromfenac


list 4 indications of the ophthalmic NSAID Diclofenac sodium

- inhibition of intra-operative miosis
- reduction of post-operative inflammation
- pain following corneal epithelial trauma
- seasonal allergic conjunctivitis


what is the trade name and available preparations of the ophthalmic NSAID Diclofenac sodium

- Voltarol Ophtha: multi dose eyedrops and unit dose minims


list 2 indications of the ophthalmic NSAID Flurbiprofen

- inhibition of intra-operative miosis
- reduction of post-operative inflammation


what is the trade name of the ophthalmic NSAID Flurbiprofen



what is the indication of the ophthalmic NSAID Ketorolac trometamol

prophylaxis and reduction of inflammation and associated symptoms following ocular surgery


what is the trade name of the ophthalmic NSAID Ketorolac trometamol



what is the indication of the ophthalmic NSAID Nepafenac

prophylaxis and treatment of postoperative pain and inflammation


what is the name of the ophthalmic NSAID Nepafenac

- Nevanac


what is the indication of the ophthalmic NSAID Bromfenac

post operative inflammation following cataract surgery


what is the name of the ophthalmic NSAID Bromfenac



the eye is a common site of __________ inflammation

the eye is a common site of allergic inflammation


what part of the eye do the majority of ocular allergies affect

the conjunctiva


what cells play a central role in an ocular allergic response

mast cells


how do mast cells play a central role in an ocular allergic response

- the degranulation of mast cells releases several mediators including histamine
- the released mediators cause the signs and symptoms of ocular allergy


list 3 examples of allergic eye disease

- Acute allergic conjunctivitis
- Seasonal/perennial allergic conjunctivitis (SAC/PAC)
- Atopic keratoconjunctivitis (Giant papillary conjunctivitis or Vernal keratoconjunctivitis)


which example of allergic eye disease are sight threatening and need steroids

Atopic keratoconjunctivitis - Giant papillary conjunctivitis


which allergic eye disease is a mast cell mediated type 1 hypersensitivity response

Seasonal/perennial allergic conjunctivitis (SAC/PAC)


which 2 mechanisms can a drug used to treat conditions such as Seasonal/perennial allergic conjunctivitis (SAC/PAC) by targeting the mast cell

- by inhibiting the degranulation
- by binding to the histamine receptors when histamine is released


what are the 2 types of mast cell mediators

- pre formed ones that are stored in the granules which are mainly histamine and heparin
- the ones that mast cells produce subsequent to mast cell degranulation, when it is degranulated it continues to produce the eicosenoids (inflammatory mediator)

these both induce the inflammatory response


list the 5 anti-allergy drugs

- Anti-histamines
- Mast cell stabilisers
- Corticosteroids
- Vasoconstrictors


which 2 forms is anti histamine available in

topical and systemic forms


what are systemic anti histamines predominantly used to treat and name 2 examples of drugs used

symptoms of hay fever
e.g diphenhydramine, and cetirizine


what are topical anti histamines predominantly used to treat

Seasonal/perennial allergic conjunctivitis (SAC/PAC)


what properties do newer/2nd generation anti histamines have and name an example of one

- posses antihistamine and mast cell stabilising properties, which makes them more effective
e.g. olopatadine


how do topical mast cell stabilisers work in order to prevent degranulation

Block calcium influx into the mast cell membrane


how long can a mast cell stabiliser take in order to produce symptomatic relief

7-14 days


how can a mast cell stabiliser be used in order to completely avoid allergic symptoms and name an advantage that this can have

to start the therapy 2-3 weeks before they become symptomatic e.g. in seasonal allergic conjunctivitis

so they can still wear their contact lenses and control their eye symptoms


what is topical mast cell stabilisers most effective in

the management of moderate to severe allergic eye disease e.g SAC, GPC, VKC


what is the original mast cell stabiliser and what category of medicine is it available as

- sodium cromoglicate
- available as a Pharmacy (P) Medicine


what is the disadvantage of the original mast cell stabiliser sodium cromoglicate, and give an example of a drug

that it must be given four times a day as a must
e.g. lodoxamide


which mast cell stabiliser may be preferred over sodium cromoglicate in seasonal and perennial allergic conjunctivitis and why
also what it the disadvantage to this drug over sodium cromoglicate

because of its twice daily instillation frequency

disadvantage is it is far more expensive than sodium cromoglicate


what is the NSAID, Diclofenac sodium licensed for and what is its advantage for this purpose

- seasonal allergic conjunctivitis SAC
- it is well-tolerated and produces symptomatic relief within 30 minutes of instillation


what is there no evidence that the NSAID, Diclofenac sodium is more effective than for treating seasonal allergic conjunctivitis SAC

other anti-inflammatory drugs


name the 5 available anti-histamines used as anti-allergy preparations

- Antazoline (P)
- Azelastine (POM)*
- Emedastine (POM)
- Epinastine (POM)*
- Ketotifen (POM)*
- Olopatadine (POM)*


which is the only one anti-histamine that is used as a anti-allergy preparation that is available as OTC

Antazoline (P)


which anti-histamine that is used as a anti-allergy preparation is only licensed for children over the age of 12 and why

- Antazoline (P)
- because is also contains a vasoconstrictor


which 4 anti-histamines used as anti-allergy preparations have a dual action (mast cell stabiliser and anti histamine properties)

- Azelastine (POM)*
- Epinastine (POM)*
- Ketotifen (POM)*
- Olopatadine (POM)*


name the 3 available mast cell stabilisers used as anti-allergy preparations

- Sodium cromoglicate (GSL/P/POM)
- Lodoxamide (P/POM)
- Nedocromil (POM)

GSL - general sales drug


which mast cell stabiliser used as anti-allergy preparation is available as a general sales drug

Sodium cromoglicate (GSL/P/POM)


name the NSAID used as an anti-allergy preparation

Diclofenac sodium (POM)


who can supply to purchase P medicines

- optometrists
- staff
- pharmacy


what is the rationale behind the additional supply list

it allowed the optometrists to manage those conditions which present very frequently in primary care

conditions such as: allergic conjunctivitis, infective conjunctivitis, dry eye, superficial injury and corneal abrasion


what type of drugs are vasoconstrictors

sympathomimetic drugs
(it mimics the action of the sympathetic nervous system, which is to cause vasoconstriction)


what structure of the eye do vasoconstrictors work on

constriction of conjunctival blood vessels


how do vasoconstrictors cause constriction of conjunctival blood vessels in the eye

by direct stimulation of alpha adrenoceptors on the conjunctival vasculature with a decrease in conjunctival hyperaemia and oedema


what hormone are sympathomimetic drugs such as vasoconstrictors agonists of



name 3 vasoconstrictors available as anti-allergy preparations (in order to reduce appearance of red eyes)

- Xylometazoline (e.g. Otrivine Antistin)
- Naphazoline (e.g. Murine, Optrex Clear Eyes)
- Phenylephrine (currently not available preparation in the UK)


why is the vasoconstrictor Phenylephrine currently not available preparation in the UK

because it has many side effects


what can the repeated use of vasoconstrictors cause

a rebound hyperaemia, where it initially works but then causes red eye again


what 2 things are vasoconstrictors contraindicated with

- heart disease
- DM