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Therapeutics > ophthalmic drugs: anti-inflammatory drugs > Flashcards

ophthalmic drugs: anti-inflammatory drugs Flashcards

1
Q

which type go optometrists can only supply corticosteroids

A

optometrists with a independent prescribing qualification

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2
Q

what is the lowest prescribed ophthalmic drug in the UK

A

NSAIDs

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3
Q

what is the highest prescribed ophthalmic drug in the UK

A

Glaucoma treatments

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4
Q

what type of compound is corticosteroids

A

a naturally occurring compound: hormones

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5
Q

what are corticosteroid hormones produced by

A

the adrenal cortex

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6
Q

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

A
  • glucocorticoids

- mineralocorticoids

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7
Q

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

A

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

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8
Q

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

A

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

e.g. hydrocortisone

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9
Q

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

A

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

e.g. aldosterone

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10
Q

why are corticosteroids used by athletes

A

because they promote recovery in injury

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11
Q

what are the two main pharmacological actions of glucocorticoids

A
  • anti-inflammatory and immunosuppressive effects

- metabolic effects in carbohydrates, proteins and fat

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12
Q

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

A

reduction in the activity of inflammatory mediators

e.g. eicosenoids, platelet-activating factor and interleukins

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13
Q

what type of formulation is topical corticosteroids available as

A

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

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14
Q

where is the receptor for corticosteroids found

A

it is found within the cytoplasm of the cell

as opposed to being on the cell surface

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15
Q

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

A

because it is lipophilic and therefore insoluble

so it is able to pass through the cell membrane in order to encounter its receptor

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16
Q

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

A
  • 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
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17
Q

where are phospholipids found

A

in all plasma membranes

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18
Q

how do steroid block inflammatory mediators and name an example

A

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

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19
Q

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

A

arachidonic acid

which enters the inflammatory pathway

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20
Q

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

A

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

we block these enzymes in order to inhibit inflammation

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21
Q

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

A

NSAIDs

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22
Q

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

A
  • lipo-oxygenase
  • still get the production of leukotrienes

e.g. ibuprofen

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23
Q

which inflammatory mediator forming enzyme do NSAIDs block

A

cyclo-oxygenase

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24
Q

list the 4 therapeutic uses of systemic corticosteroids

A
  • 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
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25
Q

adverse effects of corticosteroids are _________ and can be _________

A

adverse effects of corticosteroids are common and can be severe

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26
Q

what 2 things are the adverse effects of corticosteroids dependent on

A
  • dose

- duration of treatment

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27
Q

list 4 adverse effects of corticosteroids

A
  • 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
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28
Q

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

A

calcium supplements

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29
Q

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

A

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

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30
Q

name 2 indications for ophthalmic corticosteroids

A
  • treatment of acute and chronic inflammation e.g. anterior uveitis, vernal conjunctivitis
  • to reduce post operative inflammation
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31
Q

there is no official _________ hierarchy for topical ________ ____________

A

there is no official potency hierarchy for topical ocular glucocorticoids

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32
Q

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

A
  • 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
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33
Q

name the 2 variations of prednisolone

A
  • prednisolone acetate
    and
  • prednisolone sodium phosphate
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34
Q

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

A
  • 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.
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35
Q

what correlation is their with the potency of a corticosteroid

A

adverse reactions

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36
Q

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

A
  • prednisolone acetate
  • dexamethasone
    = strong steroids
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37
Q

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

A
  • prednisolone sodium phosphate 0.05% or 0.1%
  • hydrocortisone
    = weak unpenetrating steroids
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38
Q

list 6 available preparations of ophthalmic corticosteroids with their trade name

A
  • Betamethasone: Betnesol
  • Dexamethasone: Maxidex
  • Fluormetholone: FML
  • Loteprednol Etabonate: Lotemax
  • Prednisolone: Predsol, Pred Forte
  • Rimexolone: vexol
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39
Q

name 3 corticosteroids that are combined with antibiotics

A
  • Betnosol N
  • Maxitrol
  • Tobradex

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

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40
Q

what is a NICE approved treatment for retinal venous occlusions

A

intravitreal corticosteroids

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

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41
Q

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

A

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

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42
Q

what is an adverse reaction of prolonged use of steroids

A

an increased risk of posterior sub capsular cataract

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43
Q

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

A

the dose and duration

e.g. taking a high dose for >1 year

44
Q

how many % of cataracts does corticosteroids account for

A

approx 4%

45
Q

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

A

raised IOP

from topical or inhaled systemic steroids (not always eyedrops)

46
Q

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

A

no
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

47
Q

what do NSAIDs provide

A

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

48
Q

whats do NSAIDs prevent

A

the formation of a family of compounds called eicosanoids

49
Q

give an example of when are NSAIDs used

A

preoperatively

either given just before or just after a surgery

50
Q

what are eicosanoids the important mediators of

A

the inflammatory response

51
Q

what are the 2 principle eicosanoids

A
  • prostaglandins
    and
  • leukotrienes
52
Q

list 4 ocular effects of eicosanoids

A
  • vasodilation
  • increased IOP
  • miosis
  • macular oedema
53
Q

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

A

the inhibition of the enzyme cyclo-oxygenase (COX)

54
Q

list the 5 indications of ophthalmic NSAIDs

A
  • 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)
55
Q

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

A

Episcleritis

56
Q

list 5 ophthalmic NSAIDs

A
  • Diclofenac sodium
  • Flurbiprofen
  • Ketorolac trometamol
  • Nepafenac
  • Bromfenac
57
Q

list 4 indications of the ophthalmic NSAID Diclofenac sodium

A
  • inhibition of intra-operative miosis
  • reduction of post-operative inflammation
  • pain following corneal epithelial trauma
  • seasonal allergic conjunctivitis
58
Q

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

A
  • Voltarol Ophtha: multi dose eyedrops and unit dose minims
59
Q

list 2 indications of the ophthalmic NSAID Flurbiprofen

A
  • inhibition of intra-operative miosis

- reduction of post-operative inflammation

60
Q

what is the trade name of the ophthalmic NSAID Flurbiprofen

A

Ocufen

61
Q

what is the indication of the ophthalmic NSAID Ketorolac trometamol

A

prophylaxis and reduction of inflammation and associated symptoms following ocular surgery

62
Q

what is the trade name of the ophthalmic NSAID Ketorolac trometamol

A

Acular

63
Q

what is the indication of the ophthalmic NSAID Nepafenac

A

prophylaxis and treatment of postoperative pain and inflammation

64
Q

what is the name of the ophthalmic NSAID Nepafenac

A
  • Nevanac
65
Q

what is the indication of the ophthalmic NSAID Bromfenac

A

post operative inflammation following cataract surgery

66
Q

what is the name of the ophthalmic NSAID Bromfenac

A

yellox

67
Q

the eye is a common site of __________ inflammation

A

the eye is a common site of allergic inflammation

68
Q

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

A

the conjunctiva

69
Q

what cells play a central role in an ocular allergic response

A

mast cells

70
Q

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

A
  • the degranulation of mast cells releases several mediators including histamine
  • the released mediators cause the signs and symptoms of ocular allergy
71
Q

list 3 examples of allergic eye disease

A
  • Acute allergic conjunctivitis
  • Seasonal/perennial allergic conjunctivitis (SAC/PAC)
  • Atopic keratoconjunctivitis (Giant papillary conjunctivitis or Vernal keratoconjunctivitis)
72
Q

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

A

Atopic keratoconjunctivitis - Giant papillary conjunctivitis

73
Q

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

A

Seasonal/perennial allergic conjunctivitis (SAC/PAC)

74
Q

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

A
  • by inhibiting the degranulation

- by binding to the histamine receptors when histamine is released

75
Q

what are the 2 types of mast cell mediators

A
  • pre formed ones that are stored in the granules which are mainly histamine and heparin
    and
  • 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

76
Q

list the 5 anti-allergy drugs

A
  • Anti-histamines
  • Mast cell stabilisers
  • Corticosteroids
  • NSAIDs
  • Vasoconstrictors
77
Q

which 2 forms is anti histamine available in

A

topical and systemic forms

78
Q

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

A

symptoms of hay fever

e.g diphenhydramine, and cetirizine

79
Q

what are topical anti histamines predominantly used to treat

A

Seasonal/perennial allergic conjunctivitis (SAC/PAC)

80
Q

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

A
  • posses antihistamine and mast cell stabilising properties, which makes them more effective
    e. g. olopatadine
81
Q

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

A

Block calcium influx into the mast cell membrane

82
Q

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

A

7-14 days

83
Q

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

A

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

84
Q

what is topical mast cell stabilisers most effective in

A

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

85
Q

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

A
  • sodium cromoglicate

- available as a Pharmacy (P) Medicine

86
Q

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

A

that it must be given four times a day as a must

e.g. lodoxamide

87
Q

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

A

Nedocromil
because of its twice daily instillation frequency

disadvantage is it is far more expensive than sodium cromoglicate

88
Q

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

A
  • seasonal allergic conjunctivitis SAC

- it is well-tolerated and produces symptomatic relief within 30 minutes of instillation

89
Q

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

A

other anti-inflammatory drugs

90
Q

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

A
  • Antazoline (P)
  • Azelastine (POM)*
  • Emedastine (POM)
  • Epinastine (POM)*
  • Ketotifen (POM)*
  • Olopatadine (POM)*
91
Q

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

A

Antazoline (P)

92
Q

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

A
  • Antazoline (P)

- because is also contains a vasoconstrictor

93
Q

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

A
  • Azelastine (POM)*
  • Epinastine (POM)*
  • Ketotifen (POM)*
  • Olopatadine (POM)*
94
Q

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

A
  • Sodium cromoglicate (GSL/P/POM)
  • Lodoxamide (P/POM)
  • Nedocromil (POM)

GSL - general sales drug

95
Q

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

A

Sodium cromoglicate (GSL/P/POM)

96
Q

name the NSAID used as an anti-allergy preparation

A

Diclofenac sodium (POM)

97
Q

who can supply to purchase P medicines

A
  • optometrists
  • staff
  • pharmacy
98
Q

what is the rationale behind the additional supply list

A

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

99
Q

what type of drugs are vasoconstrictors

A 
sympathomimetic drugs
(it mimics the action of the sympathetic nervous system, which is to cause vasoconstriction)
100
Q

what structure of the eye do vasoconstrictors work on

A

constriction of conjunctival blood vessels

101
Q

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

A

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

102
Q

what hormone are sympathomimetic drugs such as vasoconstrictors agonists of

A

noradrenaline

103
Q

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

A
  • Xylometazoline (e.g. Otrivine Antistin)
  • Naphazoline (e.g. Murine, Optrex Clear Eyes)
  • Phenylephrine (currently not available preparation in the UK)
104
Q

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

A

because it has many side effects

105
Q

what can the repeated use of vasoconstrictors cause

A

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

106
Q

what 2 things are vasoconstrictors contraindicated with

A
  • heart disease

- DM

Therapeutics (19 decks)

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