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OV3017 Eye Disease > 14 - Anti Inflammatory drugs > Flashcards

14 - Anti Inflammatory drugs Flashcards

1
Q

what are some anti inflammatory drugs

A
  • corticosteroids
  • non-steroidal anti-inflammatory drugs (NSAIDs)
  • ciclosporin
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2
Q

what are corticosteroids and what are they produced by

A

hormones naturally occuring in the body, produced by the adrenal cortex

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3
Q

what 2 groups to corticosteroids consist of

A
  • glucocorticoids
  • mineralocorticoids
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4
Q

what are corticosteroid levels regulated by

A

hormones (e.g ACTH) produced in the pituitary gland

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5
Q

what do glucocortisoids do and give an example of one

A
  • maintain normal levels of blood glucose and promote recovery from injury.
  • so used therapeutically
    e.g cortisol
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6
Q

what do mineralocortisoids do and give an example

A
  • Affect Na+ balance causing Na+ reuptake and water retention and so influence blood pressure
    e.g aldosterone
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7
Q

2 main pharmacological action of glucocorticids

A
  1. anti inflammatory and immunosuppressive effects through reduction in activity of inflammatory mediators e.g. eicosanids, interleukins
  2. metabolic effects on carbohydrates, proteins and fat
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8
Q

corticosteroids action

A
  • steroid binds to receptor, steroid receptor complex moves to cell nucleus
  • binds to glucocorticoid response element
  • GRE controls transcription of particular genes that control the synthesis of inflammatory mediators
  • go to cytoplasm & inhibitory proteins are manufactured
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9
Q

components of the inflammatory response are under the control of

A

inflammatory mediators

  • vascular events of vasodilation
  • cellular event
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10
Q

corticosteroids: action Eicosanoid synthesis

A

inhibition of an enzyme

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11
Q

which enzyme does corticoisteroid inhibit

A

phospholipase a2 (key enzyme in arachidonic acid pathway)

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12
Q

what does the enzyme phospholipase a2 do

A

converts phospholipids in cell membranes into arachidonic acid

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13
Q

arachidonic acid - what happens after its been converted

A

further metabolised to generate a series of pro inflammatory mediators

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14
Q

what happens when steroids inhibit phospholipase a2

A

they reduce the synthesis of all the mediators which are downstream of that particular enzyme

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15
Q

the non-steroidal anti-flammatories (NSAIDS) inhibit a specific enzyme

A

Cyclo-oxygenase further down pathway.

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16
Q

corticosteroids therapeutic uses systemic

A
  1. anti inflammatory effects e.g asthma/eczema/IBS
  2. replacement therapies for diseases of the adrenal gland
  3. chemotherapy
  4. immunsupression
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17
Q

Corticosteroids-Adverse effects

A

common and can be severe
dependant on dose and duration

  • impaired glucose tolerance (sometimes diabetes)
  • osteoporosis:brittle bones
  • cushings syndrome
  • immune suppression
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18
Q

indications of ophthalmic corticosterids

A
  • treatment of acute + chronic inflammation e.g. anterior uveitis, vernal conjunctivitis
  • reduce post-operative inflammation
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19
Q

what does the efficacy of a particular glucocortisoid dependant on

A

-strength (how much you want drug to penetrate into eye
- what salt is used
- integrity of cornea: drug will penetrate eye better if cornea is damaged

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20
Q

what are the 2 salts of gluco cortisoids called

A
  • prednisolone acetate
  • prednisolone sodium phosphate
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21
Q

prednisolone acetate

A
  • reduces inflammation more effectively than prednisolone sodium phosphate
  • more lipid soluble, penetrates deeper into tissues
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22
Q
  • prednisolone sodium phosphate
A
  • contains charged groups, less likely to penetrate in eye
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23
Q

when are prednisolone acetate and dexamethasone used

A

when inflammation is severe

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24
Q

what is used in mild inflammation and why

A
  • low strength prednisolone sodium phosphate (0.05% or 0.1%)
  • hydrocortisone

glucocorticoid side effects need to be minimal e.g. presence of viral infection

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25
Q

Available preparations of ophthalmic corticosteroids

A

- BETAMETHASON
DEXAMETHASONE
FLUOROMETHALONE
PREDNISOLONE

26
Q

Ophthalmic corticosteroids -advserse reaction LONGTERM use

A

prolonged use: increased risk of posterior sub-capsular cataract
- dose dependant
- account for 4% of cataract
- usually only occur in px taking high dose >1 year

27
Q

Ophthalmic corticosteroids -advserse reaction (ACUTE- short term use)

A
  • raised IOP in steroid responsive individuals
  • can occur with topical inhaled or systemic steroids
28
Q

non-steroidal anti-inflamm drugs -NSAIDS

A
  • Topical NSAIDs provide mild to moderate anti-inflammatory potency without the side effects of corticosteroids
  • NSAIDs prevent the formation of a family of compounds called eicosanoids (act as inflammatory mediator)
29
Q

how do NSAIDS work

A
  • by inhibiting a specific enzyme within the arachidonic pathway
30
Q

Eicosanoids are important mediators of

A

the inflammatory response

31
Q

what are the principle Eicosanoids

A
  • prostoglandins
  • leukotrines
32
Q

ocular effects of Eicosanoids

A
  • vasodilation
  • increased IOP
  • miosis
  • macular oedema
33
Q

what is the anti-inflammatory action of NSAIDs due t

A

inhibition of enzyme cyclo-oxygenase (COX)

(eicosanoids block it)

34
Q

Ophthalmic NSAIDS: indications

A
  1. reduction of intra-operative and post-ocular inflammation
  2. sometimes used in reduction of post operative pain
  3. reduction of pain following corneal trauma (diclofenac sodium)
  4. allergic conjunctivitis diclofenac sodium)
  5. episcleritis
35
Q

available topical NSAIDS

A
  • Diclofenac sodium (volatrol)
  • flurbiprofen (ocufen)
    -ketrolac trometamol (acular)
  • nepafenac (nevanac)
  • bromfenac (yellox)
36
Q

what does ciclosporin do

A
  • inhibits release of cytokines from T-lymphocytes so therefore suppresses the cell mediated immune response
37
Q

what treatments is ciclosporin licenced for the for

A
  • severe keratitis in dry eye if not improved with lubricants
  • severe VKV
38
Q

WHERE DO MAJORITY OF OCULAR ALLERGIES AFFECT

A

conjunctiva

39
Q

which cell plays a major role in ocular allergic response

A

mast cells
- degranulation of mast cells releasing mediators including histamine

40
Q

what do released mediators do

A

they cause the signs and symptoms of the ocular allergy

41
Q

examples of allergic eye disease

A
  • acute allergic conjunctivits
  • seasonal / perennial allergic conjnctivitis
  • GPC
  • AKC
  • VKC
42
Q

what is the role of mast cells in ocular allergy

A
  1. antigens cross mucous membrane (conjunctiva)
  2. taken up by antigen presenting cell, and present to T helper cell
  3. series of cytokines are produced - interleukins
  4. B cells make igE antibodies
  5. igE binds to surface of mast cells
43
Q

after first contact with antigen, what happens to px?

A

asymptomatic

44
Q

what happens after 2nd exposure to antigen?

A

mast cell degranulation

45
Q

when antigen + igE are binded on mast cell, what occurs? (mast cell degranulation)

A

cross linking of adjacent igE molecules, ca2+ influx

46
Q

what is released after mast cell degranulation

A

2 forms of mediators
1) pre formed
2)newly formed

47
Q

what are pre formed mediators

A

Histamine.
Stored in granules in mast cell.

quickly released + immediate effect

48
Q

newly formed mediators

A

prostaglandins.
responsible for clinical effects of allergy such as redness/oedema

49
Q

anti-allergy drugs

A
  • anti histamines
  • mast cell stabilisers
  • corticosteroids ( life thratening)
  • NSAIDS
  • vasoconstrictors
50
Q

what are topical antihistamines for

A

SAC and PAC

51
Q

what are systemic antihistamines for

A

symtoms of hayfever

52
Q

what do newer antihistamines possess

A

antihistamine and mast cell stabilising properties s- dual acting

53
Q

availible topical antihistamines (most are POM)

A
  • antazoline (P) not for <12
  • azelastine (POM)
  • epinastine (POM)
  • ketotifen (POM)
  • olopatadine (POM) (dual action)
54
Q

what do topical mast cell stabilisers do

A
  • block calcium influx into mast cell membrane to prevent degranulation

basically stabilises it

55
Q

how long do topical mast cell stabilisers take ot produce symptomatic relief

A

7-14 days - warn px not instant relief as thye would get woth anti histamines

56
Q

what are topical mast cell stabilisers effective in the management of

A

moderate to severe allergic eye disease
- SAC
- GPC
- VKC

57
Q

available anti allergy preparations of topical mast cell stabilisers

A
  • sodium cromoglicate
  • lodoxamide
  • nedocromil sodium
58
Q

NSAID - which drug is lisenced for SAC

A
  • diclofenac sodium (POM)
  • well tolerated, symptomatic relief within 30 mins
59
Q

what type of drug are vasoconstrictors

A

sympathomimetic drugs - mimic action on sympathetic nervous system

60
Q

what do vasoconstrictors cause

A
  • constriction of conjunctival blood vessels by direct stimulation of alpha adrenoreceptors on the conjunctival vasaluture
  • decrease in conjunctival hyperaemia and oedema

use is limited, not advised

61
Q

vasoconstrictor drugs

A
  • cylometazoline
  • naphazolien
  • phenylephrine ( not in UK)
62
Q

topical NSAIDS and vasoconstrictos have a limited role in treating alergic eye disease

A

cooool

OV3017 Eye Disease (19 decks)

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