2 - Drugs and the eye Flashcards

1
Q

topical drugs used by optoms

A
  • dianostic: mydiatics, cyclopegics, anaesthetics
  • lubricants, sodium hyaluronate
  • anti -infectives, chloramphenicol
  • anti- allergy
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2
Q

systemic drugs used by optoms

A
  • anti histamines
  • NSAIDS
  • eye nutrients
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3
Q

factors influencing drug delivery to eye

A
  • topical drugs
  • pre- corneal factors
  • corneal penetration
  • inside the eye
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4
Q

pre - corneal factors

A
  • single drop exceeds the capacity of the conjunctival sac to contain it has little differene in the efficacy
  • tear turnover rate
  • higher rates of drainage occur with larger drop sizes with an increased risk of systemic toxicity
  • Nasolacrimal drainage (once drug gets into tears) exceeds the amount of drug that penetrates cornea

need to minimise amount of drug that goes down nasolacrimal route as that ^ risk of systemic absorption. this occurs with ^ drop sizes

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5
Q

corneal penetration (cornea is main route of entry for topical medication)

A

for a drug to pass through cornea, needs a combo of hydrophillic and hydrophobic properties - weak acids and weak bases

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6
Q

once the drug has penetrated the cornea, what happens inside the eye?

A
  • mixes with the aqueous humour. some drug is lost in process of being drained away before reaching the target. some of the drug is lost before reaching target, and some is absorbed by tissues in the anterior chamber
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7
Q

what are enzymes involved in drug metabolisation

A
  • esterases
  • monoamine oxidase
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8
Q

what happens after the drug penetrates the cornea and is eliminated from aqueous humour

A

gets absorbed by tissue of the anterior uvea

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9
Q

factors influencing drug delivery to eye continued

A

blood aqueous barriers -

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10
Q

what does the blood aqeuous barrier do

A

limits the free access of systemic drugs to the anterior chamber

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11
Q

main component of blood aqeuous barrier?

A
  • tight ciliary epithelium
  • low permeability of iris blood vessels

when eye is inflamed BAB can break down and increase drug bioavailibilty

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12
Q

what is the blood-retinal barrier

A

a more significant barrier
- formed by tight junctions between capillary endothelial cells and retinal pigment epithelial cells
- limits the passage of all but smallest lipid soluble molecules

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13
Q

ophthalmic drug stability

A
  • no drug is indefinetly stable
  • drug should habe long shelf life
    -once a multi dose bottle is opened drug is subject to oxidative damage and bacterial contamination
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14
Q

sterilisation method?

A
  • heat
    -sterile filtration
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15
Q

what do preservatives ensure

A

there is no microbial growth during lifetime of drug

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16
Q

excipients (inactive ingredients) used in ophthalmic formulations to ensure sterility and stability

A
  • preservatives
  • buffers
  • antioxidants
  • viscous agents - maintains time on ocular surface
  • pH adjusting agents
17
Q

what are anti-oxidants

A

prevent/delay deterioration of drug by oxygen in the air

e.g sodium bisulphate

to prolong stability of drug

18
Q

most common opthalmic preservative?

A
  • benzalkonium chloride (BAK)
  • phenylmercuric nitrate (used in CPL)
19
Q

more about BAK?

A

quaternary ammonium compound
- most widely uused
- effective against wide range of GM +ve and -ve organisms
- effective in low conc - 0.004-0.02 %
- good chemical stability
- binds to hydrogel lenses (problematic for CL wear)

20
Q

all preservatives are toxic to some extent

A

ok

21
Q

what is a newer ophthalmic preservative

A

polyquaternium -1 (polyquad)
- ammonium antimicrobial preservative
-found in CL solution + artifical tear formulations
- proven to have less toxicity on corneal epithelial cells than BAK

22
Q

what is another newer ophthalmic preservative

A

purite - microbicide: low toxicity to mamallian cells
- preserves solution in bottle but if exposed to light dissociates into water, Na, CL ions and oxygen

23
Q

what do buffers do

A
  • maintain pH range 6-8, most comfortable for ophthalmic instilation
24
Q

name some buffers

A
  1. boric acid.
  2. potassium bicarbonate
25
Q

what are viscous agents

A

increase contact time of drug with ocular surface by increasing viscosity of the preparation (makes it thicker)

26
Q

examples of viscous agents

A
  • methyl cellulose
  • poly vinyl alcohol
  • carbomers
27
Q

what are osmolarity adjusting agents

A
  • create an isotonic solution to improve comfort
    usually 0.6 - 1.8%
28
Q

examples of osmolarity adjusting agents

A
  • NaCl
  • Mannitol
29
Q

ph adjusting agents?

A
  • create ph that ensures optimal stability and tolerability
  • HCL
  • NaOH