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ocular disease II: glaucoma > Prostaglandin analogs > Flashcards

Prostaglandin analogs Flashcards

1
Q

if someone complains about a headache, what does this mean?

A

side effect of the drug

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2
Q

is dose crucial in PG?

A

yes

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3
Q

high doses of PG can do what to iop?

A

increase

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4
Q

most commonly utilized drug for glaucoma as a stand alone single drug?

A

prostaglandin analog

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5
Q

which drug is the most utilized in terms of a compound?

A

beta blocker

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6
Q

what are the 4 various prostaglandin analogs?

A

latanoprost, travoprost, bimatoprost, tafluprost

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7
Q

how is bimatoprost different from other PGs?

A

includes amide group

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8
Q

what is a prodrug?

A

different structure outside of body than inside of body;

compound of structure in bottle changes when placed into eye –> able to pass through

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9
Q

esterase does what?

A

turns prodrug into active drug

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10
Q

what are prodrugs of prostaglandin F2alpha

A

Prostaglandin analogs

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11
Q

what is the mechanism of action for PG?

A

! Increases outflow through uveoscleral pathway.
! Small percentage increase in conventional outflow.
! Does not reduce aqueous production
! Mechanism not fully understood

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12
Q

! All PGs have similar structure
! They are prodrugs of Prostaglandin F2α
! Converted by corneal enzymes into its active form
! Activates the F2α prostaglandin receptors on ciliary body

A

prostaglandin analogs (PGs)

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13
Q

! All PGs have similar structure
! They are prodrugs of Prostaglandin F2α
! Converted by corneal enzymes into its active form
! Activates the F2α prostaglandin receptors on ciliary body

A

prostaglandin analogs (PGs)

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14
Q

two theories of moa of PG

A

! Two theories

  1. Relaxation of ciliary muscle
  2. Dilated spaces between cliliary muscle bundles
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15
Q

what drug constricts cil muscle?

A

pilocarpine

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16
Q

pilocarpine acts oppositely to PG (T/F)

A

true

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17
Q

Supported by experiments with pilocarpine pretreatment experiments in monkeys
Human experiments no effect
Increase in ciliary body thickness when treated with latanoprost

A

relaxation of cil muscle theory

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18
Q

! PG induced stimulation of collagenase and other matrix metalloprotenases
! Still being investigated.

A

dilated spaces b/w cil muscle bundles-theory 

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19
Q

what does collagenase do?

A

cleave collagen

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20
Q

what has upregulation of collagen?

A

myopia

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21
Q

PG is the first line therapy to lower iop in what types of glaucoma?

A

◦ Primary open angle glaucoma (POAG), ◦ Normal tension glaucoma (NTG), ◦ Pigment dispersion syndrome (PDS), ◦ Exfoliation syndrome (XF) and ◦ Chronic angle closure glaucoma ◦ Caution with uveitic glaucoma and ◦ Less effective in pediatric glaucoma

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22
Q

if anatomy of eye is normal, drugs work. therefore pg doesnt work as well in what type of glaucoma?

A

pediatric glaucoma

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23
Q

if anatomy of eye is normal, drugs work. therefore pg doesnt work as well in what type of glaucoma?

A

pediatric glaucoma

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24
Q

contraindications to PG

A

Pregnant or nursing caution
Pediatric – less effective
Unclear PGs and ocular inflammation
allergic to this drug

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25
Q

contraindications to PG

A

Pregnant or nursing caution
Pediatric – less effective
Unclear PGs and ocular inflammation
allergic to this drug

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26
Q

pt A needs cataract surgery, taking PG (causes problems postoperatively). so what do we do?

A

1 month before surgery, they need to stop PG. Put them on a different med that lowers IOP (beta blocker, brimonidine, apriclonidine, CAI). Do surgery. After surgery they can start back on PG.

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27
Q

! Not first choice
! Some reports : association of PGs
(latanoprost) and cystoid macular edema
! Caution: PGs CME, iritis or hepes simplex keratitis, or immediate post-op
! Don’t use- cases with complicated surgery, CME or risk of CME, torn posterior capsules.

A

PGs and inflammation

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28
Q

! Not first choice
! Some reports : association of PGs
(latanoprost) and cystoid macular edema
! Caution: PGs CME, iritis or hepes simplex keratitis, or immediate post-op
! Don’t use- cases with complicated surgery, CME or risk of CME, torn posterior capsules.

A

PGs and inflammation

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29
Q

treatment protocol for PG

A

! Once daily evening
! Helps prevent morning spike in pressure
! Should not be utilized more than once daily
◦ Twice daily less effective than once daily

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30
Q

why do we put PG in the evening?

A

because it causes redness.

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31
Q

PG should not be exposed to high temperature. Why?

A

molecule is unstable at high temps

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32
Q

why should we refrigerate PG?

A

if cold, we can definitely tell it has gone in the eye

33
Q

what are all the side effects of PG?

A 
Conjunctival hyperemia 
! Iris color change 
! Eyelash changes
! Skin pigmentation
! Deepening of upper eye lid sulcus (DUES)
34
Q

name drugs with side effects for conj hyperemia (from greatest to lowest)

A

bimatoprost > travopost > latanoprost (least redness)

35
Q

worst side effect of PG

A

iris color change

36
Q

incidence of iris color change after PG?

A

30-40%

37
Q

Well documented side effect
• Overall incidence up to 30-40 %
• Only half the number of patients notice the change
•I ncrease in melanin content not total number of melanocytes

A

iris color change

38
Q

whats the max volume of conj sac?

A

30 ul

39
Q

a drop is how much ul?

A

50 ul

40
Q

how long should eyes be closed after putting a drop in?

A

1 minute

41
Q

how long should eyes be closed after putting a drop in for anesthetics?

A

1 minute

42
Q

how long should eyes be closed after putting a drop in for glaucoma/any therapy medication?

A

5 minutes

43
Q

if i am prescribing drug a and drug b. if a is applied first, drug b could wash it out. how much time do we wait to apply second drop?

A

15 min

44
Q

if i am prescribing AT with another drug. when do we put it in?

A

before for soothing, as long as theres a 15 min gap between the next drop

45
Q

is skin pigmentation and eyelash lengthening reversible?

A

yes

46
Q

DUES

A

extra wrinkle/fold; happens because eyeball sinks in (drugs have fat decreasing property)

47
Q

Anecdotal and retrospective studies show possible association between the two.
! No clear causal relationship
! Inflammation similar to timolol in multicentre
studies
! 10 patients of 198, few cells were observed. Two of these had cells at baseline
! Risk overall low

A

uveitis and PGs

48
Q

Anecdotal reports
! Almost all the cases had other known risk
factors to CME
“ Open posterior capsules, recent intraocular surgeries, iritis, complicated surgery with vitreous loss
! Topical PGs don’t affect retinal vasculature “ Monkey experiments with high dose
“ Human experiments with BID (twice daily)

A

PGs and CME

49
Q

if lens is removed from eye, is there a chance that CME can develop?

A

yes! but maybe PG shouldnt be blamed, it is most likely due to drug preservative, which causes edema. PF drug did not find CME.

50
Q

! Stop prostaglandin analog one (1) month prior to surgery
! Put patient on other IOP lowering medications
! Have surgery
! 1 month after surgery when out come successful restart prostaglandin analog

A

what protocol to follow if glaucoma pt needs cataract surgery?

51
Q

! Stop prostaglandin analog one (1) month prior to surgery
! Put patient on other IOP lowering medications
! Have surgery
! 1 month after surgery when out come successful restart prostaglandin analog

A

what protocol to follow if glaucoma pt needs cataract surgery?

52
Q

what drug does not have a systemic side effect?

A

PG

53
Q

what eyedrop has thimerasol (preservative)?

A

CLs solution

54
Q

Eye drops containing thimerasol (preservative) will form a precipitate when mixed with latanoprost
! Use 5 minutes apart

A

drug interactions with PG

55
Q

Eye drops containing thimerasol (preservative) will form a precipitate when mixed with latanoprost
! Use 5 minutes apart

A

drug interactions with PG

56
Q

PG IOP reduction of latanoprost ?

PG IOP reduction of timolol compared to latanoprost?

A

! Latanoprost reduces mean diurnal IOP
7.9 mmHg (about 32 %)
! Timolol 1. 6 mmHg less than latanoprost

57
Q

second line of glaucoma therapy drug?

A

timolol

58
Q

all PGs work better than timolol (T/F)?

A

true

59
Q

comparing PGs to each other, are there any that are better?

A

no

60
Q

whats different than black persons eye to white person?

A

pigment takes drug and absorbs it; therefore drug is not available to receptors

61
Q

is there a loss of effect over time for PG?

A

no

62
Q

are PGs effective in all ethnic groups?

A

yes

63
Q

PGs increase outflow

! So adding it with drugs that decrease production of aqueous makes sense

A

additivity

64
Q

PGs increase outflow

! So adding it with drugs that decrease production of aqueous makes sense

A

additivity

65
Q

IOP=

A

production and removal

66
Q

for additivity, which drugs can we use for glaucoma?

A

drug that decreases production

67
Q

! Beta blockers decrease aqueous production
! Several trials adding latanoprost to timolol produced additional IOP decline (i.e., 24-37% decline)
! Adding beta blockers to latanoprost gives additional 14% drop.

A

beta blockers and PGS

68
Q

ADDING ANY group to PG other than pilocarpine will reduce iop by what percent?

A

15%

69
Q

brimonidine is what type of drug?

A

alpha 2 agonist

70
Q

WHATS the efficacy of dorzolamide?

A

not as good as PG, lower achieving drop

71
Q

what type of drug is pilocarpine?

A

cholinergic - increases TM outflow

72
Q

In monkeys yes it does not work In humans it still works
Latanoprost qd
Add pilocarpine 2% qd Additional 7% drop in IOP

A

why do combo of pg and cholinergic agonist not work?

73
Q 
! More convenient
! Less expensive
! Improved compliance
! For example
! Timolol BID and latanoprost qd ! Or
! Xalacom qd (combination of latanoprost and timolol)
A

advantages of fixed combo drugs

74
Q 
! More convenient
! Less expensive
! Improved compliance
! For example
! Timolol BID and latanoprost qd ! Or
! Xalacom qd (combination of latanoprost and timolol)
A

advantages of fixed combo drugs

75
Q

FDA insists that combination of drug should produce additional 20% decrease in IOP
PGs give 32-33% already
Addition of timolol or any other drug does not produce additional 20% decrease in IOP

A

whats the problem with the combo of PGs?

76
Q 
Initially thought as a
prostaglandin
!  Now believed to
improving trabecular
outflow
-side effects similar to pg
-no heart/lung issues
A

unoprostone (rescula)

77
Q 
Initially thought as a
prostaglandin
!  Now believed to
improving trabecular
outflow
-side effects similar to pg
-no heart/lung issues
A

unoprostone (rescula)

78
Q

besides timolol, what can be used as a second line of drug for glaucoma?

A

unoprostone

ocular disease II: glaucoma (6 decks)

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