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Therapeutics > ophthalmic drugs: anti-glaucoma > Flashcards

ophthalmic drugs: anti-glaucoma Flashcards

1
Q

list the 5 categories of drugs used to treat glaucoma

A
  • Prostaglandin agonists
  • Beta receptor antagonists
  • Alpha 2 receptor agonists
  • Carbonic anhydrase inhibitors
  • Cholinergic agonists

all target different processes

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2
Q

which 2 ways can you bring IOP down

A
  • by inhibiting aqueous production
    or
  • by enhancing aqueous drainage
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3
Q

what are the 2 drainage pathways

A
  • conventional pathway via the trabecular meshwork and canal of schlemm
    or
  • uveoscleral pathway - 30%
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4
Q

where is the production of aqueous from

A

the ciliary body

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5
Q

what do patients with early to moderate glaucoma damage still retain

A

good central visual function

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6
Q

what is the aim for therapy used on glaucoma patients

A

to maintain ‘target IOP’ ie IOP that is expected to prevent further glaucomatous damage

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7
Q

what are most patient with OAG initially treated with and what is the other option

A 
topical medication (start with single eyedrop, then adding other drops or using multiple therapies)
other option is Laser trabeculoplasty
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8
Q

what is the name of a incisional surgical treatment for glaucoma and when is it considered

A

trabeculectomy may be considered in advanced glaucoma or high IOP

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9
Q

how much is IOP lowered by with glaucoma drugs and how much of aqueous does this correspond to

A

IOP lowered by 20-35%

corresponds to approx. 5 - 7mmHg

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10
Q

what is the normal episcleral venous pressure

A

8-10mmHg

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11
Q

what is the normal aqueous formation rate

A

2-3uL/min

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12
Q

what is the normal outflow facility of aqueous

A

0.2-0.3uL/min/mmHg

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13
Q

what is the mechanism of action with the topical anti-glaucoma drugs: CAI’s, α receptor agonists, and βreceptor antagonist

A

Reduce aqueous production

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14
Q

what is the mechanism of action with the topical anti-glaucoma drugs: cholinergics, bimatoprost

A

Increase outflow through the trabecular meshwork (the conventional method)

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15
Q

what is the mechanism of action with the topical anti-glaucoma drugs: PG agonists, brimonidine

A

Increase uveoscleral flow

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16
Q

what is the mechanism of action with the systemic anti-glaucoma drug: Carbonic anhydrase inhibitors and β receptor antagonists

A

Reduce aqueous production

tablets: Diamox or Dorzolamide

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17
Q

what is the mechanism of action with the systemic anti-glaucoma drug: mannitol, glycerol

A

Osmotic agents i.e. they pull water out of the vitreous

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18
Q

when are the systemic anti-glaucoma drugs used

A
  • as a last option for people who are on maximum eye drops and their pressure is still too high
  • used to treat acute angle closure attack when IOP really high and want to bring it down rapidly in A&E
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19
Q

list the 5 categories of anti-glaucoma drugs from highest to lowest efficacy

A
  • Prostaglandin agonists
  • Beta antagonists
  • Alpha 2 agonists
  • Cholinergic agonists
  • Carbonic anhydrase inhibitors
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20
Q

which drug is the first choice for IOP reduction in OAG and newly diagnosed patients with glaucoma

A

Prostaglandin agonists

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21
Q

by which mechanism do Prostaglandin agonists work to reduce IOP

A

Increase uveoscleral outflow, reducing IOP by 25-33%

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22
Q

after how long from administration do Prostaglandin agonists reduce IOP and when is its peak effect

A

within 2-4 hours of administration

with peak effect 8-12 hours

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23
Q

how often should Prostaglandin agonists be administered

A

One drop preferably in the evening

which is an advantage as only one drop per day

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24
Q

what other drug is Prostaglandin agonists available with as a fixed combination

A

Timolol (beta antagonist)

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25
Q

list the 3 main Prostaglandin agonist drugs

A
  • Latanoprost (Xalatan)
  • Travoprost (Travatan)
  • Tafluprost (Saflutan)
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26
Q

what is the trade name for the Prostaglandin agonist - Latanoprost

A

Xalatan

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27
Q

list 7 side effects of prostaglandin agonists

A
  • Hyperaemia
  • Eyelash growth (hypertrichosis)
  • Iris darkening
  • Darkening of periocular skin
  • Reactivation of HSK
  • Cystoid macular oedema in aphakes/pseudophakes
  • Avoid in pregnancy as prostaglandins can induce labour
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28
Q

how do beta receptor agonists work in order to reduce IOP

A

Block β receptors (sympathetic) in ciliary epithelium, reducing aqueous humour formation

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29
Q

what are the 2 types of beta blockers available to treat glaucoma

A
  • Selective beta blockers (ß1)
    and
  • non-selective (ß1 and ß2) available
30
Q

what can happen with beta receptor agonists drugs over time

A

tachyphylaxis (reduced effectiveness over time)

31
Q

list the 4 non-selective beta receptor agonists drugs available

A
  • Timolol (Timoptol, Nyogel)
  • Levobunolol (Betagan)
  • Metipranolol
  • Carteolol (Teoptic)
32
Q

name the selective beta receptor agonists drug available

A

Betaxolol (Betoptic)

33
Q

what is meant by selective beta receptor agonists

A

drugs that only work on receptors that are in the eye and not on beta receptors in the lungs
however these type of drugs don’t work very effectively

34
Q

what can non-selective beta receptor agonists be contraindicated in

A

those with airways disease

35
Q

what does blocking β2 receptors cause

A

impair respiratory function by causing constriction of the bronchioles resulting in:

  • shortness of breath
  • wheezing
  • bronchospasm
36
Q

what 2 things may blocking β1 receptors cause

A
  • bradycardia
  • hypotension
    = increased falls in elderly
37
Q

what mechanisms does Alpha-2 receptor agonists use to reduce IOP

A
  • Decrease aqueous production
    and
  • Increase aqueous outflow
38
Q

how does Alpha-2 receptor agonists decrease aqueous production

A
  • because they’re sympathomimetic drugs, therefore they mimic the action of the sympathetic nervous system
  • it inhibits aqueous production via alpha receptors by stimulating them
39
Q

what disadvantage does Alpha-2 receptor agonists have

A

it displays tachyphylaxis

the drug works initially, but its effectiveness reduces overtime

40
Q

name 2 Alpha-2 receptor agonists

A
  • Apraclonidine hydrochloride (Iopidine)

- Brimonidine tartrate (Alphagan)

41
Q

list the 7 side effects of Alpha-2 receptor agonist drugs

A
  • Follicular conjunctivitis
  • Allergy
  • Dry mouth
  • Headache
  • Fatigue
  • Dizziness
  • Drowsiness
42
Q

how does Carbonic anhydrase inhibitors reduce IOP

A

Decrease aqueous production by inhibiting enzyme involved in aqueous secretion

43
Q

which types of formulations is Carbonic anhydrase inhibitors available in

A

topical and systemic

44
Q

which formulation of Carbonic anhydrase inhibitors is used in treatment of acute angle closures

A

oral formulation

45
Q

what is the topical form of Carbonic anhydrase inhibitors called

A

Dorzolamide

46
Q

what is the systemic form of Carbonic anhydrase inhibitors called

A

Diamox/Acetazolamide tablets

47
Q

which enzyme is involved in aqueous production and how does it work

A

carbonic anhydrase
it produces bicarbonate ions ( which may exert its effect on aqueous production by influencing Cl- movement as well as by transmembrane transport) which are transported across the ciliary epithelium, setting up a osmotic gradient one which aqueous production depends on

48
Q

what happens when Carbonic anhydrase inhibitors block the carbonic anhydrase enzyme (that produces aqueous)

A

it inhibits the bicarbonate production, therefore lowers aqueous production

49
Q

name the three Carbonic anhydrase inhibitor drugs available

A
  • Brinzolamide (Azopt)
  • Dorzolomide (Trusopt)
  • Oral acetazolamide (Diamox)
50
Q

what are the 2 topical versions of Carbonic anhydrase inhibitor drugs

A
  • Brinzolamide (Azopt)

- Dorzolomide (Trusopt)

51
Q

list the 5 side effects of topical Carbonic anhydrase inhibitor drugs

A
  • Metallic taste (at back of throat, from the eye drops)
  • Rashes
  • Polyuria
  • Irritation
  • Blurred vision
52
Q

list the 8 side effects of oral Carbonic anhydrase inhibitor drugs e.g. Diamox and Acetozolamide

A
  • Allergy
  • Hypokalemia
  • Polyuria
  • Acidosis
  • Depression
  • Paresthesia
  • Kidney stones
  • Blood dyscrasia
53
Q

what type of drug are Cholinergic agonists

A

Parasympathomimetics (causes pupil constriction)

54
Q

what is the pharmacological action/how do Cholinergic agonists reduce IOP

A

by increasing aqueous outflow by opening the trabecular meshwork

55
Q

what is the mechanism of Cholinergic agonist drugs

A

they act as miotics and constrict the pupil, in doing so they potentially stretch the trabecular meshwork allowing for increased aqueous outflow

56
Q

name 2 Cholinergic agonist drugs

A
  • Pilocarpine – 0.1- 6%

- Pilogel

57
Q

list 5 side effects of Cholinergic agonist drugs

A
  • Miosis
  • Myopia
  • Symblepharon
  • Post synechiae
  • Retinal detachment (theoretical risk - very rare)
58
Q

list the 5 categories of anti glaucoma drugs from the most to least safest i.e. least side effects to most side effects

A
  • Prostaglandin agonists
  • Cholinergic agonists
  • Carbonic anhydrase inhibitors
  • Alpha adrenergics
  • Beta antagonists
59
Q

what are none of the anti glaucoma eye drops licensed for

A

use in children and pregnant women

60
Q

what are all combination drugs combined with and why are drugs combined

A
  • all combined with a topical beta blocker Timolol 0.5%

- combined and patients are more compliant than using 2 separate drugs

61
Q

list the 6 available combined anti glaucoma drugs

A
  • Xalacom
  • Duotrav
  • Ganfort
  • Combigan
  • Cosopt
  • Azarga
62
Q

which 2 drugs make up Xalacom

A

Timolol + Latanoprost

63
Q

which 2 drugs make up Duotrav

A

Timolol + Travoprost

64
Q

which 2 drugs make up Ganfort

A

Timolol + Bimaptoprost

65
Q

which 2 drugs make up Combigan

A

Timolol + Brimonidine

66
Q

which 2 drugs make up Cosopt

A

Timolol + Dorzolamide

67
Q

which 2 drugs make up Azarga

A

Timolol + Brinzolamide

68
Q

what guidelines need to be followed for new prescriptions of anti glaucoma drugs

A
  • Start only one drug regardless of presenting IOP in COAG (to look at the effectiveness of that drug)
  • Show the patients how to put the drops in
  • Check IOP again within 3 months (to see if the drug is working)
69
Q

what is used to check peak flow when a px is on beta antagonists and what does it measure

A
  • peak flow meter
  • a device that measures lung functions, it measures the lung volume to diagnose lung problems and is measured before prescribing beta blockers
70
Q

what needs to be done is more than 2 drops of anti glaucoma drugs are required

A

surgery or laser

Therapeutics (19 decks)

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