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Year 2 Ocular Pharmacology > Glaucoma Drugs > Flashcards

Glaucoma Drugs Flashcards

1
Q

What groups of drugs are used to treat glaucoma?

A

Miotics
Sympathomimetics
Beta blockers
Carbonic Anhydrase Inhibitors
Prostaglandin Analogues
Hyperosmotic agents

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2
Q

What are miotics also known as?

A

Parasympathomimetics
Cholinergic agonists

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3
Q

How do miotics reduce IOP?

A

Increase the rate of aqueous outflow by causing increased trabecular meshwork tension due to ciliary muscle contraction

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4
Q

What is the aim of glaucoma meds?

A

To reduce IOP, resulting in the maintenance of the current level of vision (bc ganglion cell axons are not being damaged due to high IOP)

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5
Q

What are the contraindications for using miotics?

A

Anterior uveitis
Iris-mounted IOL
Iridectomy
Prev RD
Secondary glaucoma with extensive obstruction of outflow

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6
Q

What are the side effects of miotics?

A

Sweating
Bradycardia
Bronchospasm
Hypersalivation
Intestinal colic
Frontal headache
Pseudomyopia (if remaining accommodation)
Constricted visual field
Retinal detachment

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7
Q

What is Pilocarpine available as and what’s its dose?

A

2% minims
1/2/4% bottles
3-6x daily

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8
Q

What is Pilocarpine’s mode of action?

A

direct-acting cholinergic agonist

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9
Q

What is sympathomimetics mode of action?

A

Selective or non-selective adrenergic agonists which reduce aqueous humour production and sometimes increase outflow via the uveoscleral route

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10
Q

What are the contraindications for sympathomimetics?

A

Closed angle glaucoma (mydriatic so closes the angle further)

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11
Q

Sympathomimetic

What is the mechanism for Brimonidine?

A

Highly selective alpha2 adrenergic agonist

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12
Q

Sympathomimetic

What is Brimonidine available as? What’s it’s dose?

Name and concentration

A

Alphagan 0.2% solution
2x daily

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13
Q

Sympathomimetic

What are the possible side effects of Brimonidine?

A

Hyperaemia
FB sensation
Stinging
Blurred vision
Dry mouth
Headache
Fatigue/drowsiness
Allergic reaction
Reduction in heart rate and BP

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14
Q

Sympathomimetic

What is the mechanism for Apraclonidine?

A

Selective alpha2 adrenoceptor agonist

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15
Q

Sympathomimetic

What is Apraclonidine available as? What is it mostly used for?

Name and concentration

A

Iopidine 1% solution
Short term treatment e.g. post surgery

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16
Q

What is Beta blockers mode of action?

A

Beta receptor adrenergic antagonists which reduce aqueous humour secretion

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17
Q

Where are beta1 receptors located?

A

Heart and kidney

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18
Q

Where are beta2 receptors located?

A

Bronchi

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19
Q

What are the systemic side effects of beta blockers?

A

Bradycardia
Reduced BP
Respiratory difficulty

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20
Q

What are the contraindications for beta blockers?

A

Obstructive airway disease (e.g. asthma)
Bradycardia
Heart block/failure

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21
Q

Beta blocker

Is Timolol selective?

A

No - blocks both beta1 and beta2

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22
Q

What are the potential ocular side effects of beta blockers?

A

Stinging
Burning
Gritty sensation

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23
Q

Beta blocker

What is Timolol available as? What’s the dose?

Name and concentration

A

Timolol 0.25%/0.5% drops (2x daily)
Timoptol 0.25%/0.5% gel (1x daily)
Tiopex 0.1% gel (1x daily)

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24
Q

Beta blocker

Is Levobunolol selective?

A

No - blocks both beta1 and beta2

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25
Q

Beta blocker

What is Levobunolol available as? What’s the dose?

Name and concentration

A

Levobunolol 0.5% drops (1-2x daily)
Betagan 0.5% with 1.4% PVA vehicle drops (1-2x daily)

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26
Q

What does a PVA vehicle do?

A

Increases the viscosity of the drop, increases contact time of the drug and therefore prolongs release time/effectivity time

27
Q

Beta blocker

Is Betaxolol selective?

A

Yes - only blocks beta1

28
Q

Beta blocker

What is Betaxolol available as? What’s it’s dose?

Name and concentration

A

Betoptic 0.5% drops or 0.25% Ophthalmic suspension (2x daily)

29
Q

What combination preparations does Timolol come in?

A

Combigan (Brimodone 0.2%, Timolol 0.5%)
CoSopt (Dorzolamide 2%, Timolol 0.5%)
Azarga (Brinzolamide and Timolol)
Ganfort (Bimatoprost and Timolol)
Xalacom (Latanoprost 50mg/ml and Timolol 5mg/ml)
Duotrav (Travoprost and Timolol)

30
Q

How do Carbonic Anhydrase Inhibitors work?

A

Stop carbonic anhydrase (enzyme) catalysing bicarbonate formation which reduces aqueous humour production

Bicarbonate is an important component in aqueous humour formation

31
Q

What can carbonic anhydrase inhibitors be used in combination with?

A

Beta blockers
Sympathomimetics

32
Q

Carbonic anhydrase inhibitor

Why is Acetazolamide only available as a systemic treatment?

A

Poor lipid solubility and corneal penetration

33
Q

Carbonic anhydrase inhibitor

What is Acetazolamide available as?

Name and concentration

A

Diamox 250mg tablets
Diamox SR 250mg sustained release tablets
Intravenous powder

34
Q

Carbonic anhydrase inhibitor

What are the side effects of Acetazolamide?

A

Metallic taste
Digit numbness
Malaise/fatigue
Weight loss
Reduced libido and impotence
GI tract irritation
Altered renal function

35
Q

Carbonic anhydrase inhibitor

What are the contraindications for Acetazolamide?

A

Pregnancy
Liver disease
Kidney disorder

36
Q

Carbonic anhydrase inhibitor

What is Dorzolamide available as?

Name and concentration

A

Trusopt 2% solution
Cosopt 2% with 0.5% Timolol

37
Q

Carbonic anhydrase inhibitor

What are the side effects of Dorzolamide?

A

Localised ocular irritation
FB sensation
Stinging
Blurred vision
Conjunctivitis/lid inflammation
Corneal oedema

38
Q

Carbonic anhydrase inhibitor

When might Dorzolamide be a useful option?

A

If beta blocker ineffective
If beta blocker contraindicated (heart and lung disease)

39
Q

Carbonic anhydrase inhibitor

What is Brinzolamide available as? What’s it’s dose?

Name and concentration

A

Azopt 10mg/ml drop suspension
Azarga (with Timolol)

40
Q

What is the model of action of Prostaglandin Analogues?

A

Promotion of aqueous humour drainage via uveoscleral route by remodelling ciliary muscle extracellular space. This reduces collagen levels in ciliary muscle and surrounding sclera, resulting in reduced resistance to aqueous outflow

41
Q

Prostaglandin Analogue

What is Latanoprost available as? What’s it’s dose?

Name and concentration

A

Xalatan 50mg/ml solution (drops) 1x daily at night
Xalacom 50mg/ml with Timolol 5mg/ml 1x daily in morning

42
Q

Prostaglandin Analogue

What are the side effects of Latanoprost?

A

Darkening of iris, lids and lashes
Thickening of lashes and increase in number
Mild conjunctival hyperaemia

43
Q

Prostaglandin Analogue

What pathologies are associated with Latanoprost and Travoprost?

A

Cystoid Macular Oedema
Anterior Uveitis
Mild punctate epithelial staining
Dendritic corneal epitheliopathy
Herpes simplex keratitis

44
Q

Prostaglandin Analogue

What is Travoprost available as?

Name and concentration

A

Travatan 40mg/ml solution
Duotrav (with Timolol)

45
Q

Prostaglandin Analogue

What are the side effects of Travoprost and Bimatoprost?

A

Darkening of iris, lids and lashes
Thickening of lashes and increase in number
Mild conjunctival hyperaemia
Headache
Photophobia

46
Q

Prostaglandin Analogue

What is Bimatoprost available as? What’s it’s dose?

Name and concentration

A

Lumigan 300mg/ml or 100mg/ml drops 1x daily
Ganfort (with Timolol)

47
Q

Prostaglandin Analogue

What other use does Bimatoprost have?

A

Cosmetic lash growth (in US)

48
Q

Prostaglandin Analogue

What is Tafluprost available as? What’s it’s dose?

Name and concentration

A

Saflutan 15mg/ml drops (single dose units)
1x daily

49
Q

For Prostaglandin Analogues, which side effects remain and which reverse?

A

Iris darkening can continue after ceasing of treatment
Lash and lid darkening normally reverses once treatment stopped

50
Q

How do Hyperosmotic agents work?

A

An increase in blood plasma osmolarity causes fluid to move into plasma from the eye (and rest of the body), reducing IOP.

51
Q

Hyperosmotic agents

What is Mannitol available as?

Concentration and Administration

A

20% solution administered intravenously

52
Q

What are hyperosmotic agents used for?

A

Severely high IOPs that need quick short term reduction
e.g. Acute AC, pre-op IOP reduction, post penetrating trauma IOP reduction

53
Q

Hyperosmotic agents

What is Glycerol available as?

Concentration and Administration

A

50% solution administered orally

54
Q

Hyperosmotic agents

What is the onset and duration of Mannitol?

A

Onset: 30-60 mins
Duration: Up to 6 hours

55
Q

Hyperosmotic agents

What is the onset and duration of Glycerol?

A

Onset: 15-30 mins
Duration: 4-5 hours

56
Q

Hyperosmotic agents

What is Isosorbide available as?

Concentration and Administration

A

45% solution administered orally

57
Q

Hyperosmotic agents

What is the onset and duration of Isosorbide?

A

Onset: 30-60 mins
Duration: 5-6 hours

58
Q

What are the side effects of hyperosmotic agents?

A

Nausea and vomiting
Dehydration
Headache
Confusion/disorientation
Diuresis
Congestive heart failure (if pre-disposed heart issues)

59
Q

Sympathomimetic

How much can Brimonidine reduce IOP by?

A

~6.5mmHg

60
Q

Beta Blocker

What effect does Timolol have on IOP?

A

25% reduction for 24 hours

61
Q

Beta Blocker

What effect does Levobunolol have on IOP?

A

25% reduction for 24 hours

62
Q

Beta Blocker

What effect does Betaxolol have on IOP?

A

Lower reduction than Timolol after first month (IOP higher than pxs on Timolol), but same after 1 year

63
Q

Prostaglandin Analogue

What effect does Latanoprost have on IOP?

A

25-30% reduction

Year 2 Ocular Pharmacology (20 decks)

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