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Ocular Pharmacology > Glaucoma Drugs > Flashcards

Glaucoma Drugs Flashcards

1
Q

What is the usual beta-blocker of choice? (and its concentrations)

A

timolol maleate 0.25% and 0.5%

Timoptic

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2
Q

What are the characteristics of Timoptic-XE?

A
  • Viscous drop (forms a gel when on contact w/ ocular surface)
  • Preserved w/ benzododecinium bromide
  • Expensive!!
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3
Q

What color caps are used for the non-selective beta-blockers (timolol and levobutanol)?

A
  1. 5% = yellow labels

0. 25% = blue labels

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4
Q

What is Ocudose?

A

Single dose of Timoptic

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5
Q

What is the dosing regime for timolol maleate?

A
  • Start w/ 1 gt 0.25%

- NEVER more than b.i.d.

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6
Q

How would you increase dosage of timolol maleate?

A
  • Switch to b.i.d.
  • Switch to 0.5%
    (usually these aren’t done due to the increased risk of ADRs!)
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7
Q

What is Cosopt?

A

timolol maleate 0.5% + dorzolamide 2%

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8
Q

What is Xalcom?

A

timolol maleate 0.5% + latanoprost 0.005%

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9
Q

What is Combigan?

A

timolol maleate 0.5% + brimonidine 0.2%

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10
Q

What is Duotrav?

A

timolol maleate 0.5% + travaprost 0.004%

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11
Q

What is Azarga?

A

timolol maleate 0.5% + brinzolamide 1%

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12
Q

What are some advantages of Istalol (timolol maleate 0.5%)

Note: NOT available in Canada

A
  • 0.45% potassium sorbate added; more LIPOPHILIC
  • Increased penetration, decreased systemic absorption
  • Dosed q.d.
  • Less systemic effects
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13
Q

What is Betimol?

A

timolol hemihydrate 0.25% and 0.5%

  • as effective as Timoptic
  • NO generics
  • used q.d.
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14
Q

What are the ocular side effects of timolol?

A
  • Burning, stinging, transient blurred vision
  • Photophobia
  • Conjunctivitis, blepharitis, punctate keratitis
  • Contact dermatitis, eyelid erythema
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15
Q

What are the systemic side effects of timolol?

A
  • Decreased HR, cardiac output
  • Bronchospasm
  • Hypotension
  • Depression
  • Decreased libido
  • Worsened lipid profile
  • Decreased stress response to hypoglycermia, surgery or anaphylaxis
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16
Q

What are the contraindications of timolol?

A
  • Asthma, COPD
  • CHF, sinus bradycardia, atrioventricular block
  • Hypersensitivity
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17
Q

What are the drugs that may interact w/ timolol?

A
  • Oral beta-blockers
  • Calcium channel blockers
  • quinidine
  • digitalis and catecholamine-depleting drugs
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18
Q

What is Betagan?

A

0.25% and 0.5% levobunolol

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19
Q

What are two disadvantages of levobunolol?

A

1) High potential for broncho-pulmonary ADRs

2) Most formulations contain sulfites

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20
Q

What are some advantages of levolbunolol?

A
  • non-selective
  • potent
  • LONGEST ACTING
  • indicated for q.d. dosing
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21
Q

What is Probeta?

A

0.5% levobunolol + 0.1% dipivefrin

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22
Q

What is the dosing for

a) levobunolol and b) Probeta?

A

a) 1 gt (0.25%) q.d.
To increase, switch to 0.5% q.d. or 0.25% b.i.d.
b) 1 gt b.i.d.

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23
Q

What are the ocular ADRs associated with levobunolol?

A

1 = mild transient blurring / stinging (52%)

  • Vision problems/blur
  • Conjunctival erythema
  • FB sensation
  • Photophobia
  • Itching
  • Eyelid erythema
  • Eyelid edema
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24
Q

What beta blocker has the largest drop size?

A

Betagan (levobunolol)

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25
Q

What is Ocupress?

A

carteolol 1.0%

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26
Q

What is Optipranolol?

A

metipranolol 0.3%

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27
Q

What is different about betaxolol 0.25% ?

A

Cardioselective (relatively selective for beta1)

  • not as potent as non-selective beta-blockers (IOP ~2mmHg higher)
  • HR decreases ~4 bpm

Still consider severe pulmonary/CV disease to be a contraindication!

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28
Q

How might betaxolol do a better job of preserving the visual field?

A
  • May increase blood supply to ON

blockade of calcium channels and consequent vessel dilation

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29
Q

What is Betopic?

A

0.5% betaxolol solution

discontinued

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30
Q

What is Betoptic-S?

A

0.25% betaxolol suspension

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31
Q

What are the characteristics that make Betopic-S different?

A
  • Microfine suspension designed to enhance absorption and reduce concentration
  • Carbomer 934P + cationic exchange resin
  • Less stinging than other beta-blockers
  • Minimal shaking required
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32
Q

What is Betaxon?

N/A in Canada

A

levobetaxolol 0.5%

levo-isomer of betaxolol

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33
Q

How is Betaxon dosed?

A

1 gt b.i.d.

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34
Q

What is Betaxon’s advantage over betaxolol?

A

Slightly enhanced therapeutic profile (reduces IOP 1-2mmHg more)

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35
Q

Which beta-blocker is contraindicated w/ uveitis?

A

OptiPranolol (metipranolol 0.3%)

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36
Q

Which beta-blocker has a high probability of bronchopulmonary ADRs?

A

OptiPranolol (metipranolol 0.3%)

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37
Q

How is OptiPranolol dosed?

A

1 gt b.i.d.

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38
Q

Which 3 beta-blockers have active metabolites?

A

carteolol, levobunolol, metipranolol

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39
Q

How does carteolol lower IOP?

A
  • Decrease production of aqueous

- Improve outflow

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40
Q

How is carteolol (Ocupress) dosed?

A

1 gt b.i.d.

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41
Q

Which beta-blocker might you recommend to a Px with dyslipidemia?

A

carteolol 1% (Ocupress)

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42
Q

Which beta-blocker may cause less stinging BUT has the greatest potential to cause corneal anesthesia?

A

carteolol 1% (Ocupress)

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43
Q

Prostanoid drops have what color caps?

A

Green or clear

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44
Q

What is Xalatan?

A

latanoprost 0.005% solution

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44
Q

Prostanoid drops have what color caps?

A

Green or clear

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45
Q

What is Xalatan?

A

latanoprost 0.005% solution

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46
Q

How is Xalatan administered?

A

1 gt q.d. (in the evening)

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46
Q

How is Xalatan administered?

A

1 gt q.d. (in the evening)

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47
Q

How does latanoprost lower IOP?

A

Increases uveoscleral outflow

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48
Q

Can tolerance develop to latanoprost? How quickly?

A

Tolerance may develop in 18 month window

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48
Q

How does latanoprost lower IOP?

A

Increases uveoscleral outflow

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50
Q

Can tolerance develop to latanoprost? How quickly?

A

Tolerance may develop in 18 month window

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52
Q

latanoprost is additive with most anti-glaucoma drugs EXCEPT…

A

Pilocarpine

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54
Q

latanoprost is additive with most anti-glaucoma drugs EXCEPT…

A

Pilocarpine

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55
Q

Two big advantages of latanoprost over beta blockers are…

A

1) Superior safety profile

2) q.d. dosing

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56
Q

Two big advantages of latanoprost over beta blockers are…

A

1) Superior safety profile

2) q.d. dosing

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57
Q

What are the ocular ADRs associated w/ latanoprost?

A
  1. Cystoid macular edema (CME)
  2. Uveitis
  3. HSV recurrence
  4. Hypertrichiasis
  5. Darkening of lashes and area around eyes
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58
Q

What are the ocular ADRs associated w/ latanoprost?

A
  1. Cystoid macular edema (CME)
  2. Uveitis
  3. HSV recurrence
  4. Hypertrichiasis
  5. Darkening of lashes and area around eyes
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59
Q

What causes darkening of the iris in Px’s taking latanoprost?

A
  • Only significant in hazel / mixed color eyes

- Caused by stimulation of iris stromal melanocytes to produce more intracellular melanin

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60
Q

What causes darkening of the iris in Px’s taking latanoprost?

A
  • Only significant in hazel / mixed color eyes

- Caused by stimulation of iris stromal melanocytes to produce more intracellular melanin

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61
Q

Warnings associated w/ latanoprost Tx

A
  • Px’s w/ severe kidney / liver impairment
  • Effects on corneal endothelium
  • Formulation contains BAK
  • Less experience in Px’s w/ angle-closure, inflammatory, or neovascular glaucoma
62
Q

Warnings associated w/ latanoprost Tx

A
  • Px’s w/ severe kidney / liver impairment
  • Effects on corneal endothelium
  • Formulation contains BAK
  • Less experience in Px’s w/ angle-closure, inflammatory, or neovascular glaucoma
63
Q

What are the most COMMON ocular ADRs associated w/ prostanoids?

A

Blurred vision, burning/stinging, conjunctival hyperemia, FB sensation, itching, increased iris pigmentation, SPK

64
Q

What are the most COMMON ocular ADRs associated w/ prostanoids?

A

Blurred vision, burning/stinging, conjunctival hyperemia, FB sensation, itching, increased iris pigmentation, SPK

65
Q

What are the major systemic ADRs associated w/ latanoprost?

A
  • URT infections, chest pain, muscle/joint/back pain, allergic skin rxn
  • Pregnancy Category C
66
Q

What are the major systemic ADRs associated w/ latanoprost?

A
  • URT infections, chest pain, muscle/joint/back pain, allergic skin rxn
  • Pregnancy Category C
67
Q

What is Travatan?

A

travoprost 0.004% solution

68
Q

Which glaucoma drug might you be more likely to Rx for an African-American Px?

A

Travatan

69
Q

What is the most common ocular ARD associated with travoprost?

A

Conjunctival hyperemia (35-50% of Px’s)

70
Q

What is Lumigan?

A

bimatoprost 0.03% solution

71
Q

Why is Lumigan different from the other prostanoids?

A

It is a PROSTAMIDE.

Higher concentration b/c amidase breakdown is less efficient than ester breakdown.

72
Q

When might you Rx bimatoprost (Lumigan)?

A

When Px is intolerant of other IOP-lowering meds or they are insufficiently responsive.

73
Q

How is Lumigan administered?

A

1 gt q.d.

More effective at night (h.s.)

74
Q

How does bimatoprost lower IOP?

A

Enhances aqueous outflow, most likely through uveoscleral route

75
Q

What is Lumigan RC?

A

bimatoprost 0.01% preserved w/ 0.02% BAK (as opposed to 0.005% BAK in Lumigan)
*Discontinued; caused A LOT of hyperaemia!!

76
Q

What are the ocular ADRs most commonly associated with bimatoprost 0.03%?

A

Conjunctival hyperemia, growth of eyelashes, ocular pruritis (15-45% of Px’s)

77
Q

What systemic ADRs are most commonly associated w/ bimatoprost 0.03%?

A

colds and URT infections (10%)

78
Q

What is Zioptan?

A

tafluprost 0.005% (Preservative-free!)

79
Q

Why do we no longer Rx epinephrine?

A
  • Uncomfortable on installation
  • Many ocular ADR’s (black concretions)
  • ALL formulations contained sulfites (allergy)
80
Q

What are some systemic side effects of epinephrine?

A 
Headache
Palpitations
Tachycardia
Hypertension
Faintness
Cardiac Arrhythmia
81
Q

When is epinephrine contraindicated?

A

Hypersensitivities (sulfa)
Narrow angles (dilation)
Soft contact lens wear

82
Q

What is dipivefrin 0.1% solution?

A
  • Propine
  • Prodrug (converted to epinephrine in cornea)
  • Same efficacy as epinephrine but fewer ADRs
83
Q

How is Propine (dipivefrin 0.1%) dosed?

A

Monotherapy: 1 gt bid

Add-on: 1 gt bid

84
Q

What is Iopidine?

A

apraclonidine 0.5%, 1%

85
Q

How does apraclonidine lower IOP?

A

Reduces aqueous production and increases uveoscleral outflow (relatively selective for alpha 2 receptors)

86
Q

When would you use 1.0% apraclonidine?

A

Control/prevent post-surgical elevations in IOP (1 gt before and after surgery). Available in AMPULES.

87
Q

When might you use 0.5% apraclonidine?

A

Short-term adjunctive therapy in Px’s who require additional IOP reduction (bid -> tid)

88
Q

When is apraclonidine contraindicated?

A
  • Hypersensitivities (clonidine)
  • Px’s on MAOI’s
  • Additive effect w/ CNS depressants
89
Q

Why is long-term use of apraclonidine limited?

A
  • Tolerance (25%, onset = 3 months)

- Allergy (25%)

90
Q

What systemic ADRs are associated w/ apraclonidine?

A 
HA
DRY MOUTH (20-50%)
Hypotension
Bradycardia
Apnea
Fatigue
Depression
91
Q

Compare brimonidine 0.2% to apraclonidine.

A
  • More selective for alpha-2 receptors (30x)
  • More lipophilic (better penetration of cornea)
  • Less prone to oxidations (allergy)
92
Q

What formulations of brimonidine are currently available?

A

brimonidine 0.2% (generic)
Alphagan-P 0.15%
Alphagan-P 0.10% (US ONLY!)

93
Q

What makes Alphagan-P different from Alphagan?

A

Purite preservative

94
Q

How is Alphagan dosed?

A

1 gt bid (add-on)

1 gt tid (monotherapy)

95
Q

When should you use caution if Rx’ing brimonidine?

A
  • Severe CV disease, hepatic disease, renal failure

- CNS depressants (potentiation)

96
Q

When is brimonidine contraindicated?

A
  • Hypersensitivities

- Co-admin of MAOI’s

97
Q

What ocular ADRs are associated w/ brimonidine?

A

Allergic conjunctivitis, conjunctival hyperemia, eye pruritus

98
Q

What is often the first agent administered to treat acute angle closure?

A

Diamox (acetazolamide)

2 x 250mg (NOT 1 500mg)

99
Q

In what forms is acetazolamide available orally?

A

Generic (125, 250 mg tablets)
Diamox sequels (sustained release 500 mg capsules)
Generic (powder for injection)

100
Q

What is Daranide?

A

dichlorphenamide 50 mg tablets

101
Q

What is Neptazane?

A

methazolamide 25 and 50 mg tablets

102
Q

When is methazolamide a good choice for an oral CAI?

A
  • Better for Px’s w/ pulmonary problems
  • Less disturbing to renal system
  • Fewer ADRs in general
103
Q

What is Trusopt?

A

dorzolamide 2.0% solution

104
Q

How is dorzolamide dosed?

A

Approved for tid (dark irides), but bid is effective.

1 gt morning, 1 gt before dinner

105
Q

What is the greatest ocular ADR associated w/ Trusopt (dorzolamide)?

A 
STINGING!
Corneal endothelial (and epithelial) function may be partially compromised.
106
Q

What systemic ADR is associated w/ dorzolamide?

A

Bitter taste

107
Q

What is Azopt?

A

brinzolamide 1.0% SUSPENSION

108
Q

What is the ocular ADR most commonly associated w/ Azopt?

A

Blurred vision

109
Q

What is Osmitrol?

A

mannitol 20% (I.V.)

110
Q

When is Osmitrol contraindicated?

A

Renal disease

111
Q

What is the onset time for Osmitrol?

A

30 min
Max in 30-60 mins
Duration ~6hrs

112
Q

What systemic ADRs are associated w/ Osmitrol?

A

Diuresis, HA, chills, chest pain

Pregnancy category C

113
Q

What is Osmoglyn?

A

glycerin oral 50% (lime flavoured)

114
Q

What is the onset time for Osmoglyn?

A

15-30 mins
Max in 45 mins
Duration ~5hrs

115
Q

When is Osmoglyn contraindicated?

A

Diabetics (hyperglycemia, ketoacidosis)
CHF, hypervolemia, dementia
Elderly, severely dehydrated

116
Q

What systemic ADRs are associated w/ Osmoglyn?

A

Nausea & vomitting
Dehydration, HA, confusion, disorientation
Pregnancy category C

117
Q

What is Ismotic?

A

isosorbide oral 45% (vanilla mint flavour)

118
Q

What is the onset time for Ismotic?

A

30-60 mins

Duration: 5-6 hrs

119
Q

What systemic ADRs are associated w/ Ismotic?

A

Lower incidence of nausea and vomitting
Dehydration, HA, confusion, disorentation
Pregnancy category B

120
Q

What is Osmitrol?

A

mannitol 20% (I.V.)

121
Q

When is Osmitrol contraindicated?

A

Renal disease

122
Q

What is the onset time for Osmitrol?

A

30 min
Max in 30-60 mins
Duration ~6hrs

123
Q

What systemic ADRs are associated w/ Osmitrol?

A

Diuresis, HA, chills, chest pain

Pregnancy category C

124
Q

What is Osmoglyn?

A

glycerin oral 50% (lime flavoured)

125
Q

What is the onset time for Osmoglyn?

A

15-30 mins
Max in 45 mins
Duration ~5hrs

126
Q

When is Osmoglyn contraindicated?

A

Diabetics (hyperglycemia, ketoacidosis)
CHF, hypervolemia, dementia
Elderly, severely dehydrated

127
Q

What systemic ADRs are associated w/ Osmoglyn?

A

Nausea & vomitting
Dehydration, HA, confusion, disorientation
Pregnancy category C

128
Q

What is Ismotic?

A

isosorbide oral 45% (vanilla mint flavour)

129
Q

What is the onset time for Ismotic?

A

30-60 mins

Duration: 5-6 hrs

130
Q

What systemic ADRs are associated w/ Ismotic?

A

Lower incidence of nausea and vomitting
Dehydration, HA, confusion, disorentation
Pregnancy category B

131
Q

What are some ocular ADRs of pilocarpine?

A

Burning, blurred vision, miosis or accommodative spasm, browache

132
Q

What are some systemic ADRs of pilocarpine?

A

Sweating, salivation

133
Q

What concentration of pilocarpine would you use on a Px w/ lightly pigmented eyes?

A

4% or less

134
Q

What concentration of pilocarpine would you need on a Px with highly pigmented eyes?

A

8 or 10%

135
Q

What is Ocusert?

A

Direct pilocarpine, released at a constant rate.
P-20 = 20 ug/hr
P-40 = 40 ug/hr

136
Q

What are the additional ADRs of Ocusert?

A

Irritation and increased mucus secretion

137
Q

What is Isopto Carbachol?

A

carbachol 1.5% and 3% solution (direct acting muscarinc agonsit)

138
Q

How does carbachol compare to pilocarpine?

A

Stronger, and greater probability to cause systemic ADRs.

139
Q

How is carbachol dosed?

A

1 gt up to tid

140
Q

Name two reversible inderect cholinesterase inhibitors.

A

phyostigmine and demecarium

141
Q

Name one irreversible cholinesterase inhibitor.

A

echiothiophate

142
Q

What concentration of pilocarpine would you use on a Px w/ lightly pigmented eyes?

A

4% or less

143
Q

What concentration of pilocarpine would you need on a Px with highly pigmented eyes?

A

8 or 10%

144
Q

What is Ocusert?

A

Direct pilocarpine, released at a constant rate.
P-20 = 20 ug/hr
P-40 = 40 ug/hr

145
Q

What are the additional ADRs of Ocusert?

A

Irritation and increased mucus secretion

146
Q

What is Isopto Carbachol?

A

carbachol 1.5% and 3% solution (direct acting muscarinc agonsit)

147
Q

How does carbachol compare to pilocarpine?

A

Stronger, and greater probability to cause systemic ADRs.

148
Q

How is carbachol dosed?

A

1 gt up to tid

149
Q

Name two reversible inderect cholinesterase inhibitors.

A

phyostigmine and demecarium

150
Q

Name one irreversible cholinesterase inhibitor.

A

echiothiophate

Ocular Pharmacology (5 decks)

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