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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
What is Ocupress?
carteolol 1.0%
26
What is Optipranolol?
metipranolol 0.3%
27
What is different about betaxolol 0.25% ?
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!**
28
How might betaxolol do a better job of preserving the visual field?
- May increase blood supply to ON | blockade of calcium channels and consequent vessel dilation
29
What is Betopic?
0.5% betaxolol solution | discontinued
30
What is Betoptic-S?
0.25% betaxolol suspension
31
What are the characteristics that make Betopic-S different?
- Microfine suspension designed to enhance absorption and reduce concentration - Carbomer 934P + cationic exchange resin - Less stinging than other beta-blockers - Minimal shaking required
32
What is Betaxon? | N/A in Canada
levobetaxolol 0.5% | levo-isomer of betaxolol
33
How is Betaxon dosed?
1 gt b.i.d.
34
What is Betaxon's advantage over betaxolol?
Slightly enhanced therapeutic profile (reduces IOP 1-2mmHg more)
35
Which beta-blocker is contraindicated w/ uveitis?
OptiPranolol (metipranolol 0.3%)
36
Which beta-blocker has a high probability of bronchopulmonary ADRs?
OptiPranolol (metipranolol 0.3%)
37
How is OptiPranolol dosed?
1 gt b.i.d.
38
Which 3 beta-blockers have active metabolites?
carteolol, levobunolol, metipranolol
39
How does carteolol lower IOP?
- Decrease production of aqueous | - Improve outflow
40
How is carteolol (Ocupress) dosed?
1 gt b.i.d.
41
Which beta-blocker might you recommend to a Px with dyslipidemia?
carteolol 1% (Ocupress)
42
Which beta-blocker may cause less stinging BUT has the greatest potential to cause corneal anesthesia?
carteolol 1% (Ocupress)
43
Prostanoid drops have what color caps?
Green or clear
44
What is Xalatan?
latanoprost 0.005% solution
44
Prostanoid drops have what color caps?
Green or clear
45
What is Xalatan?
latanoprost 0.005% solution
46
How is Xalatan administered?
1 gt q.d. (in the evening)
46
How is Xalatan administered?
1 gt q.d. (in the evening)
47
How does latanoprost lower IOP?
Increases uveoscleral outflow
48
Can tolerance develop to latanoprost? How quickly?
Tolerance may develop in 18 month window
48
How does latanoprost lower IOP?
Increases uveoscleral outflow
50
Can tolerance develop to latanoprost? How quickly?
Tolerance may develop in 18 month window
52
latanoprost is additive with most anti-glaucoma drugs EXCEPT...
Pilocarpine
54
latanoprost is additive with most anti-glaucoma drugs EXCEPT...
Pilocarpine
55
Two big advantages of latanoprost over beta blockers are...
1) Superior safety profile | 2) q.d. dosing
56
Two big advantages of latanoprost over beta blockers are...
1) Superior safety profile | 2) q.d. dosing
57
What are the ocular ADRs associated w/ latanoprost?
1. Cystoid macular edema (CME) 2. Uveitis 3. HSV recurrence 4. Hypertrichiasis 5. Darkening of lashes and area around eyes
58
What are the ocular ADRs associated w/ latanoprost?
1. Cystoid macular edema (CME) 2. Uveitis 3. HSV recurrence 4. Hypertrichiasis 5. Darkening of lashes and area around eyes
59
What causes darkening of the iris in Px's taking latanoprost?
- Only significant in hazel / mixed color eyes | - Caused by stimulation of iris stromal melanocytes to produce more intracellular melanin
60
What causes darkening of the iris in Px's taking latanoprost?
- Only significant in hazel / mixed color eyes | - Caused by stimulation of iris stromal melanocytes to produce more intracellular melanin
61
Warnings associated w/ latanoprost Tx
- 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
Warnings associated w/ latanoprost Tx
- 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
What are the most COMMON ocular ADRs associated w/ prostanoids?
Blurred vision, burning/stinging, conjunctival hyperemia, FB sensation, itching, increased iris pigmentation, SPK
64
What are the most COMMON ocular ADRs associated w/ prostanoids?
Blurred vision, burning/stinging, conjunctival hyperemia, FB sensation, itching, increased iris pigmentation, SPK
65
What are the major systemic ADRs associated w/ latanoprost?
- URT infections, chest pain, muscle/joint/back pain, allergic skin rxn - Pregnancy Category C
66
What are the major systemic ADRs associated w/ latanoprost?
- URT infections, chest pain, muscle/joint/back pain, allergic skin rxn - Pregnancy Category C
67
What is Travatan?
travoprost 0.004% solution
68
Which glaucoma drug might you be more likely to Rx for an African-American Px?
Travatan
69
What is the most common ocular ARD associated with travoprost?
Conjunctival hyperemia (35-50% of Px's)
70
What is Lumigan?
bimatoprost 0.03% solution
71
Why is Lumigan different from the other prostanoids?
It is a PROSTAMIDE. | Higher concentration b/c amidase breakdown is less efficient than ester breakdown.
72
When might you Rx bimatoprost (Lumigan)?
When Px is intolerant of other IOP-lowering meds or they are insufficiently responsive.
73
How is Lumigan administered?
1 gt q.d. | More effective at night (h.s.)
74
How does bimatoprost lower IOP?
Enhances aqueous outflow, most likely through uveoscleral route
75
What is Lumigan RC?
bimatoprost 0.01% preserved w/ 0.02% BAK (as opposed to 0.005% BAK in Lumigan) *Discontinued; caused A LOT of hyperaemia!!
76
What are the ocular ADRs most commonly associated with bimatoprost 0.03%?
Conjunctival hyperemia, growth of eyelashes, ocular pruritis (15-45% of Px's)
77
What systemic ADRs are most commonly associated w/ bimatoprost 0.03%?
colds and URT infections (10%)
78
What is Zioptan?
tafluprost 0.005% (Preservative-free!)
79
Why do we no longer Rx epinephrine?
- Uncomfortable on installation - Many ocular ADR's (black concretions) - ALL formulations contained sulfites (allergy)
80
What are some systemic side effects of epinephrine?
``` Headache Palpitations Tachycardia Hypertension Faintness Cardiac Arrhythmia ```
81
When is epinephrine contraindicated?
Hypersensitivities (sulfa) Narrow angles (dilation) Soft contact lens wear
82
What is dipivefrin 0.1% solution?
- Propine - Prodrug (converted to epinephrine in cornea) - Same efficacy as epinephrine but fewer ADRs
83
How is Propine (dipivefrin 0.1%) dosed?
Monotherapy: 1 gt bid | Add-on: 1 gt bid
84
What is Iopidine?
apraclonidine 0.5%, 1%
85
How does apraclonidine lower IOP?
Reduces aqueous production and increases uveoscleral outflow (relatively selective for alpha 2 receptors)
86
When would you use 1.0% apraclonidine?
Control/prevent post-surgical elevations in IOP (1 gt before and after surgery). Available in AMPULES.
87
When might you use 0.5% apraclonidine?
Short-term adjunctive therapy in Px's who require additional IOP reduction (bid -> tid)
88
When is apraclonidine contraindicated?
- Hypersensitivities (clonidine) - Px's on MAOI's - Additive effect w/ CNS depressants
89
Why is long-term use of apraclonidine limited?
- Tolerance (25%, onset = 3 months) | - Allergy (25%)
90
What systemic ADRs are associated w/ apraclonidine?
``` HA DRY MOUTH (20-50%) Hypotension Bradycardia Apnea Fatigue Depression ```
91
Compare brimonidine 0.2% to apraclonidine.
- More selective for alpha-2 receptors (30x) - More lipophilic (better penetration of cornea) - Less prone to oxidations (allergy)
92
What formulations of brimonidine are currently available?
brimonidine 0.2% (generic) Alphagan-P 0.15% Alphagan-P 0.10% (US ONLY!)
93
What makes Alphagan-P different from Alphagan?
Purite preservative
94
How is Alphagan dosed?
1 gt bid (add-on) | 1 gt tid (monotherapy)
95
When should you use caution if Rx'ing brimonidine?
- Severe CV disease, hepatic disease, renal failure | - CNS depressants (potentiation)
96
When is brimonidine contraindicated?
- Hypersensitivities | - Co-admin of MAOI's
97
What ocular ADRs are associated w/ brimonidine?
Allergic conjunctivitis, conjunctival hyperemia, eye pruritus
98
What is often the first agent administered to treat acute angle closure?
Diamox (acetazolamide) | 2 x 250mg (NOT 1 500mg)
99
In what forms is acetazolamide available orally?
Generic (125, 250 mg tablets) Diamox sequels (sustained release 500 mg capsules) Generic (powder for injection)
100
What is Daranide?
dichlorphenamide 50 mg tablets
101
What is Neptazane?
methazolamide 25 and 50 mg tablets
102
When is methazolamide a good choice for an oral CAI?
- Better for Px's w/ pulmonary problems - Less disturbing to renal system - Fewer ADRs in general
103
What is Trusopt?
dorzolamide 2.0% solution
104
How is dorzolamide dosed?
Approved for tid (dark irides), but bid is effective. | 1 gt morning, 1 gt before dinner
105
What is the greatest ocular ADR associated w/ Trusopt (dorzolamide)?
``` STINGING! Corneal endothelial (and epithelial) function may be partially compromised. ```
106
What systemic ADR is associated w/ dorzolamide?
Bitter taste
107
What is Azopt?
brinzolamide 1.0% SUSPENSION
108
What is the ocular ADR most commonly associated w/ Azopt?
Blurred vision
109
What is Osmitrol?
mannitol 20% (I.V.)
110
When is Osmitrol contraindicated?
Renal disease
111
What is the onset time for Osmitrol?
30 min Max in 30-60 mins Duration ~6hrs
112
What systemic ADRs are associated w/ Osmitrol?
Diuresis, HA, chills, chest pain | Pregnancy category C
113
What is Osmoglyn?
glycerin oral 50% (lime flavoured)
114
What is the onset time for Osmoglyn?
15-30 mins Max in 45 mins Duration ~5hrs
115
When is Osmoglyn contraindicated?
Diabetics (hyperglycemia, ketoacidosis) CHF, hypervolemia, dementia Elderly, severely dehydrated
116
What systemic ADRs are associated w/ Osmoglyn?
Nausea & vomitting Dehydration, HA, confusion, disorientation Pregnancy category C
117
What is Ismotic?
isosorbide oral 45% (vanilla mint flavour)
118
What is the onset time for Ismotic?
30-60 mins | Duration: 5-6 hrs
119
What systemic ADRs are associated w/ Ismotic?
Lower incidence of nausea and vomitting Dehydration, HA, confusion, disorentation Pregnancy category B
120
What is Osmitrol?
mannitol 20% (I.V.)
121
When is Osmitrol contraindicated?
Renal disease
122
What is the onset time for Osmitrol?
30 min Max in 30-60 mins Duration ~6hrs
123
What systemic ADRs are associated w/ Osmitrol?
Diuresis, HA, chills, chest pain | Pregnancy category C
124
What is Osmoglyn?
glycerin oral 50% (lime flavoured)
125
What is the onset time for Osmoglyn?
15-30 mins Max in 45 mins Duration ~5hrs
126
When is Osmoglyn contraindicated?
Diabetics (hyperglycemia, ketoacidosis) CHF, hypervolemia, dementia Elderly, severely dehydrated
127
What systemic ADRs are associated w/ Osmoglyn?
Nausea & vomitting Dehydration, HA, confusion, disorientation Pregnancy category C
128
What is Ismotic?
isosorbide oral 45% (vanilla mint flavour)
129
What is the onset time for Ismotic?
30-60 mins | Duration: 5-6 hrs
130
What systemic ADRs are associated w/ Ismotic?
Lower incidence of nausea and vomitting Dehydration, HA, confusion, disorentation Pregnancy category B
131
What are some ocular ADRs of pilocarpine?
Burning, blurred vision, miosis or accommodative spasm, browache
132
What are some systemic ADRs of pilocarpine?
Sweating, salivation
133
What concentration of pilocarpine would you use on a Px w/ lightly pigmented eyes?
4% or less
134
What concentration of pilocarpine would you need on a Px with highly pigmented eyes?
8 or 10%
135
What is Ocusert?
Direct pilocarpine, released at a constant rate. P-20 = 20 ug/hr P-40 = 40 ug/hr
136
What are the additional ADRs of Ocusert?
Irritation and increased mucus secretion
137
What is Isopto Carbachol?
carbachol 1.5% and 3% solution (direct acting muscarinc agonsit)
138
How does carbachol compare to pilocarpine?
Stronger, and greater probability to cause systemic ADRs.
139
How is carbachol dosed?
1 gt up to tid
140
Name two reversible inderect cholinesterase inhibitors.
phyostigmine and demecarium
141
Name one irreversible cholinesterase inhibitor.
echiothiophate
142
What concentration of pilocarpine would you use on a Px w/ lightly pigmented eyes?
4% or less
143
What concentration of pilocarpine would you need on a Px with highly pigmented eyes?
8 or 10%
144
What is Ocusert?
Direct pilocarpine, released at a constant rate. P-20 = 20 ug/hr P-40 = 40 ug/hr
145
What are the additional ADRs of Ocusert?
Irritation and increased mucus secretion
146
What is Isopto Carbachol?
carbachol 1.5% and 3% solution (direct acting muscarinc agonsit)
147
How does carbachol compare to pilocarpine?
Stronger, and greater probability to cause systemic ADRs.
148
How is carbachol dosed?
1 gt up to tid
149
Name two reversible inderect cholinesterase inhibitors.
phyostigmine and demecarium
150
Name one irreversible cholinesterase inhibitor.
echiothiophate

Ocular Pharmacology (5 decks)

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