Glaucoma Agents Flashcards
(195 cards)
1
Q
which class(es) of drugs primarily inhibit the production of aqueous humor?
A
- alpha-adrenergic agonists
- beta-blockers
- carbonic anhydrase inhibitors
2
Q
which class(es) of drugs primarily increase trabecular outflow?
A
- muscarinic agonists
- nitrous oxide
- rho-kinase inhibitors
3
Q
which class(es) of drugs primarily increase uveoscleral outflow?
A
prostaglandin agonists
4
Q
what color bottle caps do prostaglandin analogs have?
A
teal
5
Q
what is the brand name for latanoprost?
A
Xalatan
6
Q
what is the brand name for travoprost?
A
Travatan Z
7
Q
what is the brand name for bimatoprost?
A
Lumigan
8
Q
what is the brand name for tafluprost?
A
Zioptan
9
Q
which of the prostaglandin analogs are ester prodrug(s)?
A
- latanoprost
- travoprost
- tafluprost
10
Q
what is the primary MOA for latanoprost, travoprost & tafluprost?
A
act on PGF-2α FP receptors found in ciliary muscle & iris sphincter muscle
11
Q
which prostaglandin analog is a selective FP receptor agonist? how does it exert its ocular hypotensive effects?
A
latanoprost
- exerts its ocular hypotensive effects by increasing uveoscleral outflow by remodeling the ECM adjacent to ciliary muscle cells
12
Q
which prostaglandin analog is a synthetic analog? it mimics the actions of what?
A
bimatoprost
- mimics the actions of prostamides
13
Q
which prostaglandin analog has weak activity at the FP receptor?
A
bimatoprost
14
Q
what is the MOA for bimatoprost?
A
dual mechanism of increase aqueous outflow through trabecular & uveoscleral pathway
15
Q
which aqueous outflow pathway is pressure-sensitive?
A
trabecular
16
Q
which aqueous outflow pathway is pressure-insensitive?
A
uveoscleral
17
Q
what has to bind to the FP receptors to convert the prodrugs into their active form?
A
prostaglandin F2α
18
Q
what allows prostaglandin analogs to penetrate the corneal epithelium?
A
lipophilicity
19
Q
what converts the active form of prostaglandin analogs into free acid?
A
corneal esterases/amidases
20
Q
what allows the free acid to bind to receptors?
A
hydrophilicity
21
Q
which class of glaucoma medications is the first line treatment?
A
prostaglandins
22
Q
what is the dosing for prostaglandins?
A
1 gtt qhs OU
23
Q
when are prostaglandins most effective after administration?
A
12-24 hour period
24
Q
what percentage of IOP lowering effects do prostaglandins have?
A
27-30%
25
which prostaglandin is used in treatment of POAG & ocular hypertension? (name generic & brand)
latanoprost (Xalatan)
26
Xalatan may significantly reduce IOP in patients with glaucoma associated with what condition?
Sturge-Weber Syndrome
27
which prostaglandin can be more effective than beta-blockers in reducing IOP in patients with pigmentary glaucoma?
latanoprost (Xalatan)
28
Xalatan (latanoprost) can often produce significant IOP reduction in patients with which type of glaucoma?
normal tension glaucoma
29
using Xalatan (latanoprost) in conjunction with which drugs can be useful due to the additive effects?
- aqueous suppressant drugs
| - drugs that enhance aqueous outflow through trabecular pathway
30
what is Xalatan preserved with?
BAK
31
when should you refrigerate Xalatan?
when using medication in only one eye
32
what is the brand name for latanoprost?
Xalatan
33
what is the brand name for travoprost?
Travatan
34
what preservative is in Travatan?
BAK
35
what is Travatan Z formulated with instead of BAK?
ionic buffered compound (sofZia)
36
what adverse effect was reduced when comparing Travatan Z (sofZia preservative) & Travatan (BAK preservative)?
conjunctival hyperemia
37
what is the brand name for tafluprost?
Zioptan
38
which prostaglandin is the only non-preserved IOP lowering agent?
Zioptan
39
what is the brand name for bimatoprost?
Lumigan
40
Lumigan is formulated with what as a buffer? what preservative is used?
- citrate phosphate buffer
| - BAK preservative
41
which prostaglandin is indicated as the primary therapy for IOP reduction in open-angle glaucoma & ocular hypertension?
Lumigan
42
Lumigan is formulated as what percent solution?
0.01%
43
what is the brand name when bimatoprost is formulated as 0.03% solution? what does it treat?
Latisse → treats hypertrichosis of eyelashes
44
these ocular side effects are from which class of glaucoma medications?
- increased eyelid pigmentation
- iris color darkening
- conjunctival hyperemia
- allergic reaction
- punctate corneal erosions
- corneal pseudodendrites
- anterior uveitis
- cystoid macular edema
- pruritis
prostaglandins
45
which prostaglandin has the greater chance of causing conjunctival hypermia?
Lumigan (bimatoprost)
46
what are the contraindications of prostaglandins?
- history of uveitis or prior incisional ocular surgery
| - previous episodes of herpes simplex keratitis
47
prostaglandins should be used cautiously after cataract surgery in patients with a high risk factor of primarily developing what?
cystoid macular edema (CME)
48
beta-blockers have what colored bottle caps?
yellow, sometimes blue
49
name the non-cardioselective beta-blockers
- timolol
- levobunolol
- metipranolol
- carteolol
50
name the selective beta-blockers
- betaxolol
51
which beta-blocker is most commonly used?
timolol
52
which beta blocker comes as a suspension?
betaxolol
53
which beta-blocker has intrinsic sympathomimetic activity (ISA)?
carteolol
54
beta-1 receptors are involved with?
cardiac rate, rhythm & force
55
beta-2 receptors are involved in what?
pulmonary function
56
what is the MOA of beta-blockers?
block beta-2 receptors on the postsynaptic neuron at the ciliary body epithelium → prevents production of aqueous fluid
57
which glaucoma medication is the second most commonly used to treat glaucoma?
timolol
58
what percentage of IOP lowering effects does timolol have?
~25%
59
which glaucoma medication is known to have relatively rapid development of tolerance? what is this referred as?
timolol → "escape"
60
what else has also been described in timolol besides "escape"?
long-term "drift"/drug tolerance
61
what is the dosing for timolol?
BID or QD
62
when dosing timolol QD, when is the best time to instill the drops?
in the morning
63
IOP lowering effects of timolol are additive to what therapies?
- outflow agents (eg, pilocarpine)
| - inflow agents (eg, CAIs & alpha-agonists)
64
why are beta-blockers not as effective during the night?
supine position causes 50% reduction of aqueous when we sleep
65
along with prostaglandins, what is the most effective ocular hypotensive agent in patients with POAG & ocular hypertension?
timolol
66
which glaucoma medication is used as a prophylactic after laser iridotomy, posterior subcapsulotomy & cataract surgery?
timolol
67
in Timoptic XE, what type of vehicle is in the formulation? what is the name of the vehicle?
Gelrite → viscosity agent
68
Isatol is formulated with potassium sorbate, what does it do?
increases lipophilicity
69
which formulation of timolol maleate is preservative free?
Timoptic Ocudose
70
which beta-blocker is metabolized by dihydrobunolol?
levobunolol
71
what is the primary mechanism of levobunolol?
decrease in production of aqueous humor
72
levobunolol contains which viscosity agent & which preservative?
- viscosity agent → polyvinyl alcohol
| - preservative → BAK
73
what is the dosing for levobunolol?
QD
74
which beta-blocker is metabolized by des-acetyl-metipranolol
metipranolol
75
what increases during treatment with topical metipranolol?
retinal perfusion pressure & blood flow
76
what is the primary metabolite of carteolol?
8-hydroxycarteolol
77
because carteolol possesses intrinsic sympathomimetic activity, it may be used in patients with glaucoma coexisting with what condition?
pulmonary disease
78
which glaucoma medication is used for chronic treatment of elevated IOP in patients with ocular hypertension & open-angle glaucoma?
carteolol
79
which beta-blocker is less effective than levobunolol or timolol?
betaxolol
80
betaxolol has the ability to block what & where? what does it suggest?
sodium & calcium channels in vascular tissue & retinal ganglion cells → suggests that it may have potential as a neuroprotective agent
81
what allows betaxolol to be used successfully in patients with coexisting glaucoma & pulmonary disease?
its relative cardioselectivity
82
what is betaxolol formulated with what that is believed to increase drug residence time in the eye?
- polyacrylic polymer
| - cationic exchange resin
83
what are the cardiovascular side effects of beta-blockers
- bradycardia
- exercise induced tachycardia
- conduction arrhythmias
- hypotension
- Raynaud's phenomenon
84
which class of glaucoma medications have these pulmonary side effects?
- average decrease of 25% in FEV1 in patients w/ COPD
- bronchoconstriction/bronchospasm
- asthma
- dyspnea
beta-blockers
85
why do beta-blockers have CNS side effects?
less blood throughout the body
86
what gastrointestinal side effects do beta-blockers have?
- diarrhea
| - nausea
87
what ocular side effects do beta-blockers have?
- allergic blepharoconjunctivitis
- dry eye/decreased TBUT
- corneal anesthesia
- macular edema (aphakics)
- macular hemorrhage/retinal detachment
- uveitis
- cataract progression
88
what systemic side effect do beta-blockers have?
masking of hypoglycemia
89
beta-blockers are contraindicated in patients with?
- bronchial asthma or history of it
- severe chronic obstructive pulmonary disease (COPD)
- bradycardia
- severe heart block
- cardiac failure
- caution in patients w/ diabetes
- children & infants
90
beta-adrenoreceptor blockage may mask signs & symptoms of what condition(s)?
- thyrotoxicosis
| - acute hypoglycemia
91
in beta-blockers, which drug(s) should you avoid for best IOP control?
betaxolol
92
when cost is an issue, which beta-blocker(s) are preferred?
- generic timolol
- metipranolol
- carteolol
93
when comfort is an issue, which beta-blocker(s) is preferred?
carteolol
94
when hypercholesterolemia is an issue, which beta-blocker(s) is preferred?
carteolol
95
when preservative (BAK) allergy is an issue, which beta-blocker(s) is preferred?
- Timoptic XE
- Timoptic GFS
- Timoptic Ocudose
96
when COPD is an issue, which beta-blocker(s) is preferred?
- betaxolol
| - carteolol
97
when pregnancy is an issue, which beta-blocker(s) is preferred?
avoid all (category C)
98
adrenergic agonists have what color bottle cap?
purple
99
what drugs are classified as adrenergic agonists?
- apraclonidine
| - brimonidine
100
what is the brand name for apraclonidine?
Iopidine
101
what is the brand name for brimonidine?
Alphagan P
102
alpha receptors have been identified where in relative to sympathetic nerve activity?
on presynaptic nerve terminals & post-junctionally in ciliary body
103
activation of the presynaptic alpha-2 receptors does what?
inhibits neurotransmitter release → causes decrease in norepinephrine
104
activation of postsynaptic ciliary body alpha-2 receptors does what?
reduces intracellular levels of cyclic adenosine monophosphate (cAMP)
105
in relation to glaucoma, what may be mediated via alpha-2 receptor activity?
reduced aqueous production
106
which adrenergic agonist is a selective alpha-2 receptor agonist?
apraclonidine
107
generic brimonidine is preserved with what?
BAK
108
Alphagan P is formulated with what preservative? what does it do?
Purite → disappears when it encounters light
109
which adrenergic agonist is 30x more selective for alpha-2 receptors?
Alphagan-P
110
at the post-junction ciliary body, stimulation of beta-2 does what?
increases aqueous production
111
at the post-junction ciliary body, stimulation of alpha-2 does what?
decreases aqueous production
112
at the post-junction of the iris dilator muscle, how does apraclonidine cause dilation?
it is more alpha-2 selective but still binds to alpha-1 on the postsynaptic iris dilator muscle
113
at the post-junction iris dilator muscle, how does brimonidine prevent dilation?
it is way more alpha-2 selective vs alpha-1 → preventing release of NE → prevents binding to alpha-1 receptors on iris dilator muscle
114
what is the primary MOA of Iopidine & Alphagan P?
- both lower IOP by decreasing aqueous production
| - brimonidine also increases aqueous outflow via uveoscleral pathway
115
apraclonidine (Iopidine) has additional ocular hypotensive effects by?
influencing ocular blood flow
116
how does apraclonidine affect vascular tone?
- may also stimulate alpha-1 receptors in vascular smooth muscle → causing vasoconstriction
117
what is the dosing of apraclonidine (Iopidine)?
TID x 3 months
118
1.0% apraclonidine is indicated for?
controlling/preventing postsurgical IOP elevations after ant seg laser surgery & short-term IOP control of open-angle glaucoma before filtering procedures
119
which glaucoma medication is used to lower IOP in initial treatment of an acute angle closure glaucoma?
apraclonidine
120
apraclonidine 1.0% has also been used for what?
prophylaxis of postercyclopledgic spikes in IOP
121
are apraclonidine & brimonidone used as monotherapy or as an additive?
additive
122
brimonidine may be used to improve vision function under what condition in which patients?
under scotopic conditions in patients who had refractive surgery
123
what is the most common ocular side effects of adrenergic agonists?
conjunctival blanching
124
apraclonidine has a 40% rate of causing what ocular side effect?
contact dermatitis
125
what are the systemic (dose-related) side effects of adrenergic agonists?
- dry mouth
- dry nose
- tachyphylaxis
- shortness of breath
126
what CNS side effects do alpha adrenergic agonists have?
- fatigue
- lethargy
- headache
127
adrenergic agonists are contraindicated in patients taking what medication?
MAOIs
128
adrenergic agonists should be cautioned in patients with what condition?
severe cardiovascular disease (ie, HTN)
129
adrenergic agonists should be cautioned/avoided in which age group?
young children, especially those weighing < 20 kg & those younger than 6 y/o
130
what pregnancy category is brimonidine? apraclonidine?
- brimonidine → category B
| - apraclonidine → category C
131
carbonic anhydrase inhibitors (CAIs) have what bottle cap color?
orange
132
what are the oral carbonic anhydrase inhibitors?
- acetazolamide (Diamox)
| - methazolamide (Neptazene)
133
what are the topical carbonic anhydrase inhibitors?
- dorzolamide (Trusopt)
| - brinzolamide (Azopt)
134
formation of what is an essential component of aqueous production?
bicarbonate
135
carbonic anhydrase is found in which anterior segment structure?
ciliary processes
136
production of what in where plays a key role in aqueous humor formation?
production of bicarbonate in ciliary epithelium
137
what is the MOA for carbonic anhydrase inhibitors?
inhibits production of bicarbonate & acts on decreasing sodium entry into posterior chamber by decreasing fluid movement across nonpigmented ciliary epithelium → resulting in a decrease of aqueous production & IOP (aqueous suppressant)
138
which carbonic anhydrase inhibitor is given in angle-closure attacks? in what dose?
acetazolamide → 125 & 250mg tablets
139
which carbonic anhydrase inhibitor comes as a suspension?
brinzolamide
140
Cosopt is a combination of which glaucoma medications? what drug class do each belong to?
dorzolamide (CAI) + timolol (beta-blocker)
141
which carbonic anhydrase inhibitor is the most widely used & orally administered?
acetazolamide
142
what is the dosing for acetazolamide (Diamox)?
- 250 mg q6h
| - 500 mg sustained release capsule BID
143
why do you need relatively large doses of acetazolamide to produce a signoficant plasma level of unbound drug?
majority of it binds to plasma proteins in the blood
144
why should you be cautious of giving acetazolamide to patients with kidney issues?
drug is not metabolized → it is excreted by the kidneys
145
why is acetazolamide often reserved for short-term use?
significant adverse reactions
146
which glaucoma medication may also produce a partial/complete resolution of macular edema in patients w/ CME, retinitis pigmentosa & chronic intermediate uveitis (pars plantis)? why?
acetazolamide → diuretic
147
is acetazolamide or methazolamide more potent?
methazolamide
148
does acetazolamide or methazolamide have higher lipid & water solubilities?
methazolamide
149
is acetazolamide or methazolamide less toxic to the kidneys?
methazolamide
150
what is the dosing for methazolamide (Neptazane)
25-100 mg TID
151
which carbonic anhydrase inhibitor do many authorities believe should be the first to be used for glaucoma therapy?
methazolamide
152
these common systemic side effects are for which glaucoma medications?
- numbness & tingling of extremities & perioral region
- metallic taste
- GI irritation
- metabolic acidosis
oral carbonic anhydrase inhibitors
153
what are the two main uncommon systemic side effects of oral CAIs?
- hypokalemia
| - aplastic anemia
154
what are the ocular side effects of oral CAIs?
transient myopia
155
carbonic anhydrase inhibitors should be avoided in patients with a known hypersensitivity to what?
sulfonamides
156
oral CAIs are contraindicated in patients with what conditions?
- clinically significant liver disease
- renal disease
- severe COPD
- certain secondary glaucomas
157
topical CAIs alter aqueous humor composition by?
- lowering pH
- decreasing bicarbonate levels
- increasing posterior chamber ascorbate levels limited to the eye receiving dose
158
what allows dorzolamide to have increased corneal & scleral penetration?
addition of an alkyl amino group enhances lipid & water solubility of the drug
159
when dorzolamide is used as a monotherapy, what is the usual dosing?
1 gtt TID
160
how does dorzolamide lower IOP?
decreasing aqueous humor secretion & production
161
dorzolamide has an additive effect when used in conjunction with which glaucoma medication? which class is it in?
timolol → beta-blocker
162
the use of dorzolamide prevents IOP spikes after undergoing what?
- YAG laser
- argon laser trabeculoplasty
- laser iridotomy
163
which topical CAI is a suspension that has high affinity for carbonic anhydrase II isoenzymes?
brinzolamide
164
what is the dosing for brinzolamide?
BID/TID
165
which topical CAI doesn't sting as much upon instillation? why?
brinzolamide → pH is closer to our eye's pH
166
what is the primary ocular side effect of topical CAIs?
stinging
167
what systemic side effects do oral CAIs have?
bitter taste
168
topical CAIs are contraindicated in patients with what conditions?
- allergy to sulfonamides
- caution in patients with severe renal & hepatic impairment
- avoid in patients taking oral CAIs
169
cholinergic agonists are also known as?
- miotics
- parasympathomimetics
- cholinomimetics
170
how are cholinergic agonists classified?
- direct-acting
| - indirect-acting
171
what is the MOA for direct-acting cholinergic agonists?
activate cholinergic receptors at the neuroeffector junctions of iris sphincter muscle & ciliary muscle
172
what is the MOA for indirect-acting cholinergic agonists?
inhibit cholinesterase → increases amount of acetylcholine at the cholinergic receptors
173
what is the only formulation of cholinergic agonists still used today?
pilocarpine
174
what color bottle caps do cholinergic agonists have?
green
175
which type of glaucoma are cholinergic agonists used to treat?
open angle glaucoma
176
what is the MOA of cholinergic agonists for treating open angle glaucoma?
contraction of longitudinal fibers of the ciliary muscles inserted into the scleral spur → opens up trabecular pores → increased drainage
177
is pilocarpine direct-acting or indirect-acting?
direct acting
178
the cholinomimetic action of pilocarpine on smooth muscle muscarinic receptors results in what?
contraction
179
what are the intraocular smooth muscle response with pilocarpine?
- pupillary constriction
- spasm of accommodation
- reduction of IOP
180
what affects pilocarpine's ocular hypotensive response?
ocular pigmentation
181
long-term therapy with pilocarpine may cause what? how?
permanent miosis → loss of iris radial muscle tone & from fibrosis of the sphincter muscle
182
what is the usual dosage of pilocarpine?
QID
183
pilocarpine is indicated to treat which type of glaucoma?
acute angle-closure glaucoma
184
what is administered before pilocarpine in an acute angle-closure attack?
- apraclonidine
| - beta-blockers
185
pilocarpine is also useful for which surgery? why?
laser iridotomy → to facilitate stretching of iris
186
which types of glaucomas is pilocarpine contraindicated in?
- neovascular
| - uveitic
187
what color bottle caps do rho-kinase inhibitors have?
white
188
although netarsudil (Rhopressa) is a triple action ROCK/NET inhibitor, what is it's primary action?
improves TM outflow & lowers episcleral venous presure
189
Rhopressa is indicated to lower IOP in which types of glaucoma?
open-angle glaucoma & ocular hypertension
190
what is the recommended dosage of Rhopressa?
1 gtt QHS
191
what is the most common side effect of Rhopressa?
conjunctival hyperemia
192
what is the novel prostaglandin? what is its brand name? what color is the bottle cap?
latanoprost bunod (Vyzulta) → teal
193
what is the MOA for Vyzulta?
- latanoprost acid targets uveoscleral pathway
| - nitric oxide targets trabecular meshwork
194
how does Vyzulta affect the uveoscleral pathway?
widens the space to increase outflow
195
how does Vyzulta affect the trabecular meshwork?
relaxes the trabecular meshwork to increase outflow
