Glaucoma Drugs
Comments
Content
Prostaglandin
Analogs
Alpha-‐Adrenergic
Agonists
MOA:
increase
uveoscleral
outflow
(although
some
trabecular
outflow
has
been
shown.
o
Prodrug
o
Lantaoprost
converts
to
Latanoprost
acid
and
binds
to
FP
receptor,
upregulating
MMP
to
degrade
collagen
to
increase
uveoscleral
outflow
•
Drugs
o
Xalatn
o
Travatan
o
Zioptan
o
Classes
§
Ester
based
–
needs
less
concentration
b/c
our
body
can
break
it
down
•
Xalatan
•
Zioptan
•
Travatan
Z
o
Maintained
reduced
IOP
up
to
84
hours
of
no
drops
§
Amide
based
•
Lumigan
IOP
reduction
Dose
Onset
of
action
Class
Notes
Latanoprost
30%
q.day
12
hours
Ester
(Xalatan)
2
weeks
for
full
effect
Tafluprost
25-‐30%
1
QHS
4-‐6
hours
Ester
-‐Consider
for
(Zioptan)
12
hours
for
full
eff.
dry
eye/ocular
pt.
disease
Travoprost
30%
1
QHS
-‐-‐
Ester
-‐Travatan
Z
(Travatan
Z)
has
no
BAK
-‐Better
for
AA
patients
(4x
better)
Bimatoprost
30%
1
QHS
-‐-‐
Amide
(Lumigan)
Side
effects
•
Hyperemia
•
Skin
pigmentation
•
Eyelash
changes
•
Inflammatory
o
Iritis,
CME
(already
inflamed
so
can
make
it
worse)
•
Macular
edema
o
Aphakic
patients
o
Pseudophakic
w/
torn
lens
capsules
•
Burning
–
from
SPEE/SPK?
o
Less
w/
esters
•
Some
reactivation
of
HSV
•
PAP
o
Prostaglandin-‐associated
Periorbitopathy
§
Deepening
of
superior
sulcus
§
Ptosis
§
Enophthalmos
•
•
MOA:
o
•
o
2
types
o
o
•
Sympathomimetics:
Decreases
aqueous
production
and
increases
outflow
§
Binds
to
presynaptic
receptor
to
inhibit
NE
release
§
Binds
to
postsynaptic
receptor
(on
CB)
to
decrease
cAMP
levels,
reducing
aqueous
production
Sympatholytics:
Decreases
aqueous
production
Alpha
agonists
&
B:
stimulates
a
lot
of
things!
§
Epinephrine
(Epifrin)
§
Dipivefrin
(Propine)
Alpha
only
§
Apraclonidine
•
a2>>a1
§
Brimonidine
•
a2
only
Classic
o
Ocular
SE
§
Burning
§
Allergy
•
Biggest
side
effect
of
alpha
agonists
§
Mydriasis
§
Red
eyes
•
Initial
blanching
but
rebounds
o
Systemic
SE
§
HA,
palpitations,
tachycardia,
HTN
crisis
IOP
Dosing
Concentrations
SE
reduction
Apraclonidine
20-‐25%
TID
0.5%
&
1.0%
-‐Tachyphylaxis
(Iopidine)
-‐High
rates
of
allergies
(20%)
Brimonidine
(Alphagan-‐P)
20-‐30%
TID
vs.
BID
0.15%
&
0.1%
Combigan
BID
Tim:
0.5%
(Timolol
&
Brim:
0.2%
Brimonidine)
Sibrinza
BID
Brim:
0.2%
(Brim
&
Brin:
1%
Brinzolamide)
Cosopt:
Timolol
&
Dorzolamide
•
Not
used
often
due
to
increased
irriations
Alpha
2
agonist
SE
•
SE
o
Dry
mouth
&
nose
o
Decrease
in
systolic
BP
o
Lethargy
•
Contraindications
o
Use
of
MAOI
(HTN
crisis)
-‐Allergies
(5-‐10%)
-‐Red
lids
-‐Eyelid
retraction
Notes
-‐Horner’s
Dx
-‐Pre/post-‐op
pressure
spikes
-‐Acute
glu.
Control
-‐P=purite,
better
preservative
-‐Chronic
tx
-‐Good
miotic
for
CRT
or
refractive
Sx
-‐PAOG
-‐Fewer
allergies
than
Alphagan
Miotics
CAI’s
MOA:
causes
contraction
of
ciliary
muscles,
causing
scleral
spur
to
widen
trabecular
spaces,
increasing
aqueous
outflow
Drug:
Pilocarpine
•
Direct
acting
cholinergic
agonist
Uses
•
Acute
angle
closer
glaucoma
o
If
IOP
is
higher
than
60mmHg,
use
something
else
to
lower
pressure
first
•
Secondary
glaucoma
o
Pigmentary
glaucoma
•
PAOG
(rare!)
Pilocarpine
•
15-‐25%
decrease
in
IOP
•
Better
in
blue
eyes
•
Q4h
•
Max
effect
in
only
a
few
days
•
Gel
increases
compliance
b/c
QHS
•
Ocusert
o
Q7D
o
Inserted
into
eye
during
bed
time
o
Constant
drug
delivery
§
Membrane
placed
to
control
drug
toxicity
Ocular
SE
•
Miosis
•
Accommodative
spasm
à
blur
o
Don’t
Rx
for
pts.
under
40
•
Breakdown
of
blood
aqueous
barrier
o
Don’t
use
w/
anterior
uveitis!
(will
bring
in
more
inflammatory
cells)
•
Brow
ache
initially
•
SLUDE
(rare)
o
Salivation,
lacrimation,
urination,
defecation,
emesis
•
Bradycardia,
cardiac
arrhythmia,
pulmonary
edema
Contraindications
•
<40
yo
•
Cataracts
(Nuclear,
PSC)
•
Neovascular
and
uveitic
glaucoma
•
High
Myopia,
Aphakia
•
Narrow
angleà
4%
or
greater
can
cause
angle
closure
•
Severe
asthma
MOA:
inhibits
carbonic
anhydrase
and
decreasing
aqueous
formation
Topicals:
Tx
of
POAG
&
OHTN
•
Trusopt
(Dorzolamide)
•
Azopt
(Brinzolamide)
•
Cosopt
(Dorzolamide
&
Timolol)
•
Cosopt
PF
(not
available
in
generic)
•
Simbrinza
(Brinzolamide
&
Brimonidine)
(not
available
in
generic
either)
IOP
reduction
Dosing
SE
Notes
Dorzolamide
20-‐25%
TID
(Trusopt)
BID
(combo)
Brinzolamide
15-‐20%
TID
Fewer
-‐Suspension
(Azopt)
BID
(combo)
-‐More
comfortable
than
Trusopt
Cosopt
27%
BID
-‐Avail.
As
preservative
free
(Dorzolamide
&
Timolol)
st
Simbrinza
21-‐35%
TID
-‐1
drug
that
doesn’t
contain
(Brinzolamide
&
timolol
Brimonidine)
•
Additive
effect
with
PgA’s
–
great
add
on
when
PgA’s
are
inadequate
•
CAIs
reduce
nocturnal
IOP
in
contrast
to
B
blockers
Tx
options:
•
Qday:
Timoptic(Timolol)
AM
or
PgA
PM
•
BID
o
Timoptic
AM
&
PgA
PM
o
Azopt
AM
&
PgA
&
Azopt
PM
o
Cosopt
AM
&
PgA
&
Cosopt
PM
Topical
CAIs
SE
Topical
Contraindications
•
Blur
•
Renal
Failure
•
Allergic
Rxn
•
Hepatic
Failure
•
Irreversible
corneal
edema
in
•
Sulfa
allergies
compromised
edema
•
Burning
and
stinging
•
Concurrent
use
w/
Oral
CAIs
•
SPK,
Tearing,
Dryness,
Photophobia
•
All
CAIs
are
sulfonamides!
Oral
CAIs:
for
acute
closure
glaucoma,
secondary
glaucoma
IOP
decrease
Dosing
Indications
Notes
Acetazolamide
40-‐50%
-‐(2)
250mg
tablets
-‐ACG
(Diamox)
-‐500mg
ER
capsules
-‐Preoperative
-‐CME/macular
edema
-‐Pseudo
tumor
Methazolamide
3-‐6mmHg
-‐25-‐100mg
q8h
Same
-‐Less
effective
than
decrease
acetazolamide
Hyperosmotics
Beta
Blockers
MOA:
rapid
reduction
of
elevated
IOP
in
emergencies
•
Acute
angle
closure
•
Sulfa
allergy
Orals
Dosage
SE
Glycerin
-‐30
mins
for
onset
-‐Nausea/vomit
(Osmoglyn)
of
action
-‐Diuresis,
-‐Max
effect:
1-‐
dehydration
1.5hr
-‐HA/Confusion
-‐CHF
-‐Renal
failure
-‐Pulmonary
edema
IV
Mannitol
IV
Same
as
above
MOA:
blocking
B
adrenergic
receptors
to
decrease
aqueous
production
•
B1
receptorsàheart
o
Block
=
decrease
cardiac
contractibility
•
B2
receptorsàlung,
liver,
eye
o
Block
=
inhibit
bronchodilation
o
Block
=
mask
symptoms
of
hypoglycemia
Effectiveness
•
More
effective
in
AM
due
to
increased
aqueous
production
IOP
Dosage
SE
reduction
Timolol
0.25%
(blue)
Short:
reduction
in
IOP
(Timoptic)
or
0.5%
Long:
increase
in
IOP
(yellow)
(after
3
mos)
Timolol
0.25%
or
Hemihydrate
0.5%
(Betimol)
Timolol
0.5%
Maleate
(Istalol)
Betaxolol
0.25%
(Betoptic
S)
Urea
IV
Same
as
above
Topical
NaCl
-‐2%-‐5%
solution
(1-‐2
drops/q3-‐4h)
-‐5%
ointment
(q3-‐
4h,
nighttime
use)
-‐Stinging
-‐Burning
-‐Irritation
Notes
-‐Caution
w/
DM
(metabolized
into
glucose)
-‐Safe
for
diabetics!
Not
safe
for
diabetics
-‐Decreases
corneal
edema
Contraindications
-‐Severe
dehydration
-‐Heart,
renal
or
PE
-‐Diabetes
-‐ointment
is
PF
Carteolol
(Ocupress)
Ocular
SE:
•
Mild
stinging,
burning
•
Redness
•
Rare
allergies
•
Corneal
hypoaesthesia
Systemic
SE:
•
Bradycardia
•
Hypotension
•
Fatigue
•
Bronchospasm
•
Depression
Can
reduce
anxiety
before
performances!!
Notes
-‐Gold
standard
-‐less
cost
-‐Brand
name,
consistent
results
-‐Potassium
sorbate
to
increase
penetration
-‐
B1
selective
-‐Less
respiratory
than
other
but
be
cautious
of
asthmats
-‐Increases
VF
-‐Less
SE
of
depression
(doesn’t
cross
BBB)
-‐less
neg
effect
on
cholesterol
Sponsor Documents