Glaucoma Drugs

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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
 receptorsàheart
 
o
Block
 =
 decrease
 cardiac
 contractibility
 

B2
 receptorsàlung,
 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
 

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