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

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
-Horners 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

CAIs

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 blur

o
Dont Rx for pts. under 40

Breakdown of blood aqueous barrier

o
Dont 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 angle 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 doesnt contain
(Brinzolamide &
timolol
Brimonidine)

Additive effect with PgAs great add on when PgAs 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 receptorsheart
o
Block = decrease cardiac contractibility

B2 receptorslung, 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
(doesnt cross BBB)
-less neg effect on
cholesterol