Glaucoma Therapy Part I (Beta Blockers, Cholinergic Agonist, Adrenergic Agonists)

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aliciaekim  on April 8, 2012

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Glaucoma Therapy Part I (Beta Blockers, Cholinergic Agonist, Adrenergic Agonists)

What creates Aqueous Humor in the eye?
Ciliary body
-Cell membrane of NONPIGMENTED Ciliary epithelium contain (Alpha and beta (mainly beta-2) adrenoreceptors, Carbonic Anhydrase, Sodium and Potassium activated ATPases)
1/23
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What creates Aqueous Humor in the eye? Ciliary body
-Cell membrane of NONPIGMENTED Ciliary epithelium contain (Alpha and beta (mainly beta-2) adrenoreceptors, Carbonic Anhydrase, Sodium and Potassium activated ATPases)
Where is the aqueous drained? 80% TM, 20% Uveoscleral Flow (interstitial space btw ciliary muscle and iris root)
Vascular theory of GL? High IOP induce ischemia in prelaminar ONH> retinal ganglion cell death and axon loss
Mechanical Theory Compression of axons at ONH> impedes axoplasm flow > apoptosis of ganglion cells.
What vehicle would be beneficial in GL meds? Hydroxypropylmethylcellulose or Polyvinyl Alcohol
-Prolongs contact time
-Better penetration, less frequency dosaging, and less adverse effects
*Gels, Susp, Ocular inserts
Ocular Hypotensive Agents -Beta Blockers, Cholinergic Agonist, Adrenergic Agonits, Carbonic Anhydrase Inhibitors, PG Family, Hyperosmotic Agents
Beta Blockers *ISA: Exert some "Intrinsic Sympathomimetic Activity", thus although blocking, results in still slight stimulation of beta receptors.
-Nonselective, DECREASE IOP by 25%
-Dosage QD
*BEST TIME IS IN THE MORNING!
ADR to Beta Blockers Lethargy, weakness, Bronchospasm, Reduced pulmonary capacity, Confusion, Decreased libido, Anxiety, Depression, BC, Elevated Cholesterol levels, depression
*Even thought these drugs are topical, take them seriously!
Absolute contraindications with taking Beta Blockers 1) Asthma or hyper-reactive airway disease
2) Decompensated Congestive Heart Failure
3) Symptomatic Bradycardia or heart block
4) History of Fainting
Relative Contraindications 1) Asymptomatic Bradycardia
2) Prefainting symptoms
3) Carotid Sinus hypersensitivity
4) Severe Mental Depression
5) Children and Infants
Systemic Beta Blockers May lower IOP
Examples: ANMP, Metoprolol
TimololBeta Blocker//0.25% and 0.50%. Relatively equivalent. (baby blue vs tan)
*Maleate salt (more common) or Hemihydrate salt
Common preservative: Benzalkonium Chloride vs.
Timoptic XE: Benzododecinium Bromide
**Nonselective beta blocker
**Decreases aqueous production and does not inhibit aqueous flow during sleep!
Decreases IOP by 30% ,No ISA, *QD, BID
*Use: Primary and SEcondary GL. Also prophylactiv after Laser Iridotomy, capsulotomy, and CT surgery
-used in combo and could be taken with safety with oral version.
**Less EFFECT ON HR -> Gelrite Vechicle and Hemihydrate QD
Timoptic GFS Gel forming Beta Blocker, Timolol
Nonpreservative Timolol? Timoptic in Ocudose
Consensual Effect Unique to Timolol
"when the other eye is affected by the drug without the usage of the drops on that eye"
Escape Unique to Timolol
"Initial dramatic decrease> then a slight rise yet still better than s tx> plateau"
Rapid: days to few weeks
Acute vs Chronic Use
Drift Unique to Timolol
-Long term Effect (months to years of tx)
-Slow rise in IOP and unsure why it occurs> require additional tx> usually change/switch B-blocker then maybe come back to timolol
Other factors: change in disease state, noncompliance
~ 4 year study: 15% failure per year
Tachyphylaxis Rapid and substantial loss of efficacy during first few doses
Short Term escape -Not that rapid nor a substantial loss
-After days to several weeks, IOP is not to pretreatment level, but stable with approximately 25% decrease from pretreatment level
Wash out period Beta Blocker: Timolol
-Significant ocular hypotensive effect up to 2 weeks after d/c > done to determine pressure OFF the drug or figure out the baseline pressures
-Takes longer for dark irises but usually takes only a couple of days since there is still residual drugs
~ Similar for levobunolol
Ocular ADR to Timolol Allergic REaction, stinging, corneal anesthesia (low amont B-blockers), SPK, Dry eye sx
Systemic ADR to Timolol ***1) Cardiovascular: BC, Conduction arrhythmia, Hypotension, *Raynaud's phenomenon (when cold temp or strong emotions BLOCK blood flow to extremities, Fluid retention)
2) Pulmonary: Bronchoconstriction/bronchospasm, asthma, Dyspnea
3) CNS: Depression, Lethargy, weakness, fatigue, lightheadness, Amnesia, Confusion, HA, Migraine prophylaxis, Impotence, Insomnia, Hallucinations
4) GI: Diarrhea, Nausea
5) Others: Hypoglycemia
LevobunololBeta Blocker
-Non Cardioselective Beta 1 and 2 blockade
**Decrease in production in aqueous humor
*Dosage QD and BID, Better drug to take QD than timolol since it has a longer 1/2 life***
-No ISA or local anesthetic activity
-Metabolized by dihydrobunolol
-Preservative: Benzalkonium Chloride 0.004%
*Ditto with Timolol but has the C-Cap (tells how many drops they took)

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