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120 Cards in this Set

  • Front
  • Back
what is the only drug that works on the TM?
Trabodenson (the pores in the TM get bigger)
Prostaglandin analogues-Eicosanoids what are they?
Prostaglandin analogues-Eicosanoids-are a family of lipids made by cell membranes.
-Thromboxanes, prostaglandins, leukotrienes. Locally synthesized.
Produce effects via interaction with specific membrane bound receptors.
Involved in many bio. systems-iop, BP ,etc.
-Are rapidly metabolized after synthesis.
Ocular actions of ecosanoids?
Ocular actions of ecosanoids?
Prostaglandins-sensitize pain receptors, cause miosis, dilate vessels, raise and lower IOPS
Ocular prostaglandin analogs?
1. Latanaprost (Xalatan)
2. Travaprost (Travatan)
3. Bimataprost (Lumigan)
4. Unoprostone isopropyl (Rescula)-no longer made
5. Tafluprost (Zioptan)
MOA of prostaglandins?
MOA of prostaglandins?
-prodrugs that require hydrolysis of corneal enzymes to become active free drugs (free acids)
-free drug binds to receptors on CB
-activation of these FP receptors up-regulates MMPs that degrade extracellular proteins in the Uveoscleral pathway (MMP's basically make the uveoslercal path leaky)
-thus inc in Uveoscleral ouflow and iop down
**these drugs also enhance TM outlfow
1. MOA of prostaglandins?
2. CAI?
1. prostaglandins-INC uveoscleral path outflow (and also TM outflow)
2.CAI- reduced aq. production
first prostaglandin analog approved as a first ling glauc drug?
Latanaprost (xalatan)
**needs to be fridged and away from light; can store up to 6 weeks once opened
**more efficacous than Timilol
*additive with BB, CAI, alphas
Latanaprost (xalatan) ocular side effects?
*note-are no significant systemic effects
Latanaprost (xalatan) ocular side effects?
-mild conj hyperemia and PEK
-inc Iris pigment (may not reverse)
-darkening of periorbital skin
-inc eyelash number and length (can reverse)
(les common also mac edema and ant uveitis)
Travaprost 1st or 2nd line?
Travaprost-FDA 2nd line, but OLabel 1st line. similar side effects to latanaprost and sim IOP lowering etc.
a synthetic prostamide made by allergan? FDA approved 2nd line drug?
a synthetic prostamide made by allergan? FDA approved 2nd line drug?
Bimataprost (lumigan)
inc uveoslceral and tm OUTflow
Newest available prostaglandin-a flourinated analog of prostaglandin F2alpha
Tafluprost (Zioptan)
-indicated for open angle glaucoma or Ocular HTN
-comes in cartons of 30
-mech same as other prostags.
CAI-moa?
CAI-moa?
-reduced bicarbonate production results in reduced aqueous production
-can be oral or IV
ORAL/IV CAI'S?
ORAL CAI'S?
1. ACETAZOLAMIDE (Diamox) (ONLY iv/ORAL-ALL OTHER ORAL)
2.Methazolamide (Neptazane)
3. Dichlorphenamide (Daranide)
4. Ethoxzolamide (Cardrase)
topical CAI's?
topical CAIs'
1.Dorzolamide (Trusopt)
2. Brinzolamide (Azopt)
Which CAI can be taken IV oral and is the most commonly used CAI?
Acetazolamide
*only take IV when can't take oral
Acetazolamide uses?
Acetazolamide-uses
-break attack of AACG (acute angle clos. glauc)
-CSOAG
-MACULAR EDEMA
Acetazolamide COMMONLY HAS SYSTEMIC SIDE EFFECTS-LIST some
Acetazolamide SE's
numbess and tingling of fingers
metallic taste in mouth
despression, fatgue, weight loss, dec labido, GI irritation, acidosis, hypokalemia, renal calculi, blood dyscrasis
Acetazolamide ocular side effects?
Acetazolamide oc SE
*transient myopic shift (from edema of CB)
Acetazolamide contraindications?
Acetazolamide CIs?
**sulfa allergy or sensitity (sulfonimide)
-impaired renal
-if taking potassium depleting diuretics
-liver probs, sickle cell anemia, COPD, bladder surgery, etc
**can also have drug interactions with amphetamine, quinidine, and tricyclic antidepressants
What CAI has lower does than Diamox, less protein binding, higher ocular penetration, longer plasma half life, and less acidosis?
Methazolamide
cai-Dorzolamide mOA?

USES?

**can come as trusopt or cospot
cai-Dorzolamide mOA?
INHIBITS CA isoenzymes II, SLOWING PRODUCTION OF BICARBONATE IONS TO THE cb
*For pts with 23+IOP, reduced 3-5
-can reach systemic circulation, but NO significant effects on kidney function

**used for ocHTN and CSOAG
-AVAILABLE in single drug (Trupsot) or combo (Cosopt)
Dorzolamide ADR?
Dorzolamide ADR?
Mild oc irritation, SPK, allergy, transient myopia, photophobia, iridocyclitis, bitter taste, HA, nausea, fatigue, allergy, **sulfa drug alergy
*stevens johnson syndrome (disorder of mucus membranes and transient myopia
Dorzolamide CONTRAindications?
Dorzolamide CONTRAindications?
-impaired renal
-sens/allergy to sulfa
-pregnancy**
Brinzolamide(Azopt)--what must you do before use?

similar to what drug?
shake Brinzolamide!

similar to trupost (adr, contra's, uses, MOA)

*excreted by kidney, no significant effects on kidney in healthy adults
What are the indications for hyperosmotic therapy and routes of administration?
What are the indications for hyperosmotic therapy and routes of administration?
INDIC: Glaucoma and intraocular surgery
Route of admin: oral and IV
moa: osmotic gradient between plasma and aqueous determined by the abiliy of the drg to pass through the blood aqqeous barrier
MOA for hyperosmotic therapy.
LOW V HIGH PASS?
moa: osmotic gradient between plasma and aqueous determined by the abiliy of the drg to pass through the blood aqqeous barrier

LOW PASS=high osmotic gradient
High pass=low osmotic gradient
factors determining osmotic gradient between plasma and ocular fluids (in hyperosmotic therapy )?
-molecular weight and concentration
-dose administered
-rate of absorption into plasma
-distribution in body water
-ocular penetration
-rate of excretion
What are the systemic hyperosmotic agents?
1. Urea
2. Mannitol
3. Glycerine
4. Isossorbide
5. Sodium ascorbate
6. Ethyl alcohol
What hyperosmotic agents is rarely used and requires fresh solution, and can be oral or IV?
UREA

SE'S: tissue sloughing, phlebitis, rapid diuresis, severe HA, and arm pain.
*excretion in Urine unchanged
What hyperosmotic agents is the agent of choice (IV) and is the most effective?
(is LESS toxic than urea)
Mannitol-choice hyperosmotic
*does NOT cause tissue necoris

can cause HAm chills, chest pain
*excreted unchanged thru kidneys, but use with caution in renal disease
What hyperosmotic agents is most common for initial TX of AACG?
What hyperosmotic agents is most common for initial TX of AACG?

Glycerin (Glycerol)
-50%given over ice
-can cause nausea and vomitting
*use with caution in DM
-Cn case hyperglycemia, glucosuria, ketoacidosis, dehydtration, confusion, and disorientation
-lime flavored
What hyperosmotic agents is similar to mannitol but oral? (it is not metabloized so is safer for DM)
and has less nausea and vomitting than glycerine?
What hyperosmotic agents is similar to mannitol but oral? (it is not metabloized so is safer for DM)
and has less nausea and vomitting than glycerine?

ISOSORBIDE
*Excreted unchanged in Urine
**vanilla-mint flavored
SE:HA, confusion, GI, dizzy, thirst, lethargy
What hyperosmotic agents is infrequently used oral or IV, and oral route may NOT actually lower IOP?
What hyperosmotic agents is infrequently used oral or IV, and oral route may NOT actually lower IOP?

Sodium Ascorbate
-SE: diarrhea and GI

**metabolized and excreted in Urine
What hyperosmotic agents is infrequently used DUE TO cns Effects?
and is metabolized similar to glycerine
What hyperosmotic agents is infrequently used DUE TO cns Effects?

Ethyl Alcohol
Side effects of Hypermostics therapy?
Side effects of Hypermostics therapy?
-HA, Fever, vertigo, dehydration, diuresis
-pain in upper exremities
-potassium deficiency
-congestive heart failure
-confusion and disorientation
-subdural hematoma
Adrenergic agonists
Adrenergic agonists:
1. Epinephrine
2. Dipivalyl Epinephrine
3. Apraclonidine (Iopidine)
4.Brimonidine (Alphagan P)
5. Simbrinza (Brinzolamide/Brimonidine)
6. Brimonidine/Beta blocker (new drug combo from Allergan)
Adrenergic agonists:
Epinephrine-moa
Adrenergic agonists:
Epinephrine-moa
*inc aqeous outlfow
Direct acting causing alpha and beta stimulation
-IOP lowering mech. controversial-inc facility of aqueous flow
-iop lowering more effective in POAG than 2ndary
-unstable when exposed to light/air
Adrenergic agonists:
Epinephrine-clinical uses
Adrenergic agonists:
Epinephrine-clinical uses
**RARELY USED TODAY FOR GLAUCOMA therapy
-can be used on pt who can't tolerate pilocarpine (or can take in combo with)
Adrenergic agonists:
Epinephrine-side effects (Ocular and systemic)
Adrenergic agonists:
Epinephrine-side effects
Ocular: irritation, allergy, pigmentation, mydriasis and IOP elevation in narrow angles. cystoid macular edema (in aphakes/pseudophakes)

systemic SE: severe HA, palpitations, tachycardia, PVC's, HTN crisis
Adrenergic agonists:
Epinephrine-contraindications
Adrenergic agonists:
Epinephrine-contraindications
Ocular: narrow angles, aphakia, pseudophakia, and soft CL's

systemic contas: cardiac disease, hyperthyroid, MAO inhibitors, tricyclic antidepressants, or general anesthesia which sensitize myocardium to catecholamines)
What Adrenergic agonist types are no longer available since 2009?
What Adrenergic agonist types are no longer available since 2009?
Dipivalyl Epinephrine (Propine, DPE, and Dipivefrine)

*are a prodrug of epinephrine (more lipophilic and better absorbed into eye)
-clinical uses: glaucoma, or people who can't tolerate just Epinephrine (similar mech to EPI)
**can be used in those with soft CL
Adrenergic agonist types-
Dipivalyl Epinephrine (Propine, DPE, and Dipivefrine)-
side effects and contra's?
Adrenergic agonist types-
Dipivalyl Epinephrine (Propine, DPE, and Dipivefrine)-

side effects:
ocular: CME in aphakia and psuedophakia
systemic: same as epi but less severe
and contra's: same as epi but less dangerous
Adrenergic agonist types-
Apraclonidine (Iopidine) moa?
Adrenergic agonist types-
Apraclonidine (Iopidine) moa?
-a relatively selective alpha 2 agonist to alpha 2 receptors on postganglionic sympathetic nerve terminal
*stimulation of receptor=dec in norepinephrine release=lowered aq. production=lower IOP

**use before and after yag laser to prevent IOP up
Adrenergic agonist types-
Apraclonidine (Iopidine) Side effects?
Adrenergic agonist types-
Apraclonidine (Iopidine) Side effects?

ocular injection, upper lid elevation, irreg heart beat, ocular inflammatin, dry mouth and nose, conj blanching, mydriasis
Adrenergic agonist types-
Brimonadine (Alphagan) moa?
Adrenergic agonist types-
Brimonadine (Alphagan) moa?
-relatively selective alpha 2 agonist
-reduces aq production AND inc outflow

**reduced efficacy over time
-can use in combo with others
Adrenergic agonist types-
Brimonadine (Alphagan) SE's and drug interactions?
Adrenergic agonist types-
Brimonadine (Alphagan) SE's and drug interactions?
-conj folliculosis, ocular stinging, hyperemia, FB sensation, allergy, fatigue, drowsiness, HA, dry mouth

*can have additive effect with CNS depressants (alcohol, barbituates, etc)
-additive effect with anti-htn drugs (BB's) and cardiac glycosides

**caution with pts with severe cardio disease, cerebral or coronary insufficiency, raynaud's disease, depression, othrostatic hypotension
Simbrinza is a combo of what 2 drugs?
Brinzolamide/Brimonadine
(CAI/Alpha 2 agonist)

**is a suspension so must shake well, dosed 3x/day
*study showed better than indiv drugs
*contra's and indications similar to the 2 drugs
Beta adrenergic blockers (beta blockers) are adrenergic antagonists. How do they reduce IOP?

what is most common thing we used them to tx?
Beta adrenergic blockers (beta blockers) are adrenergic antagonists. How do they reduce IOP?
-BY LOWERING AQUEOUS PRODUCTION
*CSOAG most common of what they tx
When are Beta blockers most effective?
When are Beta blockers most effective? iop less than 30mm, and if pt has been treated with less than 2 other anti glauc meds.

*note that systemic BB for cardio probs have IOP lowering effects.
What are the non selective BB's?
What are the non selective BB's?
1. Timilol (Timoptic, Betimol, Cosopt)
2. Levobunolol (Betagan)
3. Metiprnolol (Optipranolol)
4. Carteolol (Ocupress)-partial antagonist
What are the selective BB's?
What are the selective BB's?
*Betaxolol (Betoptic/s)
(and levobetaxolol)
Timoptic MOA?
Timoptic MOA?
BB-a nonselective--no local anesthetic effect and minimal agonist

-max effect seen in a few days, good diurnal control
-as effective as pilo nd acetazolamide
-more effective than epinephrine
-additive effect with other drugs
*note that topical application can give therapeutic systemic effects that can be adverse affects
What is Timoptic the drug of choice for?
What is Timoptic the drug of choice for?
-glaucoma, including CSOAG, secondary glauc, congentical glauc, and glaucomas hard to TX with other drugs
-good for pts. under 40 and for pts. with cataracts (since no acc spasm or miosis)
-alternative to pilocarpine
**but prostaglandins becoming "the first line"
**equally effective in blacks and whites
-pretty good compliance since few applications/day
Timoptic SE's?
**typically well tolerated (with few systemic SE)
-but syst SE: CNS effects most common (HA, LETHARGY, Lighheadedness, weakness, fatigue, depression, memory loss
**cardiovascular effects next most common (bradycardia, palpitations, hyPO tension, syncope, arrhythmias, CHF
*can also get respiratory symptoms*** (bronchospasm, pulmonary edema, asthma)
-can get skin rach, nausea, vomitting, diarrhea
Ocular effects:
-Burning, tearing, stinging, Fb sensation, itching, transient dry eye, punctate keratitis
-allergic blepharoconjunctiviits and lid edema
-blurry vision from refractive shifts
-macular edema in aphakes
-macular hemorrhage
-Uveitis
What drugs does Timotic have drug interactions with?
What drugs does Timotic have drug interactions with?
1. additive with other BB
2. Calcium channel blockers (cardio probs--ex Verapamil)
3. Catecholamine depleting drugs (Resperine)
4. Quinidine (Bradycardia)
Contra: children/infants, labile DM, COPD, heart block, decmp, CHF
Timotpic XE MOA
same as timoptic except for carrier (contains a gel forming compound that extends drug contact with the eye)
-used 1 time/day
Betimol MOA

advantage over Timilol?
Betimol
is a Timilol hemihydrate: a newer salt form of timilol
*oc hypotensive and ADR's similar to timilol
*primary advantage is lower cost
Timilol combined with other drugs (5)
1. Cosopt
2. Combigan
3. Extravan
4. Bimatoprost/Timilol
5. Xalacom
Cosopt made up of?
Cosopt made up of?
Timilol maleate + Dorzolamide hydrochloride (CAI)
Combigan made up of?
Combigan made up of?
Timilol + Brimonidine (Alphagan P)

**made by allergan
Extravan made up of?
Extravan made up of?
Timilol + Travaprost (Travatan)

**not available as of feb 2010 (Alcon)
Bimatoprost/Timilol made up of?
Bimatoprost/Timilol
is combo of Timilol +Brimastoprost(Lumigan)

*being dev. by Allergan--not available as of feb 2010
Xalacom made up of?
Xalacom made up of?
Timilol +Xalatan (latanaprost)

*made by Pfizer
-avail in some parts of world but not US
Other Adrenergic Antagonists
Other Adrenergic Antagonists
1. Levobunolol (Betagan)
2. Metipranolol (Optipranolol)
3.Carteolol (Ocupress)
4. Betaxolol (Betoptic/s)
Other Adrenergic Antagonists:
Levobunolol (Betagan) MOA
Other Adrenergic Antagonists:
Levobunolol (Betagan) MOA
non-selective beta blocker, reduced IOP25-30%

*Drug interactions and SE similar to Timilol
Other Adrenergic Antagonists
Metipranolol (Optipranolol) MOA
Other Adrenergic Antagonists
Metipranolol (Optipranolol) MOA
-NON-selective beta 1 and 2 blocker
*SE and contra sim to Timilol
Other Adrenergic Antagonists
Carteolol (Ocupress) MOA
Other Adrenergic Antagonists
Carteolol (Ocupress) MOA
non-selective BB wihout anesthetic effect, but has intrinsic sympathomimetic activity (a partial agonist-antagonist)

SE ,etc similar to other BB's
Other Adrenergic Antagonists
Betaxolol (Betoptic/ Betoptic S) MOA and better for what kind of pts?

advantages over Timilol?
Other Adrenergic Antagonists
Betaxolol (Betoptic/ Betoptic S) MOA:
-Selective beta 1 blocker (Safer for COPD patients)

MOA and efficacy same as timilol
**FREE FROM SEVERE OCULAR SE's
*systemic effects less severe than Timilol
Cholinergic agonists MOA?
(Direct, reversible indirect, and irreversible indirect)
Cholinergic agonists MOA?
Direct action: they stimulate receptor; shorter duration of action
Indirect action (Reversible): inhibit acetylcholinesterase (so net is more acetylcholine), longer duration of action
Irreversible indirect action: inhibit acetylcholinesterase (longest duration of action)
Cholinergic agonists uses?
1. Glaucoma (almost never today)
2.Accommodative Esotropia
3. Diagnosis of addie's or fixed pupil (or other pupila anomalies) (ex:pilocarpine)
What are the direct acting Cholinergic agonists?
What are the direct acting Cholinergic agonists?
1. Pilocarpine
2. Carbachol
What are the indirect acting Reversible Cholinergic agonists?
What are the indirect acting Reversible Cholinergic agonists?
1. Physostigmine
2. Demecarium
What are the indirect acting irreversible Cholinergic agonists?
What are the indirect acting irreversible Cholinergic agonists?
1. Diisopropylfluorophosphate
2. Echothiophate
This drug is a naturally occurring direct acting cholinergic agonist. It is a tertiary amine (acts at the central and peripheral muscarinic sites)

It affects the cardiovascular system, exocrine glands, and smooth muscle
This drug is a naturally occurring direct acting cholinergic agonist. It is a tertiary amine (acts at the central and peripheral muscarinic sites)
It affects the cardiovascular system, exocrine glands, and smooth muscle.

Pilocarpine!
Pilocarpine causes: (including it's MOA)

who are affected most by it?
Pilocarpine causes:
miosis, spasm of accomoodation, increased aqueous outflow (reduced IOP), thickening of lens and narrowing of AC

**hyoptensive effect greatest in light colored eyes
What is the most useful miotic?
What is the most useful miotic?
Pilocarpine
Pilocarpine uses:
Pilocarpine uses:
**but rarely used for glaucoma today
(can be for POAG, AACG, secondary glauc)
-accommodative esotropia
-countering effects of mydriatics
-differential dx of abnormal pupils (Adie's)
Pilocarpine SE's?
Pilocarpine SE's?
**ocular SE's common
-miosis and acc spasm
-follicular conjunctivitis
-pupillary block and inc IOP
-RD
-BAND KERATOPHATY AFTER long term use
-allergic blepharoconjunctivits
-periorbital pain, etc

systemic: (usually due to OVER-DOSE)
HA, salivation, perspiration, nausea, vomitting, bronchospasm/pulmonary edema, HypOtension, bradycardia, muscular weakness, abdominal pain, GI, respiratory paresis
Pilocarpine contraindications?
Pilocarpine contraindications?
-Cataract, <40 age (less than), neo or uveitic glaucoma, HX of RD, ashtma, succinylcholine
What drug is a direct acting choline ester resistant to AChE which gives longer duration than pilo?

It is less lipid soluble than pilo=less ocular penetration
What drug is a direct acting choline ester resistant to AChE which gives longer duration than pilo?

Carbachol

**indirect action also: release of Ach from nerves
-muscarinic and nicotinic activity
Is Carbachol used today?
Is Carbachol used today?
Rarely if ever!

contra: corneal abrasions, allergy, bronchial ashtma, GI spasm, UT obstruction, parkisons, acute cardiac failure
What is the drug that is a reversible indirect acting alkaloid tertiary amine (inhibits AChE) that is a cholinergic agonist?
What is the drug that is a reversible indirect acting alkaloid tertiary amine (inhibits AChE) that is a cholinergic agonist?

Physostigmine (Eserine)
**HARDLY USED TODAY DUE TO SIDE EFFECTS
Physostigmine (Eserine) Pharm:

how does it reduce IOP?
Physostigmine (Eserine) Pharm:
-reversible indirect acting cholinergic agonist
-muscarinic and nicotinic stimulation
-high lipid solubility
-can have dose related ciliary spasm
-significant intraocular vascular responses (vasodilation and inc capilary permeability)
-**reduces IOP by longitudinal muscle stimulation and reduce ocular fluid volume
Physostigmine (Eserine): how does it reduce IOP?
-**reduces IOP by longitudinal muscle stimulation and reduce ocular fluid volume
Physostigmine (Eserine)
**HARDLY USED TODAY DUE TO SIDE EFFECTS--WHAT ARE SOME?
Physostigmine (Eserine)
**HARDLY USED TODAY DUE TO SIDE EFFECTS--WHAT ARE SOME?

oc stinging, conj hyperemia, spasm of acc, induced myopia, brow ache, HA, lid twitch, allergic conjunc, epithelial keratitis
-iris pigment epithelium cyst formation after prolonged use
-activation of latent iritis, inc IOP (from pupil block), RD, punctal stenosis ,etc

Muscarinic- respiratory depression
Nicotinic: musclar twitching and convulsion
This is a reversible indirect cholinergic agonist that is two molecules of neostigmine linked by 10 methyl groups.
**rarely used today
This is a reversible indirect cholinergic agonist that is two molecules of neostigmine linked by 10 methyl groups.
**rarely used today

**Demecarium
This is a new glaucoma medication currently in development (by INOTEK PHARMACEUTICALS) and is in phase to of CTrials.
It is a highly selective Adenosine receptor agonist (found in epithelial cells of TM).
Trabodenoson

This is a new glaucoma medication currently in development (by INOTEK PHARMACEUTICALS) and is in phase to of CTrials.
It is a highly selective Adenosine receptor agonist (found in epithelial cells of TM).
-It ultimately has inc TM outflow from inc TM permeability due to MMP's breaking it down, so IOP down.

*Remember Prostaglandins also have MMPs breakdown TM, but activate FP receptors and primarily in the uveoscleral pathway.
Other uses of ocular autonomic drugs-adrenergic agonists:
Other uses of ocular autonomic drugs-adrenergic agonists:
1. Epinephrine
2. Phenylephrine
3.HYDORXYAMPHETAMINE
4. Cocaine
5. Imidiazole Derivatives
Other uses of ocular autonomic drugs-adrenergic agonists:
Epinephrine-clinical uses?
Epinephrine-clinical uses?
Vasoconstriction (topical decongestant)
Other uses of ocular autonomic drugs-adrenergic
Phenylephrine-MOA
Other uses of ocular autonomic drugs-adrenergic
Phenylephrine: DIRECT ALPHA STIMULATION, little beta

may reduce IOP but less than epinephrine
-used for decongestant, mydriasis, break posterior synechia**
Other uses of ocular autonomic drugs-adrenergic
Phenylephrine-SE's? (oc and sys)
and contra's?
Other uses of ocular autonomic drugs-adrenergic
Phenylephrine-SE's?
ocular-transient pain, lacrimation, keratitis, release of pigment granules from iris, rebound miosis, rebound conjunctival congestion
systemic: HA, HTN, hemes, arrythmias, tachy/brady, skin blacnhing

and contra's? MAO inhibitors, triC anti-depressants, infants, elderly, injection, irrigation
This drug causes release of norepinephrine and inhibits MAO and inhibits uptake #1.
It has little effect on accommodation.
Hydroxyamphetamine
This drug causes release of norepinephrine and inhibits MAO and inhibits uptake #1.
It has little effect on accommodation.
Hydroxyamphetamine clinical uses:
Hydroxyamphetamine clinical uses:
-routine pupil dilation (in combo with tropicamide)
-as a single drug WAS used to differentiate pre v post ganglionic horners
This drug is an alkaloid of coca leaf and benzoic acid and acts as an anesthetic. It potentiates adrenergic activity by blocking reuptake of norepinephrine.
Cocaine
This drug is an alkaloid of coca leaf and benzoic acid and acts as an anesthetic. It potentiates adrenergic activity by blocking reuptake of norepinephrine.

**oc SE: causes anesthesia, mydriasis, and vasoconstriction

sys: causes inc heart rate, CNS stimulation and vasoconstriction
Cocaine clinical uses?
Cocaine clinical uses?
-differentiate from pre/post ganglionic horners
-corneal debridement
-forced duction test
What are the 3 imidiazole derivatives?

and how do they work?
What are the 3 imidiazole derivatives?
1. Naphazoline
2. Tetrahydrozoline
3. Oxymetazoline

*more alpha than beta stimulation
-CNS depression not stimulation
Clinical uses of the 3 imidiazole derivatives?
1. Naphazoline
2. Tetrahydrozoline
3. Oxymetazoline
Clinical uses of the 3 imidiazole derivatives?
-USED in OTC ocular decongestants
What are the 2 adrenergic antagonists--the 2 alpha adrenergic blockers?
What are the 2 adrenergic antagonists--the 2 alpha adrenergic blockers?
1. Thymoxamine (Thymoxid)
2. Dapiprazole (Rev-Eyes)
(alpha adrenergic blockers) Thymoxamine (Thymoxid) MOA?

AND CLINICAL USES
(alpha adrenergic blockers) Thymoxamine (Thymoxid) MOA?
-BLOCKS postsynaptic alpha receptors on radial muscle or iris, causing miosis, causes IOP reduction in eyes with angle closure

clnical uses: CSOAG and NAG
(alpha adrenergic blockers) Dapiprazole (REV-EYES) MOA?

AND CLINICAL USES
(alpha adrenergic blockers) Dapiprazole (REV-EYES) MOA?

SAME AS THYMOXAMINE
Cholinergic agonists:
Cholinergic agonists:
1. Diisoproplylfluorophosphate (Isofluorophate, DFP)*
2.Echothiophate (Phospholine Iodide)
Cholinergic agonists:
Diisoproplylfluorophosphate (Isofluorophate, DFP)*
moa

**not used for glaucoma today--but what are the clinical uses?
Cholinergic agonists:
Diisoproplylfluorophosphate (Isofluorophate, DFP)*
moa:
irreverisble indirect acting organophosphoroud agent, inactivates AChE and BuChE (pref for BuChe)

*causes pinpoint miosis
HIGHLY lipid soluble
easily crosses BBB causing anxiety, tremors, convlusions, coma, and respiratory arrest

**not used for glaucoma today
-dx and tx accomodative esotropia
-tx for phthiriasis palpebrarum
Cholinergic agonists:
Diisoproplylfluorophosphate (Isofluorophate, DFP)*
SE:
(Which SE is deadly?)
Cholinergic agonists:
Diisoproplylfluorophosphate (Isofluorophate, DFP)*
SE:
-blurred vision, cough, photophobia, brow ache
-Iris cysts

**drug interactions:
reversible AChE inhibitors can inhibit DFP action
-additive with parasympathomimetics
***CAN CAUSE RESPIRATORY FAILURE CAUSING DEATH
Cholinergic agonists:
Echothiophate (Phospholine Iodide) MOA:

**not presently used for glaucoma
Cholinergic agonists:
Echothiophate (Phospholine Iodide) MOA:
IRREVERSIBLE indirect acting
-inhibits AChE and BuCHe (Preference for AChE)
-low lipid solubility limits CNS penetration
Cholinergic agonists:
Echothiophate (Phospholine Iodide)

**not presently used for glaucoma-but what are clinical uses?
Cholinergic agonists:
Echothiophate (Phospholine Iodide)

**not presently used for glaucoma-but what are clinical uses?
-dx and tx of acc esotropia
Cholinergic agonists:
Echothiophate (Phospholine Iodide)

SE?
Cholinergic agonists:
Echothiophate (Phospholine Iodide)

SE? similar to DFP but also: ant/post subcapsular and nuclear cataract, RD, iris cyst, punctal stenosis
What are the clinical uses of cholinergic antagonists?
What are the clinical uses of cholinergic antagonists?
1. Pupil Dilation
2. Cycloplegic (wet) refraction
3. Tx of iridocyclitis
What is the MOA cholinergic antagonists?
What is the MOA cholinergic antagonists?
-block the Ach of iris sphincter (blocks constrictor=dilation) and ciliary muscle muscarinic receptor sites
What are the cholinergic antagonists? (5)
(aka parasympthalytics)
What are the cholinergic antagonists?
1. Atropine
2. Homatropine
3. Scopolamine
4.Cyclopentolate
5. Tropicamide

*a$$ ho's should clean themselves

**all cause mydriasis
Which parasympatholytic (cholinergic antagonist) is a myditriatc(cycloplegic) with the longest duration of action and is most resistant to reversal?
Which parasympatholytic (cholinergic antagonist) is a myditriatc(cycloplegic) with the longest duration of action and is most resistant to reversal?

ATROPINE
*is found in the anterior and posterior structures of eye within 1.5 hours
*DARK eyes exhibit slower onset, longer duration, and less mydriasis
Clinical uses of Atropine: (4)
Clinical uses of Atropine:
1. Cycloplegic refraction
2. Iridocyclitis
3. TX of myopia
4.Amblyopia

1. Cycloplegic refraction-uncover maximum plus (ex:acc esotropia)
2. Iridocyclitis-lessen pain, prevent posterior synechiae, restore normal vessel permeability
3. TX of myopia-rare
4.Amblyopia-alternative to patching (induced blur must be greater than amblyopic VA); rarely used
SE of Atropine:
ocular
systemic

antidote for CNS TOXICITY?
SE of Atropine:
-ocular:irritation, allergy, angle closure and IOP elevation
-systemic-peripheral-dry mouth reduced sweating
-CNS-fever and hallucinations

**death has occured in kids under 3

antidote for CNS TOXICITY: Physostigmine
what is another parasympatholytic (cholinergic antag) that is 1/10 as effective as atropine with a shorter duration of action? It is primarily used for iridocyclitis, but NOT for dilation or cyclo refraction?
Homatropine

is another parasympatholytic (cholinergic antag) that is 1/10 as effective as atropine with a shorter duration of action? It is primarily used for iridocyclitis, but NOT for dilation or cyclo refraction
what is another parasympatholytic (cholinergic antag) that has effects similar to atropine with a shorter duration of action? It is primarily used for tx of anterior uveitis and in pts allergic to atropine?

**but has more toxicity than atropine
Scopolamine

-is another parasympatholytic (cholinergic antag) that has effects similar to atropine with a shorter duration of action? It is primarily used for tx of anterior uveitis and in pts allergic to atropine?

**but has more toxicity than atropine
SE of Scopolamine?
SE of Scopolamine?
-sim to atropine BUT MORE CNS TOXICITY
-no deaths from topical use
-restlessness, confusion, hallucinations, amnesia, violence, vomiting, incontinance
what is another parasympatholytic (cholinergic antag) that is slightly less effective in dark irides and does NOT alter IOP in normal eyes? It is primarily used for tx of iridocyclitis in pts sensitive to other drugs, and routine cyclo exams in all ages.
Cyclopentolate
-is another parasympatholytic (cholinergic antag) that is slightly less effective in dark irides and does NOT alter IOP in normal eyes? It is primarily used for tx of iridocyclitis in pts sensitive to other drugs, and routine cyclo exams in all ages.
Cyclopentolate SE's:
Cyclopentolate SE's:
Ocular SE: transient stinging, transient IOP elevation
*rarely cause allergic rxn

syst: toxicity dose related; CNS toxicity primarily in kids (peripheral symptoms can occur too)
what is another parasympatholytic (cholinergic antag) that isa weak base with pka of 5.37, and only 2.3%ionized at physiologic ph?
It has greater ocular pennetration than other drugs in its class. Faster onset and shorter duration!
Tropicamide

- is another parasympatholytic (cholinergic antag) that isa weak base with pka of 5.37, and only 2.3%ionized at physiologic ph?
It has greater ocular pennetration than other drugs in its class. Faster onset and shorter duration!
What is the drug og choice for routine ophthalmoscopy due to rapid onset and short duration?

(can cause angle closure with pupil dilation)
-ofen used with pilocarpine
Tropicamide
-is the drug og choice for routine ophthalmoscopy due to rapid onset and short duration?

(can cause angle closure with pupil dilation)
-ofen used with pilocarpine
SE of tropicamide?

**its the safest mydriatic for those with cardio probs
SE of tropicamide?
-transient stinging
-IOP can rise in eyes with CSOAG
-significant adverse systemic effects NONEXISTANT almost
-devoid of vasopressor effect: safest mydriatic for cardio pts