Ophthalmologic agents (Linger) Flashcards

1
Q

why might topical eye drugs cause systemic effects

A

ii) Nasolacrimal drainage contributes to systemic absorption of topically administered ophthalmic medications; absorption from the nasal mucosa avoids first-pass metabolism by the liver, and consequently, significant systemic side effects may be caused by topical medications, especially when used chronically

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2
Q

what route is desired routes for localized ocular effects

A

iii) Transcorneal and transconjunctival/scleral absorption

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3
Q

after a drug is administered topically in the eye, where is it distributed

A

i) Topically administered drugs may undergo systemic distribution primarily by nasal mucosa absorption and by local ocular distribution by transcorneal/transconjunctival absorption
ii) After transcorneal absorption, aqueous humor accumulates the drug, which then is distributed to intraocular structures as well as potentially to the systemic circulation via the trabecular meshwork pathway

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4
Q

dipivefrin hydrochloride

A

prodrug for epinephrine

used for glaucoma

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5
Q

latanoprost

A

prodrug for prostaglandin F2alpha

used for management of glaucoma

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6
Q

what is anisocoria

A

inequality in the size of pupils

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7
Q

ptosis

A

lid lag

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8
Q

horners syndrome

A

Ptosis (lid lag)– lack of superior tarsal muscle
miosis (small pupil)
anhydrosis (lack of sweating)

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9
Q

how do you distinguish horner’s syndrome from cranial nerve III injury

A

Horner’s syndrome is sometimes confused with third cranial nerve injury because ptosis is a common manifestation; however, miosis distinguishes Horner’s syndrome’s from third cranial nerve injury, which causes a dilated ureactive pupil

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10
Q

sympathetic input to the eyelid

A

retracts the eyelid

so in horner’s syndrome you may see ptosis and also elevation of the eyebrow which is an unconscious maneurver to uncover the pupil

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11
Q

Adie’s pupil

A

(a) Injury to the parasympathetic tract leads to Adie’s Pupil characterized by:
(i) Mydriasis (dilated pupil)
(ii) Loss of deep tendon reflexes
(iii) Excessive sweating

(b) When the muscle is deprived of parasympathetic innervation, as in Adie’s pupil, it becomes supersensitive to stimulation by muscarinic agonists, such as pilocarpine (see figure below)
(c) The normal eye does not readily respond to dilute solutions (0.1%) of the muscarinic agonist pilocarpine, but will respond to higher concentrations (1%) of the drug

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12
Q

opioid agonists effect on eye (morphine, heroine)

A

cause pinpoint pupil

Mu opioid receptor excites parasympathetic nerves

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13
Q

cocaine effect on eye?

A

potently inhibits the normal reuptake of norepinephrine into presynaptic nerve terminals, resulting in an increased level of extracellular norepinephrine.

should dilate the eye. in horner’s syndrome cocaine has no effect in causing dilation

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14
Q

outcome in eye after hydroxyamphetamine is added in preganglionic horners

A

dilation!

Pupil still responsive to local release of NE, therefore defect must be preganglionic

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15
Q

outcome in the eye after hydroxyamphetamine is added in postganglionic horner’s

A

no dilation

Pupil still responsive to local release of NE, therefore defect must be preganglionic

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16
Q

what happens when pilocarpine is given to a patient with Adie’s pupil

A

Pilocarpine is a cholinomimetic (M agonist) and therefore stimulates parasympathetic responses and will cause constriction

Circular sphincter muscle has denervation supersensitivity to ACh

normal pupils are NOT responsive to low concentration of pilocarpine

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17
Q

carbachol

MOA
side effects

A

cholinergic agonist

Corneal edema, miosis, induced myopia, decreased vision, brow ache, retinal detachment

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18
Q

Physostigmine

Echothiophate

A

AChE inhibitors

contract ciliary muscle and open trabecular meshwork , increasing the outflow of aqeous humor through the canal of schlemm

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19
Q

pilocarpine

A

Cholinergic Agonist

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20
Q

side effects of physostigmine and echothiophate

A

Retinal detachment, miosis, cataract, pupillary block glaucoma iris cysts, brow ache, punctal stenosis of the nasolacrimal system

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21
Q

atropine

A

muscarinic antagonist

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22
Q

use of muscarinic antagonists in eye pharm

A

cycloplegic retinoscopy

dilated funduscopic exam

cycloplegia

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23
Q

side effects of muscarinic antagonists on the eye

A

photosensitivity and blurred vision

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24
Q

scopolamine

homatropine

A

muscarinic antagonist

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25
cyclopentolate
muscarinic antagonist
26
tropicamide
muscarinic antagonist
27
Dipiverfrin
epinephrine prodrug (sympathomimetic agent) used in treatment of glaucoma
28
side effects of sympathomimetic agents
photosensitivity conjunctival hyperemia hypersensitivity
29
phenylephrine
sympathomimetic | used for mydriasis
30
apraclonidine
sympathomimetic alpha 2 agonist used for glaucoma, pre and post-laser prophylaxis of intraocular pressure spike
31
Brimonidine
alpha 2 agonist | used for glaucoma
32
clinical use of cocaine for eyes
topical anesthesia evaluation of anisocoria
33
hydroxyamphetamine
sympathomimetic | used in the evaluation of anisocoria
34
Naphazoline | Tetrahydrozoline
alpha agonists used as decongestants
35
what is cycloplegia
paralysis of accomodation
36
dapiprazole
alpha antagonist reverses mydriasis side effects include conjunctival hyperemia
37
Betaxolol
B1 selective blocker
38
carteolol levobunolol metipranolol timolol
beta blockers
39
function of the ciliary body
(1) The ciliary body serves two very specialized roles in the eye: (a) secretion of aqueous humor by the epithelial bilayer (b) accommodation by the ciliary muscle
40
primary target of beta blockers and carbonic anhydrase inhibitors in treatment of glaucoma
reduction of aqueous humor production
41
Pilocarpine Carbachol Physostigmine Echothiophate what are these agents what are the main goals of these agents in treatment of glaucoma
these are cholinergic agonists (2) Aqueous humor leaves by way of the trabecular meshwork and the Canal of Schlemm (80-95% of outflow); this pathway is the main target of cholinergic agonists in glaucoma therapy; cholinergic agonists cause contraction of the ciliary muscle fibers which enlarges the openings in the trabecular meshwork, enhancing outflow
42
what is the target of Prostanoids (Latanoprost) in the treatment of glaucoma
(3) A second pathway is the uveosclera route where fluid flows through the ciliary muscles and into the suprachoroidal space; this route is the target of prostanoids, like latanoprost
43
what is the management of acute angle closure glaucoma
(1) Angle-closure (or closed-angle) glaucoma must be managed acutely on an emergency basis by surgical removal of part of the iris (iridectomy), but short-term medical management may be necessary to reduce acute IOP elevation; long-term IOP reduction may be necessary, especially if the peripheral iris has permanently covered the trabecular meshwork
44
what might anticholinergics, sympathomimetic and antihistaminic agents induce in the eye
might induce partial dilation of the pupil and a change in the vectors of force between the iris and the lens the aqueous humor is then prevented from passing through the pupil from the posterior chamber, causing the iris base to be pushed against the angle wall , thereby closing filtration angle and markedly elevating IOP thus, antimuscarinics, alpha 1 agonists, antihistamines with antimuscarinic activity are contraindicated in closed angle glaucoma
45
what are the treatment goals in open angle glaucoma
aimed at decreasing aqueous humor production and/or by increasing aqueous humor outflow (a) The therapeutic goal is to prevent progressive glaucomatous optic-nerve damage with minimum risk and side effects from either topical or systemic therapy
46
dorzolamide | brinzolamide
topical carbonic anhydrase inhibitors
47
acetazolamide dichlorophenamide methazolamide
oral carbonic anhydrase inhibitors
48
epinephrine | dipivefrin
alpha agonists non selective increase aqueous humor outflow
49
apraclonidine | Brimonidine
alpha 2 agonists decrease aqueous humor secretion
50
(b) Agents that reduce aqueous humor secretion
(i) Beta-blockers (ii) Carbonic anhydrase inhibitors (iii) α-adrenergic agonists (alpha2-selective)
51
agents that increase aqueous humor outflow
(i) Prostaglandin F2α analogs (ii) α-adrenergic agonists (non-selective) (iii) Parasympathomimetics: muscarinic agonists and acetylcholinesterase (AChE) inhibitors
52
what is the role of glucocorticoids in the eye
anti-inflammatory - allergy - anterior uveitis - external eye inflammatory disease associated with some infections - post operative inflammation following refractive, corneal or intraocular surgery (4) After glaucoma filtering surgery, topical steroids can delay the wound-healing process by decreasing fibroblast infiltration, thereby reducing potential scarring of the surgical site
53
what are the complications of steroids in the eye
(6) Steroids can have significant toxicities in the eye; ocular complications include development of posterior subcapsular cataracts, secondary infections, and secondary open-angle glaucoma; with a positive family history of glaucoma, moderate to marked steroid-induced IOP elevations may occur in up to 90% of patients; typically, steroid-induced elevations of IOP are reversible once administration of the drug is ceased
54
(a) Dexamethasone (b) Prednisolone (c) Fluorometholone (d) Loteprednol (e) Rimexolone (f) Difluprednate
(2) Some commonly used glucocorticoids formulated for topical administration to the eye are:
55
what are some commonly used NSAID's in eye
(a) Diclofenac (b) Flurbiprofen (c) Ketorolac (d) Bromfenac (e) Nepafenac
56
Flurbiprofen
counter unwanted intraoperative miosis during cataract surgery NSAID
57
Ketorolac
given for seasonal allergic conjunctivitis NSAID useful for treating cystoid macular edema occurring after cataract surgery
58
Diclofenac
used for postop inflammation NSAID useful for treating cystoid macular edema occurring after cataract surgery
59
(1) Pheniramine and antazoline, both H1-receptor antagonists, are formulated in combination with naphazoline, an alpha-adrenergic agonist vasoconstrictor for what?
relief of allergic conjunctiviitis
60
emedastine difumarate and levocabastine hydrochloride
topical antihistamines (H1 receptor antagonist) used for allergic conjunctivitis and hay fever symptoms
61
(3) Cromolyn sodium
prevents release of histamine and other autocoids from mast cells is sometimes used to treat allergy symptoms in the eyes
62
what is the corneal route of administration of eye drops
cornea to aqueous humor to iris to systemic circulation
63
what is the conjunctival route of administration of artificial tears
conjunctiva to sclera to ciliary body
64
how is cocaine and amphetamine used to figure out cause of anisocoria
Cocaine test- inhibits reuptake of NE/dopamine. In testing the eyes, inhibits uptake of NE builds up in synaptic cleft and more activation of andrenergic receptors which will cause dilation in a normal eye. If you get dilation after this in the smaller pupil, then its simple anixocoria. If not there is nerve damage somewhere/sympathetic injury. To differentiate pre versus post, use hydroxyamphetamine  these reverse reuptake and release NE into the synapse through a reverse transporter If you get dilation after amphetamine – postganglionic is healthy and there is plenty of NE in the nerve terminals and the injury is preganglionic. If you don’t get dilation then there is a problem with postganglionic nerve. DON”T complete cocaine and amphetamine steps in the same day. These two tests are the gold standard for Horner’s syndrome.
65
what are the risk factors for glaucoma
``` Elevated intraocular pressure (IOP) Positive family history African-American heritage Myopia (nearsightedness) Hypertension ```
66
side effects of latanoprost
ocular side effects include conjunctival hyperemia, irritation, increased number and length of lashes, changes in iris and lash pigmentation
67
betaxolol
b1 selective less efficacious than non selective b/c B receptors in the eye are mostly B2