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
Q

cyclopentolate

A

muscarinic antagonist

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26
Q

tropicamide

A

muscarinic antagonist

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27
Q

Dipiverfrin

A

epinephrine prodrug (sympathomimetic agent)

used in treatment of glaucoma

28
Q

side effects of sympathomimetic agents

A

photosensitivity

conjunctival hyperemia hypersensitivity

29
Q

phenylephrine

A

sympathomimetic

used for mydriasis

30
Q

apraclonidine

A

sympathomimetic alpha 2 agonist

used for glaucoma, pre and post-laser prophylaxis of intraocular pressure spike

31
Q

Brimonidine

A

alpha 2 agonist

used for glaucoma

32
Q

clinical use of cocaine for eyes

A

topical anesthesia

evaluation of anisocoria

33
Q

hydroxyamphetamine

A

sympathomimetic

used in the evaluation of anisocoria

34
Q

Naphazoline

Tetrahydrozoline

A

alpha agonists

used as decongestants

35
Q

what is cycloplegia

A

paralysis of accomodation

36
Q

dapiprazole

A

alpha antagonist

reverses mydriasis

side effects include conjunctival hyperemia

37
Q

Betaxolol

A

B1 selective blocker

38
Q

carteolol
levobunolol
metipranolol
timolol

A

beta blockers

39
Q

function of the ciliary body

A

(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
Q

primary target of beta blockers and carbonic anhydrase inhibitors in treatment of glaucoma

A

reduction of aqueous humor production

41
Q

Pilocarpine
Carbachol
Physostigmine
Echothiophate

what are these agents
what are the main goals of these agents in treatment of glaucoma

A

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
Q

what is the target of Prostanoids (Latanoprost) in the treatment of glaucoma

A

(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
Q

what is the management of acute angle closure glaucoma

A

(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
Q

what might anticholinergics, sympathomimetic and antihistaminic agents induce in the eye

A

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
Q

what are the treatment goals in open angle glaucoma

A

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
Q

dorzolamide

brinzolamide

A

topical carbonic anhydrase inhibitors

47
Q

acetazolamide
dichlorophenamide
methazolamide

A

oral carbonic anhydrase inhibitors

48
Q

epinephrine

dipivefrin

A

alpha agonists
non selective
increase aqueous humor outflow

49
Q

apraclonidine

Brimonidine

A

alpha 2 agonists

decrease aqueous humor secretion

50
Q

(b) Agents that reduce aqueous humor secretion

A

(i) Beta-blockers
(ii) Carbonic anhydrase inhibitors
(iii) α-adrenergic agonists (alpha2-selective)

51
Q

agents that increase aqueous humor outflow

A

(i) Prostaglandin F2α analogs
(ii) α-adrenergic agonists (non-selective)
(iii) Parasympathomimetics: muscarinic agonists and acetylcholinesterase (AChE) inhibitors

52
Q

what is the role of glucocorticoids in the eye

A

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
Q

what are the complications of steroids in the eye

A

(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
Q

(a) Dexamethasone
(b) Prednisolone
(c) Fluorometholone
(d) Loteprednol
(e) Rimexolone
(f) Difluprednate

A

(2) Some commonly used glucocorticoids formulated for topical administration to the eye are:

55
Q

what are some commonly used NSAID’s in eye

A

(a) Diclofenac
(b) Flurbiprofen
(c) Ketorolac
(d) Bromfenac
(e) Nepafenac

56
Q

Flurbiprofen

A

counter unwanted intraoperative miosis during cataract surgery

NSAID

57
Q

Ketorolac

A

given for seasonal allergic conjunctivitis

NSAID
useful for treating cystoid macular edema occurring after cataract surgery

58
Q

Diclofenac

A

used for postop inflammation

NSAID
useful for treating cystoid macular edema occurring after cataract surgery

59
Q

(1) Pheniramine and antazoline, both H1-receptor antagonists, are formulated in combination with naphazoline, an alpha-adrenergic agonist vasoconstrictor for what?

A

relief of allergic conjunctiviitis

60
Q

emedastine difumarate and levocabastine hydrochloride

A

topical antihistamines (H1 receptor antagonist)

used for allergic conjunctivitis and hay fever symptoms

61
Q

(3) Cromolyn sodium

A

prevents release of histamine and other autocoids from mast cells is sometimes used to treat allergy symptoms in the eyes

62
Q

what is the corneal route of administration of eye drops

A

cornea to aqueous humor to iris to systemic circulation

63
Q

what is the conjunctival route of administration of artificial tears

A

conjunctiva to sclera to ciliary body

64
Q

how is cocaine and amphetamine used to figure out cause of anisocoria

A

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
Q

what are the risk factors for glaucoma

A
Elevated intraocular pressure (IOP)
Positive family history
African-American heritage
Myopia (nearsightedness) 
Hypertension
66
Q

side effects of latanoprost

A

ocular side effects include conjunctival hyperemia, irritation, increased number and length of lashes, changes in iris and lash pigmentation

67
Q

betaxolol

A

b1 selective

less efficacious than non selective b/c B receptors in the eye are mostly B2