Ophthalmic Pharmacology Flashcards

1
Q

The ocular globe is protected by the _____ and _____ tissue and _______ structures

A

bony, soft, adnexal

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2
Q

Adnexal tissues of the eye include

A

Eyelids
* Nictitating membrane
* Conjunctiva
* Lacrimal glands
* Nasolacrimal system

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3
Q

The adenexal tissues of the eye function to?

A

Mechanical protection
and immune surveillance

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4
Q

Label the image accordingly

A
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5
Q

The globe is composed of three tunics:

A
  1. External, fibrous tunic (cornea and sclera) → It
    provides rigidity
  2. Middle vascular tunic (iris + ciliary body + choroid)
    → which provide blood supply, maintain the IOP,
    and control light entry to the retina
  3. Neural tunic (sensory retina) → signal
    transmission important for the visual function
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6
Q

External, fibrous tunic is composed of ? And functions to ?

A

(cornea and sclera) → It provides rigidity

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7
Q

Middle vascular tunic is composed of? Functions to?

A

(iris + ciliary body + choroid)
which provide blood supply, maintain the IOP, and control light entry to the retina

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8
Q

Neural tunic is composed of? Functions to?

A

(sensory retina) → signal transmission important for the visual function

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9
Q

The crystalline lens ________ light rays on the _______
retina→ optimal ________ power

A

focuses, sensory, focusing

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10
Q

Aqueous humor (AH) produced by the ______ ____
occupies the space between the _____ and the ____
(________ chamber), and nourishes the avascular ______ and _____

A

ciliary, body, cornea, lens, anterior, cornea, lens

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11
Q

Vitreous humor (VH) occupies the space between the _____ and _______ _____. It maintains _________ integrity of the __________ portion of the globe

A

lens, sensory, retina, structural, posterior

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12
Q

The globe may also be subdivided in:

A

➢ Anterior segment (structures anterior to the
junction of the retina and ciliary body)
➢ Posterior segment (structures posterior to this
junction

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13
Q

Name the two blood-ocular barriers. What is their main function?

A

The Blood-aqueous barrier and the Blood-retinal barrier. These barriers also impede entrance of many drugs

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14
Q

The Blood-aqueous barrier and the Blood-retinal barrier function to?

A

Both limit the entrance of blood components into the eye (WBC, RBC, large proteins, and lipid) –> Transparency of the ocular media necessary for vision

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15
Q

Intraocular inflammation _______ effectiveness of these barriers, allowing some drugs to enter the eye.

A

decreases

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16
Q

Autonomic ocular innervation

A

→ parasympathetic (ACh)
→ sympathetic (NE)

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17
Q

Make cards for this

A
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18
Q

Label accordingly

A
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19
Q

Which parts of the eye are parasympathetically innervated?

A

Parasympathetic innervation of:
* Lacrimal glands
* Iris sphincter muscle
* Extraocular muscles (control the movements of the eyes

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20
Q

Which parts of the eye are sympathetically innervated?

A

Sympathetic innervation of:
* Adnexal and orbital smooth muscle
* Iris dilator muscle
* Ciliary body (where AH is produced)
* Iridocorneal angle (ICA) structures (where AH drains)

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21
Q

Corneal epithelium: ?

A

lipophilic

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22
Q

Corneal stroma: ?

A

hydrophilic

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23
Q

Corneal endothelium: ?

A

lipophilic

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24
Q

Corneal epithelium: lipophilic
Corneal stroma: hydrophilic
Corneal endothelium: lipophilic

These layers limit?

A

IO movement of all but biphasic drugs

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25
Medications can be altered by the ocular environment to improve penetration. Example?
Prostaglandin analogues, are converted by sterases within the cornea → improving migration through the corneal layers
26
Enzymes can effect the ?
27
The _____-___ barriers are the major impediments to penetration of systematically administered drugs
blood-ocular
28
Which drugs can effectively penetrate noninflammed barriers?
* Lipid soluble * Low molecular-weight
29
The hyaloideocapsular ligament located at the junction of the ________ lens capsule and ___________ _______.
posterior, anterior vitreous
30
The hyaloideocapsular ligament functions as a barrier to the movement of drugs between the _______ and the ______ segments of the eye. Disruption of this barrier (___ surgery or lens _______) increases:
anterior, posterior, IO, luxation ➢ Posterior movement of topically applied drugs ➢ Anterior movement of systemically administered drugs
31
List the drig factors influencing drug levels in ocular tissues
1. Solubility 2. pH 3. Formulation
32
How does solubility influence drug levels in ocular tissues?
➢ Solubility → Biphasic drugs (topically administration) → Lipophilic drugs (systemically administration)
33
How does pH influence drug levels in ocular tissues?
➢ pH → Drugs formulated at physiological pH (7-7.4) avoid discomfort upon instilation (↑ drug availability) → Drugs formulated at nonphysiological pH need to be combined with buffers
34
How does drug formulation (solutions) influence drug levels in ocular tissues?
➢ Formulation Solutions Are generally easier to administer to small animals and may be administered to large animals through subpalpebral lavage systems → by large dosing quantities, spillage over the lids may occur * Volume of drops of commercially manufactured dropper bottles ranges from 25 μl to 70 μl * Palpebral fissure of dogs and cats holds only approx. 30 μl
35
How does drug formulation (suspensions) influence drug levels in ocular tissues?
Suspensions Are composed of larger particles suspended in an aqueous vehicle → minimally irritating
36
How does drug formulation (ointments) influence drug levels in ocular tissues?
Ointments Contain drug within various viscous vehicles (petrolatum and lanolin). Advantages: * Ability to administer lipid-soluble drugs * Achieve a longer contact time with less drainage through the nasolacrimal system Disadvantage: oily residue frequently remaining following administration
37
Medication to treat ocular disease are most commonly administered either _______ or _________/___________, with local ocular _______.
topically, orally/parenterally, injections
38
Which forms of injection are used only in specific circumstances?
* Intracameral * Intravitreal * Suprachoroidal * Subconjuntival
39
Label the drug administration routes accordingly
40
Subconjuntival administration involves the injection into the space between the _________ and the _______. Drugs will penetrate through the ________ and ______ or be absorbed by the __________ vasculature.
conjunctiva, sclera, sclera, cornea, conjunctival
41
Intracameral administration (_____ commonly used) involves the injection into the _______ chamber, allowing the drug movement within the _________ environment → drainage from the eye with _____ → This administration is associated with a ______ risk of ________ damage and ______ drug toxicity
less, anterior, intraocular, AH, high, iatrogenic, IO
42
Intravitreal administration involves the drug injection into the _________, which serves as a _____-term reservoir
vitreous, long
43
Peribulbar or retrobulbar injection involves injection ________ the globe, and is reserved for placement of ________ around the globe to provide ______ and _______
behind, anesthesics, akinesia (no movement of eye), analgesia
44
The ocular/periocular injection should be used only with detailed knowledge of potential _____ ______ and _______ of the specific drug being injected
side effect, toxicities
45
Topical administration enables ____ levels of medication to be reached ______ (locations?)
high, locally, conjunctiva, cornea, and anterior chamber
46
Topical administration ___ systemic exposure thus ___ adverse drug reactions /interactions
↓ , ↓
47
Systemic (oral/parenteral) is indicated for the treatment of:
48
Posterior segment disease → presence of the _____ and ________ barriers
corneal, hyaloidecapsular
49
Glaucoma is a result of ________ pressure (IOP) is maintained by a balance between production and drainage of ____
Intraocular, AH
50
Production of AH by the _____ body occurs via _____ secretion → _______ ______ enzyme and _____-mediated mechanism * Following production posterior to the ______, AH flows ______ through the ____ and drains out of the eye via **_______ and _______ outflow at the _____________ angle (ICA)
ciliary, active, carbonic anhydrase, cAMP, pupil, anteriorly, pupil, conventional, unconventional, iridocorneal **more important than unconventional
51
Conventional outflow through the trabecular meshwork into _____ vessels (majority of ___) Unconventional (_________) outflow drains the ______ (____% in dogs, ___% in cats, ___-___% in horses)
scleral, HA, uveoscleral, remainder, 15, 3, 60-70
52
Glaucoma is characterized by ?
increased IOP
53
Glaucoma causes?
* Retinal damage * Optic nerve damage * Vision loss * Variable degrees of discomfort
54
Glaucoma is always caused by ?
decreased drainage
55
What is the difference between primary and secondary glaucoma?
* Inherent abnormality in the drainage angle itself → primary glaucoma * Obstruction of AH flow within or from the eye → secondary glaucoma
56
Medical treatment of glaucoma has the purpose to ?
decrease AH production or to increase AH drainage
57
Topically administered ocular hypotensives available for use in veterinary ophthalmology
58
Ttimolol and betaxolol are?
beta-blockers
59
What is the function of beta-blockers in the eye?
β-blockers decrease AH production by an unknown mechanism → interaction with either cAMP or Na+/K+-ATPase (or both)
60
Beta-blockers are known to be absorbed?
systemically
61
It is recommended to avoid using beta-blockers in ?
small dogs (i.e.,< 10 Kg) and cats, particularly in case of cardiovascular disease
62
List the Carbonic Anhydrase Inhibitors (CAIs):
Dorzolamide (2%), brinzolamide (1%), methozolamine (oral), and acetozolamide (oral)
63
Carbonic Anhydrase Inhibitors (CAIs) function to?
These agents decrease AH production by blockade of the carbonic anhydrase enzyme system in the ciliary body epithelium
64
Carbonic Anhydrase Inhibitors (CAIs) are able to decrease AH production via what mechanism?
The conversion of CO2 to HCO3- and the subsequent movement of H2O into the posterior chamber is thus inhibited → decreased IOP
65
What can be used to treat acute emergency glaucoma?
Carbonic Anhydrase Inhibitors (CAIs) can be used in the emergency treatment of acute glaucoma they can be used every 15-30 minutes
66
Topical formulation of CAIs may cause?
local ocular discomfort upon administration
67
Systemic side effects of CAIs include?
Systemic side effects generally do not develop with topical administration
68
latanoprost, bimatoprost, and travoprost are?
Prostaglandin analogue
69
latanoprost, bimatoprost, and travoprost function to?
These PG analogues decrease IOP by increasing uveoscleral (nonconventional) AH outflow through activation of FP receptors
70
Current PG analogues are ________ →administered form of the drug converted by corneal esterases into the active form
prodrugs
71
Clinically significant IOP reductions of 20-60% result from the administration of these agents in dogs
72
Current PG analogues are ineffective in cats. Why?
ocular hypotensive effects in cats are mediated by EP receptors
73
Prostaglandin analogues have have ___________ side effects (?) in horses
inflammatory, conjunctival hyperemia, miosis, flare
74
List the side effects of prostaglandin analogues
Conjuntival hyperemia and moderate to marked miosis → these drugs are contraindicated in most cases of secondary glaucoma
75
Mannitol 20% (IV) and glycerol (oral) are ?
Hyperosmotic agents
76
Administration of hyperosmotic agents causes the serum to become?
hyperosmotic to intraocular fluids → fluid movement from the AH and VH
77
How is Mannitol administered?
Is administered IV (1g/Kg over 15-20 minutes), with coinciding water deprivation (for 4-6 h) postadministration → acute primary glaucoma only
78
Glycerol (1-2 g/Kg orally) as a component of ________ -term management
long
79
Side effects/contraindications * Hyperosmotic agents are contraindicated in the presence of ? * Systemic contraindications include: ? * Glycerol may also induce _______ at higher doses
Side effects/contraindications * Hyperosmotic agents are contraindicated in the presence of anterior uveitis * Systemic contraindications include: cardiovascular disease, renal disease and diabetes mellitus * Glycerol may also induce vomiting at higher doses
80
Use of hyperosmotic agents in veterinary ophthalmology is ?
limited
81
82
Parasympathomimetics: 1-2% pilocarpine is ____ acting and 0.125% - 0.25% demecarium bromide is _________ acting
direct, indirect
83
Pilocarpine and demecarium bromidedrugs function to?
increase outflow by inducing miosis, thus widening the iridocorneal angle (ICA) and incresing AH outflow
84
Pilocarpine is generally indicated for administration ?
three to four times daily. It leads to 30-40% IOP reduction in glaucomatous dogs
85
* The _______ pH of pilocarpine solutions causes irritation following topical administration * Due to the induction of ______, pilocarpine is contraindicated in patients with _____ and/or pupillary ____ glaucoma
* The acidic pH of pilocarpine solutions causes irritation following topical administration * Due to the induction of miosis pilocarpine is contraindicated in patients with uveitis and/or pupillary block glaucoma
86
The effect of parasympathomimetics on IOP is minimal compared to other classes of ocular hypertensive agents
87
Antiinflammatory therapy is important to minimize ________ effects of inflammation, and to preserve the ocular _____ and ______ ➢ ______ antinflammatory therapy is indicated for treatment of ocular surface inflammation (2) and anterior segment inflammation (1) ➢ Systemic antinflammatories are indicated for treatment of ?
secondary, structure, function, Topical, conjunctivitis, keratitis, anterior uveitis, posterior uveitis
88
Corticosteroids exert __________ effects through inhibition of the ________ acid cascade * The location and severity of ocular inflammation determines the ___________ of administration and drug ______ * Regardless of the ______ of inflammation, severely inflamed eyes may require dosing every __-___ hours and every __-__ h dosing for lesser degrees of inflammation
antiinflammatory, arachidonic, frequency, selection, location, 2-4 h, 8-12
89
List the side effects of corticosteroids * Long-term topical administration may result in the formation of corneal _________ * Systemic absorption may occur affecting coinciding ______ imbalances * Topical corticosteroids are contraindicated in the presence of corneal _______ → inhibit ________ of the wound → infections
* Long-term topical administration may result in the formation of corneal deposits * Systemic absorption may occur affecting coinciding endocrine imbalances * Topical corticosteroids are contraindicated in the presence of corneal ulcer → inhibit reepithelialization of the wound → infections
90
91
Nonsteroidal antiinflammatory agents (NSAIDs) exert their effects by ________ the production of ___ through the ? * Frequency of administration of topical NSAIDs depends upon the ____ of inflammation * NSAIDs are considered ___ effective than topical corticosteroids in the treatment of ocular ____________ diseases * _________ penetration of NSAIDs is variable. ______ agents are reported to have improved penetration
inhibiting, PG, constitutive cyclooxygenase-1 (COX-1) and the inducible cyclooxygenase-2 (COX-2), severity, less, inflammatory, Transcorneal, Newer
92
List the side effects of NSAIDs
* Safer to use in the presence of corneal ulceration than corticosteroids * Topical NSAIDs may inhibit reepithelialization of the cornea → associated with acute corneal melts
93
94
Ocular infections: antibacterial therapy ➢ Prophylactic ➢ Therapeutic
95
Most of the ocular infections are caused by ?
pathogenic effects of normal ocular surface bacteria
96
Normal ocular bacteria → predominantly gram- ______--> ?
positive, The appropriate antibiotic choice
97
___________ _____ (gram-negative) → potent ocular pathogens
Pseudomonas aeruginosa
98
General principles of antibacterial therapy: * Prophylactic use for _______, _______ corneal ulcers * Prophylactic use is indicated in association with ____ procedures in which ________ is involved * Therapeutic use is indicated for _____, complicated _____ diseases * Therapeutic use is indicated for ____________ __________ * Side effects, both ____ and ___, must be considered
superficial, uncomplicated, surgical, conjunctiva, infected, corneal, bacterial endophthalmitis, ocular, systemic
99
Ability of a specific antibiotic (formulation) to reach desired site of infection (deep cornea, anterior chamber)
100
List the most common aminoglycosides used for antibacterial therapy
Aminoglycosides: tobramycin, gentamicin, and neomycin → topical solutions and oinments
101
What is the spectrum of action of the aminoglycosides used for antibacterial therapy in ocular infections?
Spectrum: gram-negative (principally), with gram-positive restricted to Staphylococcus aureu
102
Aminoglycosides indications in antibacterial therapy
➢ Indication: * Used as prophylaxis or therapy for ocular surface infection with variable intraocular penetration * Use is limited in patients with deep corneal infections. Gentamicin is used for chemical ablation of the ciliary body (chronically glaucomatous eyes
103
Side effects of aminoglycosides in antibacterial therapy for ocular infections Low pH of gentamicin → is ______ irritating and may be ______. _____ and _______ reactions are more common with neomycin
Low pH of gentamicin → is locally irritating and may be painful. Allergic and hypersensitivity reactions are more common to neomycin
104
List the most common tetracyclines used for antibacterial therapy
oxytetracycline formulated with polymyxin B. Topical suspensions and oinments
105
What is the spectrum of action of the tetracyclines used for antibacterial therapy in ocular infections?
➢ Spectrum: * Good activity
106
Tetracyclines indications in antibacterial therapy * It is useful for _______ or therapy for ocular _____ infections * Tetracyclines have shown increased _______ ______ wound healing
* It is useful for prophylaxis or therapy for ocular surface infections * Tetracyclines have shown increased corneal epithelial wound healing
107
Side effects of tetracyclines in antibacterial therapy for ocular infections.
➢ Side effects: * Local ocular irritation may occur
108
List the most common fluroquinolones used for antibacterial therapy
norfloxacin, ofloxacin, ciprofloxacin, levofloxacin, morifloxacin, gatifloxacin, besifloxacin → topical solutions and oinments
109
What is the spectrum of action of the fluroquinolones used for antibacterial therapy in ocular infections?
➢ Spectrum: * gram-negative and gram-positive efficacy
110
Fluroquinolones indications in antibacterial therapy ➢ Indication: * Used as _______ or therapy for ocular _____ and _______ infections. Newer agents are indicated for _____ use only
➢ Indication: * Used as prophylaxis or therapy for ocular surface and intraocular infections. Newer agents are indicated for therapeutic use only
111
Side effects of fluroquinolones in antibacterial therapy for ocular infections. * The parenteral administration may cause retinal ____________ in cats → toxicity is _____- related. ____ cats are more susceptible
➢ Side effects: * The parenteral administration may cause retinal degeneration in cats → toxicity is dose- related. Aged cats are more susceptible
112
List the most common Lincosamides and macrolides used for antibacterial therapy
: erythromycin oinment; clindamycin and azithromicin orally
113
What is the spectrum of action of the Lincosamides and macrolides used for antibacterial therapy in ocular infections?
➢ Spectrum: * Gram-positive efficacy (Chlamydophila felis, Mycoplasma ssp)
114
Lincosamides and macrolides indications in antibacterial therapy
Used as prophylaxis or therapy for ocular surface infections
115
Side effects of Lincosamides and macrolides in antibacterial therapy for ocular infections.
Local ocular irritation may occur (mild)
116
Ocular infections: antifungal therapy ➢ The most frequent indication for antifungal agents is the treatment of fungal infections of the cornea (_________) in _____ ➢ These infections are common in ____, ____ climates → ? (filamentous organisms) ➢ ____-ocular infection with _____ mycotic organisms occurs mostly in dogs
keratomycosis, horses, warm, humid, Aspergillus spp. and Fusarium spp., Intra, systemic
117
List the most common Polyenes used for antifungal therapy
: natamycin, amphotericin B
118
What is the spectrum of action of the polyenes used for antifungal therapy in ocular infections?
Both agents are considered broad spectrum
119
Polyenes indications in antifungal therapy
➢ Indication: * Polyenes have poor penetration following topical administration to a cornea with an intact epithelium → used in confirmed ulcerative keratomycosi
120
Side effects of polyenes in antifungal therapy for ocular infections.
➢ Side effects: * Local ocular irritation is the primary side effect * Systemic administration of amphotericin B may induce nephrotoxicity
121
List the most common azoles used for antifungal therapy
voriconazole (formulation for IV injection); miconazole; itraconazole; ketoconazole; fluconazole
122
What is the spectrum of action of the azoles used for antifungal therapy in ocular infections?
Azoles are broad spectrum againts filamentous fungi
123
Azoles indications in antifungal therapy Administration of topical agents is indicated in cases of _________ and __________ keratomycosis
Administration of topical agents is indicated in cases of ulcerative and nonulcerative keratomycosis
124
Side effects of azoles in antifungal therapy for ocular infections.
* Topical ocular irritation is generally minimal * Monitoring liver enzymes may be indicated in animals receiving oral azoles * Fluconazole has been implicated in prolonged recovery from anesthesia in horses
125
The most commom indication for antiviral agents is the treatment of feline herpesvirus-1 (FHV-1) infections, which manifest as ______ _____ disease in cats. Dogs and horses may experience ______ ocular surface disease → investigations into efficacy of antiviral agents towards canine and equine herpesvirus variants are ______ than those involving FHV-1
The most commom indication for antiviral agents is the treatment of feline herpesvirus-1 (FHV-1) infections, which manifest as ocular surface disease in cats. Dogs and horses may experience herpectic ocular surface disease → investigations into efficacy of antiviral agents towards canine and equine herpesvirus variants are fewer than those involving FHV-1
126
List the most common pyrimidine analogs used for antiviral therapy
: trifluridine; idoxuridine
127
Pyrimidines indications in antiviral therapy
As these agents exert their action on DNA synthesis, they are active when virus is actively replicating. They are indicated by the presence of corneal and/or conjunctival ulceration
128
Side effects of pyrimidines in antiviral therapy for ocular infections.
Topical ocular irritation
129
List the most common purine analogs used for antiviral therapy
vidarabine; cidofovir; famciclovir; acyclovir; valocyclovir
130
Purine analog indications in antiviral therapy
➢ Indication: * They are used to treat FHV-1 and keratitis in horses due to equine herpesvirus-2
131
Side effects of purine analogs in antiviral therapy for ocular infections.
➢ Side effects: * Topical ocular irritation may occur * Nasolacrimal punctal occlusion has been reported in people with cidofovir administration * Acyclovir and valacyclovir should not be administered to cats (orally or topically) due to life- threatening toxicities (kidney, bone marrow)
132
Lacrimogenics are drugs that?
increase tear production
133
Dogs with neurogenetics KCS keratoconjuntivitis sicca (KCS) are lacking ___________ input to ____________ ______.
neurological, lacrimal gland
134
One agent that can be used for Dogs with neurogenetics KCS is Parasympathomimetic, a _______ Oral administration of the 2% ophthalmic solution → applied on the _____. Increases production of _______ gland. Adverse effects May be noted as dosing ______, resulting in signs of _________ overstimulation including * Excessive ________ * _________ * ________ * __________
pilocarpine, food, lacrimal, increases, parasympathetic, salivation, Lacrimation, Urination, Defecation
135
Mydriatics are drugs that ____ the pupil → indicated for diagnostic examination
dilate
136
Cycloplegic are drugs that _____ ciliary body muscle)→ therapy of anterior ____
paralize, uveitis
137
List the most common sympathomimetics used for ocular therapy (pupillary dilation).
epinephrine; phenylephrine
138
Sympathomimetic indications in ocular therapy
➢ Indication: * prior to intraocular surgery, and to diagnose Horner‘s syndrome * Their efficacy as mydriatic agents is less than that of parasympatholitic agent
139
Side effects of sympathomimetics in ocular therapy. Which side effect is the most common?
➢ Side effects: * Ocular surface irritation may occur (most common) * Systemic absorption may induce systemic hypertension * Use should be limited in patients with preexisting cardiovascular disease b/c epi and phenyl affects cardiovascular rate and systemic pressure.
140
Parasympatholytics : 0.5-1% tropicamide; 1% atropine Mydriatics and cycloplegics * They induce __________ blockade of ____ sphincter and _____ body muscles → _______ while producing ______ * Relative efficacy also depends upon iridal ________ → ______ serves as a reservoir for drug, _______ onset of action and _____ duration in _____ pigmented versus ____ pigmented eyes. ➢ Side effects: * ______ * Temporary reduction in aqueous ___ ____ production * _______ may occur due to mydriasis
anticholinergic, iris, ciliary, mydriasis, cycloplegia, pigmentation, pigment, slowing, prolonging, heavily, poorly, Salivation, tear film, Photophobia
141
Local anesthetics, such as (4) - Topical local anesthetics are used to provide _____ and _____ anesthesia → routine diagnostic and therapeutic procedures: ___ collection, and ____ or _____ surgery * Following administration of a single drop in dogs of proparacaine, anesthetic effect is noted within ___ minute, reaching maximal effect within ___ minutes (total duration ___ minutes) * ________ administration in horses has a dose-dependent effect. ➢ Side effects: * ________ causes transient tear film instability → repeated dosing may result in epithelial keratitis. * All local anesthetics inhibit ______ ______ formation and corneal ________. * ________, _____ anesthetics are contraindicated as therapy for any ocular surface disease (diagnostic setting).
0.5% proparacaine; 0.5%, 1% tetracaine; butacaine; dibucaine corneal, conjunctival, cytology, corneal, intraocular, one, 15, 45, Tetracaine, Proparacaine, blood vessel, epithelialization, Topical local