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Edited: Pharmacology Ophthalmics T3 Month 1 Week 3
Pharmacology Ophthalmics T3 Month 1 Week 3
77
Medical
Graduate
10/04/2018

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Term
Local Delivery of Ophthalmic Agent to Site
Definition
• Ophthalmic suspension • Ointment
• Gel
• Periocular injection
• Intraocular injection
Term
Systemic Delivery of Ophthalmic Agent to Site
Definition
• Oral
• Intravenous
• Intramuscular
• Subcutaneous
Term
Factors Influencing Penetration of Ophthamic Drugs
Definition
• Drug concentration • Viscosity
• Lipid solubility
• Surfactant
• pH
• Drug tonicity
• Molecular weight and size
Term
Proper Administration of Ophthalmic Drops
Definition
• Wash hands before and after instilling eye drops.
• Cleaning eyes may be necessary when crusty or purulent deposits are on eyelids.
• Gently agitate eye drop bottle prior to use to ensure the drug is properly mixed.
• Hold head in comfortable position, tilted back.
• Using fingers(s), pull/hold lower eyelid down gently while looking up.
• Instill eye drop into the space created by pulling down on eyelid.
• Release eye and gently close eyelid remaining closed for approximately two minutes.
Term
Considerations for Administration of Ophthalmic Drugs
Definition
• Best to avoid contact lens while using medication eye drops
• Do not touch the tip of the eye drop bottle to the eye or eyelid to prevent contamination
• If using more than one eye drop, best to wait five minutes between administrations
Term
Proper Administration of Ophthalmic Ointment
Definition
• Wash hands prior and after applying ointment.
• Sit or stand in front of a mirror.
• Tilt head back and pull the lower lid of eye to form a pocket.
• Hold tube near eye.
• Apply pressure to tube to release thin line of ointment along lower inside eyelid.
• Close eye for a couple seconds.
Term
Considerations for Administration of Ophthalmic Ointment
Definition
• Ointments may be easier for young children and older adults.
• Ointments may cause blurry vision.
• Avoid touching tube to eye/eyelid if possible to avoid contamination.
Term
Which of the following is FALSE regarding the proper administration of eye drops? (vs what is true)
Definition
false: All eye drops can be used when wearing contact lenses.. true: The tip of the eye drop bottle should not touch the eye/eyelid. After administering eye drops, the eye should remain closed for about 2 minutes. Always wash hands prior to and after using eye drops.
Term
Glaucoma
Definition
• Damage to the eye’s optic nerve that may result in vision loss or blindness
• Often caused by elevated intraocular pressure (IOP)
• Causes:
• Trauma to eye, infection, blocked blood vessels, inflammatory conditions
• Two types of glaucoma • Open-angle
• Angle-closure
Term
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Definition
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Term
Treatment of Open-Angle Glaucoma
Definition
• Treatment generally initiated with two instances of IOP >25 mmHg
• Pharmacologic classes of treatment
• Prostaglandins
• Beta-blockers
• Alpha adrenergic agonists
• Carbonic anhydrase inhibitors
• Cholinergic agonists
Term
Angle-Closure Glaucoma
Definition
• Less common compared to open-angle glaucoma
• QuickerriseinIOPcomparedtoopen-angle glaucoma due to pupillary blockage that prevents or decreases aqueous humor outflow
• Treatment based on presentation and acuity
• No available trials regarding medical therapy management
• May utilize agents that lower IOP in the acute setting and then followed by laser peripheral iridotomy or other surgical management
Term
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Definition
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Term
Prostaglandins Agents
Definition
Bimatoprost (buymeapost), Lantanoprost (lanternorpost), Tafluprost (teraflupost), Travoprost (travestpost)
Term
Beta-Blockers Agents
Definition
Betaxolol, Carteolol, Levobunolol, Metipranolol, Timolol
Term
Beta-blocker MOA
Definition
blockade of beta-1 and beta-2 adrenergic receptors and reduces aqueous humor production from ciliary body
Note: betaxolol is beta-1 selective; carteolol, levobunolol, metipranolol, and timolol nonselective

Betaxolol, Carteolol, Levobunolol, Metipranolol, Timolol
Term
has SE:
• Local side effects: burning, stinging
• Systemic side effects: bradycardia, sweating, anxiety, angina, depression, drowsiness, headache, insomnia, skin rash, urticaria
Definition
Beta-Blockers
Betaxolol, Carteolol, Levobunolol, Metipranolol, Timolol
Term
has Contraindications:
hypersensitivity, bronchial asthma, severe COPD, sinus bradycardia, second- or third-degree AV block, overt heart failure, cardiogenic shock
Definition
Beta-Blockers
Betaxolol, Carteolol, Levobunolol, Metipranolol, Timolol
Term
has SEs:

• Local side effects: blurred vision, stinging, epithelial keratopathy, iris hyperpigmentation, pruritus, lacrimation, dry eyes, pain, photophobia
• Systemic side effects (rare): angina, chest pain
• Other (rare): prostaglandin associated periorbitopathy (PAP)
• Eyelid and orbital changes
• Upper lid ptosis, deepening of lid sulcus, periorbital fat atrophy, endophthalmitis
Definition
Prostaglandins
Bimatoprost (buymeapost), Lantanoprost (lanternorpost), Tafluprost (teraflupost), Travoprost (travestpost)
Term
Prostaglandins MOA
Definition
increases aqueous humor outflow through the uveoscleral route. Note that bimatoprost may also improve outflow via the trabecular meshwork.
Term
Alpha Adrenergic Agonist MOA
Definition
adrenergic agonist resulting in decreased aqueous humor formation and increased uveoscleral outflow
Apraclonidine, Brimonidine
Term
is selective for alpha-2 adrenergic receptors, also known to increase uveoscleral aqueous humor outflow
Definition
Brimonidine (brim of iodine)
Term
is relatively selective for alpha-2 adrenergic receptors, but does retain some alpha-1 receptor activity
Definition
Apraclonidine (apron iodine)
Term
Alpha Adrenergic Agonist Agents
Definition
Apraclonidine (apron iodine), Brimonidine (brim of iodine)
Term
Has Contraindications:
hypersensitivity, neonates, and infants <2 years, concomitant MAO inhibitor use
Definition
Alpha Adrenergic Agonists
Apraclonidine (apron iodine), Brimonidine (brim of iodine)
Term
Has cautions for:
use in severe cardiovascular disease, depression, patients with orthostatic hypotension
Definition
Alpha Adrenergic Agonists
Apraclonidine (apron iodine), Brimonidine (brim of iodine)
Term
Has SE:
• Local side effects: allergic conjunctivitis, conjunctival hyperemia, eye pruritus
• Systemic side effects: drowsiness, hypertension, fatigue, headache, insomnia, xerostomia
Definition
Alpha Adrenergic Agonists
Apraclonidine (apron iodine), Brimonidine (brim of iodine)
Term
Carbonic Anhydrase Inhibitors MOA
Definition
inhibition of carbonic anhydrase, resulting in decreased hydrogen ion secretion at renal tubule, resulting in increased excretion of sodium, potassium, bicarbonate, and water to decrease production of aqueous humor
Brinzolamide, Dorzolamide, Acetazolamide, Methazolamide
Term
Carbonic Anhydrase Inhibitors Agents
Definition
Brinzolamide (brimzofamine), Dorzolamide (droz of amine), Acetazolamide (ace za amine), Methazolamide (meth za amine)
Term
Has cautions for:
sulfa allergy
Definition
Carbonic Anhydrase Inhibitors
Brinzolamide (brimzofamine), Dorzolamide (droz of amine), Acetazolamide (ace za amine), Methazolamide (meth za amine)
Term
Has SEs:
• Local side effects: burning, discomfort, stinging, keratitis, blurred vision, conjunctivitis, photophobia
• Systemic side effects: skin rash, fatigue, headache, nausea, urolithiasis, weakness
Definition
Carbonic Anhydrase Inhibitors
Brinzolamide (brimzofamine), Dorzolamide (droz of amine), Acetazolamide (ace za amine), Methazolamide (meth za amine)
Term
Cholinergic Agonists MOA
Definition
• Directactingcholinergicagonistthatstimulates
muscarinic receptors in the eye leading to dilation
• Decreased resistance to aqueous humor outflow leading to increased aqueous humor outflow
• Constriction of ciliary muscles leading to loss of accommodation
Carbachol (carbs or alcohol), Pilocarpine (pillow car pine)
Term
Cholinergic Agonists Agents
Definition
Carbachol (carbs or alcohol), Pilocarpine (pillow car pine)
Term
Has SEs:
• Local side effects: diminished vision, burning, vascular congestion, lacrimation, retinal detachment (rare), decreased visual acuity, headache
• Systemic side effects: hypertension, tachycardia, salivation, nausea, vomiting, pulmonary edema
Definition
Cholinergic Agonists
Carbachol (carbs or alcohol), Pilocarpine (pillow car pine)
Term
Combination Eye Drops for Glaucoma Agents
Definition
Brinzolamide-brimonidione (Simbrinza)-Simba, Timolol-brimonidine (Combigan)-combo, Timolol-dorzolamide (Cosopt)- co soap
Term
Advantages to combination eye drops
Definition
Open-angle glaucoma often requires use of multiple pharmacological classes
• Potential out-of-pocket cost savings
• One vs. two eye drop bottles
-Availability of combination products:
• Carbonic anhydrase inhibitor/alpha agonist
• Alpha agonist/beta-blocker
• Beta-blocker/carbonic anhydrase inhibitor
Term
General Principles for Treatment of Glaucoma, what is first line
Definition
• Prostaglandin analogs generally considered first line
• Prostaglandin analogs, beta-blockers, alpha agonists and carbonic anhydrase inhibitors are all acceptable first line agents
• Choice of therapy should depend on risk vs. benefit ratio
• Nonselective beta-blockers more effective at lowering IOP compared to selective beta-blockers, but more adverse reactions
• Patients may require more than one class of topical agents for glaucoma if one class is not sufficient in achieving target IOP
Term
how do Carbonic anhydrase inhibitors work
Definition
reduce aqueous humor
Term
how do Beta blockers work
Definition
reduce aqueous humor production
Term
how do cholinergic agonists work
Definition
increase aqueous humor outflow
Term
how do prostaglandins work
Definition
increase aqueous humor outflow
Term
Antibiotics usage for types of eye infections
Definition
• Topical use for active bacterial eye infection or prophylaxis (pre- and postoperatively)
• Oral use for preseptal cellulitis
• Intravenous use for orbital cellulitis
• Intravitreal use for endophthalmitis
• Common bacteria causing eye infection include S. aureus, H. influenza,
S. pneumonia, and P. aeruginosa
Term
types of antibiotics used for eye infections
Definition
• Aminoglycosides • Fluoroquinolones • Macrolides
• Sulfa analogs
• Miscellaneous
Term
Aminoglycoside agents
Definition
gentamicin, tobramycin, neomycin (available with polymyxin B)
Term
Aminoglycoside MOA
Definition
interferes with bacterial protein synthesis by binding 30S ribosomal subunit leading to defective bacterial cell membrane

gentamicin, tobramycin, neomycin (available with polymyxin B)
Term
Bacterial coverage: predominately gram negative coverage, gentamicin and tobramycin active against pseudomonas
Definition
aminoglycosides
gentamicin, tobramycin, neomycin (available with polymyxin B)
Term
has SEs:
• Local side effects: burning sensation, irritation, corneal ulcer (1%)
• Systemic side effects: <1% hallucination, purpura, thrombocytopenia
Definition
aminoglycosides
gentamicin, tobramycin, neomycin (available with polymyxin B)
Term
Fluoroquinolones Agents
Definition
besifloxacin, ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin, ofloxacin
Term
Fluoroquinolones MOA
Definition
DNA gyrase inhibitor—DNA gyrase essential for DNA replication, transcription, repair, recombination, replication, and transcription

besifloxacin, ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin, ofloxacin
Term
Has SEs:
• Local side effects: blurred vision, burning sensation, chemical conjunctivitis, pain, pruritus, redness, photophobia, lacrimation, swelling, stinging
• Systemic side effects: nausea, dizziness, Stevens- Johnson syndrome and toxic epidermal necrolysis (both rare)
Definition
Fluoroquinolones
besifloxacin, ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin, ofloxacin
Term
has bacterial coverage:
• Some gram-positive coverage, not active for s. pneumonia
• Gram-negative coverage including pseudomonas
Definition
Second generation fluoroquinolones: ciprofloxacin and ofloxacin (ciprofloxacin covers pseudomonas)
Term
has bacterial coverage:
• Better gram-positive coverage compared to second generation including s. pneumonia
• Similar gram-negative coverage compared to second generation, variable resistance to pseudomonas (non-preferred)
Definition
Third generation fluoroquinolones: levofloxacin, gatifloxacin and moxifloxacin
Term
Macrolides agents
Definition
azithromycin and erythromycin
Term
Macrolides MOA
Definition
inhibits RNA-dependent protein synthesis by binding to 50S ribosomal subunit, leading to blockade of transpeptidation
azithromycin and erythromycin
Term
Bacterial coverage: gram positive and negative coverage
Definition
Macrolides
azithromycin and erythromycin
Term
Has SEs:
• Local side effects: irritation, blurred vision, decreased visual acuity, eye pain
• Systemic side effects: uncommon, but facial edema, nasal congestion, urticarial, skin rash, dysgeusia, and xeropthalmia have been reported
Definition
Macrolides
azithromycin and erythromycin
Term
Trimethoprim and Polymyxin B MOA
Definition
• Trimethoprim: blocks production of tetrahydrofolic acid from dihydrofolic acid by binding to and reversibly inhibiting the enzyme dihydrofolate reductase therefore interrupting biosynthesis of nucleic acids and proteins
• Polymyxin B: increases permeability of bacterial cell membrane by interacting with the phospholipid components of the membrane
Term
Has SEs:
• Local side effects: burning sensation of eyes, eyelid edema, eye redness, lacrimation, stinging
• Systemic side effects: dermatological circumocular rash
Definition
Trimethoprim and Polymyxin B
Term
General Principles of Optic Antibiotics
Definition
-Bacterial conjunctivitis usually self-limiting and optic antibiotics generally not recommended
• May consider if no improvement of symptoms in 1–2 days
• Topical antibiotics may shorten course of infection if used prior to day 6
• Treatment with optic antibiotics generally for 5–7 days if necessary
-Little evidence to support one topical antibiotic is more effective than the other
-Topical fluoroquinolones non-preferred due to higher known resistance rates to this drug class—exception is contact lens wearers, where pseudomonal infection is more common
Term
how does Ciprofloxacin work
Definition
DNA gyrase inhibitor
Term
how does Trimethoprim/polymyxin B work
Definition
Interrupts protein synthesis and increases permeability of bacterial cell membrane
Term
how does tobramycin work
Definition
Binds to 30S ribosomal subunit to interfere with protein synthesis
Term
how does erythromycin work
Definition
Binds to 50S ribosomal subunit to interfere with protein synthesis
Term
Allergic Conjunctivitis
Definition
• Allergen exposure through contact of surface of the eye
• Type I immunoglobulin E (IgE) mediated hypersensitivity reaction
• Response to allergen mediated through mast cell, histamine released leading to vasodilation, vasopermeability, and itching
• Symptoms: ocular pruritus, burning, redness, eyelid edema
Term
3 types of allergic conjunctivits
Definition
1. Acute allergic conjunctivitis
2. Seasonal allergic conjunctivitis
3. Perennial allergic conjunctivitis
Term
Treatment of Allergic Conjunctivitis
Definition
• Allergen avoidance
• Cold compresses
• Do not rub eyes
• Artificial tears
• Stop the use of contact lens
• Topical therapies
- Vasoconstrictor/antihistamine
- Antihistamine with mast cell stabilizing properties
- Mast cell stabilizers
- Non-steroidal anti-inflammatory drugs
- Glucocorticoids
Term
Antihistamine MOA
Definition
competitively blocks histamine receptors and inhibits release of histamine from mast cells, typically with histamine-1 receptor selectivity
Term
Antihistamine With Mast Cell Stabilizing Properties MOA
Definition
• Mast cell stabilizers inhibit the release of histamine, tryptase, and prostaglandin D2 (PGD2) through inhibition of mast cell degranulation
Term
has SEs:
• Local side effects: blurred vision, dry eyes, burning, conjunctivitis, eyelid edema, eye pain, pruritus, keratitis, hyperemia
• Systemic side effects: headache, dysgeusia, nausea, cold symptoms, weakness, back pain, cough, rhinitis, sinusitis
Definition
Antihistamine With Mast Cell Stabilizing Properties

Alcaftadine- all caf to dine (Lastacaft), Azelastine- a zealous shrine (Optivar), Bepostatine- be poster time (Bepreve), Emedastine- emmediate time (Emadine), Epinastine- epi no time (Elestat), Ketotifen- keto fan (Alaway, Zaditor), Olopatadine- old pat and dine (Pataday, Patanol)
Term
has considerations:
may require two weeks of therapy prior to assessing the full efficacy of therapy
Definition
Antihistamine With Mast Cell Stabilizing Properties


Alcaftadine- all caf to dine (Lastacaft), Azelastine- a zealous shrine (Optivar), Bepostatine- be poster time (Bepreve), Emedastine- emmediate time (Emadine), Epinastine- epi no time (Elestat), Ketotifen- keto fan (Alaway, Zaditor), Olopatadine- old pat and dine (Pataday, Patanol)
Term
Ophthamic Antihistamine agents
Definition
Alcaftadine- all caf to dine (Lastacaft), Azelastine- a zealous shrine (Optivar), Bepostatine- be poster time (Bepreve), Emedastine- emmediate time (Emadine), Epinastine- epi no time (Elestat), Ketotifen- keto fan (Alaway, Zaditor), Olopatadine- old pat and dine (Pataday, Patanol)
Term
benzalkonium chloride
Definition
preservative in some Ophthamic Antihistamine agents that may cause opthalmic reacxtions
Term
Combination Products for Allergic Conjunctivitis MOA
Definition
• Vasoconstrictor/antihistamine
• Vasoconstrictor component leads to vasoconstriction and decreased conjunctival edema through activation of postjunctional, alpha-adrenergic receptors in blood vessels
Term
Combination Products for Allergic Conjunctivitis agents
Definition
naphazoline and pheniramine (brand names include Naphcon A, Opcon A, Visine A)
Term
use _____ with caution in patients with cardiovascular abnormalities or hypertension, diabetes, hyperthyroidism, and local infection or injury
Definition
naphazoline
Term
has SEs:
mydriasis, tingling sensation of eye
Definition
Combination Products for Allergic Conjunctivitis
naphazoline and pheniramine (brand names include Naphcon A, Opcon A, Visine A)
Term
has considerations:
use of the vasoconstrictor component longer than two weeks may lead to rebound hyperemia; may refrigerate eye drops
Definition
Combination Products for Allergic Conjunctivitis
naphazoline and pheniramine (brand names include Naphcon A, Opcon A, Visine A)
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