Ophthalmic Pharmacology Flashcards

1
Q

describe ocular barriers to drugs

A
  1. tear film: dilutes drugs
  2. cornea: hydrophobic epithelium, hydrophilic stroma
  3. blood eye barrier: prevents protein molecules from entering eye
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2
Q

describe route choice for ophtho drugs

A
  1. topical: ocular surface to posterior lens capsule; can reach high concentrations
    -1 drop is already 2-3 times what the eye can effectively absorb = NEVER a reason to give 2 drops back to back!!! will actually reduce overall absorption of the drug bc pisses off eye more
  2. systemic: lids, orbit, posterior segment, perforated globe
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3
Q

describe how drugs penetrate the cornea

A

must be both lipophilic and hydrophilic!! (chloramphenicol is great at this)

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4
Q

describe how the blood eye barrier affects drugs

A

systemic drugs enter via blood vessels of uvea but if hydrophilic will have poor penetration

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5
Q

describe the blood eye barrier as relates to treating uveitis

A

uveitis breaks down blood eye barrier making it easier for more drugs to cross

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6
Q

describe the posterior blood eye barrier

A

the choroid is well-vascularized and most infectious diseases affect the choroid so most systemic drugs work well

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7
Q

describe drug formulations

A
  1. solutions: most common
    -usually water-soluble salts, sometimes oil based
    -easily contaminated and usually preserved
  2. suspensions: most steroids
    -sterile particulate solid + sterile liquid since drug is insoluble
    -shake well!! 20x or 15 seconds!!
    -generics NOT always same as original
    -failure to shake is a major cause of short term treatment failures
  3. ointments: most are mineral oil/petroleum
    -drug mixed into melted vehicle then cooled
    -greasy, blur vision
    -preservatives not required
    -modern ointments DONT slow wound healing
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8
Q

where do topical drugs go?

A
  1. onto face: most of it
    -normal tear volume is 7ul
    -most drops are 35-50ul so one drop is more than enough!
    -drops typically gone in 5 min
  2. down naso-lacrimal duct: systemic absorption
    -anything >7ul also goes out via NL duct
  3. conjunctival absorption via blood vessels = also systemic
  4. goal is transcorneal absorption into aqueous humor but most doesn’t actually go this route
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9
Q

how do you administer eye drops?

A
  1. 1 drop only!
  2. wait 5 min between drops!!
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10
Q

what determines the frequency of topical meds?

A
  1. vehicle: ointments less frequent than solutions
  2. prophylactic versus treating established disease
  3. spacing: must leave 5 min between drops of solution and 30 min between drops of ointment
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11
Q

what makes drugs go bad?

A
  1. expiration date: label is for UNOPENED bottle properly stored; once break seal they only last for about a month
  2. light, heat, air exposure: DONT place in bathroom or kitchen window (light, temp, humidity vairy widely)
  3. bacteria, fungi
  4. improper application: touch eye, cap on table, dirty hands; ascending contamination

all above is why eye drops are in tiny little bottles

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12
Q

what are the 2 ways to dilate and eye and the 2 ways to constrict the eye?

A

dilation:
1. parasympatholytic (anticholinergic)
2. sympathomimetics

constriction:
1. parasympathomimetics (cholinergic)
2. sympatholytics

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13
Q

describe topical mydriatics that paralyze the sphincter muscle and passively dilate the eye (2) (LO)

A

anti rest and digest, anti SLUD, paralyze the sphincter muscle and passively dilate the eye

  1. 1% tropicamide
    -short acting (1-2 hours) for eye exams
    -no pain relief
    -takes 20 min to fully dilate
  2. atropine:
    -long acting (hours to days)
    -pain relief by paralyzing sphincter
    -prevents posterior synechiae
    -stabilizes blood aqueous barrier
    -ointment to prevent drooling - very bitter
    (ointment gone off market so put finger on NL duct while administering)

-can exacerbate low tear production
-can slow gut and cause colic and kill horse!! keep listening to gut sounds when using with a horse to ensure not slow down too much

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14
Q

describe sympathomimetic drugs to dilate the eye

A

phenylephrine 2.5% or 10%

  1. increase HR
  2. cause cause serious systemic effects
  3. activates dilator muscles
  4. typically a preop cataract drug or HORNERS diagnosis
  5. also creates local vasconstriction
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15
Q

when is the ONLY time you don’t want to dilate the eye?

A

if see glaucoma

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16
Q

describe topical anesthetics

A
  1. proparicaine HCL 05%, tetracaine
  2. refrigerate if won’t use in 1 month
  3. keep out of light! throw away if brown
  4. onset in seconds, peak in 5-10 min, lasts 30 min
  5. 1 drop every 1-3 min better than a flood
  6. canNOT be used as a therapy:
    -dries eyes, causes ulceration, delays healing, up-regulates pain receptors
17
Q

describe cholinergics

A
  1. increase outflow via TM
    2, contracts longitudinal ciliary muscle
  2. green means miotic!!
  3. use for dry eye and for glaucoma
18
Q

describe topical antibiotics

A
  1. chloramphenicol 0.5% solution or 1% ointment
    -for cat conjunctivitis (chlamydophila/mycoplasma)
    -septic keratitis/conjunctivitis with cocci
    -easily penetrates cornea
    -formerly resistant organisms are becoming sensitive again
  2. tetracyclines: cat conjunctivitis
    -terramycin/oxytetracycline with polymyxin B
  3. cefazolin 5.5% for gram + organisms
    -1 gram vial cefazolin
    -mix with 2.5 ml sterile water
    -put in 15ml artificial tears
  4. aminoglycosides: good for rods!
    -neomycin/polymyxin B combinations: good first choise as a prophylactic drug
    -bacitracin added to ointments, gramidicin to solutions
    -gentamicin and tobramycin: not prophy but only if rods are seen on corneal scrapings or if sensitivity testing indicates
  5. fluoroquinolones:
    -2nd gen: cipro, levo
    -1000x better against gram -, also aerobic gram +
    -use in septic keratitis with rods, cat conjunctivitis
    -not a first choice drug! some cocci are resistant

4th gen: retains gram - but even better gram + spectrum
-less likely to develop resistance and can kill non-replicating
-reserved for multi=drug resitant infections!!

19
Q

describe antiproteases

A

for melting corneal ulcers

  1. autologous plasma/serum
    -dispense in 1 or more red tops
    -sterile, keep fridge, lasts 1 week
    -1 drop topically every 1-4 hours
  2. topical oxytet
  3. oral doxy
  4. acetylcysteine and EDTA
20
Q

describe dosing tips for topical antibitoics

A

prophylactic: 2-3 times a day

septic conjunctivitis: 3-4 times a day

septic keratitis: every 1-2 hours

cytology guides initial choice:
-rods: ciprofloxacin, gentamicin, or tobramycin
-cocci: triple antibiotic or chloamphenicol
-both: cefazolin AND topical ciprofloxacin or tobramycin, possibly moxifloxacin (4th gen)

21
Q

describe topical antifungals

A
  1. almost exclusively for equine corneal fungal infections
  2. ointments are easier; if liquid usually use lavage tube
22
Q

describe xamples of topical antifungals

A
  1. natamycin 5% polyene
    -only commercially available agent
    -thick solution
    -poor penetration through inact epithelium
    -expensive!!
  2. compounded meds:
    -itraconazole ointment: good absorption even through intact epi, can’t use lavage tube
    -miconazole 1% solution: in DMSO (wear gloves), can be topically irritating
    -voriconazole: expensive but good activity against southern isolates
  3. if cannot afford to compound miconazole, can use OTC vaginal cream but can be irritating
  4. oral fluconazole:
    -aspergilla resistant
    -does not penetrate intact epi without DMSO so usually oral (good penetration orally)
23
Q

describe topical antivirals

A
  1. trifluridine: most effective, expensive, can be irritating
  2. idoxuridine- compounded
    -1/2 as effective, cheaper

both have to be given every 2-4 hours

  1. cidofovir: 1/2 as effective, BID dosing
24
Q

describe systemic antivirals

A
  1. L-lysine: 400-500mg/cat/day all at once or divided:
    -arginine competitior decreased viral replication
    -reduced recurrences, viral shedding, duration, severity
    -best is used at the start of an outbreak and during stress
  2. famcyclovir (famvir): 90mg/kg BID for 3 weeks
    -overall safe but hold back in patients with kidney or liver disease
    -reserve for refractory patients when topicals fail
25
Q

describe anti-inflammatories corticosteroids

A
  1. 0.1% dexamethasone: ointment, suspension, or in combo with neomycin and polymyxin B
    -neopolydex is often cheaper than dex alone
  2. 1% prednisolone acetate suspension
    -suspension = MUST SHAKE
    -equivalent strength to 0.1% dex
    -may have better intraocular penetration

must rule out infectious causes if using systemic steroids (unlike topical) but necessary for posterior disease!

26
Q

describe side effects of topical steroids

A
  1. delay corneal wound healing: DO NOT USE IF CORNEA ULCERATED
  2. reactivation of herpes keratitis
  3. lipid deposits in cornea
  4. iatrogenic cushing’s
27
Q

describe NSAIDS

A
  1. better in traumatic inflammation
  2. flurbiprofen sodium Ocufen 0.03%, diclofenac voltaren, bromfenec xibrom, keterolac acular
28
Q

what are the challenges of glaucoma meds?

A
  1. no ONE drug is effective in all types of glaucoma
  2. ideally selection based on mechanism of glaucoma
  3. goal is to keep IOP in safe range <20mmHg
  4. often also need surgery
29
Q

describe glaucoma drugs

A
  1. hyperosmotic diuretics
    -mannitol is 1st choice ONLY in pre-op lens luxation, otherwise now secondary to prostaglandin analogs
    -osmotic gradient dehydrates vitreous
    -additive to all other anti-glaucoma drugs
  2. prostaglandin analogs:
    -latanoprost
    -miosis is side effect
    -increases uveoscleral outflow
    -nothing can lower IOP in cats
    -first choice in angle-closure glaucoma
    -additive to all other anti-glaucoma drugs
    -AVOID in uveitis and anterior lens luxation
  3. carbonic anhydrase inhibitors
    -oral methazolamide or dichlorphenamide
    -decrease aqueous humor production
    -TID topical
    -additive to all other classes
  4. cholinergics
    -3rd choice to PGs and CAIs
    -increase outflow via TM
    -contracts longitudinal ciliary muscle
    -additive to every class
  5. beta-adrenergic blockers
    -3rd choice in some secondary glaucomas or as prophylactic
    -only mild effect in animals
    -decreases aqueous production, may increase outflow in dogs/cats (miosis)
    -additive to other classes except beta agonists
30
Q

describe dry eye treatment

A
  1. tear stimulants: T cell modulators
    -cyclosporine A
    -tacrolimus- wash hands after applying
  2. cholinergics for neurogenic dry eye, usually given in the food
    -replaces the parasympathetic neurotransmitter
  3. artificial tears:
    -mucin deficiency: cyclosporine (stimulates), others only mimic
    -lipid deficiency/blepharitis: oil based, sodium hyaluronate, and/or warm compresses for 5 min
31
Q

what doyou use for really bad pirmary corneal edema?

A

hyperosmotics 5% sodium chloride! can be irritating

for erosions secondary to corneal edema

32
Q

do any eye drops actually dissolve cataracts?

A

NO save your money for surgery

33
Q

sum up topical antibiotics for feline conjunctivitis

A
  1. usually due to chlamydia, herpes, mycoplasma so use:
    -tetracyclines
    -erythromycins
    -ciprofloxacin
    -chloramphenicol (watch fatal aplastic anemia)
  2. frequent dosing! BID to TID
34
Q

sum up topical antibiotics for corneal erosions

A

non-infected superficial epithelial loss: use a prophylactic treatment

-neomycin (aminoglycoside)/polymyxin combo routinely used

-bacitracin added to ointments

-gramicidin added to solutions

-gram negative and positive coverage

35
Q

sum up topical antibiotics for infected corneal ulcers

A
  1. aminoglycosides: gentamicin, tobramycin, neomycin OR
  2. fluoroquinolones: ciprofloxacin, ofloxacin, others
  3. combined with cefazolin
  4. want broad spectrum coverage