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184 terms

Ocular Pharm MT1

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FDA pregnancy risk factor
starting point; doesn't address the safety while breast-feeding
Fluorescein
C, excreted in breast milk, avoid in 1st trimester (small dose and 1 time, okay for us to use)
Lissamine Green
no FDA rating
Rose Bengal
no FDA rating
proparacaine
C, safe use not estab
lidocaine
B, AAP says its compatible w/ breastfeeding. local anesthetics generally cross into breast milk, 40% (don't worry unless patch or IV)
tetracaine
C, WHO- compatible with breastfeeding
phenyephrine
C, use punctal plugs
Atropine, homatropine
C, AAP says compatible with breastfeeding
cyclopentolate
C
tropicamide
c
naphazoline
C, ocular decongestant
oxymetazoline
no FDA rating, ocular decongestant
tetrahydrozoline
no FDA rating, ocular decongestant
Azelastine
C, ocular antihistamine, not reccomm when breastfeeding. antihistamines generally appear in breast milk
Cromolyn
B, ocular antihistamine
emedastine
B, ocular antihistamine
epinastine
C, ocular antihistamine
ketotifen
C, ocular antihistamine
lodoxamide
B, for allergic conjunctivitis
nedocromil
B, for allergic conjunctivitis
olopatadine
C, for allergic conjunctivitis
pemirolast
C, for allergic conjunctivitis
Corticosteroids, cycloplegics, sulfas, fluoroquinolones
all preg C category
Dexamethasone
C, corticosteroid
difluprednate
C, corticosteroid
Fluorometholone
C for class related, no indiv FDA rating
loteprednol
C, corticosteroid
rimexolone
C, corticosteroid
bromfenac
C, NSAIDs (thin blood causes placenta to detach)
flurbiprofen
B, NSAIDs (thin blood causes placenta to detach)
diclofenac
D, NSAIDs (thin blood causes placenta to detach)
nepafenac
C, NSAIDs (thin blood causes placenta to detach)
ketorolac
D, NSAIDs (thin blood causes placenta to detach), AAP says compatible w/ breast feeding
cyclosporine (restasis)
C, for dry eyes, excreted into breast milk. safer to use Artificial tears( A or B)
Dipivefrin
B, for glaucoma
Apraclonidine
C, for glauc
Brimonidine
B, for glaucoma
Echothiophate
C, for glaucoma
pilocarpine
C, for glaucoma
betaxolol
C, for glaucoma
carteolol
C, for glaucoma
levobunolol
C, for glaucoma
metipranolol
C, for glaucoma
timolol
C, for glaucoma, AAP says compatible for breastfeeding
acetazolamide
C, for glaucoma, AAP says compatible for breastfeeding
brinzolamide
C, for glaucoma
dorzolamide
C, for glaucoma
methazolamide
C, for glaucoma
latanoprost
C, for glaucoma
bimatoprost
C, for glaucoma
travoprost
C, for glaucoma
Aspirin
D. AAP caution with bf. just avoid it during preg and lactation
Acetaminophen
B, AAP says compatible with bf eventhough known to cross into breast milk
ibuprofen
D, compatible w/ breastfeeding
naproxen
C, analgesic, compatible w/ breastfeeding
codeine
C, analgesic, compatible w/ breastfeeding
hydrocodone
C or D depending on how much is taken. Avoid while breastfeeding
acyclovir
B, anti-infectives, compatible w/ breastfeeding, drug easily crosses placenta
valacyclovir
B, anti-infective,appears to be compatible with breastfeeding
famciclovir
B, anti-infective, avoid while breastfeeding
Trifluridine
C, anti-infective
Natamycin
C, antifungal. Manufacturer rec. that drug only rx preggies in life or death
all pencillins (amoxicillin, amox/clavulanate, ampicillin, penicillin VK, dicloxacillin) are
B, AAP says compatible w/ breastfeeding
Clindamycin
B, for bacterial infections, AAP says compatible w/ breastfeeding
bacitracin
C, for bacterial infections
sulfonamides
C (SMX/TMP included), compatible w/ breastfeeding in healthy infant, risky in THIRD trimester (jaundice, kernicterus, hemolytic anemia)
cephalosporins
B, compatible with breastfeeding
cefadroxil
B, compatible with breastfeeding
cefuroxime
B, compatible with breastfeeding
cefphalexine
B, compatible with breastfeeding
all fluoroquinolones are
C
besifloxacin
C
ciprofloxacin
C, AAP says compatible w/ breastfeeding
gatifloxacin
C,
levoflozacin
C
moxifloxacin
C
ofloxacin
C, AAP says compatible w/ bf
azithromycin
B, oral form in breast milk, no topical data
clarithromycin
C,
erythromycin (excludes estolate)
B, don't rx estolate to preggies
gentamycin
C, AAP says compatible w/ bf
tobramycin
C
neomycin
C
tetracycline
D, avoid during pregnancy. But AAP says compatible w/ breastfeeding
doxycycline
D, avoid during pregnancy. But AAP says compatible w/ breastfeeding
Preg Cat B
lidocaine, cromolyn & emedastine (antihistamine), lodoxamide & nedocromil (allergic conjunctivitis), flurbiprofen (NSAID), dipivefrin & brimonidine (glauc), acetaminophen, cyclovirs, penicillins, cephalosporins, clindamycin, azithromycin, erythromycin
Preg Cat D
ketorolac, diclofenac, aspirin, ibuprofen, tetracycline, doxycycline, some sulfonamides (diclofenac and aspirin not compatible w/ breastfeeding but the rest are)
preg Cat D but compatible w/ breastfeeding
ketorolac, ibuprofen, tetracycline, doxycycline, sulfonamides (in healthy infant)
Anti-infectives for pregs or lactators
1. effective (not excessive doses)
2. punctal plugs
3. culture and sensitivity tests
Reason for culture and sensitivity tests (for pregs and lactators)
-confirm drugs are effective
-assist in better preg risk factor ratings
Geriatric patients- eyelid laxity/ectropion can ? retention time in conj sac, exacerbating local drug effects/cause toxicity.
increase
Minimum font size for visually impaired
12 point
Which font is better for visually impaired
san serif (no serif)
pharmacokinetics
distinct drug processes, factors, and processes whereby drugs are absorbed and distributed in the body, biotransformed, metabolized, and excreted from the body
Drug distrib over time and bioavail of drug at target can be predicted by
interrelationships of compartments and barriers of eye
What does avascularity in the eye enable?
direct route for ocular drugs w/o high absorption into systemic circulation
Tear Film
3 layers:
1. outer: oil from meibomian, retards evaporation, saline and meds can wash away lipids
2. central: aqueous, 95%, 7mm,thin centrally after blink. TBUT healthy 25 sec
3. basal (inner): glycoproteins from goblet cells of conj. Mucous, hydrophilic coating
What proteins do the tears contain (5)?
lysozymes, lactoferrins, gamma globulins, and other immune factors
What do tears supply to the corneal epithelium?
oxygen
Tear pH
7.4
Normal volume of tear layer
8-10mcl
normal tear flow is
0.5-22mcl/min
What kind of drugs can penetrate the tight junctions (zona occludens)?
lipid-soluble, non-ionized
what kind of drugs have longer T1/2 once in epithelium
lipophilic
How can a drug effectively penetrate the cornea?
balancee of hydrophilic and lipophilic properties
What part of the cornea stores the most drug (that partition lipid media)?
epithelium
The stroma has collagen bundles and keratocyts- which sotre hydrophilic drugs?
collagen- hydrophilic
keratocytes- lipophilic
What cornea structure is major ocular depot for hydrophilic drugs
stroma
Does the endothelium have tight junctions?
no
What can pigment granules (in iris) in the eye store?
lipophilic drugs
How do drugs enter and exit the aqueous humor?
enter- blood stream or cornea
exitt- blood or Schlemm's Canal
How do systemic drugs get into aqueous?
no tight junctions in caps, pass thru CB and diffuse into iris
What is the major ocular source of drug metab enzymes (2 rxns to start drug breakdown and removal from eye)?
ciliary body
How does CB enzymes break down and remove drugs?
phase 1 CYP 450 (oxidation and reduction); phase 2- conjugation; 3- metab/drugs removed thru uveal circulation blood flow.
role of lens with drugs
a barrier to prevent drugs from entering vitreous. anterior epithel can be damaged by drugs. lipophilic can slowly pass but not hydrophilic
What 3 classes of drugs can lead to cataract formation?
miotics, steroids, and phenothiazines. (MSP-- cataracts. More senile people get cataracts)
Blood-retinal barrier
tight junction in RPE, prevents hydrophilic drugs from passing
What is actively transported from the blood to the retina
glucose
What 2 pathways can the bloodstream remove drugs/metabs from eye?
1. retinal blood vessels (vitreous and retina) by active transport
2. uveal blood vessels (CB and iris) by bulk transport
Compartment
a region of tissue or fluid thru which a drug can diffuse and equilibrate w/ relative ease. (transparent- no direct blood supply)
Why does is take more time for a drug to diffuse between compartments than w/in a compartment?
each compartment is separated by a barrier
barrier
a region of lower permeability or restricted diffusion that exists between 2 compartments
What is the barrier between the tears and the cornea?
the epithelium
Fick's Law of diffusion
the rate of diffusion across a barrier is proportional to the concentration gradient between the compartments on either side of the barrier.once concentrations are equal, no drug penetrates
What does corneal absorption of drug depend on in first 10-20 min?
tear film concentration
zero-oder kinetics
release of drug is constant over time and is independent of the concentration present; occurs when there's a rate limiting barrier (carrier)
first-order kinetics
drug movement directly proportional to concentration difference across barrier. (passive); rate changes
A drug that's metabolized to inactive form inside eye?
loteprednol (corticosteroid)
bioavailability
amt of drug present at desired receptor site
ED50
(an effective dose) dose level producing a response that's 50% of maximum response
complex drug molecules will loose
stability in solution form at some point in time. Some drugs must be dissolved or prepared immediately before use
What 4 factors can affect the stability of drugs?
Oxidation and heat can break down drugs. Microbial contamination. Drugs in acidic medium can be more stable
When you combine active drug, preservative, and vehicle it results in what kind of solution? give number
hypotonic, less than 290 mOsm
290mOsm is equal to %
0.9% saline (NaCl)= normal physiologic osmolarity
What is added to adjust osmolarity?
salts, buffering agents, certain sugar
preservatives
to prevent growth of microorganisms
BAC- Benzalkonium chloride (surfactant) and Benzethonium chloride
antimicrobial(disrupt plasma membrane). toxic effects on tear film and corneal epithelium. allergies
chlorhexidine
block microbial metab. less effect on cornea
mercurial compounds like thimerosal
blocks microbial metab. most effective in weak acid solutions. no effect on tear film stability. pts. allergis
chlorobutanol
block microb metab.less effective than BAC but no known allergies. not effective alone. combine w/ EDTA
Parabens
block microb metab. used in AT and non-med ointments. allergies. unstable at high pH.
stabilzed oxychloro-complex & sodium perborate (oxidation)
in AT, turns into water and NaCl or water and oxygen--- non toxic!
EDTA
assists thimerosal, BAC, and others. can cause dermatitis. also has antioxidant props
antioxidants
delay deterioration of product by oxygen in air
Vehicles
aid in achieving appropriate tonicity, buffering, and viscosity.
PVP-polyvinylpyrrolidine
non-ionic polymer w/ binding and detox properties. no immune rejection. viscosity
PVA-polyvinyl alcohol
water soluble viscosity. 1.4%.non-irritating and helps heal corneal epi and dry eye
hydroxypropyl methylcellulose
viscosity enhancer. can increase tear film wetting time. help fluorescein and dexamethasone to get in cornea
carboxymethylcellulose
like hydroxypropyl methylcellulose but greater addhesion to mucins. in AT
sodium hyaluronate
high viscosity then changes w/ blinking. stabilize tear film
Gel-forming systems
large molecules. aqueous drop reversibly gels when hits tear film. enhance corneal penet. & prolong action
polyionic vehicles
vary in lipophilic nature and binding. enhance bioavailability of lipophilic drugs like corticosteroids
polyacrylic acids
have pseudoplastic properties where viscosity decreases w/ blinking. good microadhesive and wetting
ointment bases
white petrolatum and liquid mineral oil. increase ocular contact time
colloidal systems
liposomes. lipid bilayers surrounding aqueous compartments. prolong drug at site w/ less toxicity
cyclodextrins
cyclic oligosaccharides that are water soluble. lipid solubel drugs incenter. improve solubility,stability
SCLs and drugs
absorb drug and slowly release them
Only drug to penetrate eye in effective concentration for retinal, ON
NSAIDs
commercial drop size
25-70mcl
opthalmic solution and ointment. which do u apply 1st?
ophthalmic solution, 5-10 min, then ointment
what can ointments be used for
after surgery to reduce antibiotic and steroid, for superficial corneal abrasions and ulcers
Lid scrubs for
tx blepharitis, clean lid margins
Gels-advantage and disadvantage
ad-qDay
disad-haze, SPK,hypotensive
hydrogel CLs drug release is what order?
first order- diffusion
where is cotton pledgets saturated w/ ophthalmic solutions inserted into
inferior conj fornix
AT insert= pellet of hydroxylpropyl cellullse. Use?
place in inferior conj fornix for dry eye but can cause blurring and fb sensation
continuous flow devices for
large volume irrigation of eye
3 places for injections
1. periocular/peribulbar
2. intracameral (ant/post chamber)
3. intravitreal
eye typically retains how much fluid of a med drop
10mcl. no value in dropping 2 in a rrow
when can you do nasolacrimal compression
3-5 mun after drops
Schedule 1
not commercially available
schedule 2
strict limitation due to high abuse. can't be refilled
schedule 3
abuse potential. OD rx refilled qs 5x in 6mo
schedule 4
None under OD scope
schedule 5
tx cough or diarrhea
what are the FDA req for generics?
stability, purity, strength (potency), and quality
IMDA for good pt compliance
Introduce and Indicate
Mechanism of Action
Dosage regimen
ADE, Ask questions, Anything else
Fluorescein sodium (flu-glo, 0.6%)
stains corneal defects not intact cornea. appear yellow/orange on tear film
Fluorexon (fluresoft, 0.35%)
less fluorescent than fluorescein. stain degenerated cells and mucous. avoid w/ water CLs to prevent staining
indocyanine green (IC-green, 25mg powder for injection, 10mL solvent)
water-soluble tricarboccyanine. contains sodium iodide. for retinal and choroidal neo in ARMD. IV only- 40mg of dye in 2mL of solvent
lissamine green 1.5mg strips
for: dry eye, recurrent corneal erosions, herpes ulcers
no ADEs reported. pt blinks after
rose bengal 1.3mg/strip
iodine deriv of fluorescein.
stains: living cultured cells, dead cells, mucus strands. 1 hr b4 replacing lens. pt blinks after
why is the use of rose bengal potentially problematic when used to identify epithelial herpetic corneal ulcers?
antiviral activity- preculde a positive result. identify microorg b4 rose bengal