C, excreted in breast milk, avoid in 1st trimester (small dose and 1 time, okay for us to use)
B, AAP says its compatible w/ breastfeeding. local anesthetics generally cross into breast milk, 40% (don't worry unless patch or IV)
C, ocular antihistamine, not reccomm when breastfeeding. antihistamines generally appear in breast milk
C, for dry eyes, excreted into breast milk. safer to use Artificial tears( A or B)
all pencillins (amoxicillin, amox/clavulanate, ampicillin, penicillin VK, dicloxacillin) are
B, AAP says compatible w/ breastfeeding
C (SMX/TMP included), compatible w/ breastfeeding in healthy infant, risky in THIRD trimester (jaundice, kernicterus, hemolytic anemia)
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.
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
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
The stroma has collagen bundles and keratocyts- which sotre hydrophilic 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)?
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)
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
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
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
release of drug is constant over time and is independent of the concentration present; occurs when there's a rate limiting barrier (carrier)
drug movement directly proportional to concentration difference across barrier. (passive); rate changes
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
BAC- Benzalkonium chloride (surfactant) and Benzethonium chloride
antimicrobial(disrupt plasma membrane). toxic effects on tear film and corneal epithelium. allergies
mercurial compounds like thimerosal
blocks microbial metab. most effective in weak acid solutions. no effect on tear film stability. pts. allergis
block microb metab.less effective than BAC but no known allergies. not effective alone. combine w/ EDTA
stabilzed oxychloro-complex & sodium perborate (oxidation)
in AT, turns into water and NaCl or water and oxygen--- non toxic!
non-ionic polymer w/ binding and detox properties. no immune rejection. viscosity
water soluble viscosity. 1.4%.non-irritating and helps heal corneal epi and dry eye
viscosity enhancer. can increase tear film wetting time. help fluorescein and dexamethasone to get in cornea
large molecules. aqueous drop reversibly gels when hits tear film. enhance corneal penet. & prolong action
vary in lipophilic nature and binding. enhance bioavailability of lipophilic drugs like corticosteroids
have pseudoplastic properties where viscosity decreases w/ blinking. good microadhesive and wetting
liposomes. lipid bilayers surrounding aqueous compartments. prolong drug at site w/ less toxicity
cyclic oligosaccharides that are water soluble. lipid solubel drugs incenter. improve solubility,stability
what can ointments be used for
after surgery to reduce antibiotic and steroid, for superficial corneal abrasions and ulcers
AT insert= pellet of hydroxylpropyl cellullse. Use?
place in inferior conj fornix for dry eye but can cause blurring and fb sensation
IMDA for good pt compliance
Introduce and Indicate
Mechanism of Action
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