Ocular Pharm Flashcards
How much of drops are lost to evaporation
25%
Bioavability
The percent of unchanged drug that gets to the desired site.
Tear layer characterisitics
Lipid=lipid soluble. Aqueous=water soluble, mucus=both water/lipid soluble
Corneal layer characteristics for drug penetration
Endothelium and epi=lipid soluble. Stroma=water sol
What type of drugs will penetrate best
small, uncharged, lipid soluble molecules. Most formulated as weak bases.
What route has the best bioavailablity
IV route
Where are parasympathetic cell bodies located
Craniosacral. PCS.
Where are sympathetic cell bodies located
Thoracic-lumbar.
NT for preganglionin in Para
Acetylcholine, has longer preganglionic neuron
NT for pre ganglion in symp
Acetylcholine, has shorter preganglionic neuron
Which autonomic pathway has longer post ganglionic
sympathetic
NT for post ganglion Parasympathetic
acetylcholine
NT for post ganglion sympathetic
norepinephrine and epinephrine.
Functions of parasympathetic nervous system (muscarinic)
Rest/digest
Wet!!
bronchoconstriction/ miosis (constriction)
SLUD = salivation, lacrimation, urination, defecation
Dilator of iris sympathetic function and receptor
alpha 1. Dilates
CB vasculature SNS function and receptor
Alpha 2. Decreaes aqeuosu
Ciliary Muscle vasculature SNS function and receptor
B2. relaxes
Trabec Mesh SNS function and receptor
B2. Increases outflow
NPCE SNS function and receptor
B1 and B2. Increases outflow.
What structures in the eye receive Parasympathetic innervation?
Iris, ciliary muscle, and lacrimal gland.
Pilocarpine
_% IOP reduction? how many times per day?
Direct acting cholinergic agonist. First every glaucoma drug. Stimulates the longitudinal fibers of the CB which pulls on the scleral spur and opens up the TM to increase outflow and reduce IOP
30% reduction
short half life so 4x/day
What pilo do you use with Adies tonic pupil
0.125%
Side fx of pilocarpine
brow ache, HA, myopic shift, can cause angle closure or RD or cataracts.
“dimmed vision” in cataracts
Edrophonium (Enlon)
Used to diagnose MG– Tensilon test. If ptosis improves 1-2 min after injection = (+) MG.
Neostigmine (prostigmin)
Treatment for MG or limb strength evaluation.
Echothiophate (phospholine)
Irreversible ACHE inhibitors. Can be used to diagnose or treat accommodative esotropia.
Pyridostigmine (mestinon)
to treat MG.
Pralidoxime
- Used for overdose of indirect cholinergic agonists. Only -works on IRREVERSIBLE AchE agents (echothiphate)
- binds to irreversible AchE agent, to allow acetylcholinesterase to break down Ach
- antidote for overtreatment of MG
Scopolamine (effects, side fx, contraindication)
Cholinergic antagonist. Used for motion sickness. High incidence of crossing Blood brain barrier = likely CNS toxicity
side fx: hallucination, amnesia, unconsciousness, confusion, restlessness, incoherence, vomit, urinary incontinence
Which cholinergic antagonist has the fastest onset and shortest duration?
tropicamide
Atropine
- onset
- duration
- used for what tx?
- side fx
- caution in what population
Most potent.
- 60 to 180 minutes onset
- 7 to 12 days duration for cycloplegic fx
- amblyopia tx– put on good eye = Penalization
- safe; dangerous if incorrect dosage
- sick, handicapped, Down Syndrome, elderly, small kids under 3
Who should you dilate with caution?
THINK. Thyroid. Iris fixed IOL. Narrow angle. Kids (DS)
which drug do you use for anterior uvieits?
homatropine. It dilates the iris, reduces pain, and stabilizes the blood aqueous barrier.
How long does Atropin work
7-10 days
How long does scopolamine work
3-7 days
How long does homatropine work
1-3 days
How long does cyclopentolate work
24 hours
How long does tropic amide work
4-6 hours.
Botox
Anticholingeric and NMJ.
Norephinerphein vs. Epinerphine
Norepinephrine does not work on B2 receptors.
Phenylephrine
Sympathetic agonist. 2.5% routinely used for dilation. Acts on alpha 1 receptor with no affect on B. Allows dilation without any SE.
Which is the weird on in sympathetic NS
Alpha 2
When to give Beta blocker
In the morning
Who should you be cautions with BB
diabetic (hid hypo signs), lungs, Heart, hyperthyroidism, MG.
Short term escape
lowers initially and then raises
Long term drift
IOP starts to gradually rise
Do you get short term escape and long term drift with BB
YES.
Cosopt
Timolol and dorzolamide
Combigan
Timolol and briminoladine
Alpha 2 agonist action
Act to decrease production and increase outflow
SE of CAI
Aplastic anemia, thrombocytopenia, agranuloctyopenia, metallic taste, metabolic acidosis.
CI for CAI
SULFA BASED
Prostaglandin Analogs
Acts on FP receptors (PGF2alpha) on the ciliary muscle which causes reduction of neighboring collage (using MMP), decreasing resistance with the uveoscleral meshwork. Also acton on skin receptors and hair follicles.
When to dose prostaglandins
bedtime
SE of prostaglandins
Iris herterochromia, darker lashes, dark pigment around the eyes.
Reduction in IOP of glaucoma drugs
Apraclondine (30-40), prost (33), Pilo (30). BB (25), biminodine and dorzolamid (18).
How do topical ocular anesthetics work
Block nerve conduction and change membrane potential by stopping the influx of Na = no depolarization
Amides anesthetics
Go inside. Injectable. Liver.
longer duration of action
Esters anesthetics
All topical anesthetics. Metabolized locally. short duration of action
Proparacaine
Ester anistehtic. Lasts 10-20 minutes.