Ocular Pharm Flashcards
(152 cards)
1
Q
How much of drops are lost to evaporation
A
25%
2
Q
Bioavability
A
The percent of unchanged drug that gets to the desired site.
3
Q
Tear layer characterisitics
A
Lipid=lipid soluble. Aqueous=water soluble, mucus=both water/lipid soluble
4
Q
Corneal layer characteristics for drug penetration
A
Endothelium and epi=lipid soluble. Stroma=water sol
5
Q
What type of drugs will penetrate best
A
small, uncharged, lipid soluble molecules. Most formulated as weak bases.
6
Q
What route has the best bioavailablity
A
IV route
7
Q
Where are parasympathetic cell bodies located
A
Craniosacral. PCS.
8
Q
Where are sympathetic cell bodies located
A
Thoracic-lumbar.
9
Q
NT for preganglionin in Para
A
Acetylcholine, has longer preganglionic neuron
10
Q
NT for pre ganglion in symp
A
Acetylcholine, has shorter preganglionic neuron
11
Q
Which autonomic pathway has longer post ganglionic
A
sympathetic
12
Q
NT for post ganglion Parasympathetic
A
acetylcholine
13
Q
NT for post ganglion sympathetic
A
norepinephrine and epinephrine.
14
Q
Functions of parasympathetic nervous system (muscarinic)
A
Rest/digest
Wet!!
bronchoconstriction/ miosis (constriction)
SLUD = salivation, lacrimation, urination, defecation
15
Q
Dilator of iris sympathetic function and receptor
A
alpha 1. Dilates
16
Q
CB vasculature SNS function and receptor
A
Alpha 2. Decreaes aqeuosu
17
Q
Ciliary Muscle vasculature SNS function and receptor
A
B2. relaxes
18
Q
Trabec Mesh SNS function and receptor
A
B2. Increases outflow
19
Q
NPCE SNS function and receptor
A
B1 and B2. Increases outflow.
20
Q
What structures in the eye receive Parasympathetic innervation?
A
Iris, ciliary muscle, and lacrimal gland.
21
Q
Pilocarpine
_% IOP reduction? how many times per day?
A
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
22
Q
What pilo do you use with Adies tonic pupil
A
0.125%
23
Q
Side fx of pilocarpine
A
brow ache, HA, myopic shift, can cause angle closure or RD or cataracts.
“dimmed vision” in cataracts
24
Q
Edrophonium (Enlon)
A
Used to diagnose MG– Tensilon test. If ptosis improves 1-2 min after injection = (+) MG.
25
Neostigmine (prostigmin)
Treatment for MG or limb strength evaluation.
26
Echothiophate (phospholine)
Irreversible ACHE inhibitors. Can be used to diagnose or treat accommodative esotropia.
27
Pyridostigmine (mestinon)
to treat MG.
28
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
29
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
30
Which cholinergic antagonist has the fastest onset and shortest duration?
tropicamide
31
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
32
Who should you dilate with caution?
THINK. Thyroid. Iris fixed IOL. Narrow angle. Kids (DS)
33
which drug do you use for anterior uvieits?
homatropine. It dilates the iris, reduces pain, and stabilizes the blood aqueous barrier.
34
How long does Atropin work
7-10 days
35
How long does scopolamine work
3-7 days
36
How long does homatropine work
1-3 days
37
How long does cyclopentolate work
24 hours
38
How long does tropic amide work
4-6 hours.
39
Botox
Anticholingeric and NMJ.
40
Norephinerphein vs. Epinerphine
Norepinephrine does not work on B2 receptors.
41
Phenylephrine
Sympathetic agonist. 2.5% routinely used for dilation. Acts on alpha 1 receptor with no affect on B. Allows dilation without any SE.
42
Which is the weird on in sympathetic NS
Alpha 2
43
When to give Beta blocker
In the morning
44
Who should you be cautions with BB
diabetic (hid hypo signs), lungs, Heart, hyperthyroidism, MG.
45
Short term escape
lowers initially and then raises
46
Long term drift
IOP starts to gradually rise
47
Do you get short term escape and long term drift with BB
YES.
48
Cosopt
Timolol and dorzolamide
49
Combigan
Timolol and briminoladine
50
Alpha 2 agonist action
Act to decrease production and increase outflow
51
SE of CAI
Aplastic anemia, thrombocytopenia, agranuloctyopenia, metallic taste, metabolic acidosis.
52
CI for CAI
SULFA BASED
53
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.
54
When to dose prostaglandins
bedtime
55
SE of prostaglandins
Iris herterochromia, darker lashes, dark pigment around the eyes.
56
Reduction in IOP of glaucoma drugs
Apraclondine (30-40), prost (33), Pilo (30). BB (25), biminodine and dorzolamid (18).
57
How do topical ocular anesthetics work
Block nerve conduction and change membrane potential by stopping the influx of Na = no depolarization
58
Amides anesthetics
Go inside. Injectable. Liver.
| longer duration of action
59
Esters anesthetics
All topical anesthetics. Metabolized locally. short duration of action
60
Proparacaine
Ester anistehtic. Lasts 10-20 minutes.
61
Fluoress
Fluorescent and benoxinate (another topical anesthetic)
62
How do antihistamines work
block type 1 hypersensitivity rxn/ the cell receptors the histamines act upon
63
Emedastine
H1 antihistamine. Use with moderate allergic conj.
64
Mast cell stabilizers
Not good for acute but use CHRONIC. Stops mast cells from becoming degranulated by stopping CA influx.
65
SE of corticosteroids
Risk of secondary infection, Cataract, ocular HTN (junk not cleared out and decreased outflow)
66
What do corticosteroids do?
Stop phosophilapase A2.
67
Soft Steroids
FML and Loteprednol.
68
NSAIDS
COX blockers so stop Leukotriens, thrombin,
69
Where is FA dye injected
Brachial vein
70
How long from injection to eyes
10-20 seconds
71
Who is glycine CI in?
Diabetics. Use isosorbide instead.
72
Methylcellulose
used to increase viscosity of AT and allow more contact time with cornea
73
75% of topical drug goes where? 3 types of routes
1. drainage into nasolacrimal apparatus
2. absorption into systemic circulation by conj/lid vasculature
3. penetration into cornea
74
to cross cornea, drugs need to have what properties
lipophilic and hydrophilic
75
topical route is to:
Pros:
Cons:
mucosa, conjunctiva, cornea, epidermis
pros: at site of desired effects
cons: site irritation, systemic side fx
76
Oral route pros/cons
pro: simple dosage, easily administered, time released
cons: GI distress, drug degradation, absorption problems
77
Subconjunctival route injects bw __ & __
| pros/cons
inject b/w conjunctiva & sclera
pros: Rapid, effectively absorbed
cons: fear, pain, inflammation
78
intravenous route
| pros/cons
into vein
pro: Highest bioavailability, Very rapid, dose accuracy, bypass digestive tract
cons: danger of cardiotoxicity (bolus), sterility
79
intramuscular pros and con
pro: rapid, controlled absorption
cons: pain, necrosis
80
function of sympathetic nervous system
fight/flight
DRY
bronchodilation/ mydriasis
decrease in secretions
81
cholinergic receptors in eye (location, receptor, general effects, innervated by CN __)
CAMS = ciliary muscle/acc, Miosis/sphincter
Iris sphincter = M3 = miosis = CN3
Ciliary muscle = M2, M3 = accommodation = CN3
Lacrimal gland = M2, M3, increase tear production = CN 7 (reflex, emotional)
82
adrenergic receptors in eye (location, receptor, general fx)
```
iris dilator = alpha-1 = dilation
trabecular meshwork = beta-2 - relaxation, increase outflow
ciliary muscle = beta -2 = relaxation, opposes accommodation
NPCE = B2 > B1 = increase aqueous formation
CB vasculature (MACI) = alpha2 = constricts, reduce aq formation
```
83
Cholinergic agonists for treatment of __ & ___
glaucoma, accommodative esotropia
| acc ET b/c acts on ciliary muscle and decreases amt of CNS stimulation to ciliary muscle = decrease convergence
84
what drug best to use during angle closure?
pilocarpine
| especially before LPI b/c drug will make iris tight and LPI is more effectively done
85
__% pilocarpine to differentiate CN 3 palsy vs sphincter tear in fixed,dilated pupil
1%; CN 3 palsy will constrict w pilocarpine
86
what are indirect cholinergic agonists
anticholinesterase; inhibit acetylcholinesterase that normally breaks down ach
- Edrophonium (Enlon)
- Neostigmine (Prostigmin)
- Echothiophate (Phospholine)
- Pyridostigmine (Mestinon)
87
What are cholinergic antagonists used for?
cycloplegic refractions
pupillary dilation
managing uveitis
blocks Ach @ muscarinic sites in CB and iris
88
functions of cholinergic antagonists
acts like sympathetic pathway
STop ACH (Scopolamine, Tropicamide, Atropine, Cyclopentolate, Homatrophine)
ASH CT ('city") MEMORIZE IN THIS ORDER!
**NOT USED FOR GLAUCOMA TX
89
tropicamide: onset for mydriatic and cycloplegic effect, duration?
25 min onset, lasts 6 hrs
90
what does atropine toxicity cause?
```
#1 dry mouth
dry flushed skin, rapid pulse, disorientation, fever b/c CNS effects
```
91
which cholinergic antagonist has fastest onset and shortest duration of cycloplegic fx
Cyclopentolate
92
cyclopentolate's max effects at what onset for mydriatic and for cycloplegic
```
20-45 min (mydriatic)
45 min (cycloplegic)
```
93
homatropine functions
dilates pupil (not the best)
keeps iris mobile so good for posterior synechiae pts
reduce pain b/c paralyze sphincter and ciliary muscles
stabilize blood aqueous barrier by constricting iris and CB vasulature
94
what is anticholinergic toxicity
hot as a hare, red as a beet, dry as a bone, mad as a hatter, blind as a bat
95
what is MOA of Botulina Toxin (Botox)
blocks release of Ach at NEUROMUSCULAR JUNCTION to inhibit muscle contraction
prevent wrinkle
96
Adrenergic agonists used for what
```
dilation
conjunctival constriction
manage minor allergic conditions
temporary ctrl of IOP spikes
tx of POAG
```
97
Norepinephrine vs epinephrine
Norepi does NOT act on Beta-2 receptors
98
Phenylephrine 2.5% uses
- alpha-1 agonist
- dilates w/o cyclo
- palpebral widening - muller's muscle retracts upper lid
- tells scleritis vs episcleritis (blanched conj vessels/white vessels = episcleritis b/c vessels superficial)
- Horner's syndrome (horner pupil dilates, normal pupil doesn't)
99
Phenylephrine 10% uses
break posterior synechiae
100
Phenylephrine 10% contraindications
- Think: HEART = cardiovascular side fx (HTN, cardiac arrhythmias)
- Graves disease (has too much sympathetic already--phenyl will make it worse)
- TCA (tricyclic antidepressants)
- atropine intake
- MAOI intake
101
what does Naphazoline (Naphcon A) & Tetrahydrozoline (Visine) do
- topical ocular decongestant (constrict conj BV)
| - acts on Alpha-1 so overuse can lead to dilated pupils
102
Alpha-2 agonists
Brimonidine (Alphagan 0.20%), Apraclonidine
- decrease aqueous humor production
- increase uveoscleral outflow
- lower IOP and long-term tx of glaucoma
103
neuroprotective properties (2 meds)
protects optic nerve
Betaxolol
Brimonidine
104
Brimonidine: uses, side fx, contraindication
side fx: follicular conjunctivitis (inferiorly), DRY MOUTH
cause miosis, reduce glare, halo
contraindications: MAOI takers
Alphagan 0.2% vs Alphagan P: the P has preservatives and conc 0.1%
105
Apraclonidine
- Iopidine
- alpha 2 agonist
- 30-40% IOP reduction
- controls IOP spikes b4 & after LPI, trabeculoplasty, posterior capsulotomy, acute angle closure)
- Acute use b/c tachyphylaxis (loss of effect of drug over time)
- Diagnose Horner's syndrome
106
Horner's syndrome
```
small ptosis b/c defect Muller muscle
Lack of Sympathetic
Dilation lag (delayed dilation) + ptosis
```
107
Med to test Horner's syndrome
Apraclonidine or Cocaine
Apraclonidine: no fx on normal pupil, dilates the miotic/horner pupil
Cocaine: dilates healthy eye, no effect on miotic/horner eye
Hydroxyamphetamine or phenylephrine
if healthy or preganglionic is damaged, , hydroxamphetamine acts on POSTGANGLIONIC NEURON -> releases norepinephrine + mydriasis. if don't dilate, postganglionic neuron is DAMAGED
phenylephrine 1% dilates postganglionic horner's syndrome
108
Name 5 beta-blockers
```
Timolol
Betaxolol
Levobunolol
Carteolol
Metipranolol
```
109
Beta-blockers side fx
CNS: disorientation, depression, fatigue
Cardiovascular: bradycardia, arrhythmias, syncope
Pulmonary: dyspnea, wheezing, bronchospasm
Digestive (GI): nausea, vomit, diarrhea, abdominal pain
Reproductive: erectile dysfunction
110
Betaxolol differs from other beta-blockers b/c
targets only B1
111
best to take timolol
daytime
112
which beta-blocker has crossover effect
Timolol: unilateral use will also reduce IOP in opposite eye
113
beta-blockers do what to hyperthyroidism
mask signs and symptoms
114
beta-blocker does what to myasthenia gravis pts
exacerbates
115
Carteolol
"Cart Heart"
reduce cholesterol in hypercholesterolemia
less side fx than other beta-blockers
116
which beta-blocker has intrinsic sympathomimetic activity?
carteolol
| reduces nocturnal badycardia
117
Betaxolol (Betoptic-S)
Beta1 specific *remember beta1 involves heart
| can worsen heart failure
118
Levobunolol
Similar to timolol
119
Metipranolol
not used anymore
120
Name cholinergic agonist (direct-acting)
Pilocarpine
121
MOA of cholinergic agonist, alpha-adrenergic agonist, beta blocker, CAI, Prostaglandin in terms of glaucoma
cholinergic agonist: Pilocarpine; increase corneoscleral outflow
alpha-adrenergic agonist (alpha 2 agonist); reduce production/ increase uveoscleral outflow
beta-blocker: reduce production
CAI: reduce production
Prostaglandin: increase outflow via uveoscleral route
122
CAI MOA, topical names, oral names
reduce aqueous production by inhibiting carbonic anyhydrase = blocking bicarb flux into posterior chamber
Topical: Brinzolamide 1% (Azopt), Dorzolamide 2% (Trusopt)
Orals; Acetazolamide (Diamox), Methazolamide (Neptazane)
123
Oral CAI side fx/ contraindications
Common: Metallic taste, tingling hands/feet, metabolic ACIDOSIS
most serious: Thrombocytopenia, agranulocytosis, aplastic anemia
fatal: bone marrow suppression and plastic anemia
other side fx: malaise, fatigue, weight loss, anorexia, impotence, depression, diarrhea, myopic shift
Contraindication: COPD, pregnancy, sulfa allergy
124
contraindicated in pregnant
```
FA2TSI:
Fluoroquinolone
AmiNOglycosides (cause N Ototoxicity)
Acutane
Tetracyclines
Sulfa
Ibuprofen
```
125
first line of tx for POAG
Prostaglandins
126
Name prostaglandin analogs
Latanoprost (Xalatan 0.005%)
Bimatoprost (Lumigan 0.03%)
Travoprost (Travatan 0.004%)
127
function of prostaglandin
27-35% IOP reducation
128
prostaglandin contraindications
CME
active inflammation (uveitis)
hx herpes simplex keratitis
129
amide anesthetic
- name
- metabolized by what organ
Lidocaine
| metabolized by liver
130
Name ester anesthetic, onset, duration
Proparacaine/ Benoxinate, 10-20 sec onset, 10-20 min duration
131
Fluoress is combination of what two drugs
Benoxinate + fluorescein
132
Steps to Type 1 hypersensitivity rxn
1) 1st exposure to antigen -> IgE antibodies produced but No symptoms occur
2) IgE binds to mast cells and basophils
3) antigen reexposure -> binds IgE/mast cell complex -> opens Ca channels
4) Ca influx -> depolarizes cell -> degranulation of mast cell -> releases histamine/other inflammatory mediators into blood
5) allergic symptoms -> binds histamin to histamine receptors
133
name of antibody in type 1 hypersensitivity
IgE
| "IgE allergee"
134
Mast cell stabilizers effective in what ocular conditions?
Chronic allergic conjunctivitis
Vernal conjunctivitis
Atopic keratoconjunctivitis
135
Name Mast cell & antihistamine combinations
```
Bepotastine (Bepreve)
Epinastine (Elestat)
Ketotifen (Zaditor)
Olopatadine 0.10% (Patanol)
Azelastine (Optivar)
Olopatadine 0.20% (Pataday)
```
effective in long-term oc itching/allergic conj, acute symptoms
136
Anti-inflammatory agents name 2 types
Corticosteroids
| NSAIDs
137
corticosteroids
anti-inflammatory/ immunosuppressive
| inhibits phospholipase A2
138
corticosteroids side fx
increased risk of secondary infxn
PSC catarcts
glaucoma
139
Potent steroids names
Prednisolone 1% Acetate
Rimexolone (Vexol)
Difluprednate (Durezol)
Dexamethasone 0.1%(Maxidex)
140
Soft steroids
Loteprednol 0.5% (Lotemax)
Fluorometholone 0.1% (FML)
less likely cause spike in IOP
141
NSAIDs names
```
Diclofenac sodium 0.1% (Voltaren)
Ketorolac Tromethamine 0.4% (Acular LS)
Nepafenac 0.1% (Nevanec)
Bromfenac 0.09% (Xibrom, Bromday)
Flurbiprofen 0.03% (Ocufen)
```
142
Voltaren & Acular how many times per day
QID
143
Nevanec dosed how many times
TID
144
Xibrom dose per day
BID
145
Ocufen dose per day
prior to ocular surgery
146
Ketorolac (Acular) only NSAID for what tx
seasonal allergic conjunctivitis
147
Voltaren side fx
corneal toxicity -> corneal melting -> most often in Voltaren so withdrawn from market
148
Ketorolac side fx
stinging upon instillation
149
Fluorescein evaluates what
tear film quality
| epithelial defects
150
Rose Bengal used for
```
dead and devitalized cells
cells w/ loss of mucous surface
NOT EPITHELIAL DEFECTS
evaluates herpetic corneal ulcer -> stains dendrite lesion
more discomfort
```
151
Lissamine Green
dead/devitalized cells
| *Dry eye evaluation
152
Methylene blue
stains corneal nerves, stains similar to Rose Bengal
for glaucoma filtering blebs
for lacrimal sac before dacryocystorhinostomy
