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Ocular Pharm Flashcards

1
Q

How much of drops are lost to evaporation

A

25%

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2
Q

Bioavability

A

The percent of unchanged drug that gets to the desired site.

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3
Q

Tear layer characterisitics

A

Lipid=lipid soluble. Aqueous=water soluble, mucus=both water/lipid soluble

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4
Q

Corneal layer characteristics for drug penetration

A

Endothelium and epi=lipid soluble. Stroma=water sol

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5
Q

What type of drugs will penetrate best

A

small, uncharged, lipid soluble molecules. Most formulated as weak bases.

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6
Q

What route has the best bioavailablity

A

IV route

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7
Q

Where are parasympathetic cell bodies located

A

Craniosacral. PCS.

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8
Q

Where are sympathetic cell bodies located

A

Thoracic-lumbar.

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9
Q

NT for preganglionin in Para

A

Acetylcholine, has longer preganglionic neuron

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10
Q

NT for pre ganglion in symp

A

Acetylcholine, has shorter preganglionic neuron

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11
Q

Which autonomic pathway has longer post ganglionic

A

sympathetic

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12
Q

NT for post ganglion Parasympathetic

A

acetylcholine

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13
Q

NT for post ganglion sympathetic

A

norepinephrine and epinephrine.

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14
Q

Functions of parasympathetic nervous system (muscarinic)

A

Rest/digest
Wet!!
bronchoconstriction/ miosis (constriction)
SLUD = salivation, lacrimation, urination, defecation

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15
Q

Dilator of iris sympathetic function and receptor

A

alpha 1. Dilates

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16
Q

CB vasculature SNS function and receptor

A

Alpha 2. Decreaes aqeuosu

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17
Q

Ciliary Muscle vasculature SNS function and receptor

A

B2. relaxes

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18
Q

Trabec Mesh SNS function and receptor

A

B2. Increases outflow

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19
Q

NPCE SNS function and receptor

A

B1 and B2. Increases outflow.

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20
Q

What structures in the eye receive Parasympathetic innervation?

A

Iris, ciliary muscle, and lacrimal gland.

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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

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22
Q

What pilo do you use with Adies tonic pupil

A

0.125%

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23
Q

Side fx of pilocarpine

A

brow ache, HA, myopic shift, can cause angle closure or RD or cataracts.
“dimmed vision” in cataracts

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24
Q

Edrophonium (Enlon)

A

Used to diagnose MG– Tensilon test. If ptosis improves 1-2 min after injection = (+) MG.

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25
Q

Neostigmine (prostigmin)

A

Treatment for MG or limb strength evaluation.

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26
Q

Echothiophate (phospholine)

A

Irreversible ACHE inhibitors. Can be used to diagnose or treat accommodative esotropia.

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27
Q

Pyridostigmine (mestinon)

A

to treat MG.

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28
Q

Pralidoxime

A
  • 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
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29
Q

Scopolamine (effects, side fx, contraindication)

A

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

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30
Q

Which cholinergic antagonist has the fastest onset and shortest duration?

A

tropicamide

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31
Q

Atropine

  • onset
  • duration
  • used for what tx?
  • side fx
  • caution in what population
A

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
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32
Q

Who should you dilate with caution?

A

THINK. Thyroid. Iris fixed IOL. Narrow angle. Kids (DS)

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33
Q

which drug do you use for anterior uvieits?

A

homatropine. It dilates the iris, reduces pain, and stabilizes the blood aqueous barrier.

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34
Q

How long does Atropin work

A

7-10 days

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35
Q

How long does scopolamine work

A

3-7 days

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36
Q

How long does homatropine work

A

1-3 days

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37
Q

How long does cyclopentolate work

A

24 hours

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38
Q

How long does tropic amide work

A

4-6 hours.

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39
Q

Botox

A

Anticholingeric and NMJ.

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40
Q

Norephinerphein vs. Epinerphine

A

Norepinephrine does not work on B2 receptors.

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41
Q

Phenylephrine

A

Sympathetic agonist. 2.5% routinely used for dilation. Acts on alpha 1 receptor with no affect on B. Allows dilation without any SE.

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42
Q

Which is the weird on in sympathetic NS

A

Alpha 2

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43
Q

When to give Beta blocker

A

In the morning

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44
Q

Who should you be cautions with BB

A

diabetic (hid hypo signs), lungs, Heart, hyperthyroidism, MG.

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45
Q

Short term escape

A

lowers initially and then raises

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46
Q

Long term drift

A

IOP starts to gradually rise

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47
Q

Do you get short term escape and long term drift with BB

A

YES.

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48
Q

Cosopt

A

Timolol and dorzolamide

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49
Q

Combigan

A

Timolol and briminoladine

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50
Q

Alpha 2 agonist action

A

Act to decrease production and increase outflow

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51
Q

SE of CAI

A

Aplastic anemia, thrombocytopenia, agranuloctyopenia, metallic taste, metabolic acidosis.

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52
Q

CI for CAI

A

SULFA BASED

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53
Q

Prostaglandin Analogs

A

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.

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54
Q

When to dose prostaglandins

A

bedtime

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55
Q

SE of prostaglandins

A

Iris herterochromia, darker lashes, dark pigment around the eyes.

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56
Q

Reduction in IOP of glaucoma drugs

A

Apraclondine (30-40), prost (33), Pilo (30). BB (25), biminodine and dorzolamid (18).

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57
Q

How do topical ocular anesthetics work

A

Block nerve conduction and change membrane potential by stopping the influx of Na = no depolarization

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58
Q

Amides anesthetics

A

Go inside. Injectable. Liver.

longer duration of action

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59
Q

Esters anesthetics

A

All topical anesthetics. Metabolized locally. short duration of action

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60
Q

Proparacaine

A

Ester anistehtic. Lasts 10-20 minutes.

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61
Q

Fluoress

A

Fluorescent and benoxinate (another topical anesthetic)

62
Q

How do antihistamines work

A

block type 1 hypersensitivity rxn/ the cell receptors the histamines act upon

63
Q

Emedastine

A

H1 antihistamine. Use with moderate allergic conj.

64
Q

Mast cell stabilizers

A

Not good for acute but use CHRONIC. Stops mast cells from becoming degranulated by stopping CA influx.

65
Q

SE of corticosteroids

A

Risk of secondary infection, Cataract, ocular HTN (junk not cleared out and decreased outflow)

66
Q

What do corticosteroids do?

A

Stop phosophilapase A2.

67
Q

Soft Steroids

A

FML and Loteprednol.

68
Q

NSAIDS

A

COX blockers so stop Leukotriens, thrombin,

69
Q

Where is FA dye injected

A

Brachial vein

70
Q

How long from injection to eyes

A

10-20 seconds

71
Q

Who is glycine CI in?

A

Diabetics. Use isosorbide instead.

72
Q

Methylcellulose

A

used to increase viscosity of AT and allow more contact time with cornea

73
Q

75% of topical drug goes where? 3 types of routes

A
  1. drainage into nasolacrimal apparatus
  2. absorption into systemic circulation by conj/lid vasculature
  3. penetration into cornea
74
Q

to cross cornea, drugs need to have what properties

A

lipophilic and hydrophilic

75
Q

topical route is to:
Pros:
Cons:

A

mucosa, conjunctiva, cornea, epidermis

pros: at site of desired effects
cons: site irritation, systemic side fx

76
Q

Oral route pros/cons

A

pro: simple dosage, easily administered, time released
cons: GI distress, drug degradation, absorption problems

77
Q

Subconjunctival route injects bw __ & __

pros/cons

A

inject b/w conjunctiva & sclera

pros: Rapid, effectively absorbed
cons: fear, pain, inflammation

78
Q

intravenous route

pros/cons

A

into vein

pro: Highest bioavailability, Very rapid, dose accuracy, bypass digestive tract
cons: danger of cardiotoxicity (bolus), sterility

79
Q

intramuscular pros and con

A

pro: rapid, controlled absorption
cons: pain, necrosis

80
Q

function of sympathetic nervous system

A

fight/flight
DRY
bronchodilation/ mydriasis
decrease in secretions

81
Q

cholinergic receptors in eye (location, receptor, general effects, innervated by CN __)

A

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
Q

adrenergic receptors in eye (location, receptor, general fx)

A 
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
Q

Cholinergic agonists for treatment of __ & ___

A

glaucoma, accommodative esotropia

acc ET b/c acts on ciliary muscle and decreases amt of CNS stimulation to ciliary muscle = decrease convergence

84
Q

what drug best to use during angle closure?

A

pilocarpine

especially before LPI b/c drug will make iris tight and LPI is more effectively done

85
Q

__% pilocarpine to differentiate CN 3 palsy vs sphincter tear in fixed,dilated pupil

A

1%; CN 3 palsy will constrict w pilocarpine

86
Q

what are indirect cholinergic agonists

A

anticholinesterase; inhibit acetylcholinesterase that normally breaks down ach

  • Edrophonium (Enlon)
  • Neostigmine (Prostigmin)
  • Echothiophate (Phospholine)
  • Pyridostigmine (Mestinon)
87
Q

What are cholinergic antagonists used for?

A

cycloplegic refractions
pupillary dilation
managing uveitis
blocks Ach @ muscarinic sites in CB and iris

88
Q

functions of cholinergic antagonists

A

acts like sympathetic pathway
STop ACH (Scopolamine, Tropicamide, Atropine, Cyclopentolate, Homatrophine)
ASH CT (‘city”) MEMORIZE IN THIS ORDER!
**NOT USED FOR GLAUCOMA TX

89
Q

tropicamide: onset for mydriatic and cycloplegic effect, duration?

A

25 min onset, lasts 6 hrs

90
Q

what does atropine toxicity cause?

A 
#1 dry mouth
dry flushed skin, rapid pulse, disorientation, fever b/c CNS effects
91
Q

which cholinergic antagonist has fastest onset and shortest duration of cycloplegic fx

A

Cyclopentolate

92
Q

cyclopentolate’s max effects at what onset for mydriatic and for cycloplegic

A 
20-45 min (mydriatic)
45 min (cycloplegic)
93
Q

homatropine functions

A

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
Q

what is anticholinergic toxicity

A

hot as a hare, red as a beet, dry as a bone, mad as a hatter, blind as a bat

95
Q

what is MOA of Botulina Toxin (Botox)

A

blocks release of Ach at NEUROMUSCULAR JUNCTION to inhibit muscle contraction
prevent wrinkle

96
Q

Adrenergic agonists used for what

A 
dilation
conjunctival constriction
manage minor allergic conditions
temporary ctrl of IOP spikes
tx of POAG
97
Q

Norepinephrine vs epinephrine

A

Norepi does NOT act on Beta-2 receptors

98
Q

Phenylephrine 2.5% uses

A
  • 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
Q

Phenylephrine 10% uses

A

break posterior synechiae

100
Q

Phenylephrine 10% contraindications

A
  • 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
Q

what does Naphazoline (Naphcon A) & Tetrahydrozoline (Visine) do

A
  • topical ocular decongestant (constrict conj BV)

- acts on Alpha-1 so overuse can lead to dilated pupils

102
Q

Alpha-2 agonists

A

Brimonidine (Alphagan 0.20%), Apraclonidine

  • decrease aqueous humor production
  • increase uveoscleral outflow
  • lower IOP and long-term tx of glaucoma
103
Q

neuroprotective properties (2 meds)

A

protects optic nerve
Betaxolol
Brimonidine

104
Q

Brimonidine: uses, side fx, contraindication

A

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
Q

Apraclonidine

A
  • 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
Q

Horner’s syndrome

A 
small ptosis b/c defect Muller muscle
Lack of Sympathetic
Dilation lag (delayed dilation) + ptosis
107
Q

Med to test Horner’s syndrome

A

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
Q

Name 5 beta-blockers

A 
Timolol
Betaxolol
Levobunolol
Carteolol
Metipranolol
109
Q

Beta-blockers side fx

A

CNS: disorientation, depression, fatigue
Cardiovascular: bradycardia, arrhythmias, syncope
Pulmonary: dyspnea, wheezing, bronchospasm
Digestive (GI): nausea, vomit, diarrhea, abdominal pain
Reproductive: erectile dysfunction

110
Q

Betaxolol differs from other beta-blockers b/c

A

targets only B1

111
Q

best to take timolol

112
Q

which beta-blocker has crossover effect

A

Timolol: unilateral use will also reduce IOP in opposite eye

113
Q

beta-blockers do what to hyperthyroidism

A

mask signs and symptoms

114
Q

beta-blocker does what to myasthenia gravis pts

A

exacerbates

115
Q

Carteolol

A

“Cart Heart”
reduce cholesterol in hypercholesterolemia
less side fx than other beta-blockers

116
Q

which beta-blocker has intrinsic sympathomimetic activity?

A

carteolol

reduces nocturnal badycardia

117
Q

Betaxolol (Betoptic-S)

A

Beta1 specific *remember beta1 involves heart

can worsen heart failure

118
Q

Levobunolol

A

Similar to timolol

119
Q

Metipranolol

A

not used anymore

120
Q

Name cholinergic agonist (direct-acting)

A

Pilocarpine

121
Q

MOA of cholinergic agonist, alpha-adrenergic agonist, beta blocker, CAI, Prostaglandin in terms of glaucoma

A

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
Q

CAI MOA, topical names, oral names

A

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
Q

Oral CAI side fx/ contraindications

A

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
Q

contraindicated in pregnant

A 
FA2TSI:
Fluoroquinolone
AmiNOglycosides (cause N Ototoxicity)
Acutane
Tetracyclines
Sulfa
Ibuprofen
125
Q

first line of tx for POAG

A

Prostaglandins

126
Q

Name prostaglandin analogs

A

Latanoprost (Xalatan 0.005%)
Bimatoprost (Lumigan 0.03%)
Travoprost (Travatan 0.004%)

127
Q

function of prostaglandin

A

27-35% IOP reducation

128
Q

prostaglandin contraindications

A

CME
active inflammation (uveitis)
hx herpes simplex keratitis

129
Q

amide anesthetic

  • name
  • metabolized by what organ
A

Lidocaine

metabolized by liver

130
Q

Name ester anesthetic, onset, duration

A

Proparacaine/ Benoxinate, 10-20 sec onset, 10-20 min duration

131
Q

Fluoress is combination of what two drugs

A

Benoxinate + fluorescein

132
Q

Steps to Type 1 hypersensitivity rxn

A

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
Q

name of antibody in type 1 hypersensitivity

A

IgE

“IgE allergee”

134
Q

Mast cell stabilizers effective in what ocular conditions?

A

Chronic allergic conjunctivitis
Vernal conjunctivitis
Atopic keratoconjunctivitis

135
Q

Name Mast cell & antihistamine combinations

A 
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
Q

Anti-inflammatory agents name 2 types

A

Corticosteroids

NSAIDs

137
Q

corticosteroids

A

anti-inflammatory/ immunosuppressive

inhibits phospholipase A2

138
Q

corticosteroids side fx

A

increased risk of secondary infxn
PSC catarcts
glaucoma

139
Q

Potent steroids names

A

Prednisolone 1% Acetate
Rimexolone (Vexol)
Difluprednate (Durezol)
Dexamethasone 0.1%(Maxidex)

140
Q

Soft steroids

A

Loteprednol 0.5% (Lotemax)
Fluorometholone 0.1% (FML)

less likely cause spike in IOP

141
Q

NSAIDs names

A 
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
Q

Voltaren & Acular how many times per day

143
Q

Nevanec dosed how many times

144
Q

Xibrom dose per day

145
Q

Ocufen dose per day

A

prior to ocular surgery

146
Q

Ketorolac (Acular) only NSAID for what tx

A

seasonal allergic conjunctivitis

147
Q

Voltaren side fx

A

corneal toxicity -> corneal melting -> most often in Voltaren so withdrawn from market

148
Q

Ketorolac side fx

A

stinging upon instillation

149
Q

Fluorescein evaluates what

A

tear film quality

epithelial defects

150
Q

Rose Bengal used for

A 
dead and devitalized cells
cells w/ loss of mucous surface
NOT EPITHELIAL DEFECTS
evaluates herpetic corneal ulcer -> stains dendrite lesion
more discomfort
151
Q

Lissamine Green

A

dead/devitalized cells

*Dry eye evaluation

152
Q

Methylene blue

A

stains corneal nerves, stains similar to Rose Bengal
for glaucoma filtering blebs
for lacrimal sac before dacryocystorhinostomy

oc pharm (3 decks)

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