Ocular Pharm Flashcards

1
Q

Cholinergic Receptors in the eye

A

Iris sphincter- M3
Lacrimal gland- M2 and M3
Ciliary muscle- M2 and M3

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2
Q

Adrenergic receptors in the eye

A

A1- Dilator muscle
A2- Ciliary body vasculature to reduce aqueous formation
B1 and B2- Non pigmented ciliary epithelium to increase aqueous formation.
B2- TM to increase outflow, ciliary muscle to oppose accommodation, NPCE to increase aqueous formation.

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3
Q

Pilocarpine

  • What class
  • How many drops per day
  • MOA
  • When to use
  • Side effects
A
  • Cholinergic agnost
  • QID
  • Stimulates longitudinal muscle of the ciliary body, which pulls on the scleral spur and opens up the TM
  • After angle closure attack, before PI. To differentiate Aide’s or 3rd nerve palsy vs sphincter tear.
  • Browaches, HA, myopia, RD
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4
Q

Indirect cholinergic agonists (anticholinesterase agents)

4

A

Endrophonium- dx MG (tensilon test)
Neostigmine- Tx MG
Pyridostigmine- Tx MG
Echothiophate- longest lasting, IRRIVERSIBLE. Dx and Tx of accommodative ET

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5
Q

What class of drugs can be used to tx accommodative ET?

A

Cholinergic agonists because they increase ACH at the receptor. The brain now sends less signals to converge.

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6
Q

Irreversible anti cholinesterase agents

A

Echothiophate and isofluorophate

-Many side effects

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7
Q

Pralidoxime MOA

A

Administered by IV. Reverse the effects of irreversible acetylcholinesterase inhibitors such as echothiophate and isofluorophate.

It binds to these drugs and releases the acetylcholinesterase, which can now break down Ach.

Can reverse systemic side effects of organophosphate poisoning.

Not effective against reversible acetylcholinesterase inhibitors like neostigmine.

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8
Q

Cholinergic antagonists (5)

A
Atropine 
Homatropine
Scopolamine - penetrates BBB best and may cause hallucinations, confusion, restlessness. 
Tropicamide 
Cyclopentolate
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9
Q

Drug with the fastest onset and shortest duration of MYDRIATIC effects

A

Tropicamide

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10
Q

Max mydriatic effect of tropicamide is in __ minutes

A

25

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11
Q

Atropine onset and duration

  • When to use
  • Avoid in
A

60-180 minutes
7-12 days
-Amblyopia Tx (drop the good eye, penalization)
-Downsyndrome, under 3, elderly

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12
Q

Special caution when using atropine in what demographics

A

**Down syndrome
Under 3 years old
Elderly

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13
Q

Atropine toxicity

A

Dry mouth, dry flushed skin, rapid pulse, disorientation, fever. Due to CNS effects

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14
Q

Fastest onset and shortest duration of CYCLOPLEGIC effects

A

Cyclopentolate.

Wait 45 minutes

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15
Q

Standard for treating anterior uveitis

A

Homatropine because it dilates the pupil, but keeps it mobile so the iris cannot become syneched in miotic or dilated stages.

BID!

  • Keeps iris mobile
  • Reduces pain by paralyzing ciliary muscles and sphincter muscles.
  • Causes vasoconstriction –> stabilizing blood aqueous barrier.
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16
Q

MOA of botox

A

Somatic drug that blocks the release of Ach at the NMJ, inhibiting muscle contraction. Can be used for blepharospasm, strab, and wrinkles.

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17
Q

What receptors do NE and Epi act on

A

Epi- Alpha 1, alpha 2, beta 1, beta 2

NE- Alpha 1, alpha 2, beta 1

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18
Q

Alpha 1 agonist

A

Phenylephrine

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19
Q

Clinical uses of 2.5% phenylephrine

A

Dilation without cyclo- only acts to increase action of dilator muscle, does not prevent sphincter muscle.

Palpebral widening- acts on mullers (sympathetic)

Differentiates scleritis from episclertisi due to blanching. (sympathetic drugs cause peripheral vasoconstriction)

10% breaks PS, but contraindicated in patients with Graves, taking MAOIs, tricyclic antidepressants, and atropine.

Horners Dx

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20
Q

Contraindications for phenyl 10%

A

Taking MAOIs, tricyclic antidepressants, atropine

Or patients with Graves disease.

May result in adverse cardiovascular effects such as HTN crisis and cardiac arrhythmias.

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21
Q

Topical ocular decongestants

A

Naphazoline and Tetrahydrozoline (Visine)

Considered an adrenergic alpha agonist, but also has some beta effects.

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22
Q

Naphcon is a combo of which 2 drugs

A

Naphazoline (adrenergic agonist, alpha > beta = vasoconstriction) and antihistamine

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23
Q

Adrenergic alpha2 agonists used for glaucoma therapy

A

Brimonidine (alphagan 0.20%–> Alphagan P 0.1% )
Apraclonidine (Iopidine)

-Both can cause dry mouth

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24
Q

Brimonidine

Alphagan 0.2% –> Alphagan P 0.1%

A
  • Highly selective alpha 2 agonist
  • Neuroprotective properties
  • Alphagan 0.2% may cause follicular conjunctivitis, which is why they switched to Alphagan P 0.1%
  • Causes miosis
  • Contra in pt’s taking MAOIs.
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25
Q

Why does brimonidine (alphagan P 0.1%) cause miosis and apraclonidine (iopidine) cause mydriasis?

A

Both act on the alpha adrenergic receptors.

Brimonidine has 30x more effect on Alpha 2 than apraclonidine.

Alpha 2 decreases sympathetic activity

AKA brimonidine decreases sympathetic activity more –> constricted pupil.

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26
Q

When to use apraclonidine (iopidine)

A

Acute angle closure because fast acting (within 1 hour) and decreases IOP by 30-40%

NOT effective in chronic therapy because tachyphylaxis and at risk of allergic response.

Can be used for dx of Horner’s Syndrome

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27
Q

What 2 signs need to be present for you to dx Horner’s without pharm testing

A
  1. Dilation lag of affected pupil in darkness. When you turn light off, abnormal pupil will not dilate because there is a sympathetic problem. Aniso will be greater in darkness.
  2. Ptosis
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28
Q

Horner’s Dx with pharm

A

Apraclonidine- Horner’s pupil will dilate.

Cocaine- Horner’s pupil will stay the same.

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29
Q

Horner’s syndrome Dx location of lesion

A

Hydroxyamphetamine

Phenylephrine- Will dilate if lesion is pre ganglionic,

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30
Q

How much does Timolol reduce IOP

A

25%

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31
Q

Which class of drugs has a crossover effect (can drop OD, get effects OS)

A

BB

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32
Q

Cosopt

A

Timolol 0.5% and Trusopt (Dorzolamide) 2%

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33
Q

Combigan

A

Timolol 0.5% and alphagan (brimonidine) 0.2%

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34
Q

Which BB has intrinsic sympathomimetic activity

A

Carteolol (Cart = heart) ISA reduces nocturnal bradycardia and is more comfortable (less sting) than Timolol.

35
Q

Which BB is B1 specific

A

Betaxolol.

Minimizes respiratory effects, but may worsen congestive heart failure

36
Q

Types of topical BB

A
Timolol 
Careolol
Betaxolol
Levobunolol
Metipranolol
37
Q

2 MOAs of alpha adrenergic agonists (for glaucoma treatment, mostly alpha 2)

A

Decrease production

Increase uveoscleral outflow

38
Q

Where do CAI’s act?

A

in the CB epithelium (pigmented and non pigmented).

39
Q

4 types of CAIs

A

Brinzolamide (Azopt)
Dorzolamide (Trusopt)
Acetazolamide (Diamox)
Methazolamide (Neptazane)

40
Q

Oral CAI side effects

A

Common- metallic taste, tingling in hands and feet, metabolic acidosis (increase in plasma toxicity due to decrease in bicarb in the body. May cause nausea, vomiting, rapid breathing)

More serious- Thrombocytopenia (decrease in platelets), agranulocytosis (decrease in WBC) and aplastic anemia (damage to bone marrow, decrease in RBC production. May be fatal.)

41
Q

Metabolic acidosis is a common SE in oral CAIs. What is it

A

(increase in plasma toxicity due to decrease in bicarb in the body. May cause nausea, vomiting, rapid breathing)

42
Q

Oral CAI contraindications

A

Sulfa allergy
COPD
Pregnancy
Liver/renal disease

43
Q

First line tx for POAG

A

Prostaglandins

44
Q

Travatan Z contains

A

Travoprost with Sofzia (preservative instead of BAK)

45
Q

MOA of prostaglandins

A

Acts on FP receptors on the ciliary muscle –> up regulates matrix metalloproteinases –> reduction of collagen in the uveoscleral meshwork–> Increase outflow.

Acts on skin receptors –> activates phospholipase C –> Alters hair follicles –> Increased pigmentation and growth of hairs, skin darkening around the eyes.

46
Q

Which enzyme leads to skin side effects of prostaglandins

A

Phospholipase C

47
Q

Contraindications of prostaglanins

A
  • patients at risk for CME (post op cataract surgery)
  • Active inflammation like uveitis
  • History of HSK
48
Q

Which topical glaucoma drug do you use qAM? What about qPM?

A

qAM- BB

qPM- prostaglandins

49
Q

Prostaglandin that causes the worst conj hyperemia. What about least?

A

Worst- Bimatoprost (Lumigan)

Best- Xalatan (Latanoprost)

50
Q

Which glaucoma drugs decrease IOP by the following amounts?

33%
25%
18%

A

Prostaglandins 33%
BB 25%
Brimonidine (Alphagan) and Dorzolamide (Trusopt) 18%- both of these drugs can be combined with Timolol.

51
Q

Ocular anesthetics. Their structure consists of 3 parts

A
Aromoatic reside (lipophilic) 
Intermediate chain (increase the chain --> Increase the potency) 
Amino group (Provides hydrophilic properties) 

The bond between the amino group and chain is called an ester or amide

52
Q

ocular anesthetics: Esters vs Amides

A

Esters: Broken down locally by esterases. Short lasting. All topical anesthetics- Proparacaine, benoxinate.

Amides: Broken down by the liver, longer lasting. Lidocaine.

53
Q

Excessive use of topical anesthetics may lead to

A

corneal melting

54
Q

How do antihistamines work?

A

They block the cell receptors that histamine acts upon- they minimize the red, watery, itchy effects of allergies. They do NOT prevent the release of histamine from mast cells and basophils.

55
Q

How does a type 1 hypersensitivity reaction occur

A

After the first exposure, activated IgE antibodies will bind to mast cells and basophils. At the second exposure, the antigen will bind to the IgE. calcium will enter the cell and cause degranulation into the bloodstream. Histamine will bind to histamine receptors –> red, itchy, watery eyes.

56
Q

Emedastine combined with a vasoconstrictor

A

Naphcon A

Naphazoline (Alpha 1 agonist that causes vasoconstriction) + Emadine)

57
Q

Mast cell stabilizers

  • 4
  • MOA
  • onset ?
A

Cromolyn Sodium, alocril, alomide, Alamast
Prevent Ca2+ influx –> prevents mast cell degran
Works days to weeks after beginning therapy

58
Q

Patanol vs pataday

A

Both olopatadine
Patanol is 0.1%
Pataday is 0.2%

59
Q

BEZ POP

A

Mast cell-antihistamine combos

Bepreve
Elestat 
Zaditor
Patanol (olopatadine 0.1%) 
Optivar 
Pataday (Olopatadine 0.2%)
60
Q

Steroid systemic and ocular side effects

A

Systemic-

  1. Decreases inflammatory mediators and capillary permeability –> Decrease in immune response
  2. Decrease fibroblast and collagen formation –> Prevents healing

Ocular

  1. Increased risk of secondary infection
  2. PSC
  3. Increase IOP –> glaucoma
61
Q

Two chemistry groups of anesthetics and steroids

A

Anesthetics: Esters (break down locally, all topical anesthetics) and amides (break down by liver, lidocaine)

Steroids: Ketones (more common) and esters (soft, loteprednol)

62
Q

2 types of soft steroids

A

Fluorometholone (FML)

Loteprednol (Lotemax)

63
Q

Best penetration to least penetration for steroids

A

Emulsion (Durezol) –> Acetate (suspensions) –> Alcohol (suspension) –> Phosphate (Solution)

64
Q

_%of the general population are high steroid responders

This increases to __% if the patient has POAG

A

5% –> 90%

**Especially consider using steroids in POAG pts.

65
Q

Why do NSAIDS make us nSAD??

A

Because they beat up the cornea!! Especially diclofenac (Voltaren) -> can cause K melt

66
Q

Which 2 topical drugs can cause K melt?

A

Diclofenac (Voltaren)

Anesthetics

67
Q

How do NSAIDS work?

A

They block COX1 and 2. Prevents conversion of arachadonic acid into prostacyclines, prostaglandins, and thromboxanes (platelets). This decreases inflammation.

68
Q

NSAIDS that are dosed QID

A

Diclofenac and Ketoralac (acular) are dosed QID

69
Q

Only NSAID approved for q day

A

Bromday

70
Q

Only NSAID approved for treatment of seasonal allergic conjunctivitis But prob don’t use if the patient has any corneal involvement

A

Ketoralac

71
Q

Clinical uses of topical NSAIDS

A

Post op cataract to decrease the risk of CME
RCE (pain)
K abrasions (pain)
Allergic conjunctivitis (ketoralac)

72
Q

Which NSAID contains the preservatives BAK and sodium sulfite (caution in sulfa allergies)

What about thimerosal?

A

Xibrom (Bromfenac)

Ocufen (Flurbifrofen)

73
Q

How can you use rose bengal and lissamine green to differentiate between HSK dendrite and HZO pseudodendiret?

A

HSK dendrite: Only boarders will stain

HZO psudeodendrite: Entire ulcer will stain

74
Q

When should you not use lissamine green, rose bengal, or methylene blue

A

If cell culturing is indicated
-Lissamine green and rose bengal are anti viral

Methylene blue is bacteriostatic

75
Q

What do each of these stain:
Lissamine green
Rose bengal
Methylene blue

A

Lissamine green and rose bengal- Dead, devitalized, and cells that have lost their mucous surface. Anti viral.

Methylene blue- Similar to rose bengal but also stains corneal nerves. Good for outlining corneal blebs after glaucoma surgery. Bacteriostatic.

76
Q

Oral hyperosmotic agents

A

Rapid reduction of elevated IOP in an emergency.

  • For acute angle closure
  • Beware of Sulfa allergy

High molecular weight, unable to cross blood aqueous barrier. Osmotic gradient: Plasma in ciliary stroma is hypertonic to the aqueous humor –> fluid exits the eye

77
Q

Difference in treatment for oral vs topical hyperosmotics

A

Oral- rapid reduction of IOP

Topical- Reduce K edema

78
Q

Sodium chloride (Muro 128)

A

Must have more ions than tears (308)
Hypertonic solution to reduce K edema.

Available as eye drops (burns, OTC) or ointment (at bed time, OTC)

79
Q

AT

  • What agent increases the viscosity of the solution?
  • What is commonly incorporated into the tear solutions?
A
Methylcellulose 
Polyvinyl alcohol (PVA)
80
Q

Ointment pros and cons

A

Longer contact time–> longer duration of action, less discomfort.

Blurry vision and may increase risk for secondary infection.

81
Q

MOA of restasis (Cyclosporin 0.05%)

A

Stops production of IL2—> Prevents new T cells being formed. T cells are what cause inflammation. Takes about 3 months to work since T cells have a 90 day lifespan. Usually start pt on this + soft steroid like FML or lotemax to improve symptoms right away.

*Best for inflammatory dry eye or aqueous deficient with normal lipid layer.

Contraindicated in active infections

82
Q

Thimerosal

  • What component causes sensitivity?
  • 2 medications that this is in
A

Mercury component

-In Trifluorodine (viroptic) and Ocufen (Flurbiprofen)

83
Q

How does EDTA work as a preservative?

A

Chelating agent- binds to calcium