Ophthalmic Drugs Flashcards

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1
Q

What are the receptors of the Iris Sphincter?

A
  1. Muscarinic

2. Few Alpha and Beta

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2
Q

What are the receptors of the Ciliary Muscle?

A
  1. Muscarinic

2. Some Beta 1

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3
Q

What are the receptors of the Iris Dilator?

A
  1. Mostly Alpha 1

2. Few Beta

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4
Q

What are the receptors of the Ciliary Process?

A
  1. Mostly Beta 2
  2. Some Alpha 2 and Beta 1
  3. Muscarinic
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5
Q

What are the receptors of Mueller’s Muscle?

A
  1. Alpha 1
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6
Q

Which ocular muscles are mainly parasympathetic?

A
  1. Iris Sphincter

2. Ciliary Muscle

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7
Q

Which ocular muscles are mainly sympathetic?

A
  1. Iris Dilator
  2. Ciliary Process
  3. Mueller Muscle
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8
Q

What are 3 functions of Adrenergic Agonists for the eye?

A
  1. Mydriasis
  2. Treatment of Glaucoma
  3. Decongestant
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9
Q

What is Epinephrine?

A

An Alpha 1,2 and Beta 1,2 Adrenergic Agonist

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10
Q

What are the ocular uses of Epinephrine?

A
  1. Vasoconstriction

2. Glaucoma (not much anymore)

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11
Q

How does Epinephrine work to treat Glaucoma?

A

Alpha 1 and Beta 2 –> Increased Aq Production, but Beta 2 also increases Aq Outflow –> Decreased IOP

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12
Q

What are the side effects of Epinephrine?

A
  1. HA
  2. Hyperglycemia
  3. Tachycardia
  4. HTN
  5. Thyrotoxicosis
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13
Q

What are the ocular side effects of Epinephrine?

A
  1. Dilation
  2. Lid Retraction
  3. Lacrimation
  4. Pigmentation of the Iris/Lens (w/ Oxidized Epinephrine)
  5. Angle Closure
  6. Increased IOP
  7. Cystoid Macular Edema
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14
Q

What is significant about the cystoid macular edema caused by Epinephrine?

A

It can –> swelling of central part of the retina –> blindness if not treated early

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15
Q

What is Phenylephrine?

A

A Direct Alpha 1 Agonist

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16
Q

What are the ocular uses of Phenylephrine?

A
  1. Mydriasis
  2. Decongestant
  3. Breaking Posterior Synchia to the lens
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17
Q

How long does Mydriasis occur with Phenylephrine?

A

Onset- 1hr

Duration- 7hrs

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18
Q

What drug is commonly used for DFE?

A

Phenylephrine

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19
Q

What is the role of the decongestant use of phenylephrine?

A

To differentiate Episcleritis from Scleritis

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20
Q

What are the ocular side effects of Phenylephrine?

A
  1. Lid Retraction
  2. Lacrimation
  3. Angle Closure
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21
Q

Why is phenylephrine not used for narrow angle dilation?

A

Because phenylephrine may –> Angle Closure, and it is harder to reverse its mydriasis

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22
Q

Which drug class worsens the sympathomimetic side effects of Phenylephrine?

A

MAOIs

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23
Q

Does Phenylephrine induce Cycloplegia?

A

No- because the ciliary body muscle has few Alpha receptors

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24
Q

Is the Active Light reflex present with Phenylephrine?

A

Yes- because the Parasympathetics to the Iris Sphincter are still intact

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25
Q

What is Apraclonidine?

A

Direct Alpha Adrenergic Agonist; some specificity for Alpha 2

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26
Q

What is the ocular use of Apraclonidine?

A
  1. Treatment of glaucoma
  2. Fast reduction of High IOP
  3. Pre and Post-Op Glaucoma/Laser Treatment
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27
Q

How long does the reduction of IOP with Apraclonidine last?

A

3-5 hours - but fast acting

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28
Q

Why is Apraclonidine not used for long term use?

A

Significant Drift

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29
Q

What are the 3 Mechanisms by which Apraclonidine reduces IOP?

A
  1. Binds presynaptic A2 receptrs –> Decreased NE, so less stimulation of B2 on the Ciliary Process –> Decreased Aq Production
  2. Binds postjunctional A2 receptors in the Epithelium of the Ciliary Process –> reduction of intracellular cAMP –> Decreased Aq Production
  3. Binds A2 receptors on the episcleral veins –> Dilation –> increased Aq outflow through the uveoscleral pathway
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30
Q

What are the side effects of Apraclonidine?

A

Dry Mouth, HA, Lethargy

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31
Q

What are the ocular side effects of Apraclonidine?

A
  1. Allergic RXN and Red Eyes

2. Mydriasis, Conjunctival Vascular Constriction, Lid Retraction (mild- due to some Alpha 1 Stimulation)

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32
Q

What is Brimonidine?

A

A Direct acting Alpha 2 Agonist (Highly Selective)

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33
Q

What is the treatment for Normal Tension Glaucoma?

A

Brimonidine

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34
Q

What is the secondary function of Brimonidine?

A

Primary Open Angle Glaucoma

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35
Q

How does Brimonidine similar/different from Apraclonidine?

A

Similar- Reduces IOP (same mechanism)

Different- Less long term drift (b/c more selective for Alpha 2), less Allergic RXN

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36
Q

What are the side effects of Brimonidine?

A
  1. Dry Mouth
  2. HA
  3. Lethargy
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37
Q

What are the ocular side effects of Brimonidine?

A
  1. Allergic RXN (less severe than Apraclonidine)

* *No Alpha 1 effects because so selective

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38
Q

What are the Direct Acting Adrenergic Agonists?

A
  1. Norepinephrine
  2. Epinephrine
  3. Phenylephrine
  4. Apraclonidine
  5. Brimonidine
39
Q

What are the Indirect Adrenergic Agonists?

A
  1. Cocaine

2. Hydroxyamphetamine

40
Q

What is the MOA of Cocaine?

A

Blocks NE reuptake

41
Q

What is the use of Cocaine?

A

Diagnosis of Horner’s Syndrome

42
Q

What is Horner’s Syndrome?

A
  • Loss of sympathetics
    1. Miosis - Loss of Iris Dilator FXN
    2. Ptosis- Mild eyelid droop (loss of Mueller’s, but LPS and CNIII still ok)
    3. Anhydrosis- loss of sweat gland FXN
43
Q

What will be the result of Cocaine admin in a Horner’s eye or a Normal eye?

A

Normal- dilation

Horner’s- Nothing

44
Q

What is the MOA of Hydroxyamphetamine?

A

Stimulates NE release onto the Iris Dilator from Presynaptic terminals of Post-Ganglionic Neurons

45
Q

If Horner’s Syndrome is PRE-ganglionic, what is the result of Hydroxamphetamin admin? What are possible causes?

A
  • Pupil dilates

- Causes of Pre-Ganglionic Horner’s: Pancoast Tumor, Thoracic Aortic Aneurysm, S/P Carotid Endarterectomy

46
Q

If Horner’s Syndrome is POST-ganglionic, what is the result of Hydroxamphetamin admin? What are possible causes?

A
  • No Pupil Dilation

- Goiter, Cavernous Sinus Syndrome

47
Q

Which drug is an Alpha Blocker?

A

Dapiprazole

48
Q

What is the function of Dapiprazole?

A

Reverse mydriasis

49
Q

What is the MOA of Dapiprazole?

A

Competitively binds to post-synaptic receptors of the iris dilator muscle

50
Q

What are the side effects of Dapiprazole?

A
  1. Hyperemia (Blocks Alpha 1)

2. Mild Ptosis (blocks Mueller’s)

51
Q

What is Timolol?

A

A non-specific Beta-Blocker

52
Q

What is the ocular use of Timolol?

A

Treatment of Glaucoma

53
Q

What is the MOA of Timolol?

A

Blocks B Receptors at the Ciliary Process which results in decreased Aq production –> decreased IOP

54
Q

What does Beta stimulation cause at the Ciliary Process and what is the mechanism?

A

Increased Aq production through adenylate cyclase/cAMP pathway

55
Q

What are 4 factors that make Timolol the first line for glaucoma treatment?

A
  1. No Intrinsic Sympathomimetic Activity
  2. No Pupil dilation
  3. Does not bind to melanin
  4. Only mild long-term drift
56
Q

What are Levobunolol and Metripranolol?

A

Non-specific Beta Blockers (work similar to Timolol)

57
Q

What drug has the same function but a longer duration than Timolol?

A

Levobunolol

58
Q

What are the side effects of the Beta Blockers?

A
  1. Bradycardia, conduction arrhythmias (B1)
  2. Respiratory depression/bronchodilation (B2)
  3. Worsens Myasthenia Gravis
  4. Depression
59
Q

Beta Blockers are contraindicated in which patients?

A
  1. CHF

2. COPD/Bronchitis and Asthma

60
Q

What are the ocular side effects of Beta Blockers?

A
  1. Corneal Anesthesia
61
Q

What are the non-selective Beta Blockers?

A
  1. Timolol
  2. Levobunolol
  3. Metipranolol
  4. Carteolol
62
Q

What is the B1 selective Beta Blocker?

A

Betaxolol

63
Q

What is the advantage of Betaxolol over the non-selective Beta Blockers?

A

Can be used in COPD/Asthma patients

64
Q

Betaxolol is contraindicated in which patients?

A

Patients with cardiac issues

65
Q

How is the potency of betaxolol?

A

Lower than non-selective Beta Blockers, because there are significantly fewer B1 receptors in the Ciliary Process

66
Q

What is Carteolol?

A

A non-selective Beta Blocker

67
Q

What is the MOA of Carteolol?

A

It has Intrinsic Sympathomimetic Activity and competes with NE and EPI in binding to Beta receptors at the Ciliary Process- but it has only 1-2% efficacy of NE and EPI, so it results in a decreased activity

68
Q

Which structures are mainly innervated by Parasympathetics (Muscarinic Receptors)?

A
  1. Iris Sphincter

2. Ciliary Muscle

69
Q

Which structures are mainly innervated by Sympathetics (Adrenergic Receptors)?

A
  1. Iris Dilator
  2. Ciliary Process
  3. Mueller Muscle
70
Q

Which structures mostly have A1 receptors?

A
  1. Iris Dilator

2. Mueller Muscle

71
Q

Which structure mostly has B1 receptors?

A
  1. Ciliary Process
72
Q

What is Pilocarpine?

A

A direct acting Cholinergic Agonist- selective for Muscarinic

73
Q

Why is pilocarpine long lasting?

A

It is not susceptible to AchE

74
Q

What is the primary usage of Pilocarpine, and what is its MOA?

A
  1. Acute treatment of Angle Closure Glaucoma

- stimulates Iris Sphincter Muscle –> Miosis –> pulls iris out of angle –> allows Aq drainage

75
Q

How is Pilocarpine used in the treatment of POAG?

A

Stimulates Muscarinic R of Ciliary Muscle –> pulls on trabecular meshwork to widen it –> increased Aq outflow

76
Q

What are the side effects of Pilocarpine?

A
  1. HA
  2. Bradycardia
  3. Hypotension
  4. Bronchoconstriction and PE
  5. Mental Status Changes
77
Q

What are the ocular side effects of Pilocarpine?

A
  1. Blurred Vision- distance
  2. Accommodative Spasm
  3. Miosis
78
Q

What are the three direct acting Cholinergic Agonists?

A
  1. Pilocarpine (M)
  2. Acetylcholine (M=N)
  3. Carbachol (M=N)
79
Q

What is the ocular effect of Acetylcholine?

A

Miosis- lasting about 25mins

80
Q

Why is Acetylcholine not frequently used?

A

Rapid metabolism by AchE

81
Q

What is the ocular use of Carbachol?

A

Miosis (up to 24hrs) used in complicated cataracts surgeries

82
Q

What are the indirect acting Cholinergic agonists?

A
  1. Short Acting- Physostigmine and Neostigmine

2. Long Acting- Ecothiophate and Isoflurophate

83
Q

What is the MOA for the Indirect Acting Cholinergic Agonists?

A

Inhibit Acetylcholinesterase

84
Q

Why are Ecothiophate and Isoflurophate not commonly used?

A

Excessive side effects:

  1. Accelerated cataract formation
  2. Increased risk of retinal detachment
  3. Iris Cysts
  4. Diarrhea, Nausea and Vomiting
85
Q

What effects do Cholinergic Antagonists have?

A
  1. Mydriasis (Inhibits Iris Sphincter)
  2. Cycloplegia (Inhibit Ciliary Muscles)
  3. Pain Relief for Uveitis/Inflammation (Inhibition of Ciliary Muscle Movement and reduces risk of Posterior Synechia to the lens)
86
Q

What is the clinical use of Cycloplegia?

A
  1. Accurate refraction in Hyperopes

2. Vision therapy in Accommodative Esotropia

87
Q

What are the Cholinergic Antagonists (Anti-muscarinics)?

A
  1. Tropicamide
  2. Cyclopentolate
  3. Homatropine
  4. Atropine
88
Q

What are the features and uses of Tropicamide?

A
  1. Good Mydriasis (20-30mins, lasts 4hrs)
  2. No Cycloplegia
    * *Used for DFE
89
Q

What are the features and uses of Cyclopentolate?

A
  1. Great Mydriasis (15-30mins, lasts 24hrs)
    * *surgical dilation
  2. Good Cycloplegia
    * *refraction in Hyperopes
90
Q

What are the features and uses of Homatropine?

A
  1. Great Mydriasis and Cycloplegia (1-30mins, lasts 48hrs)

* *Used in pain relief for inflammation

91
Q

What are the features and uses of Atropine?

A
  1. Extreme Mydriasis and Cycloplegia (30-40mins, last 7-12 DAYS)
    * *DFE in infants and children, vision therapy for accommodative seotropia)
92
Q

Atropine is contraindication in which patients?

A

Down Syndrome and Glaucoma Patients

93
Q

What are the side effects of anti-muscarinics?

A
  1. Tachycardia
  2. Dry Mouth
  3. Fever
    * Worse with Atropine, minimal with Tropicamide
94
Q

What is the ocular side effect of Atropine (and to a lesser extent the other anti-muscarinics)?

A

Increased IOP