Ophthalmic Drugs Flashcards

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
What is Apraclonidine?
Direct Alpha Adrenergic Agonist; some specificity for Alpha 2
26
What is the ocular use of Apraclonidine?
1. Treatment of glaucoma 2. Fast reduction of High IOP 3. Pre and Post-Op Glaucoma/Laser Treatment
27
How long does the reduction of IOP with Apraclonidine last?
3-5 hours - but fast acting
28
Why is Apraclonidine not used for long term use?
Significant Drift
29
What are the 3 Mechanisms by which Apraclonidine reduces IOP?
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
30
What are the side effects of Apraclonidine?
Dry Mouth, HA, Lethargy
31
What are the ocular side effects of Apraclonidine?
1. Allergic RXN and Red Eyes | 2. Mydriasis, Conjunctival Vascular Constriction, Lid Retraction (mild- due to some Alpha 1 Stimulation)
32
What is Brimonidine?
A Direct acting Alpha 2 Agonist (Highly Selective)
33
What is the treatment for Normal Tension Glaucoma?
Brimonidine
34
What is the secondary function of Brimonidine?
Primary Open Angle Glaucoma
35
How does Brimonidine similar/different from Apraclonidine?
Similar- Reduces IOP (same mechanism) | Different- Less long term drift (b/c more selective for Alpha 2), less Allergic RXN
36
What are the side effects of Brimonidine?
1. Dry Mouth 2. HA 3. Lethargy
37
What are the ocular side effects of Brimonidine?
1. Allergic RXN (less severe than Apraclonidine) | * *No Alpha 1 effects because so selective
38
What are the Direct Acting Adrenergic Agonists?
1. Norepinephrine 2. Epinephrine 3. Phenylephrine 4. Apraclonidine 5. Brimonidine
39
What are the Indirect Adrenergic Agonists?
1. Cocaine | 2. Hydroxyamphetamine
40
What is the MOA of Cocaine?
Blocks NE reuptake
41
What is the use of Cocaine?
Diagnosis of Horner's Syndrome
42
What is Horner's Syndrome?
- 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
What will be the result of Cocaine admin in a Horner's eye or a Normal eye?
Normal- dilation | Horner's- Nothing
44
What is the MOA of Hydroxyamphetamine?
Stimulates NE release onto the Iris Dilator from Presynaptic terminals of Post-Ganglionic Neurons
45
If Horner's Syndrome is PRE-ganglionic, what is the result of Hydroxamphetamin admin? What are possible causes?
- Pupil dilates | - Causes of Pre-Ganglionic Horner's: Pancoast Tumor, Thoracic Aortic Aneurysm, S/P Carotid Endarterectomy
46
If Horner's Syndrome is POST-ganglionic, what is the result of Hydroxamphetamin admin? What are possible causes?
- No Pupil Dilation | - Goiter, Cavernous Sinus Syndrome
47
Which drug is an Alpha Blocker?
Dapiprazole
48
What is the function of Dapiprazole?
Reverse mydriasis
49
What is the MOA of Dapiprazole?
Competitively binds to post-synaptic receptors of the iris dilator muscle
50
What are the side effects of Dapiprazole?
1. Hyperemia (Blocks Alpha 1) | 2. Mild Ptosis (blocks Mueller's)
51
What is Timolol?
A non-specific Beta-Blocker
52
What is the ocular use of Timolol?
Treatment of Glaucoma
53
What is the MOA of Timolol?
Blocks B Receptors at the Ciliary Process which results in decreased Aq production --> decreased IOP
54
What does Beta stimulation cause at the Ciliary Process and what is the mechanism?
Increased Aq production through adenylate cyclase/cAMP pathway
55
What are 4 factors that make Timolol the first line for glaucoma treatment?
1. No Intrinsic Sympathomimetic Activity 2. No Pupil dilation 3. Does not bind to melanin 4. Only mild long-term drift
56
What are Levobunolol and Metripranolol?
Non-specific Beta Blockers (work similar to Timolol)
57
What drug has the same function but a longer duration than Timolol?
Levobunolol
58
What are the side effects of the Beta Blockers?
1. Bradycardia, conduction arrhythmias (B1) 2. Respiratory depression/bronchodilation (B2) 3. Worsens Myasthenia Gravis 4. Depression
59
Beta Blockers are contraindicated in which patients?
1. CHF | 2. COPD/Bronchitis and Asthma
60
What are the ocular side effects of Beta Blockers?
1. Corneal Anesthesia
61
What are the non-selective Beta Blockers?
1. Timolol 2. Levobunolol 3. Metipranolol 4. Carteolol
62
What is the B1 selective Beta Blocker?
Betaxolol
63
What is the advantage of Betaxolol over the non-selective Beta Blockers?
Can be used in COPD/Asthma patients
64
Betaxolol is contraindicated in which patients?
Patients with cardiac issues
65
How is the potency of betaxolol?
Lower than non-selective Beta Blockers, because there are significantly fewer B1 receptors in the Ciliary Process
66
What is Carteolol?
A non-selective Beta Blocker
67
What is the MOA of Carteolol?
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
Which structures are mainly innervated by Parasympathetics (Muscarinic Receptors)?
1. Iris Sphincter | 2. Ciliary Muscle
69
Which structures are mainly innervated by Sympathetics (Adrenergic Receptors)?
1. Iris Dilator 2. Ciliary Process 3. Mueller Muscle
70
Which structures mostly have A1 receptors?
1. Iris Dilator | 2. Mueller Muscle
71
Which structure mostly has B1 receptors?
1. Ciliary Process
72
What is Pilocarpine?
A direct acting Cholinergic Agonist- selective for Muscarinic
73
Why is pilocarpine long lasting?
It is not susceptible to AchE
74
What is the primary usage of Pilocarpine, and what is its MOA?
1. Acute treatment of Angle Closure Glaucoma | - stimulates Iris Sphincter Muscle --> Miosis --> pulls iris out of angle --> allows Aq drainage
75
How is Pilocarpine used in the treatment of POAG?
Stimulates Muscarinic R of Ciliary Muscle --> pulls on trabecular meshwork to widen it --> increased Aq outflow
76
What are the side effects of Pilocarpine?
1. HA 2. Bradycardia 3. Hypotension 4. Bronchoconstriction and PE 5. Mental Status Changes
77
What are the ocular side effects of Pilocarpine?
1. Blurred Vision- distance 2. Accommodative Spasm 3. Miosis
78
What are the three direct acting Cholinergic Agonists?
1. Pilocarpine (M) 2. Acetylcholine (M=N) 3. Carbachol (M=N)
79
What is the ocular effect of Acetylcholine?
Miosis- lasting about 25mins
80
Why is Acetylcholine not frequently used?
Rapid metabolism by AchE
81
What is the ocular use of Carbachol?
Miosis (up to 24hrs) used in complicated cataracts surgeries
82
What are the indirect acting Cholinergic agonists?
1. Short Acting- Physostigmine and Neostigmine | 2. Long Acting- Ecothiophate and Isoflurophate
83
What is the MOA for the Indirect Acting Cholinergic Agonists?
Inhibit Acetylcholinesterase
84
Why are Ecothiophate and Isoflurophate not commonly used?
Excessive side effects: 1. Accelerated cataract formation 2. Increased risk of retinal detachment 3. Iris Cysts 4. Diarrhea, Nausea and Vomiting
85
What effects do Cholinergic Antagonists have?
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
What is the clinical use of Cycloplegia?
1. Accurate refraction in Hyperopes | 2. Vision therapy in Accommodative Esotropia
87
What are the Cholinergic Antagonists (Anti-muscarinics)?
1. Tropicamide 2. Cyclopentolate 3. Homatropine 4. Atropine
88
What are the features and uses of Tropicamide?
1. Good Mydriasis (20-30mins, lasts 4hrs) 2. No Cycloplegia * *Used for DFE
89
What are the features and uses of Cyclopentolate?
1. Great Mydriasis (15-30mins, lasts 24hrs) * *surgical dilation 2. Good Cycloplegia * *refraction in Hyperopes
90
What are the features and uses of Homatropine?
1. Great Mydriasis and Cycloplegia (1-30mins, lasts 48hrs) | * *Used in pain relief for inflammation
91
What are the features and uses of Atropine?
1. Extreme Mydriasis and Cycloplegia (30-40mins, last 7-12 DAYS) * *DFE in infants and children, vision therapy for accommodative seotropia)
92
Atropine is contraindication in which patients?
Down Syndrome and Glaucoma Patients
93
What are the side effects of anti-muscarinics?
1. Tachycardia 2. Dry Mouth 3. Fever * Worse with Atropine, minimal with Tropicamide
94
What is the ocular side effect of Atropine (and to a lesser extent the other anti-muscarinics)?
Increased IOP