Eye pharm (Linger) Flashcards

1
Q

Primary Applications of Ocular Drugs

A

Fundoscopic examination

Diagnostic (e.g., anisocoria)

Therapeutic

  • Allergic conjunctivitis
  • Infections
  • Glaucoma
  • Strabismus
  • Uveitis

Surgical

  • Preoperative
  • Intraoperative
  • Postoperative
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2
Q

Acetylcholinesterase inhibitors, muscarinic agonists such as pilocarpine, and β-blockers are among the drugs used to manage patients with glaucoma. They also share properties that are particularly relevant to patients with asthma. Which statement summarizes best what that relevance is?

A. Contraindicated for people with asthma
B. Degranulate mast cells, cause bronchocontriction
C. Raise IOP in patients with glaucoma and asthma
D. Trigger bronchoconstriction by activating H1 receptors
E. Useful for acute asthma, not for ambulatory patients

A

Contraindicated for people with asthma

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3
Q

Systemic Distribution of Ocular Drugs

A

Tears –> cornea–> aqueous humor–> iris–> systemic circulation

Tears–> conjunctiva–> sclera–> ciliary body–> systemic circulation

also cornea sclera

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4
Q

Autonomic Innervation of the Eye

A

Iris circular (Sphincter)- parasympathetic

Iris radial (dilator)- sympathetic

ciliary circular - parasympathetic

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5
Q

Iris circular

A

(Sphincter)

muscarinic agonist–> contraction; miosis

muscarinic antagonist –> relaxation; mydriasis

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6
Q

iris radial

A

alpha -1 agonist –> contraction; mydriasis

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7
Q

ciliary circular muscle

A

muscarinic agonist–> contraction; accomodation

muscarinic antagonist –> relaxation; cycloplegia

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8
Q

Carbachol, pilocarpine

A

Intraocular use for miosis during surgery, glaucoma

Side effects: Corneal edema, miosis, induced myopia, decreased vision, brow ache, retinal detachment

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9
Q

Echothiophate

A

Use for Glaucoma, accommodative esotropia (strabismus)

side effects: Blurred vision, burning sensation in eye, iritis, night blindness, uveitis

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10
Q

Atropine, homatropine, cyclopentolate, tropicamide, etc.

A

Use for: Cycloplegic retinoscopy, dilated funduscopic exam, cycloplegia

side effects: Photosensitivity, blurred vision, burning sensation in eye, raised IOP

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11
Q

pharmacologic eval of anisocoria

A

pilocarpine- cholinergic agent used for glaucoma/ can be used to test for cholinergic supersensitivity

cocaine - sympathetic agonist at norepinephrine reuptake transporter. Normal eye –> dilation. If smaller pupil does not dilate, then it means there’s not enough norepinaphrine around. Differentiates simple anisocoria from horner’s syndrome.

hydroxyamphetamine - causes release of NE stores. distinguishes preganglionic/ central horner’s (dilation) from postganglionic horner’s (no dilation)

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12
Q

horner syndrome

A

ptosis, miosis, anhydrosis

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13
Q

Pharmacologic Evaluation of Anisocoria: Apraclonidine

A

Alternative with similar efficacy as cocaine test
0.5% solution placed in both eyes
Affected pupil will dilate more than the normal pupil

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14
Q

Pharmacologic Evaluation of Anisocoria: Phenylephrine

A

Alternative with similar efficacy as hydroxyamphetamine test
1% solution placed in both eyes
Normal eye will dilate < 0.5 mm
If postganglionic lesion, affected eye will dilate more than unaffected eye

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15
Q

Glaucoma

A

Among the leading causes of blindness in the US

Increased pressure within the eyeball can result in damage to the optic disk and gradual loss of vision

Risk factors:

  • Elevated intraocular pressure (IOP)
  • Positive family history
  • African-American heritage
  • Myopia (nearsightedness)
  • Hypertension
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16
Q

drugs for glaucoma do one of 2 things

A

increase drainage

or decrease production of aqueous humor

17
Q

A patient with a history of angle-closure glaucoma experiences a sudden rise of intraocular pressure that is sufficiently severe. In addition to pain there is an imminent risk of permanent vision loss. He requires immediate treatment, one element of which is administration of echothiophate. What enzyme is affected by this drug?

Tyrosine hydroxylase – stimulated
Acetylcholinesterase (AChE) – inhibited
Catechol-O-methyltransferase (COMT) – inhibited
Monoamine oxidase (MAO) – stimulated
DOPA decarboxylase - stimulated
A

Acetylcholinesterase (AChE) – inhibited

Increasing contraction of the ciliary muscle and the sphincter iris muscle –> constriction of the pupils–> unsmushes the iris, promotes drainage of aqueous humor

Muscarinic agonists like pilocarpine and carbachol can also be used

18
Q

Angle-Closure Glaucoma

A

AKA closed-angle or narrow-angle
Usually acute
Medical emergency
Surgical iridectomy

Short-term drug therapy with muscarinic agonists; sometimes also AChE inhibitors

Antimuscarinics, some antihistamines (dirty drugs- anti-muscarinic actions), and α1-adrenergic agonists are contraindicated

19
Q

Open-Angle Glaucoma

A

AKA primary or chronic glaucoma
Most common type
Affects ~3 million Americans
Pharmacotherapy reduces IOP, but may or may not slow progression

20
Q

A variety of ophthalmic drugs, working by several main mechanisms of action, are useful for managing chronic open-angle glaucoma. Which one reduces intraocular pressure by decreasing the formation of aqueous humor, rather than by changing the size of the pupil(s)?

Carbachol
Echothiophate
Pilocarpine
Prazosin
Timolol
A

Timolol

21
Q

Drugs for Open-Angle Glaucoma: Mechanisms of Action: Decreased Aqueous Secretion

A

Beta-blockers
Alpha-2-selective agonists
Carbonic Anhydrase Inhibitors (CAIs)

22
Q

Drugs for Open-Angle Glaucoma: Mechanisms of Action: Increased Outflow

A
Prostaglandin F2α analogs
Alpha-2-selective agonists
Cholinomimetics
- Muscarinic agonists
- Acetylcholinesterase (AChE) inhibitors
23
Q

Prostaglandin F2α Analogs

A

Prototype: Latanoprost
Other agents: Bimatoprost (Latisse), Travoprost, and Unoprostone
1st line therapy for open-angle glaucoma
Low systemic side effects; ocular side effects include conjunctival hyperemia, irritation, increased number and length of lashes, changes in iris and lash pigmentation
Once-daily topical administration
Potent reduction of IOP

24
Q

Sites of drug action

A

uveoscleral outflow: prostaglandin agonists

Trebecular outflow: muscarinic agonists

Aqueous humor inflow: beta blockers, alpha 2 AR agonists, CAIs

25
Q

A 55-year-old woman has just been diagnosed with chronic open-angle glaucoma, and you conclude that drug therapy is indicated. She also tends to be tachycardic. Notes written by her family practice physician indicate that she has Stage 2 essential hypertension. Which one of the following drugs would be the most rationale choice for this woman?

Captopril
Carteolol
Diltiazem
Hydrochlorothiazide
Verapamil
A

Carteolol- beta blocker

26
Q

Beta-blockers

A

Non-selective (β1 and β2): Timolol, levobunolol, metipranolol, and carteolol

β1-selective: Betaxolol (less efficacious than non-selective agents because the β receptors in the eye are largely of the β2 subtype)

Twice daily dosing; fewer ocular side effects

Systemic distribution may cause serious adverse effects

Asthma, COPD, and some cardiac dysrhythmias are relative contraindications

27
Q

α-Adrenergic Agonists

A

α2-selective: apraclonidine, brimonidine

Nonselective: epinephrine, dipivefrin (prodrug)

Common adverse effects

  • Stinging, burning, blurring, or other discomfort in the eye
  • Dry mouth, headaches, and increased blood pressure

Drug interactions
- Antidepressants may alter metabolism

28
Q

A patient presents with chronic open-angle glaucoma. What “renal” drug, or a drug in the same chemical and pharmacologic class, might be prescribed as an adjunct to lower intraocular pressure and help manage this condition?

Acetazolamide
Amiloride
Furosemide
Spironolactone
Triamterene
A

Acetazolamide
- carbonic anhydrase inhibitor

not used a ton in HTN or glaucoma but is decent for both things at the same time

29
Q

Carbonic Anhydrase Inhibitors

A

Topical: dorzolamide, brinzolamide
Oral: acetazolamide, methazolamide
Frequent dosing; topical agents are less effective than other pharmacologic therapies

Side effects

  • Topical: stinging, redness, dry eyes, and blurred vision
  • Oral: malaise, fatigue, depression, paresthesias, and nephrolithiasis
30
Q

Cholinomimetics

A

Muscarinic agonists: pilocarpine, carbachol
AChE inhibitors: echothiophate
Previously 1st line therapy
Frequent dosing

Side effects

  • Visual blurring from induced myopia
  • Fixed, small pupils
  • Can promote retinal tears
  • AChE inhibitors can promote cataract formation
31
Q

A patient has mild cutaneous and systemic manifestations of a seasonal allergic response. Before you prescribe a short course of diphenhydramine for symptom relief, you should realize that this drug has a mechanism of action resembling, causes many side effects similar to, and shares many contraindications, that apply to an “autonomic” drug, with which you should be very familiar. What is that drug?

Atropine
Bethanecol
Norepinephrine
Phentolamine
Physostigmine
Propranolol
A

Atropine

32
Q

Drugs Contraindicated in Angle-Closure Glaucoma

A

Antimuscarinics

Some antihistamines

α1-adrenergic agonists

33
Q

Medical Marijuana for Glaucoma

A
Pros
Lowers IOP (unknown mechanism)

Cons
Short duration of action
Altered mood and mental capacity
Adverse effects include lung and brain damage
Systemic hypotension could complicate vision loss
Lack of quality control