Pharmacology of the Eye Flashcards

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1
Q

Phase I metabolism

A

Hydrolysis, oxidation, reduction

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2
Q

Phase II metabolism

A

Conjugation (methylation, etc)

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3
Q

Absorption of drugs in eye determined by?

A

Length of time drug stays in the inferior fornix and precorneal tear film

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4
Q

How to ocular drugs enter systemic circulation?

A

Via the nasal mucosa

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5
Q

How do ocular drugs get to interior ocular structures?

A

Via aqueous humor by trabecular meshwork.

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6
Q

Metabolism?

A

tear and tissue proteins, diffusion. Hepatic if enters systemically

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7
Q

Does first pass metabolism occur if absorbed by nasal mucosa?

A

No.

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8
Q

Pupillary constriction

A

Parasympathetic inputs contract circular muscle (miosis)

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9
Q

Pupillary dilation

A

Sympathetic stimulation of radial muscles (mydriasis)

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10
Q

Ciliary body consists of

A

Ciliary muscle and ciliary epithelium

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11
Q

Parasympathetic stimulation to ciliary muscle

A

Causes contraction, accommodation (near focus), zonule fibers relax

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12
Q

Cyclospasm

A

Severe ciliary muscle contraction. Can be caused by AChE inhibitors

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13
Q

Cycloplegia

A

Block of accommodation by cholinergic antagonists

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14
Q

Effect of parasympathetic stimulation on trabecular meshwork?

A

Tension opens pores and facilitates outflow of aqueous humor into canal of Schlemm. This decreases interocular pressure

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15
Q

Where does drainage from canal of schlemm go?

A

Into superchoroidal space

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16
Q

Effect of sympathetic stimulation on aqueous humor secretion?

A

Promotes secretion by stimulating beta receptors.

17
Q

Predominant beta receptor in eye?

A

B2

18
Q

Predominant beta receptor in heart?

A

B1

19
Q

Predominant beta receptor in lungs?

A

B2

20
Q

How to treat open-angle glaucoma?

A

Decrease production of aqueous humor, increase outflow at canal of schlemm or in sclera

21
Q

Latanoprost

A

Prostaglandin agonist which is 1st line for glaucoma. Works by increasing aqueous humor outflow via uveoscleral pathway. Unclear how

22
Q

Creation of prostaglandins

A

From arachidonic acid (usually in membranes), COX oxygenizes to create prostaglandins, thromboxane, and prostacyclin

23
Q

Effect of prostaglandins

A

Targets all over body including smooth muscle and eye

24
Q

Prostaglandin agonist side effects

A

Blurred vision, burning sensation in eye, punctate keratopathy (keratitis)

25
Q

Punctate keratopathy

A

Cornification of cornea thought to be due to irritation from prostaglandin agonists or from a preservative.

26
Q

Timolol

A

B1 and B2 antagonist, second line for glaucoma. Prevents creation of aqueous humor by ciliary epithelium

27
Q

Mechanism of action of B receptor mediated creation of aqueous humor

A

Linked to Gs, so produces cAMP, which is thought to increase aqueous humor.

28
Q

Side effects of B antagonists

A

Blurred vision, burning sensation in eye, dry eyes, cough, bradycardia, hypotension. Systemic side effects unlikely.

29
Q

Why do beta blockers cause hypotension?

A

Because they slow heart rate, which decreases CO, which decreases MAP.

30
Q

Brimonidine

A

Alpha2 agonist. This works in 2 ways. 1) Binding to presynaptic A2 receptor, which decreases the amount of NE in synapse. 2) Binding to postsynaptic A2 receptor (Gi) decreasing cAMP and preventing aqueous humor production

31
Q

How does brimonidine cause hypotension

A

Because it works more strongly at the autoreceptor in vascular musculature, which prevents alpha mediated constriction.

32
Q

Dorzolamide

A

Carbonic anhydrase inhibitor. Works by preventing secretion of HCO3 into aqueous humor.

33
Q

Carbachol/pilocarpine

A

Cholinergic agonists, these cause muscarinic induced ciliary muscle contraction, increasing outflow at trabecular mesh.