Ocular Pharmacology - French

Question 1

Latanoprost

Answer 1

Prostaglandin analog.

Question 2

Brimonidine

Answer 2

Alpha adrenergic agonist.

Question 3

Timolol

Answer 3

Beta adrenergic antagonist.

Question 4

Dorzolamide

Answer 4

Carbonic anhydrase inhibitor.

Question 5

Pilocarpine

Answer 5

Cholinomimetic.

Question 6

Describe the mechanism of action, role in glaucoma treatment, and list the use-limiting systemic
side effects and contraindications of:

Prostaglandin analogs.

Answer 6

First-line treatment for open angle glaucoma. (Latanoprost)

Mechanism of action is increase of outflow.

Use limiting side effects minimal (brown discoloration of iris, lengthening of eyelashes).

Question 7

Describe the mechanism of action, role in glaucoma treatment, and list the use-limiting systemic
side effects and contraindications of:

Alpha2 selective adrenergic agonists.

Answer 7

Apraclonidine
[Brimonidine]

Second-line treatment for open-angle glaucoma if prostaglandins are not sufficient

Both increased aqueous humor outflow and decreases production.

Side effects: red eye (irritation), CNS depression (hypotension and somnolence), apnea in children

Question 8

Describe the mechanism of action, role in glaucoma treatment, and list the use-limiting systemic
side effects and contraindications of:

Beta adrenergic antagonists.

Answer 8

Timolol

Next preferred treatment for open-angle glaucoma after prostaglandins.

Decrease production of aqueous humor by blocking B2 pathway.

Contraindications: asthma, COPD, bradycardia, heart block

Question 9

Describe the mechanism of action, role in glaucoma treatment, and list the use-limiting systemic
side effects and contraindications of:

Carbonic anhydrase inhibitors.

Answer 9

Dorzolamide.

Decrease production of aqueous humor via decrease in bicarb production. Add on (2nd/3rd line) after prostaglandins (Latanoprost) and Nonspecific beta blocker (timolol).

Side effect: Bitter taste.

Question 10

Describe the mechanism of action, role in glaucoma treatment, and list the use-limiting systemic
side effects and contraindications of:

Cholinomimetics.

Answer 10

Pilocarpine

Less commonly used today (historical).

INcreases outflow by muscarinic constriction of the ciliary muscle.

Side effects: Ciliary spasm leading to headaches, myopia, dim vision (small pupil).

Question 11

Relate the anatomy and function of the eye to the drug targets for pharmacotherapy for glaucoma, especially the production and outflow of aqueous humor and the role of autonomic nervous system regulation.

Answer 11

Aqueous humor secreted continuously by the epithelium covering the ciliary body. Flows between the lens and the iris, draining into the canal of schlemm.

Question 12

Systemic absorption-distribution of topically administered ophthalmic medications primarily occurs
via _____.

Does this avoid first-pass metabolism?

Answer 12

nasolacrimal drainage

Absorption from the nasal mucosa avoids first-pass metabolism, so systemic side effects from topical medications are possible (esp. with chronic use).

Question 13

the cornea can be considered as a trilamellar “fat-water-fat”. What type of drugs are best suited to cross?

Answer 13

Drugs with both hydrophilic and lipophilic properties would be best suited for transcorneal absorption

Question 14

What are the three routes of entry for eye medications?

Answer 14

Nasolacrimal
Trans-corneal
Sclera

Question 15

What is the biggest non-epidemiologic risk factor for open angle glaucoma?

What is the first-line treatment?

Answer 15

Increased IOP (>22mmHg, normal is 10-15)

Drugs that lower IOP are the first line (prostaglandin analog).

[High incidence in african-americans. The most common preventable form of blindness.]

Question 16

What is a three step approach to decreasing IOP for patients with glaucoma?

Answer 16

1) Prostaglandins.
2) Good response but insufficient then try Bblocker OR carbonic anhydrase inhibitor OR alpha2 agonist
3) Poor response–> discontinue Prostaglandins and try something else.

Question 17

What are the side effects of prostaglandins delivered to the eye?

Answer 17

Minimal. No systemic,

[Brown discoloration of iris, eyelash lengthening and darkening, ocular irritation.]

Question 18

What are the side effects of the alpha adrenergic agonists? What is the prototypical drug? What is the mechanism by which IOP is lowered?

Answer 18

Apraclonidine
[Brimonidine]

Increased outflow of humor and decreased production of humor.

Side effects: Red eye and ocular irritation; CNS depression (hypotension and somnolence); apnea in children under 2 years old.

Question 19

Why don’t we use cholinergic agonists anymore (generally)?

How did they work?

Answer 19

Ciliary spasm leading to headaches, myopia, dim vision (small pupil).

Lower IOP by causing muscarinic receptor-induced contraction of ciliary muscle which facilitates aqueous outflow.

Question 20

What drug categories increase outflow of humor?

Answer 20

Prostaglandins
Alpha2 Adrenergic agonists
Cholinergic agonists

Question 21

What drugs decrease production of humor?

Answer 21

Beta adrenergic antagonists

Carbonic anhydrase inhibitors

Question 22

What is the most common treatment after prostaglandin analogs?

How do they work?

Answer 22

Beta adrenergic antagonists.

Reduces aqueous humor production via block of beta 2 receptor pathway. May also act via decrease in ocular blood flow which decreases ultrafiltration required for production.

Question 23

What are the side effects of beta blockers?

Answer 23

Side effects: Systemic absorption of topical beta-blockers can produce all of the side effects associated with direct systemic administration. Relative contraindication in patients with bradycardia, heart block, heart failure, asthma or obstructive airway disease.

Question 24

What are side effects of the carbonic anhydrase inhibitors?

Answer 24

Main one = bitter taste in mouth.

Question 25

What drug is used to treat closed-angle glaucoma?

Answer 25

Pilocarpine. (Cholingergic agonist)

Also acetazolamide, mannitol/glycerol.