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Unit3_Pharma Flashcards

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1
Q

What is the difference between ophthalmic solution and ophthalmic suspensions?

A

Suspensions have limited solubility

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2
Q

Increased time in the cul-de-sac of the eye facilitates what in terms of drug administration?

A

Increased absorption

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3
Q

The rate and extent of drug absorption into ocular structures is determined by: ? (5 things)

A
  1. ) Time drugs remains in cul-de-sac and precornal tear film.
  2. ) Elimination by nasolacrimal drainage.
  3. ) Drug binding to tear proteins.
  4. ) Drug metabolism by tear and tissue enzymes.
  5. ) Diffusion across cornea and conjuctiva.
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4
Q

After you give the drops, the appearance of the drugs in the Aqueous Humor is dependent on what?

A

Passive diffusion through the cornea.

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5
Q

The cornea is trilamellar. What order are the layers types in?

A

Fat-Water-Fat

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6
Q

The cornea is a tri-lamellar structure (“Fat-Water-Fat”), drugs that have what properties are best suited for transcorneal absorption?

A

Drug with both HYDROphillic and LIPOphillic properties

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7
Q

the systemic absorption of topically administered ophthalmic meds primarily occurs vi ______?

A

Nasolacrimal drainage

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8
Q

What are the 3 possible absoroption pathways of topcially administred ophthalmic drugs?

A
  1. ) Nasolacrimal route
  2. ) Corneal route
  3. ) Conjuctival-scleral route
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9
Q

Localized biotransformation of ocular drugs can be significant due to the presence of a variety of enzyme systems including: ? (6)

A
  • esterases
  • oxidoreductases
  • various transferases (conjugations)
  • monoamine oxidase
  • COMT
  • 11-beta-hydroxysteroid dehydrogenase
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10
Q

Why are esterases one of the more important enzymes to consider in terms of drug breakdown?

A

Many active form of ophthalic drugs are ESTERS, b/c they have great lipid solubility –> better penetration of cornea.

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11
Q

What is the leading cause of blindness?

1st in Hispanic-Americans
2nd in African-Americans 3rd in Caucasians

A

Glaucoma

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12
Q

What are the risk factors ~ Glaucoma?

A
  • IOP
    • Hx
  • being black
  • myopia and HTN
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13
Q

What is the normal IOP?

A

10-15mmHg above ATM

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14
Q

What is increased IOP ~ glaucoma?

A

> 22mmHg above ATM

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15
Q

Aqueous humor is secreted slowly and continuously by the cells of the epithelium covering the ciliary body –> drains into (what structure)?

A

canal of Schlemm.

(runs around the eye close to the outer margin of the iris)

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16
Q

Can you surgically Tx Open-Angle Glaucoma?

A

yes, but may not be possible.

Life-ling Tx with drugs better.

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17
Q

What is the overall strategies for treatment of Open-Angle Glaucoma? (3)

A

Initial: Prostatglaning analog (PA)

Then: Good response to PA, but need more; + Beta-blocker -or- CA-inhibitor, -or- Alpha-2-Agonist.

if poor response to PA, sub in a different class of drug

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18
Q

Combining drops from different classes can cause a __________ reduction in the intraocular pressure than monotherapy

A

greater reduction

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19
Q

List the drugs used to treat open angle glaucoma that increase outflow of aqueous humor. (3)

A

Prostaglandin analogs: Latanoprost (Xalatan), topical PGF2-alpha prodrug.

Alpha-Agonist (Alpha-2 is preferred)

Cholinergic Agonist (aka miotics) [less commonly used today]

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20
Q

List the drugs used to treat open angle glaucoma that reduce production of aqueous humor. (2)

A

Beta-Atagonists. Beta-2 is best

Carbonic Anhydrase inhbitors (Dorzolamide) [2nd/3rd line Tx]

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21
Q

What is the MOA of Ophthalmic Beta-blockers (Timolol)?

A

Decrease Aq. Humor secretion from the ciliary epithelium.

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22
Q

What is the MOA of Ophthalmic Prostaglandins (Latanoprost)?

A

Increase Aq. humor outflow

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23
Q

What is the MOA of Ophthalmic Cholinomimetics (Pilocarpines)?

A
  • Increase ciliary muscle contraction
  • opening of trabecular meshwork
  • increase outflow
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24
Q

What is the MOA of Ophthalmic Alpha-Agonist (non-selective: Epi, dipivefrin)?

A

increase outflow; probably via the Uveoscleral veins.

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25
What is the MOA of Ophthalmic Alpha-2-Selective drugs (Apraclonidine, brimonidine)?
decrease Aq. humor secretion
26
What is the MOA of Ophthalmic Diuretics (Acetazolamide, dorzolamide)?
Decrease secretion due to lack of Bi-carb.
27
Which Ophthalmic drugs can be given either orally or topically?
Diuretics
28
Which Ophthalmic drugs can be given either Topically as drops or as a gel (gel = plastic film; slow release insert)
Ophthalmic Cholinomimetics (Pilocarpines)?
29
Which Ophthalmic drugs are generally administered as topical drops?
All of them!
30
Which Ophthalmic drug results in the following?: decrease production of aq. humor?
Beta-blockers!
31
Which Ophthalmic drug results in the following? - contract circular fibers (constricts pupil) - relax lens for near vision. - improve drainage.
Muscarinic Agonist
32
Which Ophthalmic drug results in the following? - Dilate pupils. - Occlude canal of Schlemm. - Raise IOP.
Muscarinic Antagonist
33
Parasympathetic (CN3) ~ ? Miosis or Mydriasis?
Miosis
34
Sympathetic (superior cervical ganglion) ~ ? Miosis or Mydriasis?
Mydriasis
35
“acute congestive” or “narrow angle” glaucoma is aka ?
Closed Angle Glaucoma
36
Which type of Glaucoma involves mechanical blockage of the trabecular meshwork by the peripheral iris?
Closed Angle Glaucoma. Blockage occurs intermittently and results in extreme fluctuations in IOP that may need to be treated as an emergency to avoid visual loss.
37
Overall, how do you Tx, Closed Angle Glaucoma?
Use drugs that decrease IOP, but also have RAPID onset time, to decrease the rapidly increasing IOP until you can get surgery done.
38
What drugs are usefull in the Tx of Closed Angle Glaucoma?
- Pilocarpine - Acetazolamide - Mannitol or glycerol
39
in the Tx of Closed Angle Glaucoma, Pilocarpine is also administered with what other drugs for a synergistic IOP lowering effect?
apraclonidine and timolol
40
What class of drugs, applied locally for ophthalmological purposes or given parenterally prior to anesthesia, can precipitate an attack of closed angle glaucoma.
Muscarinic receptor antagonists
41
What are the most common pathogens that cause Bacterial Conjuctivitis in adults?
Most common adult pathogens are S. aureus, S. pneumoniae,
42
What drugs are common and effective Tx bacterial conjuctivitis?
erythromycin (Ilotycin® ointment) or polymixin-trimethoprim (Polytrim® drops).
43
Red eye with discharge; minimal loss of vision and pain is indicative of what?
Bacterial Conjuctivitis
44
What eye injury/disease often follows injury or abrasion, or commonly is contact lens wear associated; pain, white spot on cornea, with decrease in vision.
Bacterial Keratitis
45
How do you Tx Bacterial Keratitis?
For mild case, use board spectrum topical drops ABX to prevent superinfection. For severe case: - FQ for pseudomonas, - Vanco for MRSA. - Ciprofloxacin
46
What eye disease/injury is the most common cause of ulceration in developed countries. Acute onset with variable symptoms of pain, visual blurring, and watery discharg
HSV keratitis
47
In HSV keratitis, what medications is the best to Tx?
Anti-virals. Oral (acyclovir) and topical (trifluridine-Viroptic®) agents are equally effective and oral agents are easier to use
48
What drugs class should you avoid in the Tx of HSV keratitis?
Topical steroids
49
What common eye injury/disease is self-limiting with NO specific treatment?
Viral Conjuctivitis
50
How to Tx Viral Conjuctivitis?
Sx relief with OTC anti-histamines or decongestants drops. use Lubricant ointments (Lacrilube, Refresh PM)
51
Timolol is what class of drug?
Beta-blocker
52
Latanoprost is what class of drug?
Prostaglandins
53
Dipivefrin is what class of drug?
Alpha-agonist Epi is too
54
Pilocarpine is what class of drug?
Cholinomimetics ([M] agonist)
55
Apracolnidine is what class of drug?
Alpha-2-Selective agonist
56
Brimonidine is what class of drug?
Alpha-2-Selective agonist
57
What is the MOA of Amantadine in the Tx of Parkinson's Diz?
``` Weak NMDA receptor Antagonist. & increases Dopamine Secretion. & decreases dopamine reuptake ```
58
Amantatine is traditionally used to Tx what?
Influenza
59
What class of drug is Benzotropine and what diz does it Tx?
Antimuscarinics --> Tx Parkinsons by decrease tremor and rigidity
60
In the Direct pathway of the basal ganglia, D1 receptor activation by DA ____1____ the release of GABA to the Thalamus and leads to _____2_____ and the promotion of movement.
1. decrease release of GABA | 2. dis-inhibition
61
What drug can you use to modestly Tx ALS?
Riluzole
62
Name 5 drugs used to Tx Parkinsons?
BALSA! ``` Bromocriptine Amanatadine Levodopa and Carbidopa Selegiline Anti-[M] ```
63
What drug combo decreases DA breakdown in Pt with Parkinsons?
Selegiline (MAO-inhibitor) + COMT inhibitor (e.g. entacapone or tolcapone) leads to decreased dopamine breakdown. Entacapone is a peripheral COMT inhibitor while tolcapone is a central COMT inhibitor.
64
What are the drugs used to Tx Open Angle Glaucoma? (5)
Beta-blockers (timolol) Alpha-adrenergic agonists (brimonidine) Carbonic anhydrase inhibitors (acetazolamide) Muscarinic agonists (pilocarpine, carbachol) Prostaglandin analogues (latanoprost)
65
What is the MOA of Riluzole?
Blocks glutamatergic Neurotransmission by inhibiting Glutamate release and inactivating voltage-gated NA channels.
66
What is the MOA of Bromocriptine?
Dopamine receptor agonist. used to Tx Parkinsons

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