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NS_BTRAN > Unit3_Pharma > Flashcards

Unit3_Pharma Flashcards

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
Q

What is the MOA of Ophthalmic Alpha-2-Selective drugs (Apraclonidine, brimonidine)?

A

decrease Aq. humor secretion

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26
Q

What is the MOA of Ophthalmic Diuretics (Acetazolamide, dorzolamide)?

A

Decrease secretion due to lack of Bi-carb.

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27
Q

Which Ophthalmic drugs can be given either orally or topically?

28
Q

Which Ophthalmic drugs can be given either Topically as drops or as a gel (gel = plastic film; slow release insert)

A

Ophthalmic Cholinomimetics (Pilocarpines)?

29
Q

Which Ophthalmic drugs are generally administered as topical drops?

A

All of them!

30
Q

Which Ophthalmic drug results in the following?:

decrease production of aq. humor?

A

Beta-blockers!

31
Q

Which Ophthalmic drug results in the following?

  • contract circular fibers (constricts pupil)
  • relax lens for near vision.
  • improve drainage.
A

Muscarinic Agonist

32
Q

Which Ophthalmic drug results in the following?

  • Dilate pupils.
  • Occlude canal of Schlemm.
  • Raise IOP.
A

Muscarinic Antagonist

33
Q

Parasympathetic (CN3) ~ ?

Miosis or Mydriasis?

34
Q

Sympathetic (superior cervical ganglion) ~ ?

Miosis or Mydriasis?

35
Q

“acute congestive” or “narrow angle” glaucoma is aka ?

A

Closed Angle Glaucoma

36
Q

Which type of Glaucoma involves mechanical blockage of the trabecular meshwork by the peripheral iris?

A

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
Q

Overall, how do you Tx, Closed Angle Glaucoma?

A

Use drugs that decrease IOP, but also have RAPID onset time, to decrease the rapidly increasing IOP until you can get surgery done.

38
Q

What drugs are usefull in the Tx of Closed Angle Glaucoma?

A
  • Pilocarpine
  • Acetazolamide
  • Mannitol or glycerol
39
Q

in the Tx of Closed Angle Glaucoma, Pilocarpine is also administered with what other drugs for a synergistic IOP lowering effect?

A

apraclonidine and timolol

40
Q

What class of drugs, applied locally for ophthalmological purposes or given parenterally prior to anesthesia, can precipitate an attack of closed angle glaucoma.

A

Muscarinic receptor antagonists

41
Q

What are the most common pathogens that cause Bacterial Conjuctivitis in adults?

A

Most common adult pathogens are S. aureus, S. pneumoniae,

42
Q

What drugs are common and effective Tx bacterial conjuctivitis?

A

erythromycin (Ilotycin® ointment) or polymixin-trimethoprim (Polytrim® drops).

43
Q

Red eye with discharge; minimal loss of vision and pain is indicative of what?

A

Bacterial Conjuctivitis

44
Q

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.

A

Bacterial Keratitis

45
Q

How do you Tx Bacterial Keratitis?

A

For mild case, use board spectrum topical drops ABX to prevent superinfection.

For severe case:

  • FQ for pseudomonas,
  • Vanco for MRSA.
  • Ciprofloxacin
46
Q

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

A

HSV keratitis

47
Q

In HSV keratitis, what medications is the best to Tx?

A

Anti-virals.

Oral (acyclovir) and topical (trifluridine-Viroptic®) agents are equally effective and oral agents are easier to use

48
Q

What drugs class should you avoid in the Tx of HSV keratitis?

A

Topical steroids

49
Q

What common eye injury/disease is self-limiting with NO specific treatment?

A

Viral Conjuctivitis

50
Q

How to Tx Viral Conjuctivitis?

A

Sx relief with OTC anti-histamines or decongestants drops.

use Lubricant ointments (Lacrilube, Refresh PM)

51
Q

Timolol is what class of drug?

A

Beta-blocker

52
Q

Latanoprost is what class of drug?

A

Prostaglandins

53
Q

Dipivefrin is what class of drug?

A

Alpha-agonist

Epi is too

54
Q

Pilocarpine is what class of drug?

A

Cholinomimetics ([M] agonist)

55
Q

Apracolnidine is what class of drug?

A

Alpha-2-Selective agonist

56
Q

Brimonidine is what class of drug?

A

Alpha-2-Selective agonist

57
Q

What is the MOA of Amantadine in the Tx of Parkinson’s Diz?

A 
Weak NMDA receptor Antagonist. 
& 
increases Dopamine Secretion.
&
decreases dopamine reuptake
58
Q

Amantatine is traditionally used to Tx what?

59
Q

What class of drug is Benzotropine and what diz does it Tx?

A

Antimuscarinics –> Tx Parkinsons by decrease tremor and rigidity

60
Q

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.

A
  1. decrease release of GABA

2. dis-inhibition

61
Q

What drug can you use to modestly Tx ALS?

62
Q

Name 5 drugs used to Tx Parkinsons?

A

BALSA!

Bromocriptine
Amanatadine
Levodopa and Carbidopa
Selegiline
Anti-[M]
63
Q

What drug combo decreases DA breakdown in Pt with Parkinsons?

A

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
Q

What are the drugs used to Tx Open Angle Glaucoma? (5)

A

Beta-blockers (timolol)

Alpha-adrenergic agonists (brimonidine)

Carbonic anhydrase inhibitors (acetazolamide)

Muscarinic agonists (pilocarpine, carbachol)

Prostaglandin analogues (latanoprost)

65
Q

What is the MOA of Riluzole?

A

Blocks glutamatergic Neurotransmission by inhibiting Glutamate release and inactivating voltage-gated NA channels.

66
Q

What is the MOA of Bromocriptine?

A

Dopamine receptor agonist.

used to Tx Parkinsons

NS_BTRAN (21 decks)

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