Ophthalmic Lecture Flashcards

1
Q

What is a topical dosage form?

A

Instilled onto the external surface of the eye

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is a intraocular dosage form?

A

Administer by injection inside the eye

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is periocular dosage form?

A

Adjacent to the eye

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is intraocularly implanted mean?

A

Implanted as a ophthalmic device

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are drugs that are used in the eye?

A
Anti-glaucoma drugs
Mydriatics & Cycloplegics 
Anti-inflammatory
Anti-infectives
Surgical adjuncts
Diagnostic drugs
Topical anesthetics
Protectants & artificial tears
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is an example of anti-glaucoma drugs?

A

Pilocarpine HCl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is an example of mydriatics & cycloplegics?

A

atropine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is an example of anti-inflammatories?

A

Corticosteroids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the three types of anti-infectives and an example?

A

Antibiotics and antimicrobial agents (tobramycin)
Anti-fungal agents (amphotericin B)
Antiviral agents (ganciclovir)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is an example of surgical adjuncts?

A

Irrigating solutions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is an example of diagnostic drugs?

A

Sodium fluorescein

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is an example of topical anesthetics?

A

Tetracaine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is an example of protectants & artificial tears?

A

Methylcellulose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are three common opthalmic dosage forms?

A

Solutions (eyedrops)
Suspensions
Ointments

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What are four new ophthalmic dosage forms?

A

Controlled Release devices
Ocular inserts
Gels, gel-forming solutions
Intravitreal injections and implants

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is the cornea?

A

Front clear, transparent tissue and is supplied with oxygen and other nutrients by lacrimal fluid
-Powerful refracting surface, allows light to enter the eye and provides much of the focusing power

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is the iris?

A

Part of the eye that gives it color
- Consists of muscular tissue that responds to surrounding light, making the pupil, or curricular opening in the center of the iris larger or smaller depending on brightness

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is the lens?

A

Transparent, biconvex structure, encased in a thin transparent covering
- Functions to refract and focus incoming light onto the retina

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is the retina?

A

Innermost layer in the eye
Coverts images into electrical impulses that are sent along the optic nerve to the brain where the images are interpreted

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What effects drug availability?

A

Rapid solution drainage by gravity, induced lacrimation, blinking reflex and normal tear turnover
Low corneal permeability (acts as a lipid barrier

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is a typical drop volume, precorneal space of a healthy person and optimal volume administered? (in microliters)

A

20-50
7
5-10

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

How much applied drug is typically absorbed?

A

1-5%

Usually less than 3%

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is the retention time of ophthalmic solution on the eye surface?

A

Very short, 1-2 minutes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Fluids are rapidly removed from the eye by what?

A

Lacrimal drainage

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Poor bioavailability leads to what/
Protective mechanisms (blinking, reflex lacrimation, nasolacrimal drainage) or anatomy of the eye (barrier properties of the cornea)
26
What is common to all ophthalmic dosages forms?
- Requires sterility of the finished product - Appreciation for the sensitivity of ocular tissue to irritation and toxicity - Inherent limitations in topical ocular absorption of most drugs
27
Define ophthalmic solutions
Sterile solutions, essentially free from foreign particles, suitably compounded and packaged for instillation into the eye - Sterile - Buffered - Isotonic - Non-irritating - Non-greasy - Efficacious
28
What are the most common means of administering a drug to the eye?
Solution
29
Xalatan Opthalmic solution (lantanoprost) is used for?
treatment of glaucoma
30
What are advantages of ophthalmic solutions?
Dosage uniformity | Little physical interference with vision
31
What are disadvantages of opthalmic solutions?
Relatively brief contact time | Contact time may be increase to some extent by inclusions of a viscosity-increasing agent (methylcellulose)
32
Define Ophthalmic suspensions
Drug is dispersed in the solvent and exist in fine particulate form Drug is finely divided in an aqueous vehicle containing suitable suspending and dispersing agent If the drug is not sufficiently soluble Requires vigorous shaking
33
How much of the particles should have a size less than 10 micrometers or less?
95%
34
Define ophthalmic ointment
A drug intended for ocular use is formulated in ointment base
35
Characteristics of ophthalmic ointment?
Semi-solid dosage form Contain a white petrolatum-mineral oil base Anhydrous lanolin PEG-gelled mineral oil base
36
What are advantages of ophthalmic ointment?
Longer contact time and greater total drug bioavailability
37
What are disadvantages of ophthalmic ointment?
Slower onset and time to peak absorption Dosage variability is greater than with solutions Interfere with vision unless use is limited to bedtime instillation Must be sterile and free from particulate matter
38
Define ocular inserts
Sterile solid or semisolid preparation s, with a thing, flexible and multilayered structure, for insertion beneath the eyelid and release drug at constant rate
39
Disadvantages of ocular inserts?
Non-contact lens wearers find them difficult to administer Non-biodegradable inserts must be removed from the eye when drug is gone Inner eyelid discomfort
40
Ocusert Pilo-20 and Pilo-40 Ocular system
Designed to be placed in the inferior cul-de-sac between the sclera and the eyelid and to release pilocarpine continuously at a steady rate for 7 days for treatment of glaucoma
41
Define erodible ocular insert
Soluble inserts consists of water-soluble polymer or collagen that at the end of their release, the device dissolves or erodes
42
Define Lacrisert
Sterile ophthalmic insert use in the treatment of dry eye syndrome - 5 mg of hydroxypropylcellulose in a rode-shaped form - Insert is placed in the eye 1-2 times a day where it softens and slowly dissolved
43
What is an ocular pack?
A cotton pledget saturated with an ophthalmic solution The pledget is inserted into the superior or inferior fornix Give prolonged contact of the solution with the eye
44
What is an example of ocular packs?
Used to produce maximal mydriasis such as cotton pledgets saturated with phenylephrine solution
45
Define intraocular dosage forms
ophthalmic products that introduced into the interior structure of the eye primarily during ocular surgery
46
What are characteristics of intraocular dosage forms?
Sterile and pyrogen-free Strict control of particulate matter Compatible with sensitive internal tissues Packaged as preservative-free single dosage Provides sustained or controlled releases
47
What are intraocular solutions and uses?
Used in surgical procedures such as cataract removal - Irrigating solution: helps to maintain ocular structure and tissue hydration during surgery - Dispersive: maintain and preserve space as well as displace and stabilize tissues
48
What are intraocular injections?
Allows direct application of drugs to the affected area of the eye with minimal systemic side effects
49
How are intraocular injections performed?
Topical anesthetic is applied directly to the eye Eye is rinsed with an iodine solution to reduce the risk of infections Allow 5 minutes for the anesthetic and iodine solution to take full effects Injection is given using a very fine needle just outside the pupil
50
What are the intravitreal injections?
Injections into the vitreous chamber (amphotericin B, gentamicin sulfate, certain steroids) Important for patients with retinal vascular diseases (Avastin, Lucentis, Kenalog)
51
What are intracameral injections?
Injections into the anterior chamber (acetylcholine chloride, alpha-chymotrypsin, carbamylcholine chloride, antibiotics and steriods)
52
What are ophthalmic preparation characteristics?
``` Sterile and free from particulate materials Must have phsiological pH Isotonic Stable Free from toxicity ```
53
Define sterility
``` The absence of living microorganisms and undersirable particulate material Absolute term (either is or not) ```
54
How can sterility be achieved?
Filtering the final solution using a membrane filter Packaged in a clean, particle-free, sterile container Longer than 24 hours or multi-dose, a preservative must be added Use aseptic techniques in clean and aseptic area Use of a laminar-flow hoods, and proper garments
55
What are some sterilization mechanisms?
``` Dry heat FIltration Gas sterilization Ionizing radiation Moist heat under pressure ```
56
What excipients may an ophthalmic solution may contain?
``` Vehicles Buffers Tonicity adjustors Preservatives Antioxidants Viscosity inducing agents ```
57
What is a vehicle?
USP WFI (water for injection) for intraocular production EX for solutions: sterile water or saline soltuion EX for ointments: mineral oil or petrolatum EX for moisture-sensitive and non-water soluble drugs: mineral oil and vegetable oil
58
pH of buffers?
Ideal ophthalmic preparations pH: equivalent to the tear fluid value of 7.4 Outer surfaces of the eye tolerate pH: 3.5-8.5 Normal useful pH range: 6.5-8.5
59
What is boric acid?
Vehicle 1.9% solution of boric acid in purified water It is isotonic with tears (pH ~5)
60
What is Sorensen's modified phosphate buffer?
Containing NaH2PO4 and Na2HPO4 | Not isotonic, pH range: 6.5-8.0
61
What is a tonicity modifier?
Solution that are isotonic with tears are preferred The eye can tolerate within the equivalent range of 0.6-2% NaCl without discomfort 0.9% NaCl is ideal
62
What are examples of tonicity adjustors?
Sodium chloride Sodium nitrate Sodium sulfate Dextrose
63
What is a preservative?
Added to maintain sterility of an ophthalmic preparation during use
64
What can't a preservative be used for?
Preparation used during eye surgery | Preparations used for traumatized eyes (some irritate eyes, preservative free: single use containers)
65
Before adding a preservative what should be checked?
Patient sensitivity, compatibility of the preservative with all other ingredients in the formulation
66
What are four examples of antioxidants?
Sodium bisulfite Sodium metabisfulfite Thiourea Ethylendediaminetetraacetic acid
67
What are two examples of wetting agents?
Polysorbate 80 | Polysorbate 20
68
What are viscosity enhancers?
Use to thickne the tear and prolong corneal contact time and thus enhance drug absorption and activity Viscosit increased up to the 15-50 cps range significantly improves contact time in the eye
69
What are some examples of viscosity enhancers?
``` Polyvinyl alcohol 1.4% Polyvinylpyrrolidone 1.7% Methylcellulose 2.0% Hydroxypropyl methylcellulose 1.0% Hydroxyethylcellulose 0.8% ```
70
What are advantages of packaging in plastic dropper bottles?
Flexibility and inertness: low-density polyethylene resin dropper Compatible/low contamination potential/low cost
71
What are disadvantages of packaging in plastic dropper bottles?
Permeable to a variety of substances | Label glues, inks, dyes, that may penetrate polyethylene, leach out of the plastic into the contained solution
72
What are advantages of packaging in a glass dropper bottle?
Used for products that are extremely sensitive to oxygen or contains permeable components that are not stable in plastic Type 1 glass should be used Amber glass for light resistance
73
What are packaged in metal tubes?
Ophthalmic ointments with ophthalmic tip Sterilized conveniently by autoclaving or ethylene oxide Tubes can be lined with epoxy or vinyl plastic if metal reactive