Chapter 183- Principles of Topical Therapy Flashcards

1
Q

Efficacy of topically applied drug depends on 3 things:

A
  1. Whether drug was applied
  2. Delivery of active molecule by its vehicle
  3. Inherent potency of active molecule
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2
Q

Factors that affect penetration of drug: (4)

A
  1. Soluble drug concentration
  2. Regional variations in skin barrier properties
  3. Frequency of application
  4. Effects of vehicle on barrier function
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3
Q

Primary barrier that limits percutaneous absorption of compounds is

A

Stratum corneum

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4
Q

Topical therapy involves 3 key steps:

A
  1. Topical application
  2. Percutaneous absorption
  3. Binding of active molecule to target site
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5
Q

Nonadherence to prescribed medicines in chronic conditions is between ___%

A

30 to 50%

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6
Q

Low absorption does not necessarily translate into low efficacy.
True or False

A

True

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7
Q

3 compartment model of skin

A
  1. Skin surface
  2. Stratum corneum
  3. Viable tissue
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8
Q

Most significant role in determining diffusion of compunds into body

A

Stratum corneum

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9
Q

When a patient applies a dermatologic preparation, the layer of formulation is ___ .

A

0.5 to 2 mg/cm2

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10
Q

Matching type

  1. Diffusion
  2. Reservoir
  3. Thermodynamic activity
  4. Binding
  5. Resorption
  6. Evaporation

A. Vehicle
B. Stratum corneum
C. Epidermis
D. Dermis

A
  1. B>A
  2. B
  3. A
  4. C> B
  5. C
  6. A
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11
Q

Amount of active ingredient that is still in contact with nonvolatile constituents of formulation after latter has been massaged into skin surface

A

Reservoir

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12
Q

Optimum size of particles for penetration into hair follicles is between ___ nm to a depth of 100 to 500 um

A

300-600 nm

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13
Q

Several paramaters to consider when selecting a formulation (5)

A
  1. Thermodynamic activity of the active ingredient
  2. Amount of compund that can be incorporated into the formulation
  3. Stability of formulation
  4. Partition coefficient of active ingredient between the vehicle and the stratum corneum
  5. Enhancer activity
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14
Q

Percutaneous absorption is proportional to ___

A

Thermodynamic activity of the compound

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15
Q

Stratum corneum measures __um

A

10 - 20 um

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16
Q

Arrange the ff reservoir from highest to lowest
Scalp
Forehead
Calf

A

Scalp» forehead&raquo_space; calf

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17
Q

Three pentration oathways

A

Intracellular
Intercellular
Follicular

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18
Q

Nanoparticles are stored ___ times longer in hair follicles than in the stratum corneum

A

10

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19
Q

Accurate and reproducible measurement of skin barrier activity is

A

Transepidermal water loss

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20
Q

Transepidermal water loss varies __% by site; __% by day of measurement; and __% amongst individuals

A

8%
21%
35 to 48%

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21
Q
Barrier function ranked from highest to lowest
Forehead 
Postauricular
Arm
Abdomen
A

Arm= abdomen&raquo_space; postauricular&raquo_space; forehead

22
Q

Metabolic processing of ___ is involved in the presentation of allergens to the immune system

A

Langerhans cells

23
Q

Metabolic activity is found in (5)

A
Skin surface microorganisms
Appendages
Stratum corneum
Viable epidermis
Dermis
24
Q

Extent of metabolism in the skin is normally modest only __%

25
Uptake of compounds by cutaneous microvasculature, directly related to surface area of exchanging calillaries as well as their blood flow
Resorption
26
Under resting conditions, only __% of blood flow passes via exchanging capillaries capable of acting as a sink for absorbed compounds
40%
27
Resorption does not change the rate of diffusion to central compartment after topical application. True or False
True
28
For compunds with rapid diffusion across the stratum corneum, resorption limits maximum rate of absorption. True or False
True
29
Stratum corneum is composed of __ in a 1:1:1 ratio
Ceramides Free fatty acids Cholesterol
30
By weight, stratum corneum consists of __% ceramides, __% fatty acids, and __% cholesterol
50% 15% 35%
31
2 main routes for permeation through stratum corneum
Transepidermal | Transappendageal
32
Most important route for cutaneous drug delivery
Intercellular pathway
33
Simple hydration of the stratum corneum enhances the absorption of topically applied steroids by ___x
4 to 5
34
Occlusion increases drug delivery by ___ times the amount of drug delivery when not occluded
10
35
Occlusion may promote the ff side effects (3)
Infection Folliculitis Miliaria
36
In rare cases, lidocaine toxicity can result to __; prilocaine toxicity can result to ___
Cardiac complications | Methemoglobinemia
37
Measurement that allows healthcare providers and patients to easily communicate about treatment application
Fingertip unit
38
1 FTU = ___ of topical agent = ___ BSA
500mg; 2%
39
Inactive part of a topical preparation that brings a drug into contact with the skin
Vehicle
40
Examples of emulsfying agents (4)
Cholesterol Emulsifying wax Sodium laureth sulfate Polysorbates
41
Auxiliary emulsifying agents or emulsion stabilizers: (3)
Cetearyl alcohol Glycerin monostearate Polyethylene glycol
42
Examples of stabilizers/preservatives (5)
``` Benzyl alcohol Citric acid EDTA Parabens Sorbic acid ```
43
Examples of solvents
Alcohol | Water
44
Examples of thickening agents
Beeswax Xanthan gum Petrolatum
45
Examples of auxiliary agents and emollients
Cetyl alcohol Stearyl alcohol Lanolin
46
Examples of Humectants
Glycerin Propylene glycol Sorbitol solution
47
``` Glycerin and propylene glycol have the same functions except A. Stabilizer B. Humectant C. Solvent D. Emollients ```
D. Emollients, only glycerin
48
Most powders contain __ for antiseptic and covering properties, ___ for lubricating and drying, and __ for improved adherence to skin
Zinc oxide Talc / magnesium silicate Stearate
49
Calamine consists of
98% zinc oxide | 1% ferric oxide
50
Wet solid mass of particles, sometimes heated, that is applied to diseased skin
Poultice or cataplasm
51
Used as wound cleansers and absorptive agents in exudative lesions such as decubiti and leg ulcers
Poultices