3.10 Flashcards

1
Q

Tremendous variability of the skin as much as a _____ ____ patient permeability difference at a given skin site

A

ten-fold inter(patient)

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2
Q

Features of the skin can vary in different regions of the body especially the ___ can significantly vary from one site to another

A

SC (Stratum Corneum)

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3
Q

The viable epidermis contains many drug-metabolizing _____

A

Enzymes such as CYP and esterases

cutaneous first pass effect much less than hepatic

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4
Q

Example of Cutaneous first pass effect include

A

Nitroglycerin (up to 15-20% can be metabolized in skin)

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5
Q

Example of Cutaneous first pass effect include ____ which undergoes hydrolysis (esterase) to its active metabolite.

A

Tazarotene (prodrug for psoriasis)

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6
Q

Drug binding can occur where drug can bind to components of the stratum corneum such as the …

A

proteins and lipids

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7
Q

Drug binding (combine with slow drug passage) can have important implications:

A
  1. delay onset of drug action

2. create drug reservoir ( hold onto medication and can prolong drug effects)

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8
Q

SC in premature babies is not fully developed and SC in aged can _____ and become less hydrated

A

thickens

effects not easily predictable and complicated by changes in dermal microcirculation

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9
Q

The water uptake in the SC can take up to ____% of water (still dead cells)

A

75

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10
Q

Both the cells and the _____ spaces can take up water leads to swelling and softening of the SC.

A

interlamellar

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11
Q

_____ of the skin can enhance drug permeation through the skin because of its effect on SC.

A

Hydration

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12
Q

____ of the skin can be an important consideration in topical drug therapy, as it can increase drug permeation at the site.

A

Occlusion

blocks transepidermal water loss (TWL), leading to skin hydration at the site of occlusion

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13
Q

____ and ____ drugs are more lipophilic

A

Nonpolar and nonionized

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14
Q

Properties of the final ______ can have considerable effects on drug permeation: Ability to release the drug and occlude the skin

A

dosage form

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15
Q

_____ increases hydration and penetration.

A

Occlusion

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16
Q

_______ are semisolid preparations intended for external application to skin or mucous membranes and classified according to their interaction with water.

A

Ointment

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17
Q

Four classifications of ointment bases are …

A
1. Hydrocarbon/
Oleaginous Base (least) 
2. Absorption base
3. Emulsion Base -w/o and o/w 
4. Water-soluble Base (most)
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18
Q

____ ointment base are insoluble in water they are anhydrous, and incompatible with water.

A

Hydrocarbon (Oleaginous)

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19
Q

White petrolatum USP…

A

a highly refined mixture of saturated hydrocarbons (decolorized, e.g. Vaseline)

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20
Q

White Ointment USP…

A

White petrolatum+ white wax (beeswax)

Less greasy

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21
Q

Most occlusive topical agent because application to the skin, a hydrocarbon base will…

A

form an adherent, continuous, greasy, water-repellant film

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22
Q

Emollient…

A

an agent that softens the skin or soothes irritation in the skin or mucous membrane

23
Q

Hydrocarbon base has good occlusiveness, have an emollient effect and enhances…

A

drug permeation because it blocks water-loss, thereby hydrating the SC

24
Q

Hydrocarbon base have prolonged contact with the skin because it …

A

increases drug residence time at the skin, which can enhance drug delivery

25
Q

Absorption ointment base, they are oleaginous, anhydrous, have an ability to absorb water because they contain _____, and can absorb alcohol.

A

lipophilic surfactants

form W/O emulsion

26
Q

______ purified, fat-like substance from the wool of sheep. Insoluble in water, but will take up twice its weight without separation.

A

Lanolin (anhydrous)

-has surface active long chain acids and alcohols

27
Q

Hydrophilic petrolatum..

A

white petrolatum

+ white wax+ stearyl alcohol + cholesterol

28
Q

Aquaphor,..

A

petrolatum, mineral oil, mineral wax, + woolwax alcohol

29
Q

Water content of anhydrous absorption base …

A

decreased oiliness and continuity, as water content increases

(more water=less occlusive)

30
Q

Absorption base have good emollient, permeation enhancing but have less…

A

occlusion, less blockage of water loss

31
Q

W/O emulsion bases can absorb less water than anhydrous absorption bases…

A

because they already contain some water

32
Q

Eucerin is…

A

Aquaphor with water and preservatives

33
Q

Cold cream is…

A

cetyl esters wax, white wax, mineral oil, sodium borate + water

34
Q

W/O emulsion bases with oil as continuous phase they are still occlusive, but less so than ________

A

anhydrous absorption bases or hydrocarbon bases

35
Q

W/O emulsion bases have moderately good emollient and protective properties …

A

less ability to block water loss, because of a lower hydrocarbon fraction

36
Q

_______ are more pleasant than anhydrous absorption bases.

A

W/O emulsion bases (not as greasy)

37
Q

O/W emulsion bases, they are water-washable ointment bases that have come to be called ______-

A

cream

38
Q

O/W emulsion bases are water-washable because…

A

water is the continuous phase

39
Q

Upon application, external phase evaporates and the application shrinks to a thin film, which is transparent, thus the term ______

A

vanishing cream

40
Q

Concentration without crystallizing out gives a (high or low) concentration gradient, and high concentration is good for drug delivery.

A

high

41
Q

O/W creams is not continuous and not ______, will be less occlusive and won’t block water-loss = less permeation

A

oleaginous

42
Q

Since O/W creams are less occlusive they are less ___, but it can be enhanced by moisturizers.

A

emollient

43
Q

O/W creams are less adherent than oily ointments and can be…

A

wash off more easily

44
Q

_______ base are least used, usually PEGs of different MW blended to achieve an ointment-like consistency.

A

Water-soluble ointment

45
Q

Water-soluble ointment bases are non-occlusive and have little to no emollient properties. They are water-washable and greaseless and can be …

A

irritating

e.g. mupirocin

46
Q

___ are ointments that contain a high amount of fine powder (usually 20-50%) and base is usually petrolatum.

A

Pastes

e.g. sunscreens, diaper rash protectants
ZInc oxide, starch, aluminum oxide, bentonite

47
Q

Pastes form a ____ film ointment base and powder matrix,

A

thick

48
Q

The presence of high powder component in pastes changes the ointment base in …

A
  1. less greasy (powder absorb some base)
  2. less occlusive (oily film is disrupted by powder)
  3. absorptive
  4. more protective
  5. can be more stiff, hard to apply (e.g. irritated or hairy areas)
49
Q

____ are fluid emulsions or suspensions for external application. The continuous phase is aqueous.

A

lotions

50
Q

_____ is an O/W emulsion described as a lipid-free lotion. It is useful as a general purpose lotion vehicle.

A

Cetaphil Lotion (Galderma)

51
Q

Lotion, upon application the continuous phase evaporates, leaving a thin uniform film of powder or liquid, The formed film is ____

A

non-continuous, non-occlusive

52
Q

Lotion: Evaporation cools and soothes the skin and can be …

A

valuable for acutely inflamed areas

53
Q

Lotion fluidity allows fast application to broad and difficult areas such as …

A

Hirsute areas and intertriginous areas (where skin touches skin= e.g. armpit)

54
Q

Lotions face all of the problems of oral suspensions and emulsions including physical, chemical, and microbiological instability bc lotions are …

A

aqueous and hetergeneous