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Derm Pharm 2020 > 1 - TOPICAL RETINOIDS > Flashcards

1 - TOPICAL RETINOIDS Flashcards

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Dermatology Board Prep flashcards
1
Q

Tretinoin (all-trans retinoic acid) is an oxidised form of all-trans retinol and is synthesised endogenously from all-trans retinol after delivery of the compound to basal keratinocytes from the bloodstream

A

True

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2
Q

Alitretinoin (9-cis retinoic acid) is a naturally occurring endogenous retinoid

A

True (same as tretinoin and all-trans retinol)

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3
Q

All topical retinoids should be avoided during pregnancy due to risk of teratogenecity

A

True (although topical absorption of retinoids is generally slight, there is concern when large surface areas are treated)

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4
Q

A pregnancy test is recommended before the use of Tazarotene and Bexarotene (third generation retinoids) in women of child bearing potential, and appropriate birth control measures in place for the duration of treatment

A

True

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5
Q

All-trans retinol and all-trans retinoic acid are naturally occurring retinoids

A

True

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6
Q

Cytosolic all-trans retinoic acid-binding protein (CRABP) is predominantly in human skin and may be the determining factor in the bioavailability of retinoids

A

True (all-trans retinoic acid binds to CRABP)

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7
Q

All-trans retinol is oxidised to all-trans retinoic acid when needed by the cell

A

True

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8
Q

All-trans retinol is the natural alcohol form of vitamin A that is transported in the blood stream from storage in the liver to the peripheral target tissues bound to the serum transport protein retinol-binding protein

A

True

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9
Q

All-trans retinol traverses the interstitial spaces in the papillary dermis and is taken up by basal keratinocytes

A

True

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10
Q

When all-trans retinol is topically applied to the skin, the drug is taken up by the keratinocytes in the outer epidermis and diffuses through the skin as a fat soluble drug

A

True

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11
Q

Within the keratinocytes, excess all-trans retinol is esterified to long chain fatty acids to form retinyl esters which form lipid droplets (similar to how vitamin A is stored in the liver)

A

True

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12
Q

Acyl CoA - retinol acyltransferase is an enzyme system that is involved in direct esterification and hydrolysis of retinyl esters important for topically applied all-trans retinol

A

True

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13
Q

Lecithin - retinol acyltransferase is an enzyme system that is involved in direct esterification and hydrolysis of retinyl esters important for endogenously supplied all-trans retinol

A

True

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14
Q

All-trans retinoic acid (first generation retinoid Tretinoin) induce genes which are involved in cell proliferation and anti-apoptosis, leading to inhibition of cell growth

A

True

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15
Q

All-trans retinol and all-trans retinoic acid causes epidermal hyperplasia in thin or atrophic photo damaged epidermis

A

True

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16
Q

All-trans retinol and all-trans retinoic acid causes normalisation of epidermal thickness in hypertrophic skin

A

True

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17
Q

Topical application of All-trans retinol and all-trans retinoic acid causes irritation, erythema and desquamation

A

True

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18
Q

All-trans retinol do not bind to any retinoid receptors

A

True

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19
Q

All-trans retinoic acid/Tretinoin (first generation retinoid) binds to RAR receptors

A

True

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20
Q

Alitretinoin (third generation retinoid) binds to all RAR and RXR retinoid receptors

A

True

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21
Q

Bexarotene (third generation retinoid) binds to RXR retinoid receptors

A

True

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22
Q

Both Adapalene and Tazarotene (third generation retinoid) bind to RAR retinoid receptors and not RXR retinoid receptors

A

True (in contrast to third generation Bexarotene which binds to RXR and not RAR retinoid receptors)

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23
Q

Tazarotene (third generation retinoid) is converted to its active metabolite tazarotenic acid

A

True (Tazarotene is a prodrug)

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24
Q

All-trans retinol, all trans-retinoic acid (both first generation retinoids), Adapalene and Tazarotene (both third generation retinoids) result in comedolysis in acne

A

True

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25
Q

Topical Adapalene and Tazarotene (both third generation retinoids) may result in irritation, erythema, desquamation, pruritus and burning

A

True

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26
Q

Adapalene (third generation retinoid) is similar to all-trans retinoic acid (first generation retinoid) in its effects on acne, though it is more stable chemically, less photolabile, more lipophilic which enables it to penetrate follicles quickly

A

True

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27
Q

Adapalene (third generation retinoid) is more chemically stable than all-trans retinoic acid (first generation retinoid)

A

True

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28
Q

Adapalene (third generation retinoid) is less photolabile than all-trans retinoic acid (first generation retinoid)

A

True (however it is still recommended that patients on Adapalene exercise caution with respect to UV exposure with photoprotection)

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29
Q

Adapalene (third generation retinoid) is more lipophilic than all-trans retinoic acid (first generation retinoid)

A

True (enable it to penetrate follicles more quickly in acne and contribute to Adapalene’s success in treating acne)

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30
Q

Adapalene (third generation retinoid) has selective affinity for RAR beta and gamma receptors

A

True

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31
Q

Adapalene (third generation retinoid) suppresses/inhibits polymorphonuclear (neutrophil) chemotaxis and release of oxygen free radicals from neutrophils

A

True (neutrophils commonly found in acne)

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32
Q

Adapalene is systemically absorbed

A

False (only trace amounts systemically absorbed and excreted through the hepatobiliary route, otherwise excreted via skin desquamation)

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33
Q

Systemically absorbed Adapalene (only trace amounts) are excreted through the hepatobiliary route

A

True

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34
Q

Adapalene is carcinogenic

A

False (only trace amounts absorbed systemically)

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35
Q

Adapalene is mutagenic

A

False (only trace amounts absorbed systemically)

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36
Q

Adapalene is teratogenic

A

False (only trace amounts absorbed systemically) - although still recommended that Adapalene be discontinued during pregnancy as there are no controlled studies in pregnant women

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37
Q

Adapalene is genotoxic

A

False (only trace amounts absorbed systemically)

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38
Q

It is still recommended that Adapalene be discontinued during pregnancy although no significant teratogenic effects of topical Adapalene have been observed

A

True (as there are no controlled studies in pregnant women)

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39
Q

There are no clinical studies that show that Adapalene is photosensitising

A

True (Adapalene more photostable than Tretinoin, however it is still recommended that patients on Adapalene exercise caution with respect to UV exposure with photoprotection)

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40
Q

Adapalene (third generation retinoid) is active without metabolic transformation

A

True

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41
Q

Adapalene (third generation retinoid) is mainly excreted through skin desquamation

A

True (only trace amounts systemically absorbed)

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42
Q

All-trans retinoic acid becomes the active metabolite of all-trans retinol

A

True

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43
Q

All-trans retinol and all-trans retinoic acid are excreted through the hepatobiliary route and skin desquamation

A

True (so does Adapalene)

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44
Q

There is increased systemic absorption of All trans-retinoic acid (first generation retinoid Tretinoin) in dermatitic skin

A

True (1-2% systemically absorbed in normal skin, and up to 31% absorbed in dermatitic skin)

45
Q

Both all-trans retinol and all-trans retinoic acid are absorbed by the keratinocytes with minimal dermal uptake

A

True

46
Q

Tazarotene (third generation retinoid) results in normalisation of differentiation and proliferation of the epidermal keratinocytes in psoriasis

A

True (also comedolysis in acne)

47
Q

Tazarotene (third generation retinoid) suppresses and downregulate the inflammatory markers in psoriasis

A

True

48
Q

Tazarotene (third generation retinoid) blocks induction of ornithine decarboxylase activity resulting in decreased cell proliferation and hyperplasia

A

True

49
Q

The systemic absorption of topical Tazarotene (third generation retinoid) is practically non-existent because of its rapid skin metabolism to tazarotenic acid

A

True (although up to 5% systemically absorbed when applied to normal skin, up to 15% systemically absorbed in psoriatic skin)

50
Q

Total systemic absorption of Tazarotene (third generation retinoid) is up to 5% in normal skin and 15% in psoriatic skin

A

True

51
Q

The small amounts systemically absorbed Tazarotene (third generation retinoid) which are not degraded, are excreted in both urine and faeces

A

True (in contrast to degradation of tazarotenic acid to inactive metabolites being excreted in urine)

52
Q

Tazarotene (third generation retinoid) is absorbed by keratinocytes with dermal penetration and uptake into the bloodstream

A

True

53
Q

Even though teratogenicity in topical Tazarotene (third generation retinoid) was not observed in animal models, the oral administration of Tazarotene resulted in teratogenicity

A

True (reason for topical Tazarotene to be absolutely contraindicated in pregnancy with pregnancy category X)

54
Q

Tazarotene (third generation retinoid) is also excreted via skin desquamation

A

True (also in urine and faeces)

55
Q

Bexarotene (third generation retinoid) is a synthetic retinoid which bind selectively to RXR retinoid receptors

A

True

56
Q

Adapalene (third generation retinoid) is a synthetic retinoid

A

True

57
Q

Tazarotene (third generation retinoid) is a synthetic retinoid

A

True

58
Q

Alitretinoin (third generation retinoid) is a natural retinoid

A

True (same as all-trans retinol and all-trans retinoic acid)

59
Q

There are 3 natural topical retinoids: all-trans retinol, all-trans retinoic acid and Alitretinoin

A

True

60
Q

There are 3 synthetic topical retinoids: Adapalene, Tazarotene and Bexarotene (all third generation retinoids)

A

True

61
Q

Tazarotene (third generation retinoid) may worsen psoriasis

A

True (although it is use in psoriasis)

62
Q

Bexarotene (third generation retinoid) inhibits the cell cycle leading to decreased proliferation and increased apoptosis

A

True (used in Mycosis Fungoides)

63
Q

Tazarotene (third generation retinoid) may be used in both acne vulgaris and psoriasis

A

True

64
Q

Topical Bexarotene (third generation retinoid) may be used in early stage persistent or refractory mycosis fungoides

A

True

65
Q

Bexarotene (third generation retinoid) has antitumour effects

A

True (used in mycosis fungoides)

66
Q

Oral Bexarotene (third generation retinoid) induces tumour regression and inhibits growth of tumour cell lines of haematopoetic and keratinocytes

A

True (used in mycosis fungoides)

67
Q

Bexarotene (third generation retinoid) increases cellular differentiation and decreased cellular growth

A

True (used in mycosis fungoides)

68
Q

The metabolism of topical Bexarotene is primarily unknown as in contrast to oral Bexarotene, studies and results are not available with respect to drug-drug interactions, renal or hepatic insufficiency

A

True (Oral Bexarotene is highly bound to plasma proteins and metabolised through the CYP3A4 pathway)

69
Q

Many of the precautions for topical Bexarotene were derived from studies of oral Bexarotene

A

True

70
Q

Topical Bexarotene is considered pregnancy category X

A

True (derived from studies of oral Bexarotene)

71
Q

Better efficacy of topical Bexarotene for mycosis fungoides has been associated with an increased frequency of application to affected areas

A

True

72
Q

There are no studies to indicate that topical Bexarotene results in central hypothyroidism from decreased thyrotropin levels as reported with oral Bexarotene

A

True

73
Q

Even though Clinical studies have failed to demonstrate topical Bexarotene may be photosensitising, patients are still advised to exercise precaution with regards to UV exposure

A

True

74
Q

Trace amounts of topical Bexarotene may be absorbed systemically (< 5 Ng/mL)and the increases in plasma concentration of Bexarotene are directly related to the percentage of body surface area treated

A

True

75
Q

Topical Alitretinoin (third generation retinoid) is used for the treatment of AIDS related Kaposi’s sarcoma

A

True

76
Q

Alitretinoin (third generation retinoid) binds to all RAR and RXR retinoid receptors

A

True

77
Q

In general, the RAR retinoid receptors are associated with cellular differentiation

A

True (Tretinoin for photoaging and acne vulgaris, Adapalene for acne vulgaris, Tazarotene for acne vulgaris and psoriasis)

78
Q

In general, the RXR retinoid receptors are associated with apoptosis

A

True (Alitretinoin for AIDS relate Kaposi’s sarcoma and Bexarotene for mycosis fungoides)

79
Q

Systemic absorption of topical Alitretinoin (third generation retinoid) is minimal

A

True (though still pregnancy category D)

80
Q

Tretinoin (first generation retinoid) may cause temporary worsening of acne and photosensitivity

A

True

81
Q

There is possible neutralisation of Tretinoin with simultaneous benzoyl peroxide

A

True

82
Q

Photosensitising drugs I.e. Thiazides, tetracyclines, fluoroquinolones, Phenothiazines antipsychotic agents, sulfonamides may increase the photosensitivity to topical Tretinoin

A

True

83
Q

Concomitant skin irritants may precipitate the irritation, erythema, peeling with topical Tretinoin

A

True

84
Q

Pregnancy is relatively contraindicated in use of topical all-Trans retinol and all-trans retinoic acid

A

True

85
Q

Pregnancy is absolutely contraindicated in topical Tazarotene and Bexarotene

A

True

86
Q

Topical Tazarotene may cause Koebnerisation of psoriasis

A

True

87
Q

All topical retinoids may cause skin irritation I.e. Erythema, pruritus

A

True

88
Q

Topical Sulfur, resorcinol and salacylic acid may interact with topical Adapalene

A

True

89
Q

Products with high % alcohol, astringents, spices and lime may interact with topical Adapalene

A

True

90
Q

Dermatologic medications and cosmetics with a strong drying effect should be avoided in patients on topical Tazarotene

A

True

91
Q

Photosensitising medications should be avoided in patients using topical Tazarotene

A

True

92
Q

Co-administration of products containing the insect repellent DEET should be avoided in patients using Alitretinoin and a bexarotene due to increased potential for DEET toxicity

A

True

93
Q

Patients on topical retinoids notice a decreased tolerance to UV radiation, leading to photosensitivity reactions

A

True

94
Q

It is helpful for patients on all topical retinoids to avoid concomitant use of irritating topical products I.e. Medicated/abrasive soaps and cosmetics, products with high concentrations of alcohol, astringents, spices or lime, topical products containing Sulfur, resorcinol or Salicylic acid

A

True (to minimise risk of skin irritancy)

95
Q

Topical retinoids do not play a direct inhibitory role on excess sebum

A

True

96
Q

Topical retinoids are first line treatment for non-inflammatory acne

A

True

97
Q

Topical retinoids are also helpful in the management of inflammatory acne where they may be used in combination with topical or systemic antimicrobials or hormone therapies

A

True

98
Q

Topical retinoids are generally not used in severe nodular acne vulgaris

A

True

99
Q

Once the acne is controlled, the topical retinoid should be continued to maintain the favourable results

A

True

100
Q

Topical retinoid therapy consists of once daily application to the entire region of the face prone to develop acne lesions

A

True (not used as spot treatment of individual lesions)

101
Q

Topical Tretinoin is photolabile and should be applied at bedtime

A

True

102
Q

Topical Adapalene and Tazarotene are more photostable than Tretinoin and may be applied morning or night

A

True

103
Q

Alternate day applications of topical retinoid (especially early in therapy) and drug holidays should be suggested if skin irritation in problematic

A

True

104
Q

Retinoid dermatitis (erythema and peeling) is most problematic during the first weeks of therapy

A

True

105
Q

It generally takes 3-6 months of continuous use of a topical retinoid to note a significant clinical improvement in photoaging

A

True

106
Q

Topical retinoids can increase the sensitivity to sunlight owing to reduced stratum corneum thickness

A

True (therefore sunscreen use is particularly stressed and patients are instructed to apply sunscreen daily)

107
Q

Topical Bexarotene may be used in psoriasis especially in combination with UVB treatment

A

True

108
Q

Application of Tretinoin to the skin 2 weeks or more before wounding has been demonstrated to enhance wound healing and speed the healing time

A

True (pretreatment with topical retinoids before dermabrasion, medium depth chemical peels and CO2 resurfacing results in decreased healing time overall increase improvement in cosmetic outcome)

109
Q

Pretreatment with topical retinoids (Tretinoin) before dermabrasion, medium depth chemical peels and CO2 resurfacing results in decreased healing time overall increase improvement in cosmetic outcome

A

True

Derm Pharm 2020 (47 decks)

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