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Flashcards in 1 - TOPICAL RETINOIDS Deck (109):
1

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

True

2

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

True (same as tretinoin and all-trans retinol)

3

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

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

4

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

True

5

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

True

6

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

True (all-trans retinoic acid binds to CRABP)

7

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

True

8

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

True

9

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

True

10

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

True

11

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)

True

12

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

True

13

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

True

14

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

True

15

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

True

16

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

True

17

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

True

18

All-trans retinol do not bind to any retinoid receptors

True

19

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

True

20

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

True

21

Bexarotene (third generation retinoid) binds to RXR retinoid receptors

True

22

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

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

23

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

True (Tazarotene is a prodrug)

24

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

True

25

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

True

26

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

True

27

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

True

28

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

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

29

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

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

30

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

True

31

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

True (neutrophils commonly found in acne)

32

Adapalene is systemically absorbed

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

33

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

True

34

Adapalene is carcinogenic

False (only trace amounts absorbed systemically)

35

Adapalene is mutagenic

False (only trace amounts absorbed systemically)

36

Adapalene is teratogenic

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

37

Adapalene is genotoxic

False (only trace amounts absorbed systemically)

38

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

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

39

There are no clinical studies that show that Adapalene is photosensitising

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

40

Adapalene (third generation retinoid) is active without metabolic transformation

True

41

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

True (only trace amounts systemically absorbed)

42

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

True

43

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

True (so does Adapalene)

44

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

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

45

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

True

46

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

True (also comedolysis in acne)

47

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

True

48

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

True

49

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

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

50

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

True

51

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

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

52

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

True

53

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

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

54

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

True (also in urine and faeces)

55

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

True

56

Adapalene (third generation retinoid) is a synthetic retinoid

True

57

Tazarotene (third generation retinoid) is a synthetic retinoid

True

58

Alitretinoin (third generation retinoid) is a natural retinoid

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

59

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

True

60

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

True

61

Tazarotene (third generation retinoid) may worsen psoriasis

True (although it is use in psoriasis)

62

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

True (used in Mycosis Fungoides)

63

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

True

64

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

True

65

Bexarotene (third generation retinoid) has antitumour effects

True (used in mycosis fungoides)

66

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

True (used in mycosis fungoides)

67

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

True (used in mycosis fungoides)

68

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

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

69

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

True

70

Topical Bexarotene is considered pregnancy category X

True (derived from studies of oral Bexarotene)

71

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

True

72

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

True

73

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

True

74

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

True

75

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

True

76

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

True

77

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

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

78

In general, the RXR retinoid receptors are associated with apoptosis

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

79

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

True (though still pregnancy category D)

80

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

True

81

There is possible neutralisation of Tretinoin with simultaneous benzoyl peroxide

True

82

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

True

83

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

True

84

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

True

85

Pregnancy is absolutely contraindicated in topical Tazarotene and Bexarotene

True

86

Topical Tazarotene may cause Koebnerisation of psoriasis

True

87

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

True

88

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

True

89

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

True

90

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

True

91

Photosensitising medications should be avoided in patients using topical Tazarotene

True

92

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

True

93

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

True

94

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

True (to minimise risk of skin irritancy)

95

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

True

96

Topical retinoids are first line treatment for non-inflammatory acne

True

97

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

True

98

Topical retinoids are generally not used in severe nodular acne vulgaris

True

99

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

True

100

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

True (not used as spot treatment of individual lesions)

101

Topical Tretinoin is photolabile and should be applied at bedtime

True

102

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

True

103

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

True

104

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

True

105

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

True

106

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

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

107

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

True

108

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

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

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

True