Chapter 185 - Retinoids Flashcards

1
Q

Predominant retinoid receptors in human skin are

A

RAR alpha
RAR gamma
RXR alpha
RXR beta

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2
Q

Approved of topical steroids (6)

A
Acne 
Psoriasis
Cutaneous T cell lymphoma
Kaposi sarcoma
Melasma
Photoaged skin
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3
Q

Approved use of oral steroids (4)

A

Acne
Cutaneous T cell lymphoma
Chronic hand eczema
Psoriasis

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4
Q

Most concerning side effect

A

Teratogenicity

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5
Q

Molecular storage form of retinol

A

Retinyl esters

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6
Q

First generation retinoids (3)

A

All-trans-retinoic acid (tretinoin)
13-cis-retinoic acid (isotretinoin)
9-cis-retinoic acid (alitretinoin)

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7
Q

Second generation retinoids (2)

A

Etretinate

Acitretin

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8
Q

Third generation retinoids (3)

A

Adapalene
Tazarotene
Bexarotene

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9
Q

Known as synthetic retinoids

A

2nd and third gen retinoids

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10
Q

Predominant retinol-esterifying activity

A

Lecithin/retinol acyltransferase

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11
Q

Class of drugs that target CYP26 activity

A

Retinoic acid metabolism blocking agents (RAMBAs)

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12
Q

For isotreinoin, a ____ posttherapy period of contraception provides an adequate safety margin

A

1 month

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13
Q

Etretinate is ___ times more lipophilic than acitretin

A

50

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14
Q

Etretinate has a half life of ___ and acitretin has a half life of ____

A

120 days; 2 days

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15
Q

Major metabolite of acitretin via isomerization

A

13-cis-isomer

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16
Q

Compulsory contraception in patients taking acitretin is ____ years

A

2

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17
Q

Approved for the treatment of acne, photoaged skin, and melasma in the United States

A

Tretinoin

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18
Q

Approved for acne

A

Topical adapalene and tazarotene

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19
Q

Approved for psoriasis and photoaging

A

Tazarotene

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20
Q

For management of cutaneous T cell lymphoma

A

Bexarotene

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21
Q

For treatment of patients with Kaposi sarcoma

A

Alitretinoin

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22
Q

2 features improved by application of tazarotene or tretinoin

A

Fine wrinkles

Dyspigmentation

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23
Q

Antiviral role against HHV8

A

Alitretinoin

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24
Q

Retinoid of choice in psoriasis

A

Acitretin

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25
Q

Approved in Europe and Canada for treatment resistant chronic hand eczema

A

Alitretinoin 10-30mg/day for 6 months

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26
Q

FDA approved for CTCL that is refractory to at least one systemic therapy

A

Bexarotene 300mg/m2 with 60% response rate in first two months

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27
Q

Topical combination approved for the treatment of melasma

A

Tretinoin 0.05%/
hydroquinone4%/
Fluocinolone 0.1%

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28
Q

Posttherapy relapse is minimized by administering cumulative dose of at least ___

A

120 mg/kg

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29
Q

The most common adverse effect

A

Skin irritation, peaks within first month

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30
Q

Central hypothyroidism is observed with topical bexarotene gel
True or False

A

False, not observed

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31
Q

No evidence exists for teratogenicity of topical tretinoin in humans
True or False

A

True

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32
Q

Retinoid therapy does not appear to produce abnormalities in spermatogenesis, sperm morphology, or sperm motility.
True or False

A

True

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33
Q

Most common cutaneous side effect of bexarotene

A

Localized or extensive exfoliative dermatitis

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34
Q

___ appears to induce fewer mucocutaneous and ocular side effects than other classes of retinoids

A

Bexarotene

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35
Q

___ colonization tends to correlate with isotretinoin -induced reduction in sebum production and may lead to overt cutaneous infections

A

Staphylococcus aureus

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36
Q

Diffuse or localized hair loss is more severe during treatment with

A

Acitretin

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37
Q

Muscle effects like cramps are more frequent with

A

Isotretinoin

38
Q

Major risk factor for development of pseudotumor cerebri

A

Concomitant use of isotretinoin with tetracycline

39
Q

Central hypothyroidism is irreversible even with DC of systemic bexarotene therapy.
True or False

A

False, reversible

40
Q

Most frequent abnormalities in lab test results

A

Serum lipid changes
50-80% triglyceride levels
30-50% cholesterol levels

41
Q

Disturbance of blood lipid levels is higher with acitretin than isotretinoin and bexarotene.
True or False

A

False, higher with isotretinoin and bexarotene

42
Q

Therapy should be discontinued if TGL reaches ____ mg/dl

A

800

43
Q

Transient abnormal elevations in serum transaminases has been reported in approximately __%of patients treated with __

A

20%

Acitretin and etretinate

44
Q

Transaminase levels more than ___x should lead to discontinuation of retinoid therapy

A

3

45
Q

28% who use bexarotene therapy presents with

A

Dose-related neutropenia 2-4 weeks form initiation of treatment

46
Q

Concurrent use of ___ increase half life of tretinoin; use of _____, bexarotene

A

Ketoconazole and liarozole

Gemfibrozil

47
Q

Use of ff should be avoided with use of retinoids

A

Tetracyclines
Alcohol
Methotrexate
VitA supplements

48
Q

___ therapy is not recommended for women with childbearing potential due to long term treatment of more chronic diseases and slow elimination of aromatic retinoids

A

Acitretin or etretinate

49
Q

Woman with childbearing potential must have ___ negative results on pregnancy test spaced ___ days apart and practice effective contraception during treatment and after ___

A

2, 30 days, 1 month

50
Q

Unapproved indications with clinical studies supporting benefit

A
Pityriasis rubra pilaris
Premalignancies
Photoaging
Ichythyosis
Darier White disease
51
Q

Characteristic common to retinoids is that they bind to regulatory regions in DNA called

A

Hormone response elements or target sequences

52
Q

Treatment of human skin with all-trans-retinol or retinaldehyde increases retinyl ester levels in epidermal layer by more than ___ fold

A

10

53
Q

CYP26 activity inhibitor

A

Ketoconazole

Liarozole

54
Q

Metabolism of retinoids involve 2 steps

A
  1. Esterification and oxidation of retinol

2. Hydroxylation of all-trans-retinoic acid

55
Q

Major metabolite of isotretinoin

A

4-oxo-isotretinoin

56
Q

All women taking acitretin should avoid taking alcohol during treatment and for __ months thereafter

A

2

57
Q

Bexarotene is __ fold more potent in activating RXR than RAR

A

100

58
Q

Bexarotene is metabolized by ___

A

CYP 3A4

59
Q

Alitretinoin and tretinoin have been reported to inhibit herpes simplex virus replication.
True or False

A

True

60
Q

Most significant response of alitretinoin occurred __ weeks of therapy

A

14

61
Q

Topical retinoids can be used in all age groups, except

A

Neonates

62
Q

Teratogenicity is not caused by topical retinoids.

True or False

A

True

63
Q

Best results for acitretin have been obtained in

A

Pustular psoriasis of palmoplantar or generalized (von Zumbusch) type
ARCI, esp. lamellar type

64
Q

Rebound occurs after cessation of treatment of acitretin.

True or False

A

False, does not occur

65
Q

Acitretin causes decrease of __% in PASI score depending on the dosage

A

60 to 70%

66
Q

Effective in the treatment of premalignancies, including HPV-induced tumors and actinic keratosis, malignant skin lesions in renal transplant recipients, basal cell nevus syndrome, and xeroderma pigmentosum patients

A

Acitretin 30 mg/ day for 6 months

67
Q

Treatment for Darier White Disease

A

10mg/ day acitretin

68
Q

The most important element in topical retinoid therapy

A

Patient education

69
Q

Matching type

  1. Tagretin
  2. Avita
  3. Differin
  4. Triluma
  5. Panretin
  6. Avage
A. Tretinoin
B. Adapalene
C. Tazarotene
D. Bexarotene
E. Alitretinoin
A
D
A
B
A
C
70
Q

0.025% tretinoin and 0.01% tretinoin are equally efficacious

True or False

A

True

71
Q

Length of therapy for

  1. Isotretinoin
  2. Acitretin
  3. Bexarotene
  4. Alitretinoin
A
  1. 4-6 months
  2. > 3 months
  3. > 2 months
  4. > 6 months
72
Q

__ of acne patients require second course of isotretinoin therapy for either persistent disease or relapse

A

1/3

73
Q

If CTCL does not respond after 8 weeks, dose may be increased to __

A

400 mg/m2/day

74
Q

Local irritation is observed as the most common side effect in the ff

A

Bexarotene

Alitretinoin

75
Q

All retinoids does not produce neutropenia, except

A

Bexarotene

76
Q

Hypothyroidism has been associated with

A

Alitretinoin

Bexarotene

77
Q

Most common retinoid associated with ocular side effects

A

Isotretinoin

78
Q

Most common retinoid associated with alopecia side effects

A

Isotretinoin

79
Q

Most common retinoid associated with headache as side effect

A

Alitretinoin

80
Q

Most common retinoid associated with musculoskeletal side effects

A

Isotretinoin

81
Q

Most common retinoid associated with hepatotoxic side effects

A

Isotretinoin

Alitretinoin

82
Q

Most common retinoid associated with hyperlipidemia side effects

A

Isotretinoin

Bexarotene

83
Q

Blepharoconjunctivitis occurs in __ of patients treated with isotretinoin due to its effects on Meibomian glands

A

1/3

84
Q

Bone pain without objective evidence and without sequelae are frequent in retinoid treated patients.
True or False

A

True

85
Q

DISH syndrome stands for

A

Diffuse idiopathic skeletal hyperostosis

86
Q

Increased muscle tone, axial rigidity, myopathy were related to treatment with

A

Etretinate and acitretin

87
Q

Bleeding complications has been reported with isotretinoin induced fibrinolysis.
True or False

A

True

88
Q

Program used to minimize risk of isotretinoin teratogenicity

A

IPLEDGE

89
Q

Labs requested before oral retinoid therapy

A

Serum lipid levels
CBC
Thyroid function tests
Liver enzyme levels

90
Q

Retinoid induced hyperlipidemia is not associated with accelerated atherosclerosis or increased risk of CV disease.
True or False

A

True