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
Approved in Europe and Canada for treatment resistant chronic hand eczema
Alitretinoin 10-30mg/day for 6 months
26
FDA approved for CTCL that is refractory to at least one systemic therapy
Bexarotene 300mg/m2 with 60% response rate in first two months
27
Topical combination approved for the treatment of melasma
Tretinoin 0.05%/ hydroquinone4%/ Fluocinolone 0.1%
28
Posttherapy relapse is minimized by administering cumulative dose of at least ___
120 mg/kg
29
The most common adverse effect
Skin irritation, peaks within first month
30
Central hypothyroidism is observed with topical bexarotene gel True or False
False, not observed
31
No evidence exists for teratogenicity of topical tretinoin in humans True or False
True
32
Retinoid therapy does not appear to produce abnormalities in spermatogenesis, sperm morphology, or sperm motility. True or False
True
33
Most common cutaneous side effect of bexarotene
Localized or extensive exfoliative dermatitis
34
___ appears to induce fewer mucocutaneous and ocular side effects than other classes of retinoids
Bexarotene
35
___ colonization tends to correlate with isotretinoin -induced reduction in sebum production and may lead to overt cutaneous infections
Staphylococcus aureus
36
Diffuse or localized hair loss is more severe during treatment with
Acitretin
37
Muscle effects like cramps are more frequent with
Isotretinoin
38
Major risk factor for development of pseudotumor cerebri
Concomitant use of isotretinoin with tetracycline
39
Central hypothyroidism is irreversible even with DC of systemic bexarotene therapy. True or False
False, reversible
40
Most frequent abnormalities in lab test results
Serum lipid changes 50-80% triglyceride levels 30-50% cholesterol levels
41
Disturbance of blood lipid levels is higher with acitretin than isotretinoin and bexarotene. True or False
False, higher with isotretinoin and bexarotene
42
Therapy should be discontinued if TGL reaches ____ mg/dl
800
43
Transient abnormal elevations in serum transaminases has been reported in approximately __%of patients treated with __
20% | Acitretin and etretinate
44
Transaminase levels more than ___x should lead to discontinuation of retinoid therapy
3
45
28% who use bexarotene therapy presents with
Dose-related neutropenia 2-4 weeks form initiation of treatment
46
Concurrent use of ___ increase half life of tretinoin; use of _____, bexarotene
Ketoconazole and liarozole | Gemfibrozil
47
Use of ff should be avoided with use of retinoids
Tetracyclines Alcohol Methotrexate VitA supplements
48
___ therapy is not recommended for women with childbearing potential due to long term treatment of more chronic diseases and slow elimination of aromatic retinoids
Acitretin or etretinate
49
Woman with childbearing potential must have ___ negative results on pregnancy test spaced ___ days apart and practice effective contraception during treatment and after ___
2, 30 days, 1 month
50
Unapproved indications with clinical studies supporting benefit
``` Pityriasis rubra pilaris Premalignancies Photoaging Ichythyosis Darier White disease ```
51
Characteristic common to retinoids is that they bind to regulatory regions in DNA called
Hormone response elements or target sequences
52
Treatment of human skin with all-trans-retinol or retinaldehyde increases retinyl ester levels in epidermal layer by more than ___ fold
10
53
CYP26 activity inhibitor
Ketoconazole | Liarozole
54
Metabolism of retinoids involve 2 steps
1. Esterification and oxidation of retinol | 2. Hydroxylation of all-trans-retinoic acid
55
Major metabolite of isotretinoin
4-oxo-isotretinoin
56
All women taking acitretin should avoid taking alcohol during treatment and for __ months thereafter
2
57
Bexarotene is __ fold more potent in activating RXR than RAR
100
58
Bexarotene is metabolized by ___
CYP 3A4
59
Alitretinoin and tretinoin have been reported to inhibit herpes simplex virus replication. True or False
True
60
Most significant response of alitretinoin occurred __ weeks of therapy
14
61
Topical retinoids can be used in all age groups, except
Neonates
62
Teratogenicity is not caused by topical retinoids. | True or False
True
63
Best results for acitretin have been obtained in
Pustular psoriasis of palmoplantar or generalized (von Zumbusch) type ARCI, esp. lamellar type
64
Rebound occurs after cessation of treatment of acitretin. | True or False
False, does not occur
65
Acitretin causes decrease of __% in PASI score depending on the dosage
60 to 70%
66
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
Acitretin 30 mg/ day for 6 months
67
Treatment for Darier White Disease
10mg/ day acitretin
68
The most important element in topical retinoid therapy
Patient education
69
Matching type 1. Tagretin 2. Avita 3. Differin 4. Triluma 5. Panretin 6. Avage ``` A. Tretinoin B. Adapalene C. Tazarotene D. Bexarotene E. Alitretinoin ```
``` D A B A C ```
70
0.025% tretinoin and 0.01% tretinoin are equally efficacious | True or False
True
71
Length of therapy for 1. Isotretinoin 2. Acitretin 3. Bexarotene 4. Alitretinoin
1. 4-6 months 2. > 3 months 3. > 2 months 4. > 6 months
72
__ of acne patients require second course of isotretinoin therapy for either persistent disease or relapse
1/3
73
If CTCL does not respond after 8 weeks, dose may be increased to __
400 mg/m2/day
74
Local irritation is observed as the most common side effect in the ff
Bexarotene | Alitretinoin
75
All retinoids does not produce neutropenia, except
Bexarotene
76
Hypothyroidism has been associated with
Alitretinoin | Bexarotene
77
Most common retinoid associated with ocular side effects
Isotretinoin
78
Most common retinoid associated with alopecia side effects
Isotretinoin
79
Most common retinoid associated with headache as side effect
Alitretinoin
80
Most common retinoid associated with musculoskeletal side effects
Isotretinoin
81
Most common retinoid associated with hepatotoxic side effects
Isotretinoin | Alitretinoin
82
Most common retinoid associated with hyperlipidemia side effects
Isotretinoin | Bexarotene
83
Blepharoconjunctivitis occurs in __ of patients treated with isotretinoin due to its effects on Meibomian glands
1/3
84
Bone pain without objective evidence and without sequelae are frequent in retinoid treated patients. True or False
True
85
DISH syndrome stands for
Diffuse idiopathic skeletal hyperostosis
86
Increased muscle tone, axial rigidity, myopathy were related to treatment with
Etretinate and acitretin
87
Bleeding complications has been reported with isotretinoin induced fibrinolysis. True or False
True
88
Program used to minimize risk of isotretinoin teratogenicity
IPLEDGE
89
Labs requested before oral retinoid therapy
Serum lipid levels CBC Thyroid function tests Liver enzyme levels
90
Retinoid induced hyperlipidemia is not associated with accelerated atherosclerosis or increased risk of CV disease. True or False
True