Chapter 185 - Retinoids Flashcards
Predominant retinoid receptors in human skin are
RAR alpha
RAR gamma
RXR alpha
RXR beta
Approved of topical steroids (6)
Acne Psoriasis Cutaneous T cell lymphoma Kaposi sarcoma Melasma Photoaged skin
Approved use of oral steroids (4)
Acne
Cutaneous T cell lymphoma
Chronic hand eczema
Psoriasis
Most concerning side effect
Teratogenicity
Molecular storage form of retinol
Retinyl esters
First generation retinoids (3)
All-trans-retinoic acid (tretinoin)
13-cis-retinoic acid (isotretinoin)
9-cis-retinoic acid (alitretinoin)
Second generation retinoids (2)
Etretinate
Acitretin
Third generation retinoids (3)
Adapalene
Tazarotene
Bexarotene
Known as synthetic retinoids
2nd and third gen retinoids
Predominant retinol-esterifying activity
Lecithin/retinol acyltransferase
Class of drugs that target CYP26 activity
Retinoic acid metabolism blocking agents (RAMBAs)
For isotreinoin, a ____ posttherapy period of contraception provides an adequate safety margin
1 month
Etretinate is ___ times more lipophilic than acitretin
50
Etretinate has a half life of ___ and acitretin has a half life of ____
120 days; 2 days
Major metabolite of acitretin via isomerization
13-cis-isomer
Compulsory contraception in patients taking acitretin is ____ years
2
Approved for the treatment of acne, photoaged skin, and melasma in the United States
Tretinoin
Approved for acne
Topical adapalene and tazarotene
Approved for psoriasis and photoaging
Tazarotene
For management of cutaneous T cell lymphoma
Bexarotene
For treatment of patients with Kaposi sarcoma
Alitretinoin
2 features improved by application of tazarotene or tretinoin
Fine wrinkles
Dyspigmentation
Antiviral role against HHV8
Alitretinoin
Retinoid of choice in psoriasis
Acitretin
Approved in Europe and Canada for treatment resistant chronic hand eczema
Alitretinoin 10-30mg/day for 6 months
FDA approved for CTCL that is refractory to at least one systemic therapy
Bexarotene 300mg/m2 with 60% response rate in first two months
Topical combination approved for the treatment of melasma
Tretinoin 0.05%/
hydroquinone4%/
Fluocinolone 0.1%
Posttherapy relapse is minimized by administering cumulative dose of at least ___
120 mg/kg
The most common adverse effect
Skin irritation, peaks within first month
Central hypothyroidism is observed with topical bexarotene gel
True or False
False, not observed
No evidence exists for teratogenicity of topical tretinoin in humans
True or False
True
Retinoid therapy does not appear to produce abnormalities in spermatogenesis, sperm morphology, or sperm motility.
True or False
True
Most common cutaneous side effect of bexarotene
Localized or extensive exfoliative dermatitis
___ appears to induce fewer mucocutaneous and ocular side effects than other classes of retinoids
Bexarotene
___ colonization tends to correlate with isotretinoin -induced reduction in sebum production and may lead to overt cutaneous infections
Staphylococcus aureus
Diffuse or localized hair loss is more severe during treatment with
Acitretin