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20 Cards in this Set

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RXR
nuclear receptor for 9-cis retinoi acid
RAR
nuclear receptor for all-trans retinoic acid
RAR and RXR are related to what recptors?
thyroid receptor, vitamin D receptor, testosterone receptor
How do RAR and RXR work
form heterodimers with other recptors for complex regulation of DNA
vitamin A deficiency
night blindness
diarrhea
thick cancellous bone
slow growth
anemia, low blood volume
effects taste, smell hearing
hypervitaminosis A
dry, red, ithcing skin, desquamation fissure of lips, hair loss, peeling
hepatosplenomegaly, cirrhosis
teratogen
headache, anorexia, fatigue, hemorrha

Vitamin E helps
carotenoids
derived from plants and yield two molecules of retinal

retinal-->retinol
1st generation retinoic acid analogs
tretinoin and isotretinoin
Isotretinoin
Accutane, PO

for recalcitrant nodular acne
reduces sebacious gland size and number
Pharmokinetics and precautions with isotretinoin
T1/2 = 24hrs, some last for up to 1 month. NOT FOR WOMEN WHO MAY BECOME PREGNANT

may cause worsening night vision, trouble with contacts, worsening IBD
use of all-trans retinoic acid
stimulation differentiation of APL (caused by PML-RAR fusion)

prevention of oral squamous cell carcinoma

for rare hepatocellular carcinoma
tretinoin
synthetic ATRA

for acnes and sun damaged skin
application of isotretinoin vs tretinoin
isotretinoin works systemically only, metab in bile

tretinoin works topically, but would be metabolized in liver
Etretinate and Acitretin
treat Psoriasis, psoriatic arthiritis, ichthosis
Etretinate vs Acitretin
Etretinate is an ethyl ester of Acitretin, the active drug
Pharmokinetics of Acitretin
50% oral bioavailability, higher with food, milk, fat.

Store in fat and tissue with T1/2 of 5 MONTHS!

SE like vitamin A, use contraception
Arotenoids
3rd generation retinols witha romatic ring

more potent with different spectrum of actiosn
Topical treatment of acne and skin damage
Tretinoin
Take orally for nodular acne
Isotretinoin
Not for use on young women who make become pregnant
Isotretinoin (and all other oral vitamin A analogs)