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20 Cards in this Set
- Front
- Back
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RXR
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nuclear receptor for 9-cis retinoi acid
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RAR
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nuclear receptor for all-trans retinoic acid
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RAR and RXR are related to what recptors?
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thyroid receptor, vitamin D receptor, testosterone receptor
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How do RAR and RXR work
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form heterodimers with other recptors for complex regulation of DNA
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vitamin A deficiency
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night blindness
diarrhea thick cancellous bone slow growth anemia, low blood volume effects taste, smell hearing |
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hypervitaminosis A
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dry, red, ithcing skin, desquamation fissure of lips, hair loss, peeling
hepatosplenomegaly, cirrhosis teratogen headache, anorexia, fatigue, hemorrha Vitamin E helps |
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carotenoids
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derived from plants and yield two molecules of retinal
retinal-->retinol |
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1st generation retinoic acid analogs
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tretinoin and isotretinoin
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Isotretinoin
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Accutane, PO
for recalcitrant nodular acne reduces sebacious gland size and number |
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Pharmokinetics and precautions with isotretinoin
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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 |
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use of all-trans retinoic acid
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stimulation differentiation of APL (caused by PML-RAR fusion)
prevention of oral squamous cell carcinoma for rare hepatocellular carcinoma |
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tretinoin
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synthetic ATRA
for acnes and sun damaged skin |
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application of isotretinoin vs tretinoin
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isotretinoin works systemically only, metab in bile
tretinoin works topically, but would be metabolized in liver |
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Etretinate and Acitretin
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treat Psoriasis, psoriatic arthiritis, ichthosis
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Etretinate vs Acitretin
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Etretinate is an ethyl ester of Acitretin, the active drug
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Pharmokinetics of Acitretin
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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 |
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Arotenoids
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3rd generation retinols witha romatic ring
more potent with different spectrum of actiosn |
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Topical treatment of acne and skin damage
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Tretinoin
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Take orally for nodular acne
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Isotretinoin
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Not for use on young women who make become pregnant
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Isotretinoin (and all other oral vitamin A analogs)
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