2022-11-01T05:18:09+03:00[Europe/Moscow] en true <p>INR</p>, <p>bleeding risk</p>, <p>clot risk </p>, <p>VKORC1</p>, <p>leads to decrease of VKORC1 transcription factors and less protein</p>, <p>more sensitive </p>, <p>CYP2C9</p>, <p>bleeding risk</p>, <p>ATP-Binding Cassete </p>, <p>Solute Carrier transporter</p>, <p>MDR1, MRP, MXR</p>, <p>OCT, OAT</p>, <p>Organic cation transporters (OCT)</p>, <p>Organic anion transporters (OAT)</p>, <p>MDR1</p>, <p>encodes for P-gp pumps that remove foreign substances out of the cell</p>, <p>gene expression (how much protein is made), functionality of P-gp (which substrates will bind)</p>, <p>can't efflux morphine out of neurons and back into bloodstream; too much analgesic effect</p>, <p>SLCO1B1</p>, <p>can't influx statin into their cell; results in high plasma concentrations</p> flashcards
Drug Targets & Transporters

Drug Targets & Transporters

Customize
collection saved
Share
Long Term Learning Spaced Repetition
Add to Long Term Learning Desk
Fast learning Repeat this set of flashcards
Preview Test Spell
Play
Match
Review

  • INR

    -time it takes for blood to clot (prothrombin time) and compares it to a standard or control

  • bleeding risk

    INR>3 signifies _______

  • clot risk

    INR<2 signifies ________

  • VKORC1

    Which gene does Warfarin inhibit?

  • leads to decrease of VKORC1 transcription factors and less protein

    VKORC1 mutation effects?

  • more sensitive

    People with a mutation in the VKORC1 gene are _________ to warfarin

  • CYP2C9

    Warfarin is metabolized by ______

  • bleeding risk

    People with CYP2C9*3/*3 alleles are associated with __________ in regards to Warfarin.

  • ATP-Binding Cassete

    -efflux

    -active transporters that are ATP-dependent

    -work against the concentration gradient

  • Solute Carrier transporter

    -influx

    -family that contains both active and passive transporters that rely on electrical gradient

  • MDR1, MRP, MXR

    What are our major efflux transporters?

  • OCT, OAT

    What are our major influx transporters?

  • Organic cation transporters (OCT)

    -found in kidney and liver tissue, mediate the uptake of organic cations from the blood into the tubules or mediate the uptake of organic cations into the hepatocytes where they are exposed to drug metabolizing enzymes.

  • Organic anion transporters (OAT)

    - found in the intestines, liver, and kidneys

    -mediate the uptake of anions (primary focus)

  • MDR1

    -encodes for P-glycoprotein

  • encodes for P-gp pumps that remove foreign substances out of the cell

    What is the primary function of ABCB1?

  • gene expression (how much protein is made), functionality of P-gp (which substrates will bind)

    P-gp function is dependent on 2 factors, what are they?

  • can't efflux morphine out of neurons and back into bloodstream; too much analgesic effect

    What happens to patients who have ABCB1 mutation in regards to morphine?

  • SLCO1B1

    OATP1B1 encodes for what protein?

  • can't influx statin into their cell; results in high plasma concentrations

    What are the implications of someone who has a genetic mutation in OATP1B1?