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Kinetics > Drug Transporters > Flashcards

Drug Transporters Flashcards

1
Q

Major drug transporters

A

-Efflux
-Uptake

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2
Q

Efflux transporters

A

-P-glycoprotein

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3
Q

Uptake transporters

A

-OATP
-PEPT1

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4
Q

P-glycoprotein (P-gp)

A

-efflux transporter
-affect PERMEABILITY of drugs
-leads to resistance to certain drugs
-aka MDR1

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5
Q

P-gp expressed where

A

-brain
-liver
-kidney
-testis
-cancer

-apical side of tissue

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6
Q

P-gp in intestinal epithelia

A

-pumps drug out into intestine

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7
Q

P-gp in hepatocytes

A

-pumps drug to bile canaliculi
-secreted to bile
-bile goes to intestine

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8
Q

Pgp in kidney prox tubules

A

-pumps drug to urine

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9
Q

P-gp in blood brain barrier

A

-pumps drug away from brain into blood

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10
Q

Blood Brain Barrier

A

-tight junction
-lipophilic molecules can diffuse in
-P-gp pumps out foreign substances

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11
Q

P-gp substrates

A

-many lipophilic compounds
-Paclitaxel
-anti cancer
-anti HIV
-anti infectives
-CV

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12
Q

Paclitaxel

A

-P-gp substrate
-does not reach brain in Xray example

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13
Q

P-gp inhibition

A

more drug in brain

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14
Q

P-Gp in placenta

A

-part of fetal protection system
-pumps drug back into maternal drug

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15
Q

P-Gp inhibitors will increase drug exposure to

A

-brain
-fetus

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16
Q

Organic anion transporting protein (OATP)

A

-300 member family, 11 in humans
-uptake transporters
-pump drug IN

17
Q

OATP substrates

A

-bilirubin, bile salts, steroid hormone metabolites
-Fexofenadine, statins

18
Q

OATP tissue distribution

A

-liver
-small intestine

19
Q

OATP1B1 in liver

A

-pump drug INTO liver

20
Q

Statins

A

-need to reach liver to work
-OATP substrates
-myopathy risk

21
Q

myopathy mech

A

-OATP1B1 inhibition
-dec statin concentration in liver
-inc statin in plasma
-inc statin myopathy (muscle)

22
Q

OATP1B1 inhibition

A

-lower efficacy
-inc side effects (myopathy)

23
Q

OATP1B1 genetic polymorphisms

A

-mutation leads to nonfunctional form (V174A)
-inc statin exposure

24
Q

PEPT1 tissue distribution

A

-intestine

25
Q

PEPT1

A

-uptake transporter
-pumps drug into enterocytes
-inc drug absorption

26
Q

GrPEFRUIT JUICE

A

-inhibits intestinal OATP
-dec drug absorption
=lower drug concentration

27
Q

PEPT1 substrates

A

-di/tripeptides
-B-lactam antibiotics

28
Q

PEPT1 clinical use

A

-improve oral absorption of drugs

Kinetics (22 decks)

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