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Foundations I > Drug Transport > Flashcards

Drug Transport Flashcards

1
Q

ABC Transporters

A
  • P-gp
  • MRP2
  • BCRP
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2
Q

SLC Transporters

A
  • OCT1
  • OCT2
  • MATE1/MATE2
  • OATP1B1/OATP1B3
  • OAT1/OAT3
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3
Q

P-gp

A
  • efflux
  • numerous drugs
  • small intestine, liver, kidney, bbb
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4
Q

MRP2

A
  • efflux
  • glucuronice and sulfate drug conjugates and some drugs
  • liver, kidney
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5
Q

BCRP

A
  • numerous drugs
  • efflux
  • intestine, liver, bbb
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6
Q

Which intestinal transporters determine F?

A

P-gp, BCRP

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7
Q

⬆️ P-gp, BCRP

A
  • ⬆️ efflux into intestine
  • ⬇️ F
  • ⬇️ Cmax, ⬇️ AUC, ⬇️ Efficacy
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8
Q

⬇️ P-gp, BCRP

A
  • ⬇️ efflux into intestine
  • ⬆️ F
  • ⬆️ Cmax, ⬆️ AUC, ⬆️ toxicity
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9
Q

What are the hepatic transporters important for drug and metabolite biliary elimination?

A

P-gp, BCRP, MRP2

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10
Q

⬇️ P-gp, BCRP, MRP2

A
  • ⬇️ efflux into bile
  • ⬇️ CLb, ⬆️ plasma levels, ⬇️ k
  • ⬆️ Fh, ⬆️ Cmax
  • ⬆️ hepatocyte levels, ⬆️ toxicity
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11
Q

⬆️ P-gp, BCRP, MRP2

A
  • ⬆️ efflux into bile
  • ⬆️ Clb, ⬇️ plasma levels, ⬆️ k
  • ⬇️ Fh, ⬇️ Cmax
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12
Q

What are the hepatic uptake transporters that determine efficacy and exposure?

A

OCTs, OATs

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13
Q

⬇️ OCTs, OATs

A
  • ⬇️ uptake in the liver
  • ⬇️ metabolism, ⬇️ Clh, ⬆️ Fh
  • ⬇️ biliary secretion, ⬇️ Clb, ⬇️ Fh
  • ⬇️ Cl, ⬆️ F
  • ⬆️ C, ⬆️ AUC
  • ⬆️ Cmax if first pass
  • ⬇️ k
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14
Q

What are the renal transporters important for renal elimination?

A

P-gp, MATEs, MRP2, OCT2, OAT1, OAT3

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15
Q

⬇️ P-gp, MATEs, MRPs

A
  • ⬇️ Efflux
  • ⬇️ Clr
  • ⬇️ Cl, ⬆️ C
  • ⬆️ kidney levels, ⬆️ nephrotoxicity
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16
Q

⬇️ OCT2, OAT1, OAT3

A
  • ⬇️ uptake
  • ⬇️ Clr
  • ⬆️ C, ⬆️ AUC
17
Q

OCT1

A
  • uptake
  • liver
  • organic cations
18
Q

OCT2

A
  • uptake
  • kidney
  • organic cations
19
Q

MATE1/MATE2

A
  • efflux
  • kidney
  • cations
20
Q

OATP1B1/OATP1B3

A
  • uptake
  • liver
  • anions
21
Q

OAT1/OAT3

A
  • uptake
  • kidney
  • anions
22
Q

Diffusion

A

high to low

23
Q

Facilitated diffusion

A
  • transport protein
  • saturable
  • OCTs
24
Q

Primary active transport

A
  • transport protein
  • saturable
  • low to high (against)
  • energy dependent
  • P-gp, BCRP, MRP2
25
Q

Secondary/Tertiary active transport

A
  • transport protein
  • saturable
  • low to high (against)
  • energy dependent
  • MATEs, OATs

Foundations I (14 decks)

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