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Drug Transporters

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Efflux Transporters

P-glycoprotein

Substrates

Main drug classes predominantly transported by Pgp include:

Main Drugs

carvedilol

digoxin

loperamide

rifampicin

celiprolol

diltiazem

morphine

roxithromycin

colchicine

erythromycin

nifedipine

simvastatin

dabigatran etexilate

fexofenadine

progesterone

 

ciclosporin

etoposide

nelfinavir

vinblastine

daunorubicin

indinavir

paclitaxel

vincristine

docetaxel

mitomycin C

saquinavir

 

doxorubicin

mitoxantrone

tacrolimus

 

Inhibitors (usually lead to increased systemic concentrations)

amiodarone

grapefruit juice

progesterone

trifluoperazine

ciclosporin

itraconazole

quinidine

verapamil

diltiazem

ketoconazole

tamoxifen

 

Inducers (usually lead to decreased systemic concentrations)

carbamazepine

phenytoin

rifampicin

St Johns wort

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Ion Transporters (Solute Transporters)

Organic Anion Transporters (OATs)

Substrates

Main drug classes predominantly transported by OATs include:

Main Drugs

aciclovir

cephalosporins

furosemide

penicillins

bosentan

ciprofloxacin

methotrexate

 

Inhibitors (usually lead to increased systemic concentration)

atazanavir

lopinavir

rifampicin

saquinavir

ciclosporin

probenecid

ritonavir

 

Organic Anion-Transporting Polypeptides (OATPs)

Substrates

Main drug classes predominantly transported by OATPs include:

Main Drugs

aciclovir

ciprofloxacin

furosemide

rosuvastatin

atorvastatin

fexofenadine

glibenclamide

simvastatin

bosentan

 

 

 

Inhibitors (usually lead to increased systemic concentrations)

atazanavir

gemfibrozil

probenecid

ritonavir

ciclosporin

lopinavir

rifampicin

saquinavir

Organic Cation Transporters (OCTs)

Substrates

Main drug classes predominantly transported by OCTs include:

Main Drugs

doxazosin

oxaliplatin

terazocin

varenicline

metformin

pramipexole

 

 

Inhibitors (usually lead to increased systemic concentrations)

cetirizine

cimetidine

 

 

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Topic Code: 93361