ADT Exam 1

Multi-drug resistance phenotype in tumors is associated with

over expression of certain ABC transporters (MDR proteins)
MDR1 Structure
- amino and carboxy terminal are intracellular
- 12 trans membrane
- 2 ABC binding domains
MRP1 structure
- 17 transmembrane
- amino terminus is extracellular
- carboxy terminus is intracellular
- 2 ABC binding domains
ABCG2 (MXR/BCRP) receptor
- Amino and carboxy terminus are intracelluar
- 6 transmembrane
Efflux transporters located on the basolateral side of the intestine
- MRP 1, 3, 4, 5 & 6
- efflux drugs from cells to blood
Efflux transporters located on the apical side of the intestinal lumen
- BCRP
- MDR1
- MRP2
- MRP4
- push drugs back into the intestines
PGP mediated drug efflux

activation of efflux pump by hydrolysis of ATP drives cytotoxic molecules out of the cell
can be used to inhibit PGP and increase doxorubicin

PSC 833
CYP3A4 inducers
- carbamazepine
- rifampin
- ritonavir
- st. john's wort
CYP3A4 inhibitors

Ritonavir
Tipranavir/ritonavir

statsistically superior to CPI/ritonivir
efavirenz and nevirapine ____ kaletra levels

decrease
rescro[tpr (de;avordome) will ____ kaletra levels

increase
St. John's wort ____ serum concentrations of many drugs by ___.
- decreases
- induces PGP and CYP3A4
SJW and narcotic induced sleeping time

increased
SJW and reserpine

SJW antagonizes effects
Herbal constituents will exhibit _____ of PGP and cyp initially then ___.
- inhibition
- induction

Author

Rx2013

107950

Card Set

ADT Exam 1

Description

MRP

Updated

2011-10-11T02:35:25Z