Drug Transporters Flashcards
(12 cards)
1
Q
What is an example of an efflux transporter?
A
P-gp (P-glycoprotein)
2
Q
What is an example of an uptake transporter?
A
OATP (organic anion transporting protein)
OR
PEPT1 (peptide transporter 1)
3
Q
What are the qualities of P-glycoprotein?
A
- Efflux transporter affecting permeability of drugs
- Expression of P-glycoprotein leads to resistance of certain drugs
- Also, called MDR1 (multi-drug resistance 1)
- P-gp pumps drugs in the direction of eliminating them from the body
- Inhibition of P-gp in cancer cell is expected to improve anticancer drug efficacy by increasing intracellular drug concentrations
4
Q
What are the anti-HIV P-gp agents?
A
Lopinavir
Ritonavir
Saquinavir
Eleprevir
Tiprinavir
5
Q
What are the anti-infective P-gp agents?
A
Clarithromycin
Itraconazole
6
Q
What are the cardiovascular P-gp agents?
A
Amiodarone
Carvidolol
Quinidine
Propafenone
Verapamil
7
Q
A
7
Q
What is PEPT1 (peptide transporter 1)?
A
- A peptide transporter in the small intestine
- Uptake transporter
- Substrates (Dipeptides, Beta-lactam antibiotics)
- PEPT1 can be utilized to improve abs of drugs (Acyclovir, Valacyclovir)
Valacyclovir is a prodrug, allowing it complete absorption
8
Q
What are the anticancer agents?
A
- Paclitaxel
- Topotecan
- Etoposide
9
Q
What are the anti-HIV agents?
A
- Indinavir
- Ritonavir
- Saquinavir
10
Q
What are the lipid-lowering agents?
A
- Lovastatin
- Atorvastatin
11
Q
What is an example of an opioid?
A
Loperamide
