Flashcards in Pharm Exam 1 Deck (45)
1 potent inhibitor of OAT?
* Why is it given w/cidefovir? (explain)
- Given w/cidefovir to protect from otherwise severe renal toxicity by blocking uptake into the proximal tubules (from the blood)
3 Drugs transported by OAT?
1 drug class transported by OATP?
1 potent inhibitor of OATP?
* If given w/statins, where would it inhibit the uptake of statins and what would this cause?
- Inhibits statin uptake from blood to liver, increasing toxicity risk and decrease statin efficacy
4 Drugs transported by OCT?
Ci-Ci, pro met
2 Drugs transported by P-gp/MDR-1?
1 potent inhibitor of P-gp/MDR-1?
St. John's Wort and rifampin induce which transporter protein type?
1 drug class transported by BCRP?
3 endogenous substrates of MRP?
What drugs induce expression of CYP450 enzymes?
Phen-Phen rifles St. John’s glowing pink cars.
- St. John's wort
What drugs inhibit expression of CYP450 enzymes?
Eric’s red grape kept its clear fluid
- Grapefruit juice (enterocytes, NOT liver)
E.g. of drug class that may compete for protein binding and increase the unbound fraction of other drugs?
2 drugs eliminated by zero-order kinetics?
3 types of rxns involved in phase I rxns?
- Oxidation (CYP450)
3 most common CYP450 enzyme subfamilies?
What classes of biochemical binding-site interactions are irreversible inhibitors of CYP3A4? (1). Reversible? (2)
- REVERSIBLE: Competitive or allosteric
- IRREVERSIBLE: Suicide inhibitor (covalent binding)
Is gray baby syndrome related to phase 1 or 2 enzymes? (Excess or deficiency?)
- What drug leads to it?
- Phase 2 deficiency
(results in circulatory collapse and cyanosis)
Chemicals in cigarette smoke, charbroiled food and cruciferous vegetables all induce CYP___.
Chronic alcohol induces expression of CYP___
Substrate specificity for OAT?
Broad range of low MW substrates
Substrate specificity for OATP?
Broad range of substrates; Amphipathic Anions, MW > 350 Da
Most drug interactions mediated by OCT/MATE are caused by what drug?
- How? (what organ)
- Prevents renal elimination of other OCT-dependent drugs
What 2 channels does cyclosporin inhibit?
OATP and P-gp/MDR-1
What 2 channels transport statins?
- OATP (influx)
- BCRP (efflux)
What drug is given w/cisplatin to avoid nephrotoxicity?
Substrate specificity for P-gp/MDR-1?
- Broad substrate specificity, typically bulky hydrophobic structures with neutral/positive charge
Would tumor cells upregulate or downregulate p-gp/MDR-1? Why?
Tumor cells often upregulate expression of P-gp/MDR1 to promote efflux of anti-cancer drugs
Of the transporters mentioned, which one is not present at the apical gut lumen?