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PCEUT 510 > DDI-Transporters > Flashcards

DDI-Transporters Flashcards

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1
Q

Membrane transporters/carriers are located where?

A
  1. Epithelial barrier

2. Endothelial barrier

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2
Q

Why are transporters important?

A

They play a significant role in drug:

  1. absorption
  2. distribution
  3. excretion
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3
Q

Active Solute Transport
Biochemical Characteristics:
1.
2.

A
  1. Move solute against a concentration gradient

2. REQUIES energy

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4
Q

Active Solute Transport
Classification based on driving force mechanism
1.
2.

A
  1. Primary active transporters = generate energy themselves (ATP hydrolysis)
  2. Secondary active transporters = utilize energy stored in voltage and ion gradients generated by a primary active transporter (NA+/K+ ATPase)
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5
Q

Digoxin and _________ was the original transporter-related DDI

A

quinidine

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6
Q

There are two types of secondary active transporters

A
  1. Symporters (Co-transporters)

2. Antiporters ( Exchangers)

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7
Q

A [primary/secondary] active transporter utilizes energy stored in gradients

A

Secondary

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8
Q

A [primary/secondary] active transporter utilizes energy from ATP hydrolysis

A

Primary

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9
Q

These secondary active transporters are also known as co-transporters

A

Symporters

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10
Q

These secondary active transporters are also known as antiporters

A

Exchangers

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11
Q

Pgp, MRPs and BCRP are all part of the ________ superfamily of transporters

A

ATP-Binding Cassette (ABC)

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12
Q

OATP, OCT & MATEs are part of the ________ superfamily of transporters

A

SoLute Carrier (SLC)

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13
Q

This transporter is also known as MDR1

A

Pgp

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14
Q

Pgp mediates the transport of [lipo/hydro]philic [an/cat]ionic drugs?

A

Lipophilic Cationic drugs

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15
Q

Steroids and other cyclic peptides are [acidic/basic/neutral] drugs with ________ ring structures, mediated by_______

A

NEUTRAL rings with BULKY ring structures

Pgp mediated

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16
Q

What 4 tissues is Pgp expressed in?

A
  1. intestine
  2. kidneys
  3. liver
  4. BBB
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17
Q

Pgp has two actions on xenobiotics

A
  1. Guard against entry

2. Promote excretion

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18
Q

Pgp is located on the [Apical/Basolateral] membrane of INTESTINAL mucosal epithelium?

A

APICAL

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19
Q

Pgp is located on the [Apical/Basolateral] membrane of proximal tubular epithelium of KIDNEYS?

A

APICAL

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20
Q

Pgp is located on the [Apical/Basolateral] membrane of hepatocytes in the LIVER?

A

APICAL(canalicular)

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21
Q

Pgp is located on the [Apical/Basolateral] membrane of brain capillary endothelium BBB

A

APICAL

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22
Q

What is the purpose of Pgp in the INTESTINE?

A

DECREASES net absorption due to exsorption and/or secretion

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23
Q

What is the purpose of Pgp in the KIDNEY?

A

FACILITATES renal secretion

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24
Q

What is the purpose of Pgp in the LIVER?

A

FACILITATES biliary secretion

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25
What is the purpose of Pgp in the BBB?
PREVENTS drug entry into the brain
26
T/F | Pgp facilitates biliary secretion
True
27
T/F | Pgp both increases renal secretion AND protects the brain/fetus from drug entry
True
28
INHIBITION of INTESTINE Pgp leads to [increase/decrease] of bioavailability?
INCREASE 1. Digoxin-Clarithromycin 2. Digoxin-Itraconazole 3. Digoxin-atorvastatin
29
INDUCTION of INTESTINE Pgp leads to [increase/decrease] of bioavailability?
DECREASE 1. Digoxin-rifampin 2. Digoxin-St. Johns wort
30
Adding clarithromycin to digoxin [increased/decreased] digoxin AUC by 64%
Increased
31
Modulation of biliary clearance due Digoxin + quinidine will [induce/inhibit] Pgp transport?
INHIBIT
32
Modulation of biliary clearance due to Digoxin + Rifampin will [induce/inhibit] Pgp transport?
INDUCE
33
Pgp mediated transport in the Kidney of Digoxin will have [decreased/increased] renal drug clearance when inhibiting agents are used?
``` DECREASED Remember: Inhibitors; quinidine verapamil cyclosporine itraconazole cyclosporine ```
34
Brain uptake will [increase/decrease] when loperamide + quinidine are used together due to [inhibition/induction]?
INCREASE | INHIBITION
35
__________ in Pgp expression and function in different tissues makes it difficult to predict the outcomes of Pgp based DDIs
Multiplicity
36
``` All of the following are examples of Multiplicity in Pgp based inhibitory interactions with Digoxin EXCEPT? A. quinidine B. Clarithromycin C. Rifampin D. Talinolol ```
C is incorrect Rifampin is an inducer and not one of the examples given (Ritonavir is the other inhibitor example provided)
37
This drug inhibits intestinal Pgp and increases digoxin F, but does not affect systemic clearance of digoxin
Talinolol
38
This Pgp inhibitor didn't have an effect on renal or biliary inhibition
Talinolol
39
This drug increased digoxin AUC and Cmax 1 hour after administration, but lowered it 1 week after administration
Rifampin
40
Rifampin [increased/decreased] digoxin AUC and Cmax 1 hour after administration, but [increased/decreased] it 1 week after administration
INCREASED | DECREASED
41
The increasing then decreasing effects of Cmax and AUC of Rifampin on Digoxin over a 2 week period are an example of what type of interaction?
Biphasic | Rifampin has both Inhibition and induction effects on Pgp transports
42
Most statins prefer this OATP in the liver
OATP1B1
43
These two statins are up taken by all three OATP (1B1, 1B3,2B1) liver proteins
Fluvastatin | Pravastatin
44
This immunosuppressant is a major OATP inhibitor
Cyclosporine
45
This antibiotic is a major OATP inhibitor
Rifampin
46
Other than Pgp, cyclosporine and rifampin notably inhibit this family of transporters
OATP
47
Interactions between first generation statins and this drug were recognized to result in severe myotoxicity of statins including rhabdomyolysis
Cyclosporine
48
This is the most dangerous potential occurrence from the cyclosporine/first gen statin DDI
rhabdomyolysis
49
Newer statins are more [lipophilic/hydrophilic] and older statins are more [lipophilic/hydrophilic]
``` Newer = hydrophilic Older = lipophilic ```
50
[Gut Pgp/Hepatic OATP] induction sustained over 24+ hours, while the other dissipated by 12.5 hours in the repaglinide/rifampin interaction
Gut Pgp
51
The repaglinide/rifampin interaction showed that induction of 2C8 and 3A4 emerged by __________
24 hours
52
[GI/Hepatic/Renal] DDIs are the least common
Renal
53
There's a ~__x limit in magnitude of renal interaction because only the secretory component is affected
2
54
There's a ~2x limit in magnitude of renal interaction because only the _________ component is affected
Secretory
55
Renal DDI occurs only for drugs that: 1) Are mainly cleared by the kidneys 2) Undergo extensive active secretion (____ > _______) or active tubular reabsorption
CLr > fu*GFR
56
Renal DDI occurs only for drugs that: 1) Are mainly cleared by the kidneys 2) Undergo extensive active _________ (CLr > fu*GFR) or active tubular ____________
Secretion | Reabsorption
57
Organic anion Transporters in the Kidney include?
OAT | MRP
58
Organic Cation Transports in the Kidney include?
OCT2 | MATEs
59
OCT2 transporters are on the [APICAL/BASOLATERAL] side?
BASOLATERAL
60
MATEs transporters are on the [APICAL/BASOLATERAL] side?
APICAL
61
What was the effect on AUC of Metformin + Cimetidine?
``` AUC = increased CLr = Decreased ```
62
Cimetidine inhibits which transporter?
MATE
63
Who is the perpetrator in the metformin + cimetidine DDI?
Cimetidine
64
Methotrexate DDI involve which transport? | [Pgp/MRP/BCRP]
BCRP
65
Who is the precipitating agent involved in the BCRP transporter and Methotrexate?
PPI: Omeprazole Pantoprazole
66
What is the overall effect of Methotrexate ABC Transporter DDI?
Delayed elimination = toxicities
67
What is the overall effect of DDIs between Li + Thiazide diuretics?
Increased renal absorption = enhanced lithium retention

PCEUT 510 (12 decks)

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