Drug Absorption #2 Flashcards
T/F Passive diffusion is uni-directional
FALSE: can move in either direction (the concentration gradient determines which direction the molecule moves)
What are the 2 routes in which blood can diffuse?
intracellular(transcellular)
-paracellular
intracellular transport
molecules move directly through the membrane
-this is the most common
paracellular transport
molecules move between cells
-has a limiting factor (size of the molecules)
What is the limiting factor of paracellular transport?
the size of the molecule
T/F Carriers are typically proteins
TRUE
What are the 2 types of carrier mediated transport?
- facilitated
- active
Carrier Mediated Transport (2)
- are specific (only move one type of molecule)
- typically located in specific areas of the GI tract
T/F Carriers CAN NOT be saturated
FALSE; there are only a certain number of carriers, which means they can be saturated
T/F Carriers can be inhibited
TRUE
T/F Carrier transport is one direction
TRUE (mucosal side –> to the blood)
Which transport system requires ATP energy?why?
Active transport b/c it can occur from a region of lower concentration to higher concentration
metabolism
chemical altering of the drug molecule by the body
What is the effect of metabolites on bioavailability?
although metabolites are inactive–> they decrease bioavailbility because there would be a reduced amount of drug that would get to the site of action
efflux transporters (2)
- going in the opposite direction than what we would like
- typically P glycoproteins
P glycoproteins (3)
- energy driven
- pump the drug back in the direction in which it came from
- not as specific as carrier proteins
_____ are thought to cause tolerance to cancer therapeutic agents
P glycoproteins
What would be the effect of P glycoproteins on the bioavailability of the drug?
it would DECREASE the bioavailability because its taking the drug molecules in the opposite direction than we want them to go–> not allowing them to ultimately get to the site of action
What part of the stomach is where most secretion occurs?
the middle of the stomach
Antrum
holds material in the stomach to control how it moves to the pylorus
T/F The stomach is very muscular
TRUE
What are the functions of the stomach? (4)
- reservoir
- site of the beginning of digestion
- regulate the delivery of nutrients
- bacteriostatic
The secretion of ____ typically destroys the bacteria that make it to the stomach
HCl
What are the secretion cells in the stomach? (4)
- mucoid cells
- chief cells
- parietal cells
- g cells
mucoid cells
secrete mucus
mucus provides ____ and ____ protection
chemical and physical
chief cells
secrete pepsinogen (gets converted to pepsin)
____ begins the digestion process in the stomach
pepsin
parietal cells
secrete primarily HCl and intrinsic factors
intrinsic factors are necessary for…
absorption of B12
G cells
secrete gastrin (which in turn controls the secretion of HCl)
About ___L/day of fluids are secreted by the stomach
3
Would you anticipate significant absorption from the stomach? Why?
- no, almost no drug is absorbed by the stomach
- drugs do not stay in the stomach long enough and the stomach has a small surface area
Where is the site of most absorption of drug?
small intestine due to the large membrane surface area
What is the pH of the stomach? with food?
~ 1-2
food neutralizes the stomach–> pH goes up to around 4,5, or 6
What are the 3 segments of the small intestine?
- duodenum: connected to the pylorus (upper)
- jejunum (middle)
- illeum (lower)
T/F Each segment of the small intestine have regional differences
TRUE. transporter proteins are located at specific sites in the intestine