Pharma 1.1: Quantite Absorbe Flashcards
What are the two main type of active transporters?
ATP-binding cassette (ABC) vs solute
carrier (SLC)
Efflux vs influx
Efflux -> Leaves the cell
influx-> enters the cell
In general, what type of transporters are ABC transporters
They are eflux transporters. This means that the that they are taking medication outside of the cells
In general what type of transporters are slc transporters
They can be both E flux and influx transporters
What happens to the pharmacosynetics if you block the eflux transporters of the apical membrane?
If we are blocking the E flux transporters on the Abaco membrane, that means that there will be a lot more medication that will be absorbed. As a result your cmax will increase and your auc will increase.
Would the elimination rate change if you blocked eflux transporters on the basal lateral side?
Know the rate of elimination is not dependent on the absorption transports
This is because this situation is not varying the K A or the K E L
With the T Max change with a change in the absorption transporters by blocking the influx absorbers in the apical side?
No the tmax remains the same
This is because this situation is not varying the K A or the K E L
What effect does calcium have on absorption?
An intake in calcium will block the Oatp transporters which are the influx transporters leading to a decrease cmax decrease area under the curve less effect
Name four factors that influence the quantity of medication absorbed
The intestinal ph
The interactions with food or other medication
Variation in the expression of the active transporters [eflux, influx]
A variation of metabolism
Name four factors that can influence the activity of the active transporters on the intestinal wall
Natural products (food; grapefruit)
Medication interactions
Genetics
Different pathologies
Describe the effect of grapefruit on pharmacosynetics
Taking great fruit with medication inhibits the eflux receptors on the apical side of the intestinal wall or the intereocytes for example the mdr 1 P dash glycoprotein receptor. As such grapefruit increases the amount of medication absorbed, which increases the C Max increases the area under the curve and as a result also increases the therapeutic effect.
What is the effect of taking grapefruit with a medication that is administered intravenously?
There is no effect because intravenous taken medication goes directly into the bloodstream and does not have to be absorbed by the intestine null tract. As such the effect on the eflux transporters is irrelevant when the medication aid is administered intravenously
What is MDR1?
Efflux PGP active transport on the appical side of the enterocyte
