Review Flashcards
P-glycoprotein
Efflux transporter
ABC
Efflux transporter (Active Transport)
- Found on apical membrane
- Found along Brush Border Membrane
SLC
Influx transporters (Facilitated Transport)
- Found along basolateral membrane (faces blood)
- Found along Sinusoidal Space
Ex. OAT, GLUT, SGLT2
Transporters
- Highest concentration in liver and kidney
Tumour cells have increased P-gp resulting increased efflux of drugs
- Need to inhibit P-gp to have drug effect
Total Clearance
Renal Liver and Other
Rate of elimination
Rate of renal elimination + Rate of liver metabolism + other
Cheapatic
Hepatic Clearance
Clint
Clearance of both bound and unbound drug
Clint’
Clearance of unbound drug
Order of Vd
In multi-compartment model
Vbeta > Vss > Vc > Vplasma
What body organ has the highest perfusion rate
Kidneys
- Liver, Heart, Brain
What body organ has the lowest perfusion rate
Bone, Muscle, Skin
Intrinsic Tissue Permeabulity
Dependent on physiochemical properties
- LogP
- Molecular size
- Pka
How to monitor renal clearance
Creatinine Clearance
How to monitor hepatic clearance
Liver Function Tests
How to know if drug is High E or Low E
CLhepatic / Qhepatic
Non-Linear Kinetics
- Vmax
Affected by inhibitors and inducers
Non-competitive
Non-Linear Kinetics
- Km
Affected by displacement
Competitive