Drug Absorption LO Flashcards
Lecture 2 Svensson
Name the factors that determine drug absorption across a membrane
- Characteristics of the membrane
- mechanisms of passage across membrane
- dwell time of drug-membrane interface
- physicochemical characteristics of the drug
- pH of the microenvironment
- surface of absorption surface
Identify the site in the GI tract where most drug absorption occurs
DA happens most in the small intestine because it has folds of kerckring. The folds greatly increase the surface area for drug absorption. Transit time is 3-5 hours.
Describe the mechanisms by which drugs cross biological membranes
Facilitated diffusion & active transport are both examples of carrier-mediated transport. About 95% of drugs are predominantly absorbed by passive transcellular diffusion. Passive transcellular diffusion can be increased by removing charged (ionized) groups, increasing lipophilicity, reducing size
Differentiate the two forms of carrier-mediated absorption: facilitated diffusion and active transport
Facilitated diffusion is a type of passive transport that moves molecules or ions across a cell membrane with the help of specific proteins.
Active transport is an energy driven process where membrane proteins transport molecules across cell.
Describe the impact of efflux transporter on drug absorption from the small intestine.
Efflux transporter is called the p-glycoprotein. 1. Limited drug absorption 2. Enhanced drug elimination 3. Limited drug distribution
Identify the mechanism by which nanoparticles cross biological membranes.
Endocytosis is the process that helps larger particles.