Week 1 Flashcards
Pharmacokinetics
study of drug movement throughout the body
ADME
Absorption
Movement of drug from site of administration into the systemic circulation
Factors Affecting Drug Absorption
Rate of dissolution Surface area Blood flow Lipid solubility pH partitioning
Distribution
Movement of drugs from blood to site of action
Drug distribution is determined by what factors
Blood flow to tissues
Exiting the vascular system
Entering cells
Exiting the vascular system
Typical capillary beds
- pass through them
Blood-brain barrier
Capillaries of the central nervous system have tight junctions that prevent free diffusion
Blood brain barrier
Only drugs that are lipid soluble or that have a transport system can cross the blood-brain barrier to a significant degree
Placental Drug Transfer
Membranes of the placenta do NOT constitute an absolute barrier to the passage of drugs
Protein Binding
Drugs can form reversible bonds with various proteins
Plasma albumin is the most abundant and important protein
Entering Cells
Some drugs must enter cells to reach the site of action
Most drugs must enter cells to undergo metabolism and excretion
Many drugs produce their effects by binding with receptors on the external surface of the cell membrane
Bioavailability
Amount of active drug that reaches the systemic circulation from its site of administration
drug metabolism
aka biotransformation
drub metabolism
Defined as the enzymatic alteration of drug structure
most often takes place in liver
1st pass effect
Drugs are absorbed
enter hepatic circulation
liver metabolizes drug to inactive form
inactive drug leaves liver and enters general circulation
P450 system
Hepatic metabolism takes place by hepatic microsomal enzyme system
I Drugs can be P450 substrates, inducers, or inhibitors