TOPIC 2 Flashcards
What are the pharmacokinetic phases?
absorption
distribution
metabolism
excretion
absorption
movement of the drug from the GI tract into the bloodstream after administration
distribution
movement of drugs from circulation into body tissues
metabolism (biotransformation)
body chemically changes drugs to a form that can be excreted
excretion
elimination of drugs from the body
disintegration
breakdown of oral drug into small particles
dissolution
process of combining small drug particles with liquid to form a solution
What are the two components of passive transport?
diffusion and facilitated transport
diffusion
drugs movement across cell membrane from high to low concentration
facilitated transport
relies on a carrier protein to move drug from high to low concentration
active transport
REQUIRES ENERGY (ATP) and carrier substance (enzyme)
pinocytosis
cell carries drug across membrane by engulfing drug particles
What are the factors that affect absorption?
blood circulation
pain, stress
food texture, fat content, temperature
pH
route of administration
How do drugs move from the GI tract to the liver?
via the hepatic portal vein
What is the first pass effect?
After oral administration, many drugs are absorbed intact from the small intestine and transported first via the portal system to the liver, where they undergo extensive metabolism, therefore usually decreasing the bioavailability of certain oral medications.
bioavailability
percent of administered drug available for activity
what reaches systemic circulation (blood stream)
Which has more bioavailability, oral route or IV?
oral route will have less bioavailability because it passes through the liver
IV administration bypasses the liver
What are factors that affect bioavailability?
drug form
route of administration
gastric mucosa and motility
administration with food and other drugs
changes in liver metabolism
What happens when 2 highly protein bound drugs are administer together?
the drugs will compete for protein binding sites and this will lead to an increase in the free drugs of the drug that had the lower percent of protein binding
free drugs
can exit blood vessels and reach their site of action causing pharmacological response
(too high of free drug accumulation can cause side effects, adverse effects, or toxicity)
What are the requirements of a drug to pass the blood brain barrier?
high lipid soluble
low molecular weight
and can pass with a transport protein
half life (t1/2)
time it takes for the amount of drug in the body to be reduced by half
loading dose
a large initial dose given to achieve a rapid minimum effective concentration in the plasma
therapeutic effects can be obtained while steady state is reached
Where is the primary site of metabolism?
liver
What lab test help determine if liver function is good?
aspirate transaminase (AST)
alanine aminotransferase (ALT)
alkaline phosphate (ALP)
Where is the main site of excretion?
kidneys
What helps determine kidney function?
creatinine clearance
BUN
GFR
Where can drugs be excreted?
kidneys (mainly)
liver (bile)
feces
lungs
saliva, sweat, breast milk
What can protein binding be affected by?
competition for protein binding sites
low plasma protein levels
What affects drug distribution?
blood flow to tissues
ability of drug to enter the cell
ability of drug to exit blood vessels
What are the 3 excretion processes? Explain each.
glomerular filtration: moving the drug from the blood to urine
passive reabsorption: lipid soluble drugs move back to blood
active transport: “pumps” for organic acid and base to move drugs from blood to urine
When the liver eliminates bile, in what form is it excreted?
excreted in feces