What is the first-pass effect?
When a drug is metabolized in the liver before it reaches systemic circulation.
The first pass effect happens with what kind of drugs?
Oral
Explain the process of the first pass effect (where it starts and eventually ends up)
Mouth
Stomach
Small Intestine
Portal vein
Liver
Systemic Circulation
What does the first pass effect reduce?
Bioavailability
What are 2 things that drugs with the first pass effect may need?
Higher oral doses
Non-oral routes like IV, sublingual, transdermal
Where to protein bound drugs bind to?
Plasma proteins, mainly albumin
______ is a highly protein bound drug
Warfarin
If another drug displaces a warfarin, what is there a risk for?
Bleeding
Should 2 highly protein-bound drugs be given together?
No
_____ activates receptors, producing a biological response and mimicking the body’s natural responses
Agonists
_______ binds to receptors, but does not activate them, blocking the agonist’s actions
Antagonists
What do partial agonists do?
Activates the receptor, but has a weaker effect
What do competitive antagonists do?
competes for same receptor site, as an agonist, but doesn’t turn on the receptor
A _________ happens when one drug changes the effect of another drug.
drug interaction
What are the pharmacokinetic interactions?
Absorption
Distribution
Metabolism
Excretion
If Drug A prevents absorption, what happens to drug B
It’s effectiveness is reduced
What liver enzymes are involved in metabolism of drug interactions?
CYP450
If Drug A and B are administered at the same time, but Drug A induces the metabolism of Drug B, what needs to be done?
Drug B amount needs to be increased
If Drug A and B are administered at the same time, but Drug A inhibits the metabolism of Drug B, what needs to be done?
Drug B amount needs to be decreased