Chapter 3 Flashcards
Once a drug is administered, what two phases occur?
Pharmacokinetic phase
Pharmacodynamic phase
What is a pharmacokinetic phase?
What the body does to the drug, describes movement of the drug through the body
What are the 4 steps in pharmacokinetic ?
Absorption
Distribution
Metabolism
Excretion
What does pharmacodynamic phase mean?
What the drug does to the body, involves receptor binding, postreceptor effects and chemical reactions
What does drug absorption mean?
The movement of the drug into the bloodstream after administration
What does dissolution mean?
Disintegrate the tablet or drug with a combination of liquid
What does excipients mean?
Items like honey, syrup that are used in a drug to help it dissolve more
There are some drugs like enteric coated that have resist disintegration in the gastric acid of the stomach
So instead, disintegration doesn’t happen until when?
It reaches a more alkaline environment like the small intestine
Most oral drugs enter the bloodstream after absorption across the mucosal lining of the small intestine.
What is this small intestine epithelial lining covered in? And what is its job?
Villi
Increased surface area for absorption
How does absorption occur in the muscosal lining of the small intestine? (3)
Passive transport
Active transport
Pinocytosis
passive transport happens in two processes name them and what they do?
Diffusion
- drugs move from high to low concentration
Facilitated diffusion
- carriers protein move from high to low
Does passive transport need energy?
No
What is active transport ?
Enzyme or protein move the drug against concentration gradient
Does active transport need energy for active absorption?
Yes
What is pinocytosis?
Process by which cells carry a drug across their membranes by engulfing the drug particles in a vesicle
What is first pass effect or first pass metabolism?
Where the liver metabolizes a drug into an inactive state and then are excreted out, reducing the effect
How is the absorption of oral drugs work?
Oral -> GI -> intestine -> liver
What is bioavailability mean?
Percentage of administered drug available for activity
What does distribution mean?
Movement of the drug from the circulation into the body tissue
What are some things drug distribution is influenced by?
Vascular permeability
Blood flow
PH
Cardiac output
Tissue perfusion
What does highly protein bound drugs mean?
Example?
Drugs that are more than 90% going to bind with a protein
Warfarin
What does weakly protein bound drugs mean?
Example?
Drugs less than 10% bound to a protein
Metformin
The portion of the drug that binds with the protein is inactive, meaning ?
It is not available to interact with tissue receptors, ultimately not being able to exert a pharmacologic effect
The portion of the drug that doesn’t bind with the protein is known as ?
Free drugs
Since free drugs are not bound to a protein, they do what?
Are able to exit the blood vessel, reach site of action and cause a pharmacologic response
What is a blood brain barrier ?
Blood vessels in the brain that are pressed together and protects the brain from forgein substances
What does metabolism mean?
Process by which the body chemically changes drugs into a form that can be excreted
What is the primary site of metabolism?
Liver
If it takes 5 mins for a drug to be absorbed how long should it take?
Really fast! 5mins probably !
What is the fastest and slowest form of drug to get in the body?
IV
Oral
We want to be careful with giving 2 protein bound together because?
They will compete for protein sites and potentially have too much active drug circulating ( toxic )
What can cross the blood brain barrier?
Lipid soluble drug