Pharmacokinetics & Pharmacodynamics Flashcards
what are the four parts to the phamacokinetic phase?
- absorption
- distribution
- metabolism
- excretion
What are the three parts to the pharmacodynamic phase?
- receptor binding
- postreceptor effects
- chemical reaction
Drug movement from GI tract into bloodstream
drug absorption
what does drug absorption require?
- -disintegration
- dissolution
breakdown of oral drug form into small particles
disintegration
process of combining small drug particles with liquid to form a solution
dissolution
enteral
by mouth
what are the different absorption methods?
- passive transport
- active transport
- pinocytosis
most drugs are taken by this route
enteral
resist disintegration in the gastric acid of the stomach, may be delayed in onset
EC Enteric Coated Drugs
Where are EC drugs absorbed at?
small intestine
what factors affect drug absorption?
- bloodflow, pain, stress, gastric pH
- food texture, fat content, temperature
- route of administration
less blood flow =
less absorption
shock, BP bottoms out =
decreased blood absorption
which route of administration has the fastest onset of action?
IV
Which route of administration is slower, dependent on blood flow area?
SubQ
Which route of administration has a slow onset and is unpredictable?
Oral
passive transport occurs through
- diffusion
- facilitated diffusion
drugs move across the cell membrane from an area of higher concentration to lower concentration
diffusion
relies on a carrier protein to move the drug from an area of higher concentration to lower
facilitated diffusion
which transport does not require energy?
passive
requires a carrier such as an enzyme or protein to move the drug against a concentration gradient
Active Transport
energy is required for which transport?
active
cell carries drug across membrane by engulfing drug particles
pinocytosis
after absorption of oral drugs from the GI tract, they pass from the intestinal lumen via what?
portal vein
what organ metabolizes drugs?
Liver
List drug movement in order starting with GI tract
- portal vein
- liver
- body
when the liver metabolizes a drug to an inactive form and is excreted, reducing the amount of active drug available to exert a pharmacologic effect
first pass affect or first pass metabolism
affected by the first past affect
bioavailability
% of administered medication that reaches systemic circulation (amount of drug actually available for use)
bioavailability
factors that affect bioavailability
- absorption
- first pass metabolism
- drug form
- route
- gastric mucosa and motility
- administration with food and other drugs
- changes in liver metabolism
decreasing liver function increases what?
bioavailability
movement of drug from circulation to body tissues
drug distribution
what are the influencing factors of drug distribution?
- protein binding
- free drugs
- blood brain barrier
as drugs are distributed in the plasma, many bind with
plasma proteins
list the different plasma proteins
- albumin
- lipoproteins
- Alpha-h acid-glycoprotein
what happens if a drug binds to protein?
it doesn’t work
the portion of the drug bound to protein is inactive because
it is not able to interact with tissue receptors and is unable to exert a pharmacologic effect
portion of drug that is not bound to protein and is free
free drug
able to exit blood vessels and reach site of action causing a pharmacologic response
free drug
blood vessels of the brain made of special endothelial lining where the cells are pressed tightly together and protects the brain from foreign substances
blood brain barrier
what drugs are able to cross the blood brain barrier?
drugs that are highly lipid soluble and of low molecular weight such as benzo’s
can drugs cross the placenta?
yes
drug metabolism is also known as
biotransformation
process of body chemically changing drug into form that can be excreted
drug metabolism
if the liver function is decreased, what happens to the drug effects?
increases
biologically inactive compound which is metabolized into the body and to produce a drug
prodrug
used to improve drug delivery, decrease toxicity or to target specific cells or tissues
prodrug
example of prodrug
codeine
why is codeine and example of a prodrug?
- little activation of opioid receptors as codeine
- metabolized into morphine by liver
- morphine activates opioid receptors
period of time required for concentration or amount of drug in body to be reduce by one-half
half life
affected by metabolism and elimination
half life
used to determine dosing interval
half life