What are the 3 A's of pharmacokinetics?
What factors affect the time it takes for a drug to get to the target?
transfer across membranes
What factors affect the amount of time that a drug is available in the body?
excretion out of the cell
excretion from body (kidneys)
What does ADME stand for?
The rate of delivery and distribution of a drug is dependent on what 3 things?
regional blood flow
In what parts of the body is Phase 1 delivery slower?
In what parts of the body is Phase 1 delivery faster?
What factors affect phase II delivery?
binding to plasma proteins
rate of metabolism/elimination
What is the most common cause of Warfarin problems?
plasma protein binding
plasma proteins act as a reservoir of the drug
also the reason you may need a loading dose
Albumin is a?
What is an example of a drug that has a high rate of redistribution?
lipid soluble anesthetics
What regions of the body are hardest to treat with drugs? And why?
CNS, CSF, brain
because of BBB and tight junctions that are made to prevent toxins from getting in
reason why brain cancer is so hard to treat..
_____ soluble drugs are better at getting across biological membranes?
What are some examples of teratogenic drugs and why are they teratogenic?
because they are very lipid soluble, they can cross the placenta
T/F: Certain tissues have a higher affinity of drug uptake than others.
T/F: some drugs are eliminated completely unchanged.
true, but very few
When you add glucuronic acid to something during metabolism, it becomes more ____ soluble?
Which are more easily excreted- polar or nonpolar?
How can we make a lipid soluble drug more polar so that it can be more easily excreted?
Phase 1 metabolism
Phase 2 conjugation
: attach a water soluble molecule
What will enterohepatic recycling cause?
prolonged drug effects
--> oral contraceptives work this way
What is the primary mechanism of excretion?
(biliary or renal excretion)
Renal excretion decreases how much per year in adulthood?
What are the 3 mechanisms that can occur in the kidneys with respect to excretion? (different paths to be taken)
passive tubular reabsorption
How do we measure renal function?
GFR (glomerular filtration rate)
T/F: exogenous or endogenous substances that are freely filtered by the glomerulus can undergo tubular secretion and tubular reabsorption.
Which are expensive and time-sensitive compounds that are used to test GFR- exogenous or endogenous?
exogenous (like EDTA)
What is the ideal endogenous compound used to test GFR?
Name another endogenous marker used to determine GFR (besided SCr).
Which ROA is best for large volumes or for high MW drugs?
What are 2 disadvantages of IM injections?
they interfere with diagnostics
can't be used with anticoagulants
What is the safest ROA?
What is the fastest ROA?
What is the most risky ROA?
the ability of a drug to absorb water from the air is called ______?
What is a cocrystal?
helps control solubility
can be found in insulin products
fairly new area of product dev.
T/F: some drugs can have up to 20 polymorphs.
What drug had an unexpected polymorph spontaneously form and had to be removed from market?
How a molecule packs together in a crystal or more than one crystalline modifications is called ______?
What factors can cause the formation of a new polymorph?
presence of water
rate of cooling
method of filtering or drying
What drug was an example of having two different polymorphs, the anhydrous crystal and the hydrate?
triamcinolone (Kenalog inj)
Slides 1-61 for Quiz 1