absorption and distribution. ch 1 pg 15-24 Flashcards
the olive oil partition coefficient is used to express?
the lipid solubility of the drug
put drug into a mixture of half water half oil and see how much of the drug dissolves in each substance
drugs that are more highly lipid soluble will be more concentrated and which substance in the olive oil test?
the olive oil
why is it important to tell how lipid soluble a drug is?
measure the degree to which a drug will dissolve in fat tissue in the body
when a molecule carries an electrical charge (ion) it looses its ability to?
dissolve in lipids (unable to pass through membrane)
3 ways to determine the percentage of ionized molecules in a solution?
1) whether the drug is a weak acid or base
2) whether it is dissolved in an acid or a base
3) its pKa
what is the pKa of a drug?
the pH at which half its molecules are ionized
on the pH scale #s below 7 are? and #s above 7 are?
below= acid
above=base
what is the pH of the lining of the intestine?
3.5
morphine is a ? with a pH of?
base , 8
will morphine be absorbed by the digestive system?
no. because bases are highly ionized in solutions with low pH such as the intestine (3.5). ionized molecules cannot cross the membrane
caffeine is a base that has a pKa of 0.5 what does this say about its absorption in the body?
almost completely nonionized in the digestive system (can be absorbed)
if 97% of a drug is ionized in the digestive system, and only 3 % is lipid soluble, what will happen?
the 3 % will diffuse through the membrane and be removed by the blood and then a new 3% becomes non ionized and diffuses. the process continues until equilibrium is reached.
the percentage of ionization determines the ? of absorption.
rate
transdermal administration?
drug is absorbed through the skin
what is the main layer of skin that is a barrier to absorption?
epidermis (outer layer)
the epidermis is made of flattened cells densely packed with?
keratin?
characteristics of epidermis
impermeable to water
- can only be penetrated by lipid soluble substances
the drug is separated by the skin by a special membrane that controls the rate of absorption
- this is what kind of drug use?
a patch
highly lipid soluble drugs tend to concentrate where?
in body fat outside the CNS
why is it not good when drugs get absorbed by fat?
it keeps them there preventing them from reaching their SOA.
what can the pKa also influence?
why?
where a drug gets to in the body
–> anywhere int he body it can get trapped inside a membrane depending on its pH
drugs that are weak bases tend to ionize in? and drugs that are weak acids tend to ionize?
- acidic solutions
- basic solutions
a difference in pH across the membrane of 1.0 will cause a drug to be ? more concentrated on one side than the other
- and difference of 2.0?
10 x
100x
?is a result of special cells in the central nervous system that wrap themselves around the capillaries and block the pores through which substances normally diffuse
blood brain barrier