Exercise #9

Transport & Distribution

1. Explain plasma protein binding of drug molecules & state its clinical
significance.
Plasma protein binding of drug molecules is due to the presence of plasma protein
albumin in the blood. It is a reversible or temporary process which describes a drug’s
biologic activity in plasma. Each drugs experience different percentages of plasma protein
binding. 60% of drug molecules will be temporarily inactive but flow along circulation but
can’t interact with the organs. Moreover, the other 40% are active that will interact and
produce effect. There are 100 drug molecules in the circulation 30 minutes after
swallowing a tablet. 60 was plasma protein bound, 40 was active. If 90% of plasma
protein is binding, it will take longer time since there will only be 10% active molecules
that will interact with organ. Thus, plasma protein binding indicates the duration of
action of the drug.
Clinical significance
1. Absorption -more protein binding disturbs the absorption equilibrium
2. Distribution- protein binding decreases the distribution of drugs because it does
not cross the placental barrier and the glomerulus.
3. Metabolism- protein binding also decreases the metabolism of drugs but enhances
the biological half-life. Half life refers to the time needed by the body to eliminate
half the peak amount of the drug that is in the circulation.
4.
2. Enumerate & explain the various factors that contribute to the unequal
distribution of drugs in the body.
1. Plasma protein binding- affects transport in plasma where some drugs can
displace other drugs from their protein binding sites. Albumin is the major drug-
binding protein and may act as a drug reservoir, i.e., when the concentration of the
free drug decreases due to metabolism or excretion, the bound drug dissociates
from the protein. It maintains the equilibrium. Only free drug can distribute, binds
to receptors, metabolized, and excreted.
2. Cellular binding- it is where drug molecules exhibit a certain cellular affinity. It is
usually due to some affinity for a particular cell type or intracellular component.
Examples: tetracycline- hard tissues of the body, quinacrine- liver and skeletal
muscles
3. Blood brain barrier- it restricts passage of drugs into the CNS where the limiting
barrier made up of the brain is the capillary walls and glial cells. Examples:
penicillin- only during inflammation of the meninges, pentothal- can easily pass
through
 - Blood placental barrier- it is like blood brain barrier, but it is majority by simple
diffusion. They are also very lipid soluble that they can pass through the membrane
easily.

Source: