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Low albumin = more free drug (bc the
How does hypoalbuminemia affect the
drug can't bind to albumin aka protein) =
process of prescribing?
increased adverse effects
is considered a contraindication to ad-
What is a Black Box Warning:
minister that drug.
Half-life specifically means the amount of
What is the drugs half-life? time it takes for an administered drug to
be halfway cleared from the system.
the time between drug administration
Peak of action: and maximum concentration of drug in
the blood stream. Best therapeutic effect.
the time between onset of action and
metabolism of drug below the minimum
Duration of action:
needed for an effect. The length of time
you have the drug in your system.
According to the WHO what is the first The first step is to define the patient's
step in the prescribing process? problem
The second step is to specify the therapeutic objective
choose which drug or treatment is need-
The third step is to
ed.
Step 4 of the WHO approach: Start the treatment
Step 5 of the WHO approach: Educate the patient
Step 6 of the WHO approach: Monitor the treatment
Phase 1 of drug development: The drug is tested on healthy volunteers
trials with people who have the disease
Phase 2 of drug development: for which the drug is thought to be effec-
tive
Large numbers of patients in medical re-
search centers receive the drug in phase
Phase 3 of drug development: 3. This larger sampling provides infor-
mation about infrequent or rare adverse
effects. The FFA will approve a new drug
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application if phase 3 studies are satis-
factory.
This phase is voluntary and involves
postmarket surveillance of the drug's
therapeutic effects at the completion of
phase 3. The pharmaceutical company
receives reports from doctors and other
Phase 4 of drug development: health care professionals about the ther-
apeutic results and adverse effects of the
drug. Some medications, for example,
have been found to be toxic and have
been removed from the market after their
initial release.
much of the drug is lost in the absorp-
tion process. The liver metabolizes many
Explain first pass metabolism
drugs, thus reduces the bioavailabilty of
the drug.
The fastest route of absorption is inhala-
What is the fasted route of absorption: tion, and not as mistakenly considered
the IV administration.
The GI tract is lined with epithelial cells;
Why does the GI tract take longer to drugs must permeate through these cells
absorb? in order to be absorbed into the circula-
tory system.
the cell membrane. Cell membranes are
essentially lipid bilayers which form a
semipermeable membrane. Pure lipid
What is One particular cellular barrier
bilayers are generally permeable only
that may prevent absorption of a given
to small and uncharged solutes, hence
drug?
whether or not a molecule is ionized will
affect its absorption, since ionic mole-
cules are charged.
Solubility favors charged species, per-
What is solubility? meability favors neutral species. Some
molecules have special exchange pro-
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teins and channels to facilitate move-
ment from the lumen into the circulation.
Absorption occurs at a slower rate be-
Why does absorption occur at a slower cause the complex membrane systems
rate for oral, IM, SQ routes? of GI mucosal layers, muscle, and skin
delay drug passage.
whether the drug is water or lipid (fat)
soluble. Lipid-soluble drugs easily cross
The ability of a drug to cross a cell mem- through cell membranes; water-soluble
brane depends on: drugs can't. Lipid-soluble drugs can also
cross the blood-brain barrier and enter
the brain.
proteins such as the plasma protein albu-
min. The drug can remain free or bind to
the protein. The portion of a drug that's
bound to a protein is inactive and can't
As a drug travels through the body, it
exert a therapeutic effect. Only the free,
comes in contact with?
or unbound, portion remains active. A
drug is said to be highly protein-bound if
more than 80% of the drug is bound to
protein.
CYPs are the are the major enzymes
Identify drug metabolism and the role of
involved in drug metabolism accounting
isoenzymes in the p450 system
for about 75% of the total metabolism.
For example, bioactive compounds
found in grapefruit juice and some oth-
er fruit juices including dihydroxy forgot-
Naturally occurring compounds may in- ten and parasitin A have been found to
duce or inhibit CYP activity. inhibit CYP3a4 mediated metabolism of
certain medications leading to increased
bioavailability and the strong possibility
of overdosing.
Grapefruit is an inhibitor and will de-
What does grapefruit have to do with
crease the metabolism of drugs by the
CYP?
cyp enzymes
When 2 drugs are both metabolized by
the p450 system the drug should be