Analgesic (morphine)
Opioid agonist activity decreased
Opioid antagonist activity increased
Inactive opioid agonist or antagonist
Opioid antagonist activity increased
14x potency of morphine
If the hydrocarbon chain is directly involved in interactions with its biologic target, then (blank) can produce major changes in pharmacologic activity.
branching
The primary pharmacologic activity of promethazine is that of an
antihistamine
The primary pharmacologic activity of promethazine is that of an antihistamine, whereas promazine is an
antipsychotic.
The physicochemical properties of a drug molecule are
dependent on:
a. what functional groups are present in the
molecule
b. spatial arrangement of these groups.
Proteins and other biologic targets are (blank) in
nature.
asymmetric
How a particular drug molecule interacts with these
macromolecules is determined by the (blank)of the functional groups
present.
three-
dimensional orientation
If critical functional groups in the drug molecule do not
occupy the proper spatial region, then productive
interactions with the biologic target will not be
possible
Approximately one in every four drugs currently on
the market is some type of
isomeric mixture
For many of these drugs, the biologic activity may
only reside in
one isomer
The majority of these isomeric mixtures are termed
“racemic mixtures” (or “racemates”).
is comprised of equal amounts of
both possible drug enantiomers.
racemic mixture
Study of the influence of FORMULATION FACTORS on
the therapeutic activity of a drug product or dosage forms.
BIOPHARMACEUTICS
Involves the study of the relationship between some of
the physicochemical properties of a drug and the biologic
effects observed after the administration of a drug via
various dosage forms or drug delivery systems.
BIOPHARMACEUTICS
Almost any ALTERATION in a drug delivery system is likely to
(blank) and (blank) to the desired place in the body.
ALTER THE DRUG DELIVERY RATE , AMOUNT OF
DRUG DELIVERED