Receptor binding-answer: d
(katzung, pp 418, brunton, pp 371)
local anesthetics are weak bases and in the in the body fluids they exist either as the uncharged
base (nonionized form ) or as a cation (ionized form). since the non ionized form is lipid soluble, it
is important for diffusion through the cell membrane, but the cationic form is thought to be the one
that binds to the receptor site, which is located on the na+ channel near the inner surface of the
membrane.
a, b, c) all these properties are actually more related to the nonionized form of the drug. in fact
tissue redistribution usually occurs in lipid rich tissues, the liver biotransforms mainly lipid soluble
drugs, systemic toxicity mainly affects the cns and only the lipid soluble form of the drug can
easily cross the blood brain barrier.
e) the half life of a drugs is related to its volume of distribution and its clearance, which in turn
depend on many factors, not only on the ionized form of the drug.