Which of the following is a local anesthetic subject to inactivation by
plasma esterases?
a. Procaine
b. Lidocaine
c. Prilocaine
d. Mepivacaine
e. Bupivacaine
(a) Proccaine is the only ester listed – all the rest are amides
(a) this is basically a true-false type question. (a) is the only
statement that is true
i. (a), (b) and (c)
ii. (a), (d) and (e)
iii. (b) and (c) only
iv. (b), (c) and (d)
v. (b), (d) and (e)
(ii) another ester vs. amide type identification question.
Lidoccaine is an amide, thus other amides will be crossallergenic
- mepivacaine, prilocaine and dibucaine are the other
amides listed. Procaine and tetracaine are esters and will not be
cross-allergenic
(c) procaine is an ester; esters are metabolized predominately
by pseudocholinesterases in the plasma.
(c) esters are metabolized by plasma esterases - tetracaine is
the only ester listed, all the rest are amides
(d) remember #9 above? see the word “mainly”? same
question, but worded a little differently to throw you off. Again,
procaine is an ester; esters are metabolized predominately by
pseudocholinesterases in the plasma, but also to some extent
by esters in the liver.
(c) the word “EXCEPT” should alert you that this is basically a
true-false type question with 4 true statements and 1 false
statement; you just have to figure out which one! In this case,
you just have to remember that plasma cholinesterase levels
are only important for the duration of action of ester-type LAs,
not amides, which are metabolized in the liver. All the other
statements are variables which affect duration of the block, but
apply to both esters and amides.
(c) again, just another question that requires you to be able to
pick out an ester or an amide from a list. Since procaine is an
ester, only another ester LA would be cross-allergenic. In this
list the only ester listed is tetracaine
(d) According to textbooks, local anesthetics fall into the
following classes in terms of duration of action: short: procaine;
moderate: prilocaine, mepivacaine, lidocaine; long: bupivacaine,
tetracaine, etidocaine.
Statements (a), 3, and 4 would be true if
the question was comparing mepivacaine to bupivacaine, which
are structurally similar; but the comparison is to lidocaine. The
only difference that applies is duration of action ((d)),
bupivacaine is longer. (b) is wrong, both are amides.
(b) don’t forget: esters in plasma; amides in liver
(b) this is an interaction I tested you on several times – now you
know why! Propranolol interacts with lidocaine in two ways.
By slowing down the heart via beta receptor blockade, blood
delivery (and lidocaine) to the liver is reduced, thus lidocaine
remains in the systemic circulation longer, and can potentially
accumulate to toxic levels. Propranolol and lidocaine also
compete for the same enzyme in the liver, thus metabolism of
lidocaine can be reduced
(b) Answer is (b)- You should be able to recognize that all of
these drugs are local anesthetics. Local anesthetics are of one
of two types, either esters or amides. Ester types are subject to
hydrolysis in the plasma and thus have short half lives. Amides
are metabolized primarily in the liver and have longer half lives.
Thus the biotransformation (e.g., metabolism; again, the rats are
using a different word to confuse you, even though they are
asking the same basic question) of an amide type local
anesthetic would be the most altered in the presence of sever
liver disease. The key word here is “least”. Of the drugs listed,
only procaine is an ester. The rest are amides.
(b) strictly memorization
(d) same as above but asked backwards. Methemoglobinemia
may result from a toluidine metabolite of prilocaine,
orthotoluidine
(e) Most toxic reactions of a serious nature are related to
excessive blood levels arising from inadvertent intravascular
injection. Hypersensitivity reactions (options b & c) are rare, but
excessive blood levels will induce toxic reactions like CNS
stimulation in most everyone. This is a case where option (e) is
the “best” answer, because it is more likely than the other
alternatives, which might be true, but are not as likely (e.g,
“most probable”) to happen.
(d) Initially LAs inhibit central inhibitory neurons, which results in
CNS stimulation, which can proceed to convulsions. At higher
doses, they inhibit both inhibitory and excitatory neurons,
leading to a generalized state of CNS depression which can
result in respiratory depression and death.
20a. Unfortunately, you injected your lidocaine intra-arterially. The first
sign of lidocaine toxicity that might be seen in the patient would be
a. Elevated pulse rate
b. Sweating
c. CNS excitation
d. Cardiovascular collapse
e. CNS depression
(c) same question as above just worded differently. The intraarterial
injection would result in the high plasma levels
mentioned in the previous question
(c) it is a sympathomimetic after all. All the
(a) Grave’s disease is an autoimmune disease that causes
hyperthyroidism – the resulting high levels of circulating thyroid
hormone result in a hypermetabolic state with heightened
sympathetic activity, which combined with injected epinephrine
could result in a hypertensive crisis.
(d) Cardiovascular collapse is due to a direct action of the local
anesthetic on the heart muscle itself (LA’s in toxic doses
depress membrane excitability and conduction velocity), thus
(d) is the correct answer. All of the other alternatives are indirect
ways to affect the heart
(e) Of the options listed, this is the one that will kill the patient,
which I guess makes it the most serious
(a) All the listed local anesthetics except cocaine are
vasodilators, especially ester-ctype drugs such as proccaine
and the amide lidocaine. Cocaine is the only local anesthetic
that predictably produces vasoconstriction. Cocaine is also the
only local anesthetic to block the reuptake of NE into adrenergic
neurons, and thus potentiate the NE that has been released
from nerve endings
(a) see explanation above
(e) Na+ ions are involved, which limits your choices to
(c) and (e). (c) would increase or facilitate nervous impulse
conduction, which is the opposite of what you want the local
anesthetic to do, so pick (e).