Pharma TUFT Flashcards
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
- Procaine differs from lidocaine in that
a. Procaine is a p-aminobenzoic acid ester and lidocaine is not
b. Lidocaine is a meta-aminobenzoic acid ester and procaine is not
c. The duration of action of procaine is longer than that of an equal
total dose of lidocaine
d. Procaine hydrochloride is metabolized into diethylaminoethanol
and benzoic acid.
(a) this is basically a true-false type question. (a) is the only
statement that is true
- Which of the following local anesthetics would be expected to produce
a sensitization reaction in a patient allergic to lidocaine?
a. Mepivacaine
b. Tetracaine
c. Procaine
d. Prilocaine
e. Dibucaine
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
- The hydrolysis of procaine occurs mainly in the
a. Liver
b. Lungs
c. Plasma
d. Muscles
e. Kidneys
(c) procaine is an ester; esters are metabolized predominately
by pseudocholinesterases in the plasma.
- Which of the following is local anesthetic subject to inactivation by
plasma esterases?
a. Lidocaine
b. Prilocaine
c. Tetracaine
d. Mepivacaine
e. Bupivacaine
(c) esters are metabolized by plasma esterases - tetracaine is
the only ester listed, all the rest are amides
- The activity of procaine is terminated by
a. Elimination by the kidney
b. Storage in adipose tissue
c. Metabolism in the liver only
d. Metabolism in the liver and by pseudocholinesterase in the
plasma
(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.
- All of the following factors are significant determinants of the duration
of conduction block with amide-type local anesthetics EXCEPT the
a. pH of tissues in the area of injection
b. Degree of vasodilatation caused by the local anesthetic
c. Blood plasma cholinesterase levels
d. Blood flow through the area of conduction block
e. Concentration of the injected anesthetic solution
(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.
- Which of the following is contraindicated for a patient who had an
allergic reaction to procaine six months ago?
a. Nerve block with lidocaine
b. Topical application of lidocaine
c. Topical application of tetracaine
d. Infiltration with an antihistamine
(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
- Bupivacaine (Marcaine ) has all of the following properties relative to
lidocaine (Xylocaine ) EXCEPT bupivacaine
a. Is more toxic
b. Is an ester-type local anesthetic
c. Has a slower onset of action
d. Has a longer duration of action
(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.
- Amide-type local anesthetics are metabolized in the
a. Serum
b. Liver
c. Spleen
d. Kidney
e. Axoplasm
(b) don’t forget: esters in plasma; amides in liver
- The duration of action of lidocaine would be increased in the presence
of which of the following medications?
a. Prazosin
b. Propranolol
c. Hydrochlorothiazide
d. Lisinopril
e. Digoxin
(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
- Severe liver disease least affects the biotransformation of which of
the following?
a. Lidocaine
b. Procaine
c. Prilocaine
d. Mepivacaine
(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.
- A patient has been given a large volume of a certain local anesthetic
solution and subsequently develops cyanosis with
methemoglobinemia. Which of the following drugs most likely was
administered?
a. Procaine
b. Prilocaine
c. Dibucaine
d. Lidocaine
e. Mepivacaine
(b) strictly memorization
- Use of prilocaine carries the risk of which of the following adverse
effects?
a. Porphyria
b. Renal toxicity
c. Gastric bleeding
d. Methemoglobinemia
(d) same as above but asked backwards. Methemoglobinemia
may result from a toluidine metabolite of prilocaine,
orthotoluidine
- The most probable cause for a serious toxic reaction to a local
anesthetic is
a. Psychogenic
b. Deterioration of the anesthetic agent
c. Hypersensitivity to the vasoconstrictor
d. Hypersensitivity to the local anesthetic
e. Excessive blood level of the local anesthetic
(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.
- High plasma levels of local anesthetics may cause
a. Inhibition of peristalsis
b. stimulation of baroreceptors resulting in severe hypotension
c. Inhibition of the vagus nerve to the heart
d. Depression of inhibitory neurons in the CNS
(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
- The first sign that your patient may be experiencing toxicity from too
much epinephrine would be
a. Cardiovascular collapse
b. Convulsions
c. Elevated pulse rate
d. Slurred speech
(c) it is a sympathomimetic after all. All the
- Which disease condition would make the patient most sensitive to the
epinephrine in the local anesthetic?
a. Grave’s disease
b. Diabetes
c. HIV
d. Alcoholism
e. Schizophrenia
(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.
- Cardiovascular collapse elicited by a high circulating dose of a local
anesthetic may be caused by
a. Syncope
b. Vagal stimulation
c. Histamine release
d. Myocardial depression
e. Medullary stimulation
(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
- The most serious consequence of systemic local anesthetic toxicity is
a. Vertigo
b. Hypertension
c. Hyperventilation
d. Post depressive central nervous system convulsions
e. Postconvulsive central nervous system depression
(e) Of the options listed, this is the one that will kill the patient,
which I guess makes it the most serious
- Hypotensive shock may result from excessive blood levels of each of
the following local anesthetics EXCEPT
a. Cocaine
b. Procaine
c. Lidocaine
d. Tetracaine
e. Mepivacaine
(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
- Which of the following anesthetic drugs produces powerful
stimulation of the cerebral cortex?
a. Cocaine
b. Procaine
c. Lidocaine
d. Tetracaine
e. Mepivacaine
(a) see explanation above