NAGELHOUT – PHARM 2 EXAM 2 QUESTIONS AND
ANSWERS LATEST VERSION
ANSWER: Cocaine, Procaine, and Chloroprocaine are the five ester local
anesthetics.
Tetracaine and benzocaine (the names only contain one "i")
Lidocaine, Prilocaine, Ropivicaine, Bupivacaine, Articaine, and Mepivicaine
are the two "i's" in the name of Amide Local Anesthetics (6).
Other medications related to local anesthetics: ANSWER, EMLA Cream,
Hyaluronidase, and Oraverse
The local anesthetic molecule must contain three essential chemical
components: ANSWER 1. Lipophilic part (benzene ring)
2. The quaternary amine's hydrophilic component
3. Divided by an intermediary chain, which could be an amide or ester chain.
Features of amide intermediate bonds: ANSWER NH (positively charged) and
carbonyl oxygen (negatively charged) are drawn to one another and are
therefore difficult to separate, making them difficult to metabolize.
Characteristics of ester intermediate bonds: ANSWER Negatively charged
oxygen and carbonyl oxygen reject one another, creating an open connection
that makes metabolism simple.
Depending on the pH, all local anesthetics can be either non-ionized or ionized.
ANSWER 1. Water-soluble quarternary amine (charged nitrogen group)
2. Lipid-soluble tertiary amine (non-charged nitrogen group)
metabolism of esters
Fast or slow metabolism 1. Metabolized by 2. Metabolized in 3.
4. Action duration 5. Length of action Ester: (particular location) ANSWER 1.
Esterases 2. All around
3. Quick 4. Brief 5. Tetracaine
Amide metabolism
, Fast or slow metabolism 1. Metabolized by 2. Metabolized in 3.
4. Action duration
5. Hazard of Amide Local Anesthetic Metabolism ANSWER 1. CYP1A2 and
CYP3A4 Liver Enzymes
2. The liver
3. Slow
4. Long: liver metabolism and heavily protein bound
5. Significant blood level toxicity can result from rapid absorption.
Which kind of local anesthetic is most likely to cause allergies? ANSWER
Esters
1. Is a patient allergic to all other ester anesthetics if they have an allergy to an
ester local anesthetic?
2. Do they have an amide allergy? ANSWER 1: Sure 2. No
1. Is a patient allergic to all amide anesthetics if they have an allergy to one
particular amide local anesthetic?
2. Do they have an allergy to esters? Response 1: No 2. No
mechanism of action of local anesthetics (apart from benzocaine) 1. Local
anesthetic should be injected into the tissue. 2. The non-ionized form should
pass through the membrane.
3. A portion of the non-ionized LA becomes ionized in the cytoplasm at the
altered pH.
4. Ionized LA limits sodium inflow by entering the sodium channel.
The mechanism of action of benzocaine 1. Apply a topical anesthetic to the
tissue. 2. The drug's ionized form enters the neuron's sodium channel and
prevents sodium influx.
These three locations are where Injected Local Anesthetic is used. ANSWER 1.
Non-ionized nerve blockade
2. Absorption and elimination from the bloodstream (absorption → medication
wears off)
3. Tissue binding that is not specific
These two locations receive local anesthesia in the bloodstream. ANSWER 1.
Distribution of systemic tissues
2. Hydrolysis of plasma (Ester) or liver (Amide)
Amide local anesthetics that are eliminated by the kidneys
ANSWERS LATEST VERSION
ANSWER: Cocaine, Procaine, and Chloroprocaine are the five ester local
anesthetics.
Tetracaine and benzocaine (the names only contain one "i")
Lidocaine, Prilocaine, Ropivicaine, Bupivacaine, Articaine, and Mepivicaine
are the two "i's" in the name of Amide Local Anesthetics (6).
Other medications related to local anesthetics: ANSWER, EMLA Cream,
Hyaluronidase, and Oraverse
The local anesthetic molecule must contain three essential chemical
components: ANSWER 1. Lipophilic part (benzene ring)
2. The quaternary amine's hydrophilic component
3. Divided by an intermediary chain, which could be an amide or ester chain.
Features of amide intermediate bonds: ANSWER NH (positively charged) and
carbonyl oxygen (negatively charged) are drawn to one another and are
therefore difficult to separate, making them difficult to metabolize.
Characteristics of ester intermediate bonds: ANSWER Negatively charged
oxygen and carbonyl oxygen reject one another, creating an open connection
that makes metabolism simple.
Depending on the pH, all local anesthetics can be either non-ionized or ionized.
ANSWER 1. Water-soluble quarternary amine (charged nitrogen group)
2. Lipid-soluble tertiary amine (non-charged nitrogen group)
metabolism of esters
Fast or slow metabolism 1. Metabolized by 2. Metabolized in 3.
4. Action duration 5. Length of action Ester: (particular location) ANSWER 1.
Esterases 2. All around
3. Quick 4. Brief 5. Tetracaine
Amide metabolism
, Fast or slow metabolism 1. Metabolized by 2. Metabolized in 3.
4. Action duration
5. Hazard of Amide Local Anesthetic Metabolism ANSWER 1. CYP1A2 and
CYP3A4 Liver Enzymes
2. The liver
3. Slow
4. Long: liver metabolism and heavily protein bound
5. Significant blood level toxicity can result from rapid absorption.
Which kind of local anesthetic is most likely to cause allergies? ANSWER
Esters
1. Is a patient allergic to all other ester anesthetics if they have an allergy to an
ester local anesthetic?
2. Do they have an amide allergy? ANSWER 1: Sure 2. No
1. Is a patient allergic to all amide anesthetics if they have an allergy to one
particular amide local anesthetic?
2. Do they have an allergy to esters? Response 1: No 2. No
mechanism of action of local anesthetics (apart from benzocaine) 1. Local
anesthetic should be injected into the tissue. 2. The non-ionized form should
pass through the membrane.
3. A portion of the non-ionized LA becomes ionized in the cytoplasm at the
altered pH.
4. Ionized LA limits sodium inflow by entering the sodium channel.
The mechanism of action of benzocaine 1. Apply a topical anesthetic to the
tissue. 2. The drug's ionized form enters the neuron's sodium channel and
prevents sodium influx.
These three locations are where Injected Local Anesthetic is used. ANSWER 1.
Non-ionized nerve blockade
2. Absorption and elimination from the bloodstream (absorption → medication
wears off)
3. Tissue binding that is not specific
These two locations receive local anesthesia in the bloodstream. ANSWER 1.
Distribution of systemic tissues
2. Hydrolysis of plasma (Ester) or liver (Amide)
Amide local anesthetics that are eliminated by the kidneys
