Nagelhout - Pharm Exam 2 Questions

Nagelhout - Pharm Exam 2 Questions With Complete Solutions Ester Local Anesthetics (5) - Correct Answers ✅- Cocaine

• Procaine
• Chloroprocaine
• Tetracaine
• Benzocaine

(only 1 "i" in the name) Amide Local Anesthetics (6) - Correct Answers ✅- Lidocaine

• Prilocaine
• Ropivicaine
• Bupivacaine
• Articaine
• Mepivicaine

(2 "i's" in the name) Miscellaneous drugs associated with Local Anesthetics - Correct Answers ✅- EMLA Cream

• Hyaluronidase
• Oraverse

Oraverse - Correct Answers ✅Rigatine: causes vasodilation that results

faster recovery from LA in dental procedures (reversal of the epi effects) Three required chemical components of the local anesthetic molecule - Correct Answers ✅1. Lipophilic portion (Benzene ring)

• Hydrophilic portion (Quarternary amine)
• Separated by an Intermediate Chain (either an Ester or Amide chain) 1 / 4

Nagelhout - Pharm Exam 2 Questions With Complete Solutions Amide Intermediate bond characteristics - Correct Answers ✅NH (positively charged) and Carbonyl oxygen (negatively charged) = attracted to each other → difficult to separate = difficult to metabolize Ester Intermediate bond characteristics - Correct Answers ✅Oxygen (negatively charged) and Carbonyl oxygen (negatively charged) = repel each other → open bond = easy to metabolize All local anesthetics take on these 2 forms to be non-ionized or ionized depending on the pH - Correct Answers ✅1. Quarternary amine (charged nitrogen group) → water soluble

• Tertiary Amine (non-charged nitrogen group) → lipid soluble

Ester metabolism

• Metabolized by
• Metabolized in
• Fast or slow metabolism
• Duration of action
• Longest acting Ester - Correct Answers ✅1. (Location specific) Esterases
• Everywhere
• Fast
• Short
• Tetracaine

Amide metabolism

• Metabolized by
• Metabolized in 2 / 4

Nagelhout - Pharm Exam 2 Questions With Complete Solutions

• Fast or slow metabolism
• Duration of action
• Risk with Amide local anesthetic metabolism - Correct Answers ✅1.

Liver enzymes (CYP1A2 and CYP3A4)

• Liver
• Slow

4. Long: highly protein bound and liver metabolism

• Rapid absorption can lead to significant blood level → toxicity

Which local anesthetic type has a higher allergy probability? - Correct Answers ✅Esters

• If a patient is allergic to an ester local anesthetic, are they allergic to all

other ester anesthetics?

• Are they allergic to the amides? - Correct Answers ✅1. Yes
• No
• If a patient is allergic to an amide local anesthetic, are they allergic to all

other amide anesthetics?

• Are they allergic to the esters? - Correct Answers ✅1. No
• No

Local anesthetic mechanism of action (except Benzocaine) - Correct Answers ✅1. Inject local anesthetic into tissue

• Non-ionized form crosses the cell membrane
• In new pH of the cytoplasm, some of the non-ionized LA becomes ionized
• Ionized LA enters the sodium channel and blocks sodium influx 3 / 4

Nagelhout - Pharm Exam 2 Questions With Complete Solutions Benzocaine mechanism of action - Correct Answers ✅1. Inject local anesthetic into tissue

• Ionized form of the drug enters the sodium channel of the neuron and

blocks sodium influx Injected Local Anesthetic goes to these 3 places - Correct Answers ✅1.Nerve blockade (non-ionized)

• Blood stream uptake & removal (absorption → drug wears off)
• Non-specific tissue binding

Local anesthetic in blood stream goes to these 2 places - Correct Answers ✅1. Systemic tissue distribution

• Liver (Amide) or Plasma Hydrolysis (Ester)

Amide local anesthetics excreted by - Correct Answers ✅Kidney The lower the pKa (closer to 7.4), the ____ the onset of the local anesthetic (except ____) - Correct Answers ✅Faster Chloroprocaine (higher pH but fastest onset) The higher the protein binding, the ___ the duration - Correct Answers ✅Longer Local anesthetics greater than 90% protein bound (5) - Correct Answers ✅- Etidocaine (94%)

• Ropivicaine (94%)
• Tetracaine (94%)
• Bupivicaine (95%)
• Cocaine (98%)
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