Nagelhout Pharm 2 Test 2 Exam Q’s and A’s
Ester nomenclature - -Drugs with one "i"
- Amide nomenclature - -Drugs with two "i"s
- Naturally occurring Local? - -Cocaine
- Most widely used Local? - -Lidocaine
- Reversal for Locals? - -Oraverse
- 3 Sections of a Local Anesthetic Molecule? - -1. Benzene Ring (Lipophilic-
Lipid Soluble)
2. Ester (O) or Amide (N) Linkage
3. Quartenery Amine (Hydrophilic-Water Soluble)
- Ester metabolism - -metabolized by cholinesterase, which are found in
plasma. this metabolism is rapid which makes esters short acting.
- Longest acting ester - -tetracaine
- Amide metabolism - -metabolized by liver enzymes= longer acting
- Explain allergies to Local Anesthetics - -1. Most commonly found with
esters (bc people are exposed to the lipophilic portion PABA daily via
cosmetics).
2. When allergic to an ester you're allergic to all esters but not to amides
3. When allergic to an amide youre ONLY allergic to that amide
- MOA of Locals - -blocking Na channels in nerves
- Ionized portion of Locals - -Water soluble, can't penetrate nerve but able
to block Na channel once inside the axoplasm.
- Non-ionized portion of locals - -lipid soluble, penetrate nerve
- Exception to typical MOA of Locals? - -Benzocaine, is water soluble but can
penetrate and block nerve.
- Target site of drugs is on what side of the membrane? - -cytoplasmic
- What makes the Local diffuse in? makes it stop? - -Concentration gradient
(greater outside the nerve than inside)
, Absorption
- Locals are _____ drugs? - -basic
- pKa effects what parameter of Locals? how? - -Onset, lower pKa (closer to
7.4=more non ionized) the faster the onset
- Fastest Local Anesthetic? Why is this drug special? - -Choloropropaine
Exception to pKa rule of Locals.
- Protien Binding effects what parameter of Locals? how? - -duration, more
protein binding = longer duration.
- 6 ways epi effects Local Anesthetic administration? How does this compare
to increased dose? - -1. Faster onset
2. Increases the efficacy of the Block (both sensory and motor)
3. Increases the duration
4. Increases area of the block
5. Decreases incidence of toxicity (opposite with increased dose-only
difference between the two)
- Procaine max dose? - -14 mg/kg
- Chloroprocaine max dose? - -14 mg/kg
- Tetracaine max dose? - -1 mg/kg MOST TOXIC
- Cocaine max dose? - -3 mg/kg or 200 total (topical)
- Lidocaine max dose? - -7 mg/kg
- Mepivicaine max dose? - -7 mg/kg
- Priolocaine max dose? - -8 mg/kg
- Bupivicaine max dose? - -3 mg/kg
- Ropivicaine max dose? - -3 mg/kg
- Main toxic effect of Locals? most often a result of? - -Seizures; injecting
into a vein
- Ion Trapping - -The respiratory depression associated with OD of Locals
causes hypoxia and acidosis. This acidosis inc the ionized fraction of
Ester nomenclature - -Drugs with one "i"
- Amide nomenclature - -Drugs with two "i"s
- Naturally occurring Local? - -Cocaine
- Most widely used Local? - -Lidocaine
- Reversal for Locals? - -Oraverse
- 3 Sections of a Local Anesthetic Molecule? - -1. Benzene Ring (Lipophilic-
Lipid Soluble)
2. Ester (O) or Amide (N) Linkage
3. Quartenery Amine (Hydrophilic-Water Soluble)
- Ester metabolism - -metabolized by cholinesterase, which are found in
plasma. this metabolism is rapid which makes esters short acting.
- Longest acting ester - -tetracaine
- Amide metabolism - -metabolized by liver enzymes= longer acting
- Explain allergies to Local Anesthetics - -1. Most commonly found with
esters (bc people are exposed to the lipophilic portion PABA daily via
cosmetics).
2. When allergic to an ester you're allergic to all esters but not to amides
3. When allergic to an amide youre ONLY allergic to that amide
- MOA of Locals - -blocking Na channels in nerves
- Ionized portion of Locals - -Water soluble, can't penetrate nerve but able
to block Na channel once inside the axoplasm.
- Non-ionized portion of locals - -lipid soluble, penetrate nerve
- Exception to typical MOA of Locals? - -Benzocaine, is water soluble but can
penetrate and block nerve.
- Target site of drugs is on what side of the membrane? - -cytoplasmic
- What makes the Local diffuse in? makes it stop? - -Concentration gradient
(greater outside the nerve than inside)
, Absorption
- Locals are _____ drugs? - -basic
- pKa effects what parameter of Locals? how? - -Onset, lower pKa (closer to
7.4=more non ionized) the faster the onset
- Fastest Local Anesthetic? Why is this drug special? - -Choloropropaine
Exception to pKa rule of Locals.
- Protien Binding effects what parameter of Locals? how? - -duration, more
protein binding = longer duration.
- 6 ways epi effects Local Anesthetic administration? How does this compare
to increased dose? - -1. Faster onset
2. Increases the efficacy of the Block (both sensory and motor)
3. Increases the duration
4. Increases area of the block
5. Decreases incidence of toxicity (opposite with increased dose-only
difference between the two)
- Procaine max dose? - -14 mg/kg
- Chloroprocaine max dose? - -14 mg/kg
- Tetracaine max dose? - -1 mg/kg MOST TOXIC
- Cocaine max dose? - -3 mg/kg or 200 total (topical)
- Lidocaine max dose? - -7 mg/kg
- Mepivicaine max dose? - -7 mg/kg
- Priolocaine max dose? - -8 mg/kg
- Bupivicaine max dose? - -3 mg/kg
- Ropivicaine max dose? - -3 mg/kg
- Main toxic effect of Locals? most often a result of? - -Seizures; injecting
into a vein
- Ion Trapping - -The respiratory depression associated with OD of Locals
causes hypoxia and acidosis. This acidosis inc the ionized fraction of
