Local Anesthetic Agents Flashcards
The reversible block of the generation and propagation of the action potential in neural tissue is known as what?
Local anesthetic
Transient loss of what 3 functions can be seen with local anesthetics?
- Sensory
- Motor
- Autonomic
Local anesthetics target what?
Axons of A and C fibers (sensory nerves)
Which are more prone to hydrolysis, amide or ester links?
Ester
Which have a shorter duration of action, anesthetics with amide or ester links?
Ester
What are 4 examples of local anesthetics with esters?
- Cocaine
- Procaine
- Tetracaine
- Benzocaine
What are 6 examples of local anesthetics with amides?
- Lidocaine
- Prilocaine
- Mepivacaine
- Bupivacaine
- Ropivacaine
- Levo-bupivacaine
Where do local anesthetics act?
Site of injection.
Slow absorption into systemic circulation is usually desired with what?
Local anesthetics
What are 3 factors increasing systemic absorption?
- High dosage
- Increased blood flow at site of injection
- Vasodilation
Which remains at the receptor site longer, the cationic or non-charged form?
Cationic
Which is able to rapidly penetrate membranes, the cationic or non-charged form?
Non-charged
What effect does pka have on onset?
- High pka has slow onset.
- Low pka has fast onset
Which has a faster onset, procaine or lidocaine?
Lidocaine
Which has a faster onset, lidocaine or mepivacaine?
Mepivacaine
Which local anesthetic has the slowest onset?
Procaine
Which has a faster onset, mepivacaine or bupivacaine?
Mepivacaine
An infection can have what effect on the internal environment?
Make it acidic.
Increased protein binding has what effect on duration of action?
Increased duration
Which has a higher percentage of protein binding, procaine or lidocaine?
Lidocaine
Which has a higher percentage of protein binding, lidocaine or mepivacaine?
Mepivacaine
Which has a higher percentage of protein binding, mepivacaine or bupivacaine?
Bupivacaine
How is lipid solubility related to potency?
Positively
What effect does lipid solubility have on onset and duration?
Slower onset and longer duration
How does perfusion affect systemic absorption?
Highly perfused area leads to faster systemic absorption.
What are 2 examples of highly perfused areas?
- Mucus membranes
- Intercostal muscles
What are 3 examples of poorly perfused areas?
- Tendons
- Dermis
- Fat
What are 2 examples of vasoconstrictors?
- Epinephrine
- Phenylephrine
What can lead to reduced blood perfusion?
By how much?
- Vasoconstrictors
- 30%
T/F: Vasoconstrictors enhance the concentration of available drug in the premises of neuronal tissue.
True
What effect do vasoconstrictors have on duration of action?
Increase it.
What effect do vasoconstrictors have on analgesia?
Prolonged analgesic effects.
What are 2 advantages of epinephrine?
- Reduces systemic absorption of local anesthetics
- Reduces risks of systemic toxicity induced by local anesthetics
What is a disadvantage of epinephrine?
Potential for life-threatening arrhythmias
Where are amides metabolized?
Excreted?
- In the liver by cytocrome P450
- Kidneys
Where might amides accumulate?
Liver
Where are esters metabolized?
Excreted?
- In plasma by pseudocholinesterase
- Kidneys
What effect do local anesthetics have on nerve conduction?
Prevent sodium channels opening in neuronal axons, thus maintaining fully polarized state and blocking nerve propagation.
Action potentials are conducted along what part of the axon?
Ranvier nodes
Where do local anesthetics act on the axon?
Ranvier nodes
How many nodes of Ranvier need to be blocked in order for a local anesthetic to be effective?
2-3 nodes of Ranvier
T/F: Local anesthetics are only capable of blocking sensory nerves.
False - They are capable of blocking all nerves, not only sensory nerves.
Local anesthetics may cause what due to the blockade of motor neurons?
Muscle paralysis
Local anesthetics may cause what 2 things due to the blockade of autonomic nerves?
- Vasodilation
- Hypotension
Which type of fibers are more susceptible to local anesthesia?
Smaller non-myelinized fibers
Which type of fibers are less susceptible to local anesthesia?
Larger myelinized fibers
Is a blockade by local anesthetics more or less marked at higher frequencies of depolarization?
More marked
What type of nerves have a higher firing rate?
Why?
- Sensory nerves
- More susceptible
What effects does firing rate have on susceptibility?
- Higher firing rate means more susceptible
- Slower firing rate means less susceptible
Which have a higher firing rate, small or large diameter fibers?
Small diameter
Which fibers get blocked earlier or with low concentrations of local anesthetics?
Small diameter sensory nerves
Some local anesthetics can be used as what?
What are 2 examples of these?
- Antiarrhythmic agents
- Lidocaine and procaine
Some local anesthetics can cause what at high doses?
what are 2 examples of these?
- Lethal arrhythmias
- Bupivacaine and ropivacaine
What are 3 effects local anesthetics can have on cardiac cells?
- Suppress re-entrant ventricular arrhythmia
- Increase ventricular fibrillation threshold
- Decrease automaticity
What is the progression of toxicity for local anesthetics seen in the CNS?
First sedation, followed by tonic-clonic seizures, coma
What effect do local anesthetics have on the respiratory system?
Depression
What are 3 effects local anesthetics have on the CV system?
- Bradycardia
- Arrhythmias
- Hypotension
What are 4 possible toxic effects that can be seen with local anesthetics?
- Tissue irritation
- Allergic reactions
- Methemoglobinemia
- Apoptosis
In which species can methemoglobinemia be more of a problem with local anesthetics?
Cats
What is the order of presentation for most amide type of local anesthetic toxicity?
- CNS signs
- Respiratory system depression
- Cardiovascular system depression
Which drug is the exception to the normal order of presentation of local anesthetic toxicity?
What is the difference?
- Bupivacaine
- Causes cardiovascular depression first
What are 2 examples of isomers of bupivacaine that have less cardiac toxicity?
- Ropivacaine
- Levo-bupivacaine
A toxic dose of local anesthetic can cause side effects when injected how?
Rapidly IV
What is considered to be a toxic dose of lidocaine?
8 mg/kg
Do not inject more than what dose of lidocaine in a dog?
A cat?
- 4 mg/kg
- 2 mg/kg
What is considered to be a toxic dose of bupivacaine?
4 mg/kg
Do not inject more than what dose of bupivacaine in a dog?
A cat?
- 2 mg/kg
- 1 mg/kg
T/F: Dogs are more sensitive to local anesthetics than cats.
False - Cats more more sensitive than dogs.
Always do what before injecting a local anesthetic?
Aspirate to check for accidental IV needle placement. Look for blood.
Allergic reactions are mainly seen with what type of local anesthetic?
Ester-type
What is a possible sign of methemoglobinemia?
Pulseox will be about 85% due to significant hypoxia
Cats are more prone to develop methemoglobinemia with which 2 local anesthetics?
- Prilocaine
- Benzocaine
What are 3 forms of supportive care that can be used for local anesthetic toxicity?
- CV and/or respiratory support
- Steroid for allergies
- Anti-epileptic drugs
What is one possible specific treatment for local anesthetic toxicity?
Lipid emulsion