N16/17 - Anesthetics (Zhu) Flashcards
Types of local anesthetics (chemical property)
Esters
Amides
local anesthetic that mainly exists in neutral form (pka 3.5)
Benzocaine
hydrophobicity of most effective LAs
moderate
2 changes due to binding of LA to binding site
occlusion
restriction of conformational change
- AP generation is blocked (prevented channel opening)
- AP conduction is blocked (prolonged refractory period)
modulated receptor hypothesis
Low binding affinity at resting state
High binding affinity at:
- intermediate closed state
- open state
- inactivated state: LA stabilizes channel in innactivated state, channel cannot be reopened even after repolarization
channel states when LAs have major effect
Intermediate closed - prevents opening
Inactivated - extends refractory period
attenuates effectiveness of LAs
hypocalcemia - increased Na excitability
Potentiates the effectivenss of local anesthetics
Hyperkalemia - membrane is persistently depolarized
General blockade order
First pain
Second pain
Temperature
Touch, proprioception (pressure, position, stretch)
Motor function
blocks pain, without significant motor block
Epidural bupivacaine
A-gamma fibers
muscle tone
A-delta fibers
First pain & temperature
C fibers
second pain & temperature
to avoid systemic absorption of LAs
co-administration of vasoconstrictors
Co-administered vasoconstrictor:
Except in which areas?
epinepherine
Except in: fingers, toes, ears, nose, penis
Pain relief
oral, nasal, laryngeal, rectal disorders, surgery
Topical: Mucous membrane application
Tx: pruritus
poison ivy, insect bites, eczema, venipuncture, chickenpox, etc
topical anesthesia: skin application
suturing wounds
removal of foreign bodies
dental procedures
Infiltration LA - intradermal or subq
Lidocaine, procaine, bupivacaine
toxicity due to
systemic absorption
systems affected by LA toxicity
CNS - excitement followed by depression (inhibition of inhibitory pathways, then both excite & inhib)
Cardiovascular - vasoconstriction, then vasodilation
Acts as antiarrhythmic at very low concentration
Lidocaine
hypersensitivity
Ester-type LAs
met. product = p-aminobenzoic acid (PABA)
cautioned use for potentiation of neuromuscular blockers
Myasthenia gravis
(use great caution)
Vasoconstriction
cardiotoxicity
CNS stimulation
Tx: opthalmic, nasal surgery (blocks bleeding), topical
Cocaine
(Ester-type)
nasal surgery
Cocaine
No topical application
Procaine (Novocain)
Chloroprocain (Nesacaine)
(Ester-type)
High hydrophobicity
Fast onset
High potency
Long acting
Spinal & topical
Tetracaine
(Ester-type)
Weak
Used in nonprescription topicals
Benzocaine
(Ester-type)
Risk for hypotension & cardiotoxicity
Bupivacaine
Similar to bupivacaine
less cardiotoxicity
Levobupivacaine
Ropivacaine - structural analog
Mepivacaine - structural analog
(Amide-type)
Amide-type drugs - name hint
2 I’s
Ester-type drugs: name hint
1 “I” in name
Topical & infiltraion anesthesia
Prilocaine
Infiltration and nerve block anesthesia
Etidocaine