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24 Cards in this Set

  • Front
  • Back
Procaine drug type & MOA
Its an ester
MOA:
Penetrates voltage-gated Na+ channel as unionized moiety, once inside blocks channel as ionized moiety
Nerve exhibits use-dependent block

Low potency, slow onset, short duration
Procaine - what sort of nerves does it block?
active nerves! - has to get inside to block
Procaine use?
infiltration anesthesia
Procaine clearance
rapidly hyrdrolyzed by plasmaesterases!
Procaine side effects?
CNS (severity parallels potency): sedation (low dose), excitation & seizures (high dose—blocks inhibitory neurons), coma, respiratory depression
tetracaine MOA & drug type
Long acting ester

MOA:
Penetrates voltage-gated Na+ channel as unionized moiety, once inside blocks channel as ionized moiety
Nerve exhibits use-dependent block

slow onset, more potent, longer acting
Tetracaine uses?
Spinal Block and topical preparatin
Tetracaine side effects?
CNS (severity parallels potency): sedation (low dose), excitation & seizures (high dose—blocks inhibitory neurons), coma, respiratory depression
Tetracaine clearance?
• Inactivated mainly by plasma esterases

Tetrocain has slow metabolism

• Little drug normally reaches the systemic circulation, especially when administered with vasoconstrictor
lidocaine drug type & MOA
Amide; intermediate acting

Penetrates voltage-gated Na+ channel as unionized moiety, once inside blocks channel as ionized moiety

Nerve exhibits use-dependent block
lidocaine uses?
Local anesthetic (intermediate acting)
lidocaine toxicity?
CNS effects at lower concentrations than cardiac effects
Lidocaine clearance
Hepatic: high extraction (clearance sensitive to changes in renal blood flow)
N-dealkylation & amide hydrolysis
bupivacaine drug type & MOA
AMIDE; long acting

Penetrates voltage-gated Na+ channel as unionized moiety, once inside blocks channel as ionized moiety
Nerve exhibits use-dependent block
Bupivacaine use?
long acting local anesthetic
Bupivocaine side effects??
Bupivocaine: cardiac complications may appear before CNS side effects!
Bupivocaine clearance?
Hepatic
levopivacaine drug type & moa?
Amide; long acting

Penetrates voltage-gated Na+ channel as unionized moiety, once inside blocks channel as ionized moiety
Nerve exhibits use-dependent block
← fewer cardio effects
Levopivacaine use?
Local anesthetic, long acting
Levopicvacaine clearance
hepatic
prilocaine drug type, moa, and use
Amide; intermediate acting

MOA: Na+ pump inhibitor

use: Local anesthetic (intermediate-acting)
Prilocaine clearance
hepatic
Benzocaine drug type & use
Ester

--> ONLY USED TOPICALLY AS OINTMENT
what reverses the actions of lidocaine?
EPINEPHRINE!!!