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Drugs Acting at the Sodium Channel
Lecture 2
12
Pharmacology
12/12/2011

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Cards

Term
Clinical uses of Na+ channel blockers
Definition

local anesthetics

anti-arrhythmic

anti-epileptics

Term
Suffix for local anesthetics
Definition
--caine
Term

Local anesthetic

one i

Definition

ester local anesthetic

Example: procaine

Term

local anesthetic:

two i

Definition

amide local anesthetic

exampe: lidocaine

Term

Ester or amide local anesthetic?

cocaine

lidocaine

procaine

prilocaine

Definition

ester

amide

ester

amide

Term

Cocaine: unique feature

mode of action

Definition

the only local anesthetic that is a vasoconstrictor;

it stimulates the CNS by causing the release and blocking the reuptake of neurotransmitters (epinephrine, NE, and dopamine)

Term
Definition
ester loca anesthetic
Term
Definition
amide local anesthetic
Term

Ester local anesthetic characteristics:

half-life

metabolism

allergic reactions

toxicity

Definition

half-life: short

metabolism: rapid/plasma

allergic reactions: possible

toxcity: low

Term

amide local anesthetic characteristics:

half-life

metabolism

allergic reactions

toxicity

Definition

half-life: long

metabolism: complex/hepatic

allergic reactions: rare/non-existant

toxicity: higher; dose dependent

Term

What happens in each phase?

Definition

0--Na+ in

1--K+ out

2--Ca2+ in; K+ out

3--K+ out

4--Ca2+ in

Term
Definition