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September 26, 1977, Vol 238, No. 13 >
ARTICLE | September 26, 1977

Neural Blockade by Local Anesthetics FREE

Rudolph H. de Jong, MD
[+] Author Affiliations

Reprint requests to Division of Scientific Publications, American Medical Association, 535 N Dearborn St, Chicago, IL 60610 (Dr de Jong).


JAMA. 1977;238(13):1383-1385. doi:10.1001/jama.1977.03280140061020
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References

Local anesthetics block nerve impulse propagation by occluding transmembrane sodium channels, so preventing depolarization. First, the uncharged lipid-soluble anesthetic base penetrates the membrane; then the positively charged cation binds to anionic components of the sodium channel's internal axoplasmic mouth. Though primarily a carrier, the base contributes to blockade by causing the membrane to swell, so pinching the sodium channels.

Dissolved in water, local anesthetic salt crystals dissociate into anesthetic cation and base—proportional to the drug's fixed pKa and the tissue's variable pH. The cation-base concentration ratio is critical to optimal neural blockade. If there is too little base, few anesthetic molecules will penetrate to the neural target; if too little cation, few sodium channels will be plugged.

(JAMA 238:1383-1385, 1977)

REFERENCES

1 +
de Jong RH: Local Anesthetics , ed 2. Springfield, Ill, Charles C Thomas Publisher, 1977;.
2 +
Covino BG, Vassallo HG: Local Anesthetics: Mechanism of Action and Clinical Use . New York, Grune & Stratton Inc, 1976;.
3 +
Ritchie JM:  Mechanism of action of local anesthetic agents and biotoxins . Br J Anaesth 47:191-198, 1975;.
4 +
Strichartz G:  Molecular mechanisms of nerve block by local anesthetics . Anesthesiology 45:421-441, 1976;.
5 +
Courtney KR:  Mechanism of frequency-dependent inhibition of sodium currents in frog myelinated nerve by the lidocaine derivative GEA 968 . J Pharmacol Exp Ther 195:225-236, 1975;.
6 +
Smythies JR, Benington F, Bradley RJ, et al:  The molecular structure of the sodium channel . J Theor Biol 9:595-600, 1974;.
7 +
Narahashi T, Frazier DT:  Site of action and active form of procaine in squid giant axons . J Pharmacol Exp Ther 194:506-513, 1975;.
8 +
Hille B, Courtney K, Dum R:  Rate and site of action of local anesthetics in myelinated nerve fibers , in Fink BR (ed): Molecular Mechanisms of Anesthesia . New York, Raven Press, 1974;.
9 +
Condouris GA, Goebel RH, Brady T:  Computer simulation of local anesthetic effects using a mathematical model of myelinated nerve . J Pharmacol Exp Ther 196:737-745, 1976;.
10 +
Franz DN, Perry RS:  Mechanisms for differential block among single myelinated and non-myelinated axons by procaine . J Physiol 236:193-210, 1974;.

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1 +
de Jong RH: Local Anesthetics , ed 2. Springfield, Ill, Charles C Thomas Publisher, 1977;.
2 +
Covino BG, Vassallo HG: Local Anesthetics: Mechanism of Action and Clinical Use . New York, Grune & Stratton Inc, 1976;.
3 +
Ritchie JM:  Mechanism of action of local anesthetic agents and biotoxins . Br J Anaesth 47:191-198, 1975;.
4 +
Strichartz G:  Molecular mechanisms of nerve block by local anesthetics . Anesthesiology 45:421-441, 1976;.
5 +
Courtney KR:  Mechanism of frequency-dependent inhibition of sodium currents in frog myelinated nerve by the lidocaine derivative GEA 968 . J Pharmacol Exp Ther 195:225-236, 1975;.
6 +
Smythies JR, Benington F, Bradley RJ, et al:  The molecular structure of the sodium channel . J Theor Biol 9:595-600, 1974;.
7 +
Narahashi T, Frazier DT:  Site of action and active form of procaine in squid giant axons . J Pharmacol Exp Ther 194:506-513, 1975;.
8 +
Hille B, Courtney K, Dum R:  Rate and site of action of local anesthetics in myelinated nerve fibers , in Fink BR (ed): Molecular Mechanisms of Anesthesia . New York, Raven Press, 1974;.
9 +
Condouris GA, Goebel RH, Brady T:  Computer simulation of local anesthetic effects using a mathematical model of myelinated nerve . J Pharmacol Exp Ther 196:737-745, 1976;.
10 +
Franz DN, Perry RS:  Mechanisms for differential block among single myelinated and non-myelinated axons by procaine . J Physiol 236:193-210, 1974;.

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