Skip to main content Accessibility help

We use cookies to distinguish you from other users and to provide you with a better experience on our websites. Close this message to accept cookies or find out how to manage your cookie settings.

Close cookie message
×
Hostname: page-component-669899f699-7tmb6 Total loading time: 0 Render date: 2025-05-05T02:35:12.976Z Has data issue: false hasContentIssue false

3 - Local Anesthetics

from PART I - LOCOREGIONAL PAIN CONTROL

Published online by Cambridge University Press:  04 September 2009

By
Jan Namyslowski
Edited by
Charles E. Ray, Jr.
Charles E. Ray, Jr.
Affiliation:
Denver Health Medical Center
Get access

Summary

HISTORY

Ruetsch et al. provide an in-depth review of the history of local anesthesia in their 2001 paper titled “From Rocaine to Ropivacaine: The History of Local Anesthetic Drugs” (1). What follows is a summary of pertinent points in their eloquent historical review.

Cocaine has its linguistic origin in a Peruvian plant, revered by the natives for its stimulating properties. The word Khoka, meaning “the plant,” evolved into the European coca over time. We owe the term cocaine to Albert Niemann who isolated the main alkaloid from the coca leaves. A Viennese pharmacologist, Karl Damian Ritter von Schroff, described coca-induced skin insensibility. Samuel Percy was “the first to propose the use of the coca leaves as an anesthetic” in 1856. Carl Koller, in 1884, first used cocaine for ophthalmological anesthesia at the suggestion of Sigmund Freud. Addictive properties of cocaine were soon discovered as well, and many practitioners became affected, Freud and William Halsted among them. The dependency placed a significant damper on the availability of local anesthesia for medical procedures.

Subsequent pharmacological advances have led to the development of several local anesthetic compounds in the late 19th and throughout most of the 20th centuries. The delivery of local anesthetics would not have been possible, were it not for the invention, in 1844, of a hollow hypodermic needle and syringe by an Irishman, Francis Rynd (2).

Type
Chapter
Information
Pain Management in Interventional Radiology , pp. 21 - 31
Publisher: Cambridge University Press
Print publication year: 2008

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)

Book purchase

Temporarily unavailable

References

Ruetsch, YA, Böni, T, Borgeat, A. From cocaine to ropivacaine: the history of local anesthetic drugs. Current Top Med Chem 2001, 1(3):175–82.CrossRefGoogle ScholarPubMed
http://www.patentsoffice.ie/en/student_inventors.aspx (accessed November 2006).
http://www.inventnetireland.com/fii.asp (accessed November 2006).
Clemente, CD. Gray's Anatomy of the Human Body. 13th Edition. Philadelphia: Lea and Febiger, 1985:1350.Google Scholar
Guyton, AC, Hall, JE. Somatic sensations: II. Pain, headache, and thermal sensations (Ch. 48). In: Guyton AC, Hall JE, eds. Textbook of Medical Physiology. 10th Edition. Philadelphia: W.B. Saunders Company, 2001:552–63.Google Scholar
Guyton, AC, Hall, JE. Sensory receptors; neuronal circuits for processing information (Ch. 46). In: Guyton AC, Hall JE, eds. Textbook of Medical Physiology. 10th Edition. Philadelphia: W.B. Saunders Company, 2001:528–39.Google Scholar
Strichartz, GR, Berde, CB. Local anesthetics (Ch. 14). In: Miller RD, ed. Miller's Anesthesia. 6th Edition. Philadelphia: Elsevier, 2005:573–603.Google Scholar
Gissen, AJ, Covino, BG, Gregus, J. Differential sensitivities of mammalian nerve fibers to local anesthetic agents. Anesthesiology 1980, 53(6):467–74.CrossRefGoogle ScholarPubMed
DiFazio, CA, Carron, H, Grosslight, KR, Moscicki, JC, Bolding, WR, Johns, RA. Comparison of pH-adjusted lidocaine solutions for epidural anesthesia. Anesth Analg 1986, 65(7):760–4.CrossRefGoogle ScholarPubMed
Gokin, AP, Philip, B, Strichartz, GR. Preferential block of small myelinated sensory and motor fibers by lidocaine: in vivo electrophysiology in the rat sciatic nerve. Anesthesiology 2001, 95(6):1441–54.CrossRefGoogle ScholarPubMed
Johns, RA, Seyde, WC, DiFazio, CA, Longnecker, . Dose-dependent effects of bupivacaine on rat muscle arterioles. Anesthesiology 1986, 65(2):186–91.CrossRefGoogle ScholarPubMed
Johns, RA, DiFazio, CA, Longnecker, . Lidocaine constricts or dilates rat arterioles in a dose-dependent manner. Anesthesiology 1985, 62(2):141–4.CrossRefGoogle ScholarPubMed
Braid, DP, Scott, DB. The systemic absorption of local analgesic drugs. Br J Anaesth 1965, 37:394–404.CrossRefGoogle ScholarPubMed
Braid, DP, Scott, DB. The effect of adrenaline on the systemic absorption of local anaesthetic drugs. Acta Anaesthesiol Scand Suppl 1966, 23:334–46.CrossRefGoogle ScholarPubMed
Braid, DP, Scott, DB. Dosage of lignocaine in epidural block in relation to toxicity. Br J Anaesth 1966, 38(8):596–602.CrossRefGoogle Scholar
Scott, DB, Jebson, PJ, Braid, DP, Ortengren, B, Frisch, P. Factors affecting plasma levels of lignocaine and prilocaine. Br J Anaesth 1972, 44(10):1040–9.CrossRefGoogle ScholarPubMed
Moore, DC, Batra, MS. The components of an effective test dose prior to epidural block. Anesthesiology 1981, 55(6):693–6.CrossRefGoogle ScholarPubMed
Nation, RL, Triggs, EJ, Selig, M. Lignocaine kinetics in cardiac patients and aged subjects. Br J Clin Pharmacol 1977, 4(4):439–48.CrossRefGoogle ScholarPubMed
Englesson, S. The influence of acid-base changes on central nervous system toxicity of local anesthetic agents. I. An experimental study in cats. Acta Anaesthesiol Scand 1974, 18(2):79–87.CrossRefGoogle ScholarPubMed
Wagman, IH, Jong, RH, Prince, DA. Effects of lidocaine on the central nervous system. Anesthesiology 1967, 28(1):155–72.CrossRefGoogle ScholarPubMed
Moller, RA, Covino, BG. Cardiac electrophysiologic effects of lidocaine and bupivacaine. Anesth Analg 1988, 67(2):107–14.CrossRefGoogle ScholarPubMed
Jong, RH, Ronfeld, RA, DeRosa, RA. Cardiovascular effects of convulsant and supraconvulsant doses of amide local anesthetics. Anesth Analg 1982, 61(1):3–9.Google ScholarPubMed
Coyle, , Sperelakis, N. Bupivacaine and lidocaine blockade of calcium-mediated slow action potentials in guinea pig ventricular muscle. J Pharmacol Exp Ther 1987, 242(3):1001–5.Google ScholarPubMed
Kotelko, DM, Shnider, SM, Dailey, PA, et al. Bupivacaine-induced cardiac arrhythmias in sheep. Anesthesiology 1984, 60(1):10–18.CrossRefGoogle Scholar
Morishima, HO, Pedersen, H, Finster, M, et al. Bupivacaine toxicity in pregnant and nonpregnant ewes. Anesthesiology 1985, 63(2):134–9.CrossRefGoogle ScholarPubMed
Bjerring, P, Arendt-Nielsen, L. Depth and duration of skin analgesia to needle insertion after topical application of EMLA cream. Br J Anaesth 1990, 64(2):173–7.CrossRefGoogle ScholarPubMed
Jakobson, B, Nilsson, A. Methemoglobinemia associated with a prilocaine-lidocaine cream and trimetoprim-sulphamethoxazole. A case report. Acta Anaesthesiol Scand 1985, 29(4):453–5.CrossRefGoogle ScholarPubMed
Elsner, P, Dummer, R. Signs of methaemoglobinaemia after topical application of EMLA cream in an infant with haemangioma. Dermatology 1997, 195(2):153–4.CrossRefGoogle Scholar
Chen, BK, Cunningham, BB. Topical anesthetics in children: agents and techniques that equally comfort patients, parents and clinicians. Curr Opin Pediatr 2001, 13:324–30.CrossRefGoogle ScholarPubMed
McCafferty, DF, Woolfson, AD, Handley, J, et al. Effect of percutaneous local anesthetics on pain reduction during pulse dye laser treatment of portwine stains. Br J Anaesth 1997, 78:286–9.CrossRefGoogle ScholarPubMed
Woolfson, A, McCafferty, DF.Percutaneous local anaesthesia: drug release characteristics of the amethocaine phase-change system. Int J Pharm 1993, 94:75–80.CrossRefGoogle Scholar
O'Brien, L, Taddio, A, Lyszkiewicz, DA, Koren, G. A critical review of the topical local anesthetic amethocaine (AmethopTM) for pediatric pain. Pediatr Drugs 2005, 7(1):41–54.CrossRefGoogle Scholar
Maloney, JM, Bezzant, JL, Stephen, RL, Petelenz, TJ. Iontophoretic administration of lidocaine anesthesia in office practice. An appraisal. J Dermatol Surg Oncol 1992, 18(11):937–40.CrossRefGoogle ScholarPubMed
Rogers, TL, Ostrow, CL. The use of EMLA cream to decrease venipuncture pain in children. J Pediatr Nurs 2004, 19(1):33–9.CrossRefGoogle ScholarPubMed
Taddio, A, Gurguis, MGY, Koren, G. Lidocaine-prilocaine cream versus tetracaine gel for procedural pain in children. Ann Pharmacother 2002, 36(4):687–92.CrossRefGoogle ScholarPubMed
Schatz, M, Fung, DL. Anaphylactic and anaphylactoid reactions due to anesthetic agents. Clin Rev Allergy 1986, 4(2):215–27.Google ScholarPubMed
Eggleston, ST, Lush, LW. Understanding allergic reactions to local anesthetics. Ann Pharmacother 1996, 30(7–8):851–7.CrossRefGoogle ScholarPubMed
Soni, MG, Taylor, SL, Greenberg, NA, Burdock, GA. Evaluation of the health aspects of methyl paraben: a review of the published literature. Food Cham Toxicol 2002, 40(10):1335–73.CrossRefGoogle ScholarPubMed
Larson, CE. Methylparaben – an overlooked cause of local anesthetic hypersensitivity. Anesth Prog 1977, 24(3):72–4.Google ScholarPubMed
Feldman, T, Moss, J, Teplinsky, K, Carroll, JD. Cardiac catheterization in the patient with history of allergy to local anesthetics. Cathet Cardiovasc Diagn 1990, 20(3):165–7.CrossRefGoogle ScholarPubMed
Landau, SW, Nelson, WA, Gay, LN. Antihistaminic properties of local anesthetics and anesthetic properties of antihistaminic compounds. J Allergy 1951, 22(1):19–30.CrossRefGoogle ScholarPubMed
Brown, BR Jr. Pharmacology of local anesthesia. In: Clark WG, Brater DC, Johnson AR, eds. Goth's Medical Pharmacology. St. Louis: Mosby-Year Book, 1992:397–405.Google Scholar
Dire, DJ, Hogan, . Double-blinded comparison of diphenhydramine versus lidocaine as a local anesthetic. Ann Emerg Med 1993, 22(9):1419–22.CrossRefGoogle ScholarPubMed
Ernst, AA, Anand, P, Nick, T, Wassmuth, S. Lidocaine versus diphenhydramine for anesthesia in the repair of minor lacerations. J Trauma 1993, 34(3):354–7.CrossRefGoogle ScholarPubMed
Ernst, AA, Marvez-Valls, E, Mall, G, Patterson, J, Xie, X, Weiss, SJ. 1% lidocaine versus 0.5% diphenhydramine for local anesthesia in minor laceration repair. Ann Emerg Med 1994, 23(6):1328–32.CrossRefGoogle ScholarPubMed
McKay, W, Morris, R, Mushlin, P. Sodium bicarbonate attenuates pain on skin infiltration with lidocaine, with or without epinephrine. Anesth Analg 1987, 66(6):572–4.CrossRefGoogle ScholarPubMed
Nakayama, M, Munemura, Y, Kanaya, N, Tschuchida, ANamiki, . Efficacy of alkalinized lidocaine for reducing pain on intravenous or epidural catheterization. J Anesth 2001, 15:201–3.CrossRefGoogle ScholarPubMed
Watts, AC, Gaston, P, Hooper, G. Randomized trial of buffered versus plain lidocaine for local anesthesia in open carpal tunnel decompression. J Hand Surg [Br] 2004, 29(1):30–1.CrossRefGoogle ScholarPubMed
Masters, JE. Randomised control trial of pH buffered lignocaine with adrenaline in outpatient operations. Br J Plast Surg 1998, 51(5):385–7.CrossRefGoogle ScholarPubMed
Burns, CA, Ferris, G, Feng, C, Cooper, JZ, Brown, MD. Decreasing the pain of local anesthesia: a prospective, double-blind comparison of buffered, premixed 1% lidocaine with epinephrine versus 1% lidocaine freshly mixed with epinephrine. J Am Acad Dermatol 2006, 54(1):128–31.CrossRefGoogle ScholarPubMed
Palmon, SC, Lloyd, AT, Kirsch, JR. The effect of needle gauge and lidocaine pH on pain during intradermal injection. Anesth Analg 1998, 86(2):379–81.Google ScholarPubMed
Scarfone, RJ, Jasani, M, Gracely, EJ. Pain of local anesthetics: rate of administration and buffering. Ann Emerg Med 1998, 31(1):36–40.CrossRefGoogle ScholarPubMed
Min, RJ, Khilnani, NM. Endovenous laser ablation of varicose veins. J Cardiovasc Surg 2005, 46(4):395–405.Google ScholarPubMed
Klein, JA. Tumescent technique for regional anesthesia permits lidocaine doses of 35 mg/kg for liposuction. J Dermatol Surg Oncol 1990, 16(3):248–63.CrossRefGoogle ScholarPubMed
Klein, JA. Tumescent technique chronicles. Local anesthesia, liposuction, and beyond. Dermatol Surg 1995, 21(5):449–57.CrossRefGoogle ScholarPubMed
Grossmann, M, Sattler, G, Pistner, H, et al. Pharmacokinetics of articaine hydrochloride in tumescent local anesthesia for liposuction. J Clin Pharmacol 2004, 44(11):1282–9.CrossRefGoogle ScholarPubMed
Oertel, R, Rahn, R, Kirch, W. Clinical pharmacokinetics of articaine. Clin Pharmacokinet 1997, 33(6):417–25.CrossRefGoogle ScholarPubMed
Malamed, SF, Gagnon, S, Leblanc, D. Efficacy of articaine: a new amide local anesthetic. J Am Dent Assoc 2000, 131(5):635–42.CrossRefGoogle ScholarPubMed
Ostad, A, Kageyama, N, Moy, RL. Tumescent anesthesia with a lidocaine dose of 55 mg/kg is safe for liposuction. Dermatol Surg 1996, 22(11):921–7.CrossRefGoogle ScholarPubMed

Save book to Kindle

To save this book to your Kindle, first ensure [email protected] is added to your Approved Personal Document E-mail List under your Personal Document Settings on the Manage Your Content and Devices page of your Amazon account. Then enter the ‘name’ part of your Kindle email address below. Find out more about saving to your Kindle.

Note you can select to save to either the @free.kindle.com or @kindle.com variations. ‘@free.kindle.com’ emails are free but can only be saved to your device when it is connected to wi-fi. ‘@kindle.com’ emails can be delivered even when you are not connected to wi-fi, but note that service fees apply.

Find out more about the Kindle Personal Document Service.

Available formats
×

Save book to Dropbox

To save content items to your account, please confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your account. Find out more about saving content to Dropbox.

Available formats
×

Save book to Google Drive

To save content items to your account, please confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your account. Find out more about saving content to Google Drive.

Available formats
×