AHFS Class:

• Local Anesthetics 72:00

Generic Name(s):

• Lidocaine Hydrochloride

Lidocaine hydochloride is an intermediate-acting local anesthetic of the amide type.

Lidocaine hydrochloride is used for infiltration anesthesia and for nerve block techniques including peripheral, sympathetic, epidural (including caudal), and spinal block anesthesia. Lidocaine has been administered intraperitoneally† for anesthesia of the peritoneum and pelvic viscera.

Administration

Lidocaine hydrochloride may be administered by infiltration or by epidural (including caudal) block, peripheral or sympathetic nerve block, and subarachnoid block. The manufacturers state that only the preservative-free, epinephrine-free 0.5% lidocaine injection should be used for IV regional anesthesia. Local anesthetics, including lidocaine hydrochloride, have been administered by continuous intra-articular infusion† (e.g., for control of postoperative pain); however, such use has been associated with chondrolysis.200,201,202,203,204,205,206,207,208,209,211,212 Lidocaine hydrochloride solutions containing preservatives should not be used for spinal or epidural (including caudal) block. Partially used bottles of solutions that do not contain preservatives should be discarded.

Aspiration for blood should be performed prior to injection of lidocaine hydrochloride to avoid inadvertent intravascular administration; however, a negative aspiration does not ensure protection against inadvertent intravascular injection.211,212,213,214

Local anesthetics should only be administered by clinicians who are experienced in the diagnosis and management of dose-related toxicities and other acute emergencies associated with these agents.211,212,213,214 Resuscitative equipment, oxygen, drugs, and personnel required for treatment of adverse reactions should be immediately available when lidocaine is administered.211,212,213,214 Proper positioning of the patient is extremely important in spinal anesthesia. For specific procedures and techniques of administration, specialized references should be consulted.

Dosage

Dosage of lidocaine hydrochloride varies with the anesthetic procedure, the degree of anesthesia required, and individual patient response. The usual dosages should generally be reduced in children, geriatric patients, debilitated or acutely ill patients, and patients with cardiac and/or hepatic disease.211,212,213,214 The smallest dose and lowest concentration required to produce the desired effect should be used. Use of dilute solutions (i.e., 0.25-0.5%) and total dosages not to exceed 3 mg/kg are recommended for induction of IV regional anesthesia in children.211

Single doses of lidocaine hydrochloride (for anesthesia other than spinal) should not exceed 4.5 mg/kg (or 300 mg) in healthy adults or 4.5 mg/kg in children younger than 10 years of age.211,212,213 When administered with epinephrine, lidocaine hydrochloride doses should not exceed 7 mg/kg (or 500 mg) in healthy adults or 7 mg/kg in children younger than 10 years of age.211,212,213 For spinal anesthesia, up to 100 mg of the drug may be given. For continuous epidural or caudal anesthesia, the maximum dose should not be repeated at intervals of less than 1.5 hours. When continuous lumbar or caudal epidural anesthesia is used for nonobstetric procedures, additional drug may be administered if necessary to attain adequate anesthesia.211 For paracervical block for nonobstetric and obstetric analgesia (including abortion), the maximum recommended dosage (200 mg) should not be repeated at intervals of less than 1.5 hours.211 For IV regional anesthesia in adults using a 0.5% solution without epinephrine, the dose administered should not exceed 4 mg/kg.

Solutions of 1-2% lidocaine hydrochloride with or without epinephrine and containing no preservatives are used for epidural or caudal anesthesia. To prevent intravascular or subarachnoid injection of a large epidural dose of lidocaine, a test dose (e.g., 2-3 mL of a 1.5% solution) of anesthetic solution should be injected at least 5 minutes prior to administering the total dose.211 When clinical conditions permit, use of a test dose solution that contains epinephrine (e.g., 10-15 mcg) should be considered to detect inadvertent intravascular injection.211 The test dose should be repeated if the patient is moved such that the epidural catheter may have been displaced.211 Rapid injection of a large, single dose through a catheter should be avoided; instead, the drug should be administered, when feasible, in fractional doses.211 In epidural anesthesia, 2-3 mL of the indicated solution is usually required for each dermatome to be anesthetized. In caudal block for production of obstetric analgesia or in epidural thoracic block, 20-30 mL of a 1% solution (200-300 mg) of the drug may be used. For surgical anesthesia with caudal block, 15-20 mL of a 1.5% solution (225-300 mg) is given. For epidural lumbar analgesia, the dose is 25-30 mL (250-300 mg) of a 1% solution, and for epidural lumbar anesthesia, the recommended dose is 15-20 mL of a 1.5% solution (225-300 mg) or 10-15 mL of a 2% solution (200-300 mg).211

A solution of 5% lidocaine hydrochloride with 7.5% dextrose is used for spinal anesthesia in adults and adolescents 16 years of age or older.214 For obstetric low spinal or saddle-block anesthesia in a normal vaginal delivery, the dose is approximately 1 mL (50 mg).214 For cesarean section or deliveries which require intrauterine manipulations, 1.5 mL of the 5% solution (75 mg) may be given.214 For surgical anesthesia, 1.5-2 mL of the 5% solution (75-100 mg) may be administered.214

The following doses of lidocaine hydrochloride have been suggested for various nerve blocks: brachial nerve block, 15-20 mL of a 1.5% solution (225-300 mg); dental nerve block, 1-5 mL of a 2% solution (20-100 mg); intercostal nerve block, 3 mL of a 1% solution (30 mg); paravertebral nerve block, 3-5 mL of a 1% solution (30-50 mg); pudendal nerve block (each side), 10 mL of a 1% solution (100 mg); and paracervical nerve block (each side) for obstetric analgesia, 10 mL of a 1% solution (100 mg).211 For sympathetic nerve blocks, the following doses may be used: cervical (stellate ganglion) nerve block, 5 mL of a 1% solution (50 mg), and lumbar nerve block, 5-10 mL of a 1% solution (50-100 mg).211 For percutaneous infiltration anesthesia, the dose of lidocaine hydrochloride is 1-60 mL of a 0.5 or 1% solution (5-300 mg). For IV regional anesthesia, 10-60 mL of a 0.5% solution (50-300 mg) may be employed.

For retrobulbar injection, 3-5 mL of a 4% sterile solution (120-200 mg) or 1.7-3 mg/kg is suggested; a portion of the dose is injected retrobulbarly and the remainder may be used to block the facial nerve.212

For transtracheal injection, 2-3 mL of a 4% solution (80-120 mg) is administered rapidly.212 When both transtracheal injection and topical application (oropharyngeal spray) of a 4% solution are needed to achieve complete analgesia, the combined total dose of lidocaine hydrochloride administered by injection and by oropharyngeal spray should not exceed 5 mL of a 4% solution (200 mg) or 3 mg/kg.212

Lidocaine hydrochloride with or without epinephrine is used for various dental procedures by infiltration injection or nerve block. In oral infiltration and/or mandibular block, initial doses of 1-5 mL of 2% lidocaine hydrochloride (20-100 mg) with epinephrine 1:100,000 are usually effective. If greater hemostasis is required, epinephrine 1:50,000 may be used. In children younger than 10 years of age, 0.9-1 mL of 2% lidocaine hydrochloride (18-20 mg) is adequate for a procedure involving 1 tooth (local infiltration), 2-3 teeth (maxillary infiltration), or teeth in an entire quadrant (mandibular block).213

Lidocaine hydrochloride shares the toxic potentials of local anesthetics, and the usual precautions of local anesthetic therapy should be observed.

Some commercially available formulations of lidocaine hydrochloride contain sodium metabisulfite, a sulfite that may cause allergic-type reactions, including anaphylaxis and life-threatening or less severe asthmatic episodes, in certain susceptible individuals. The overall prevalence of sulfite sensitivity in the general population is unknown but probably low; such sensitivity appears to occur more frequently in asthmatic than in nonasthmatic individuals.

Serious adverse effects (e.g., seizures, coma, irregular heart beat, respiratory depression) have been reported following topical application of local anesthetics to the skin. These events have occurred following application of extemporaneously prepared topical preparations containing high concentrations of anesthetics for cosmetic procedures and following use for indications approved by the US Food and Drug Administration (FDA).

Life-threatening adverse effects (e.g., irregular heart beat, seizures, breathing difficulties, coma, death) may occur when topical anesthetics are applied to a large area of skin, when the area of application is covered with an occlusive dressing, if a large amount of topical anesthetic is applied, if the anesthetic is applied to irritated or broken skin, or if the skin temperature increases (from exercise or use of a heating pad).101,102 When applied in such a manner, the amount of anesthetic that is absorbed systemically is unpredictable and the plasma concentrations achieved may be high enough to cause life-threatening adverse effects.101,102

Topical application of lidocaine 4% gel has been investigated to reduce discomfort during mammography.101,103 In this study, up to 30 g of lidocaine 4% gel was applied to a wide area of the chest (from the clavicles to the inferior costal margins and laterally to the midaxillary lines) and covered with an occlusive dressing; the gel was left on the skin for an average of 48 minutes and was removed 30-65 minutes before the first mammographic film.101,103 No serious adverse effects were reported in this study; however, the study was not large enough to evaluate whether uncommon but serious reactions could occur with such use.101 Patients should speak with their clinician if they are considering using a topical anesthetic before obtaining a mammogram.101

When a topical anesthetic is needed for a procedure, use of a preparation approved by the FDA has been recommended. A preparation containing the lowest concentration of anesthetic likely to be effective should be used; a small amount of topical anesthetic should be applied to the affected area for the shortest period necessary for the desired effect. The patient should apply the topical preparation as directed by a clinician, and should not apply the topical preparation to broken or irritated skin.101

Pharmacokinetics

When used for block or infiltration anesthesia without epinephrine, the onset of anesthesia of lidocaine hydrochloride is more rapid and the duration of action is longer than that of an equal dose of procaine hydrochloride. When used for lumbar epidural block, the duration of action of a 2% solution of lidocaine hydrochloride is about 100 minutes. In caudal block, the duration of a 1 or 2% solution of the drug is about 75-135 minutes. When used for spinal anesthesia, 1 mL of 5% lidocaine hydrochloride solution provides motor anesthesia for about 100 minutes and sensory anesthesia for an additional 40 minutes. Administration of 1.5-2 mL of 5% lidocaine hydrochloride solution provides spinal anesthesia for 2 hours. Lidocaine produces some vasodilation and epinephrine 1:200,000 to 1:100,000 may be added to slow vascular absorption and prolong duration of action of the anesthetic.

Chemistry and Stability

Chemistry

Lidocaine hydochloride is a local anesthetic of the amide type with an intermediate duration of action. Lidocaine hydrochloride occurs as a white, odorless, crystalline powder having a slightly bitter taste. The drug is very soluble in water and in alcohol. The pK_a of lidocaine hydrochloride is 7.86.

Commercially available solutions of lidocaine hydrochloride have a pH of 5-7; sodium hydroxide and/or hydrochloric acid may have been added during manufacture of the solutions to adjust pH. Solutions containing epinephrine have a pH of 3.3-5.5 and may contain sodium metabisulfite as an antioxidant. Hyperbaric solutions for spinal anesthesia are commercially available and contain lidocaine hydrochloride 5% with dextrose 7.5%. Hyperbaric solutions containing lidocaine hydrochloride 5% have a pH of 5.5-7 and a specific gravity of 1.030-1.035.

Stability

Lidocaine hydrochloride injections should be stored at a 20-25°C; solutions containing epinephrine should be protected from light.211,212,213,214

Lidocaine hydrochloride solutions are highly resistant to acid or alkaline hydrolysis and can be autoclaved repeatedly; dental cartridges, however, should not be autoclaved because the closures used in the cartridges will not withstand autoclaving. Epinephrine-containing solutions are not stable to autoclaving. Since lidocaine solutions for spinal anesthesia contain dextrose, caramelization may occur with prolonged heating or, in some instances, with prolonged storage. The solutions for spinal anesthesia may be autoclaved at 15 PSI and 121°C for 15 minutes; these solutions should not be resterilized more than once.214 The solutions for spinal anesthesia should not be allowed to remain in the sterilizer any longer than necessary; solutions containing a precipitate should not be used.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Only references cited for selected revisions after 1984 are available electronically.

101. Food and Drug Administration. FDA Public Health Advisory: Potential hazards of skin products containing numbing ingredients for relieving pain from mammography and other medical tests and conditions. 2009 Jan 16. From FDA website. [Web]

102. Food and Drug Administration. Topical Anesthetics. MedWatch alert. Rockville, MD; 2009 Jan 16. From FDA website. [Web]

103. Lambertz CK, Johnson CJ, Montgomery PG et al. Premedication to reduce discomfort during screening mammography. Radiology . 2008; 248:765-72. [PubMed 18647845]

200. Food and Drug Administration. Information for healthcare professionals: Chondrolysis reported with continuously infused local anesthetics (marketed as bupivacaine, chloroprocaine, lidocaine, mepivacaine, procaine, and ropivacaine). Rockville, MD; Updated 2010 Feb 16. From FDA website.

201. Todd JF. Chondrolysis linked to intra-articular infusions. Medical Devices Alerts and Notices. Silver Spring, MD: Food and Drug Administration; 2010 June. From FDA website.

202. Hansen BP, Beck CL, Beck EP et al. Postarthroscopic glenohumeral chondrolysis. Am J Sports Med . 2007; 35:1628-34. [PubMed 17609526]

203. Bailie DS, Ellenbecker TS. Severe chondrolysis after shoulder arthroscopy: a case series. J Shoulder Elbow Surg . 2009 Sep-Oct; 18:742-7.

204. Anakwenze OA, Hosalkar H, Huffman GR. Case Reports: Two Cases of Glenohumeral Chondrolysis after Intraarticular Pain Pumps. Clin Orthop Relat Res . 2010; :.

205. Anderson SL, Buchko JZ, Taillon MR et al. Chondrolysis of the glenohumeral joint after infusion of bupivacaine through an intra-articular pain pump catheter: a report of 18 cases. Arthroscopy . 2010; 26:451-61. [PubMed 20362823]

206. Rapley JH, Beavis RC, Barber FA. Glenohumeral chondrolysis after shoulder arthroscopy associated with continuous bupivacaine infusion. Arthroscopy . 2009; 25:1367-73. [PubMed 19962061]

207. Scheffel PT, Clinton J, Lynch JR et al. Glenohumeral chondrolysis: A systematic review of 100 cases from the English language literature. J Shoulder Elbow Surg . 2010; :. [PubMed 20421168]

208. Ballieul RJ, Jacobs TF, Herregods S et al. The peri-operative use of intra-articular local anesthetics: a review. Acta Anaesthesiol Belg . 2009; 60:101-8. [PubMed 19594092]

209. Busfield BT, Romero DM. Pain pump use after shoulder arthroscopy as a cause of glenohumeral chondrolysis. Arthroscopy . 2009; 25:647-52. [PubMed 19501296]

211. APP Pharmaceuticals. Xylocaine^® (lidocaine hydrochloride injection, USP) and Xylocaine^® (lidocaine hydrochloride injection and epinephrine injection, USP) prescribing information. Schaumburg, IL; 2010 Feb.

212. APP Pharmaceuticals. 4% Xylocaine^®-MPF (lidocaine hydrochloride) sterile solution prescribing information. Schaumburg, IL; 2010 Feb.

213. Dentsply Pharmaceutical. Xylocaine^® Dental (lidocaine hydrochloride injection) prescribing information. York, PA; 2001 Oct.

214. Hospira. 5% lidocaine hydrochloride and 7.5% dextrose injection, USP prescribing information. Lake Forest, IL; 2004 Nov.