Local or regional anesthesia in surgical procedures (including oral surgery), diagnostic and therapeutic procedures, and obstetrical procedures.
Dosage and Administration
General
Determine dosage based on type and extent of surgical procedure, area to be anesthetized, vascularity of tissues, depth and duration of anesthesia, degree of muscular relaxation, and condition of the patient. Use lowest concentration and smallest dose required to produce the desired effect.
Administration
Injection
For solution and drug compatibility information, see Compatibility under Stability.
Administer by local infiltration, peripheral nerve block, paracervical block, sympathetic nerve block, central neural block (e.g., epidural block), caudal block, or subarachnoid (spinal) block.
Consult specialized references for specific techniques and procedures for administering local anesthetics.
For IV regional anesthesia, use 50-mL single-dose vials containing lidocaine hydrochloride 0.5% only.
For paracervical block, inject slowly; allow a 5-minute interval between sides.
For caudal or lumbar epidural block, avoid rapid injection of large volumes; when feasible, administer in fractional (incremental) doses.
For epidural or spinal block, avoid using preparations containing antimicrobial preservatives (e.g., methylparaben), since safety of intrathecal administration using these preparations not established.
For spinal block, inject slowly. Barbotage not recommended.
For dental anesthesia, lidocaine hydrochloride 2% solution with epinephrine 1:100,000 preferred for most routine procedures; when greater depth and a more pronounced hemostasis are required, use preparation containing epinephrine 1:50,000.
For chemical disinfection of container surface, moisten cotton or gauze with isopropyl (rubbing) alcohol (91%) or ethyl alcohol (70%) and wipe surface thoroughly just prior to use. Do not use alcohol brands that are not of USP grade, since these preparations may contain denaturants that may be injurious to rubber.
Dilution
Dilute with 0.9% sodium chloride injection to obtain desired concentration.
Dosage
Available as lidocaine hydrochloride, as fixed combination containing lidocaine hydrochloride and epinephrine bitartrate or epinephrine hydrochloride, and as lidocaine hydrochloride in dextrose injection. Dosage expressed in terms of lidocaine hydrochloride.
When larger dosages (volumes) are required, use preparations containing epinephrine (unless contraindicated).
Pediatric Patients
Local or Regional Anesthesia
Local Infiltration, Peripheral/Sympathetic Nerve Block, Epidural/Caudal Block
Use lower dosages than those suggested for healthy adults (see Adults under Dosage and Administration).
Anesthesia in Maxillary and Mandibular Area (for oral surgery)
Children <10 years of age: 18–20 mg (0.9–1 mL) of lidocaine hydrochloride 2% solution is adequate for a procedure involving 1 tooth (local infiltration), 2–3 teeth (maxillary infiltration), or teeth in an entire quadrant (mandibular block).
Adults
Local or Regional Anesthesia
Local Infiltration
Percutaneous: 5–300 mg (1–60 mL) of lidocaine hydrochloride 0.5 or 1% solution (without epinephrine).
IV regional: 50–300 mg (10–60 mL) of lidocaine hydrochloride 0.5% solution (without epinephrine).
Prior to lumbar epidural block, administer test dose to detect accidental intravascular injection. Test dose should contain 10–15 mcg epinephrine and 30–45 mg (2–3 mL) of 1.5% lidocaine hydrochloride. Repeat test dose if patient is moved in a manner that could displace catheter.
Thoracic epidural: 200–300 mg (20–30 mL) of lidocaine hydrochloride 1% solution (without epinephrine). Dosage is determined by number of dermatomes to be anesthetized (generally 2–3 mL per dermatome).
Lumbar epidural (for anesthesia): 225–300 mg (15–20 mL) of lidocaine hydrochloride 1.5% solution (without epinephrine) or 200–300 mg (10–15 mL) of lidocaine hydrochloride 2% solution (without epinephrine). Dosage is determined by number of dermatomes to be anesthetized (generally 2–3 mL per dermatome).
Caudal Block
Prior to caudal block, administer test dose to detect accidental intravascular injection. Test dose should contain 10–15 mcg epinephrine and 30–45 mg (2–3 mL) of 1.5% lidocaine hydrochloride. Repeat test dose if patient is moved in a manner that could displace catheter.
Vaginal delivery: 9–15 mg (0.6–1 mL) of lidocaine hydrochloride 1.5% in dextrose 7.5% injection.
Anesthesia in Maxillary and Mandibular Area (for oral surgery)
20–100 mg (1–5 mL) of lidocaine hydrochloride 2% solution with epinephrine 1:50,000 or 1:100,000.
Prescribing Limits
Pediatric Patients
Local or Regional Anesthesia
Local Infiltration, Peripheral/Sympathetic Nerve Block, Epidural/Caudal Block
For children >3 years of age with normal lean body mass and normal development, maximum dose is determined by child’s age and weight. For example, dosage for a 5-year old child weighing 50 lbs should not exceed 75–100 mg (3.3–4.4 mg/kg or 1.5–2 mg/lb). For IV regional anesthesia, maximum 3 mg/kg (1.4 mg/lb), using more dilute solutions (e.g., lidocaine hydrochloride 0.25 or 0.5% solution). (See Dilution under Dosage and Administration: Administration.)
Anesthesia in Maxillary and Mandibular Area (for oral surgery)
For children <10 years of age with normal lean body mass and normal development, maximum dose is determined by using standard pediatric drug formulas (e.g., Clark’s rule). For example, dosage for a 5-year old child weighing 50 lbs should not exceed 75–100 mg (3.3–4.4 mg/kg or 1.5–2 mg/lb).
Maximum 4.5 mg/kg (2 mg/lb) of body weight (without epinephrine) or 7 mg/kg (3.2 mg/lb) of body weight (with epinephrine).
Adults
Local or Regional Anesthesia
Local Infiltration, Peripheral/Sympathetic Nerve Block
Maximum 4.5 mg/kg (2 mg/lb) of body weight (up to 300 mg) (without epinephrine) or 7 mg/kg (3.2 mg/lb) of body weight (up to 500 mg) (with epinephrine).
IV regional: Maximum 4 mg/kg.
Paracervical Block
Maximum 200 mg (100 mg each side) per 90-minute period.
Continuous Epidural/Caudal Block
Maximum recommended dosage should not be administered at intervals of <90 minutes.
Anesthesia in Maxillary and Mandibular Area (for oral surgery)
Maximum 4.5 mg/kg (2 mg/lb) of body weight (up to 500 mg) (without epinephrine) or 7 mg/kg (3.2 mg/lb) of body weight (up to 300 mg) (with epinephrine).
Special Populations
Hepatic Impairment
Reduce dosage in patients with hepatic impairment.
Geriatric Patients
Reduce dosage in geriatric patients.
Other Populations
Reduce dosage in patients with cardiac disease, debilitated patients, and acutely ill patients.
Cautions
Contraindications
Contraindications to spinal anesthesia: severe hemorrhage, shock, heart block, local infection at site of proposed puncture, and septicemia.
Known hypersensitivity to local anesthetics of the amide type or to any ingredient in the formulation.
Warnings/Precautions
Warnings
Experience of Supervising Clinician
Should be used only by clinicians who are sufficiently knowledgeable in the diagnosis and management of dose-related toxicity and other acute emergencies that might arise. Oxygen, resuscitative equipment, and drugs must be available for immediate use. Delay in proper management of dose-related toxicity, underventilation, and/or altered sensitivity may result in acidosis, cardiac arrest, and, possibly, death.
Accidental Intravascular Injection
Accidental intravascular injection may result in confusion, seizures, CNS excitement and/or depression, myocardial depression, coma, and/or respiratory arrest. (See Nervous System Effects and also see Cardiovascular Effects, under Cautions.)
Aspirate prior to administration to guard against intravascular injection.
Injection During Uterine Contractions
Do not inject spinal anesthetics during uterine contractions, since spinal fluid current may carry drug further cephalad than desired.
Epinephrine Administration
Some lidocaine hydrochloride preparations contain epinephrine, which may cause ischemic injury or necrosis. Consider usual precautions associated with epinephrine administration. (See Cardiovascular Effects under Cautions.)
Sensitivity Reactions
Hypersensitivity Reactions and Cross Hypersensitivity
Possible cutaneous lesions, urticaria, edema, or anaphylactoid reactions.
No cross hypersensitivity reported in patients allergic to para-aminobenzoic derivatives (e.g., benzocaine, procaine, tetracaine).
Use with caution in patients with known drug sensitivities.
Sulfite Sensitivity
Some epinephrine-containing lidocaine preparations contain sodium metabisulfite, which may cause allergic-type reactions (including anaphylaxis and life-threatening or less severe asthmatic episodes) in certain susceptible individuals.
General Precautions
Nervous System Effects
Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse CNS effects (e.g., lightheadedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat, cold or numbness, twitching, tremors, seizures, unconsciousness, respiratory arrest). Carefully monitor level of consciousness after each local anesthetic injection.
Spinal anesthesia may be associated with adverse neurologic effects (e.g., loss of perineal sensation and sexual function, persistent anesthesia, paresthesia, weakness and paralysis of the lower extremities, headache).
Cardiovascular Effects
Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse cardiovascular effects (e.g., bradycardia, hypotension, and cardiovascular collapse, cardiac arrest). Carefully monitor cardiovascular and respiratory vital signs after each local anesthetic injection.
Use with caution in patients with impaired cardiovascular function, severe shock, or heart block.
Some lidocaine hydrochloride preparations contain epinephrine; risk of exaggerated vasoconstrictor response in patients with peripheral or hypertensive vascular disease. Use with caution and in carefully restricted quantities in areas of the body supplied by end arteries or having otherwise compromised blood supply (e.g., digits, nose, external ear, penis).
Familial Malignant Hyperthermia
Many drugs used during the conduct of anesthesia may trigger familial malignant hyperthermia; not known whether amide-type local anesthetics trigger this reaction. However, standard protocol for management should be available. Early unexplained signs of tachycardia, tachypnea, labile BP, and metabolic acidosis may precede temperature elevation. If familial malignant hyperthermia is confirmed, discontinue triggering agent and initiate appropriate therapy (e.g., oxygen, dantrolene) and other supportive measures.
Preexisting Conditions
Employ lumbar epidural and caudal block with extreme caution in patients with preexisting neurological disease, spinal deformities, septicemia, and severe hypertension.
Conditions that may preclude the use of spinal anesthesia (depending upon the clinician’s evaluation of the situation and ability to manage potential complications) include preexisting CNS disease (e.g., disease associated with pernicious anemia, poliomyelitis, paralysis from nerve injuries and syphilis); hematological disorders predisposing to coagulopathies; current anticoagulant therapy; chronic backache; preoperative headache; hypotension or hypertension; technical problems (persistent paresthesias, persistent bloody spinal tap); arthritis or spinal deformity; extremes of age; and psychosis or other causes of poor patient cooperation.
Risks Associated with Various Administration Techniques
Paracervical block: Possible rapid systemic absorption. Maternal seizures and cardiovascular collapse reported following paracervical block with certain local anesthetics (used to induce anesthesia for elective abortion). Administer dose slowly; do not exceed recommended maximum dose. (See Administration and Prescribing Limits, under Dosage and Administration and also see Labor and Delivery under Cautions.)
Retrobulbar block: Possible permanent injury to extraocular muscles requiring surgical repair.
Serious Adverse Effects Associated with Local Anesthetics
Risk of serious adverse effects (e.g., seizures, coma, irregular heart beat, respiratory depression) with use of topical local anesthetics; generally reported following application of extemporaneously prepared topical preparations containing high concentrations of anesthetics.
Potential for life-threatening adverse effects (e.g., irregular heart beat, seizures, breathing difficulties, coma, death) when topical local 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).
Lidocaine 4% gel has been investigated to reduce discomfort during mammography. Whether such use could result in serious reactions has not been determined. Patients should speak with their clinician if they are considering using a topical anesthetic before obtaining a mammogram.
When a topical anesthetic is needed for a procedure, use of an FDA-approved preparation has been recommended.Use a preparation containing the lowest concentration of anesthetic likely to be effective; apply a small amount of the preparation to the affected area for the shortest period necessary for the desired effect, and do not apply to broken or irritated skin.
Use of Fixed Combination
When used in fixed combination with other agents, consider the cautions, precautions, and contraindications associated with the concomitant agents.
Specific Populations
Pregnancy
Category B.
Labor and Delivery
Maternal hypotension reported. To prevent decreases in BP, elevate patient’s legs and position patient on her left side. Monitor fetal heart rate continuously; electronic fetal monitoring highly advisable.
Accidental intravascular or fetal intracranial injection following paracervical and/or may result in unexplained neonatal depression at birth or seizures within 6 hours after birth.
Paracervical block may decrease duration of first stage labor and facilitate cervical dilation. Possible fetal bradycardia and acidosis; always monitor fetal heart rate. For paracervical block in prematurity, toxemia of pregnancy, or presence of fetal distress, weigh benefit of therapy versus risk.
Epidural and spinal anesthesia may prolong second stage of labor (by removing parturient’s reflex urge to bear down or by interfering with motor function); may increase need for forceps assistance.
Possible diminished muscle strength and tone on neonate’s first or second day of life.
Lactation
Not known whether lidocaine is distributed into milk. Caution if used in nursing women.
Pediatric Use
Safety and efficacy of lidocaine hydrochloride in dextrose injection not established in pediatric patients.
Geriatric Use
Dosage reduction recommended.
Hepatic Impairment
Possible increased risk of toxicity, particularly in patients with severe hepatic impairment. Use with caution. Dosage adjustments recommended.
Common Adverse Effects
Adverse nervous system and cardiovascular effects. (See Nervous System Effects and Cardiovascular Effects, under Cautions.)
Possible severe, persistent hypertension or cerebrovascular accidents due to epinephrine component.
Test for CPK
Possible increased CPK concentrations following IM injection of lidocaine.
Accuracy as diagnostic test for AMI compromised if used without isoenzyme separation.
Pharmacokinetics
Absorption
Bioavailability
Systemic absorption dependent upon route of administration, administration site, and presence or absence of epinephrine in formulation. Except for intravascular administration, intercostal nerve block results in highest blood levels, and sub-Q administration results in lowest blood levels.
Onset within 30–60 seconds following spinal block.
For dental anesthesia, onset <2 minutes following infiltration with 2% solution (with or without epinephrine). Onset of 2–4 minutes following nerve block with 2% solution (with or without epinephrine).
Duration
Longer duration of anesthesia compared with procaine hydrochloride.
Duration of about 100 minutes following lumbar epidural block with 2% solution.
Duration of about 75–135 minutes following caudal block with 1 or 2% solution.
Following spinal block, duration of sensory anesthesia is usually adequate for completion of routine, uncomplicated vaginal delivery; motor anesthesia is limited to the levator and perineal muscles.
For dental anesthesia, pulp anesthesia persists for 5 minutes following infiltration with 2% solution without epinephrine. Pulp anesthesia persists for at least 60 minutes following infiltration with 2% solution with epinephrine; average duration of soft tissue anesthesia is approximately 2.5 hours. Following nerve block with the 2% solution with epinephrine, pulp anesthesia persists for at least 90 minutes, and soft tissue anesthesia persists for 3.25 hours.
Distribution
Extent
Crosses blood-brain and placental barriers.
Plasma Protein Binding
Protein binding dependent upon drug concentration and concentration of α-1-acid glycoprotein; fraction bound decreases with increasing drug concentration. At concentrations of 1–4 mcg/mL, 60–80% of drug is bound.
Elimination
Metabolism
Systemically absorbed lidocaine is rapidly metabolized in the liver.
Pharmacological or toxicological effects of metabolites are similar to but less potent than those of parent drug.
Elimination Route
Excreted principally in urine as metabolites (90%) and small amounts (<10%) of unchanged drug.
Half-life
1.5–2 hours following IV injection.
Special Populations
Prolonged half-life in patients with hepatic dysfunction.
Increased accumulation of metabolites in patients with renal impairment.
Stability
Storage
Parenteral
Injection
Room temperature (approximately 25°C). Protect from light.
Compatibility
For information on systemic interactions resulting from concomitant use, see Interactions.
Local anesthetics block the generation and conduction of nerve impulses by increasing the threshold for electrical excitation, slowing the propagation of the nerve impulse, and reducing the rate of rise of the action potential.
Some preparations formulated with epinephrine to decrease lidocaine’s rate and extent of systemic absorption and to prolong its duration of action.
Has intermediate duration of action.
Advice to Patients
Prior to administration, advise patients of the possibility of temporary loss of sensation and muscle function (e.g., in lower half of body following lumbar epidural or subarachnoid block).
Advise patients to avoid inadvertent trauma to the lips, tongue, cheek mucosae, or soft palate when these structures are anesthetized for dental procedures; postpone ingestion of food until normal function returns. Advise patient to consult dentist if anesthesia persists or if rash develops.
Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular or liver disease).
Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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