Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Injection, solution:
Xylocaine with Epinephrine:
0.5% / 1:200,000: Lidocaine hydrochloride 0.5% [5 mg/mL] and epinephrine 1:200,000 (50 mL) [contains methylparaben]
1% / 1:100,000: Lidocaine hydrochloride 1% [10 mg/mL] and epinephrine 1:100,000 (10 mL, 20 mL, 50 mL) [contains methylparaben]
2% / 1:100,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:100,000 (10 mL, 20 mL, 50 mL) [contains methylparaben]
Generic:
0.5% / 1:200,000: Lidocaine hydrochloride 0.5% [5 mg/mL] and epinephrine 1:200,000 (50 mL)
1% / 1:100,000: Lidocaine hydrochloride 1% [10 mg/mL] and epinephrine 1:100,000 (20 mL, 30 mL, 50 mL)
1.5% / 1:200,000: Lidocaine hydrochloride 1.5% [15 mg/mL] and epinephrine 1:200,000 (5 mL) [contains sodium metabisulfite]
2% / 1:100,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:100,000 (30 mL, 50 mL)
Injection, solution [preservative free]:
Xylocaine-MPF with Epinephrine:
1% / 1:200,000: Lidocaine hydrochloride 1% [10 mg/mL] and epinephrine 1:200,000 (5 mL, 10 mL, 30 mL) [contains sodium metabisulfite]
1.5% / 1:200,000: Lidocaine hydrochloride 1.5% [15 mg/mL] and epinephrine 1:200,000 (5 mL, 10 mL, 30 mL) [contains sodium metabisulfite]
2% / 1:200,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:200,000 (5 mL, 10 mL, 20 mL) [contains sodium metabisulfite]
Generic:
1.5% / 1:200,000: Lidocaine hydrochloride 1.5% [15 mg/mL] and epinephrine 1:200,000 (5 mL, 30 mL)
2% / 1:200,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:200,000 (20 mL)
Injection, solution [for dental use]:
Lignospan Forte: 2% / 1:50,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:50,000 (1.7 mL) [contains edetate disodium, potassium metabisulfite]
Lignospan Standard: 2% / 1:100,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:100,000 (1.7 mL) [contains edetate disodium, potassium metabisulfite]
Xylocaine Dental with Epinephrine:
2% / 1:50,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:50,000 (1.7 mL; 1.8 mL [DSC]) [contains sodium metabisulfite]
2% / 1:100,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:100,000 (1.7 mL; 1.8 mL [DSC]) [contains sodium metabisulfite]
Generic:
2% / 1:50,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:50,000 (1.7 mL, 1.8 mL)
2% / 1:100,000: Lidocaine hydrochloride 2% [20 mg/mL] and epinephrine 1:100,000 (1.7 mL, 1.8 mL)
Kit, Injection:
D-Care 100X: 1% / 1:200,000: Lidocaine hydrochloride 1% [10 mg/mL] and epinephrine 1:200,000
Pharmacology
Mechanism of Action
Lidocaine: Blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane’s permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction.
Epinephrine: Increases the duration of action of lidocaine by causing vasoconstriction (via alpha effects) which slows the vascular absorption of lidocaine.
Pharmacokinetics/Pharmacodynamics
Onset of Action
Dental: ≤2 to 4 minutes
Duration of Action
Dental: ~2.5 hours (infiltration); 3 to 3.5 hours (nerve block); dose and anesthetic procedure dependent
Use: Labeled Indications
Anesthesia, local: Production of local anesthesia by nerve block or infiltration for dental procedures.
Contraindications
Hypersensitivity to lidocaine, other local anesthetics of the amide type, epinephrine, or any component of the formulation.
Canadian labeling: Additional contraindications (not in US labeling): Hypersensitivity to para amino benzoic acid (PABA).
Dosage and Administration
Dosing: Adult
Anesthesia:
Dental: Oral infiltration/mandibular block: Initial: 1 to 5 mL (lidocaine 20 mg to 100 mg). Note: For most routine dental procedures, lidocaine 2% with epinephrine 1:100,000 is preferred. When a more pronounced hemostasis is required, use a 1:50,000 epinephrine concentration. Do not exceed 7 mg/kg body weight, up to a maximum range of 300 mg (usual dental practice) to 500 mg (approved product labeling) of lidocaine and 3 mcg (0.003 mg) of epinephrine/kg of body weight or 0.2 mg epinephrine per dental appointment.
Epidural: Administer a test dose (eg, 2 to 3 mL of lidocaine 1.5%) at least 5 minutes prior to injecting the total volume required for a lumbar or caudal block. Dosage varies with the number of dermatomes to be anesthetized (generally 2 to 3 mL of lidocaine 1%, 1.5%, or 2% with epinephrine [1:200,000] per dermatome). For continuous epidural or caudal anesthesia, the maximum dose should not be administered at intervals of <90 minutes. Maximum total dose for paracervical block: 200 mg/90 minutes (50% of the total dose to each side, with 5 minutes between sides).
Local: Infiltration: Dosage varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient. Maximum dose of lidocaine: 7 mg/kg (up to 500 mg). Use lidocaine 1%, 1.5%, or 2% with epinephrine (1:200,000) as single dose units.
Dosing: Geriatric
Refer to adult dosing; use with caution and at reduced dosages.
Dosing: Pediatric
Note: Dose varies with procedure, depth of anesthesia, vascularity of tissues, duration of anesthesia, and condition of patient should only be administered under the supervision of a qualified physician experienced in the use of anesthetics. Dosing units variable (mL/kg, mg/kg); use extra precaution to ensure accuracy.
Note: Dosing should be based on lean body mass (Cote 2013). Due to shorter duration of action and potential toxicity with repeat dosing, lidocaine is not typically used for central (spinal) or regional (epidural/caudal) anesthesia (Cote 2013; Miller 2015).
Local anesthesia; dermal/cutaneous infiltration: Infants, Children, and Adolescents: Usual concentration ≤2% (eg, 1% or 2%) solution: Infiltrate area locally; maximum dose is 7 mg/kg, not to exceed adult maximum dose of 500 mg (Cote 2013; Kliegman 2016). Note: Aspiration should be performed prior to each injection; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided (Mulroy 2010).
Peripheral nerve block; excluding digital or penile: Infants ≥6 months, Children, and Adolescents: Usual concentrations ≤1%: Dosage (concentration [0.25, 0.5 or 1%]) and volume varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient. Maximum dose of lidocaine: 7 mg/kg, not to exceed adult maximum of 500 mg (Cote 2013; Kliegman 2016). For infants <6 months, maximum doses should be reduced by 30% (Cote 2013; Miller 2015).
Dental anesthesia; oral infiltration/mandibular block: Note: For most routine dental procedures, lidocaine 2% with epinephrine 1:100,000 is preferred. When a more pronounced hemostasis is required, a 1:50,000 epinephrine concentration should be used.
Children <10 years: Lidocaine 2% with epinephrine solution: ≤0.9 to 1 mL (lidocaine 18 mg to 20 mg) per procedure; maximum dose: 4.4 mg/kg not to exceed 300 mg (AAPD 2009); dosing is for procedures involving a single tooth, maxillary infiltration for 2 to 3 teeth, or mandibular block of an entire quadrant; it is rare that a patient would require a higher dose (ie, >1 mL)
Children ≥10 years and Adolescents: Lidocaine 2% with epinephrine solution: Initial: 1 to 5 mL (lidocaine 20 mg to 100 mg). Do not exceed usual dental guideline recommended maximum dose of 4.4 mg/kg up to a maximum total dose of 300 mg (AAPD 2009); some suggest a higher maximum of 7 mg/kg up to total maximum of 500 mg (approved product labeling) of lidocaine and 3 mcg (0.003 mg) of epinephrine/kg of body weight or 0.2 mg epinephrine per dental appointment.
Administration
Avoid intravascular injections. Aspirate the syringe after tissue penetration and before injection to minimize chance of direct vascular injection. Use with caution or avoid use when there is inflammation and/or sepsis in the region of the proposed injection. Do not use injections containing preservatives (eg, methylparaben) for epidural or spinal anesthesia, or for any route of administration that would introduce solution into the cerebrospinal fluid. For continuous epidural or caudal anesthesia, the maximum dose should not be administered at intervals of <90 minutes.
Storage
Store at 20°C to 25°C (68°F to 77°F). Protect from light. Do not freeze. Do not autoclave cartridges.
Drug Interactions
Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. Monitor therapy
Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Monitor therapy
AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Benperidol: May diminish the therapeutic effect of EPINEPHrine (Systemic). Monitor therapy
Benzylpenicilloyl Polylysine: Alpha-/Beta-Agonists may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Consider use of a histamine skin test as a positive control to assess a patient's ability to mount a wheal and flare response. Consider therapy modification
Beta-Blockers (Beta1 Selective): May diminish the therapeutic effect of EPINEPHrine (Systemic). Monitor therapy
Beta-Blockers (Nonselective): May enhance the hypertensive effect of EPINEPHrine (Systemic). Exceptions: Arotinolol; Carvedilol; Labetalol. Monitor therapy
Beta-Blockers (with Alpha-Blocking Properties): May diminish the therapeutic effect of EPINEPHrine (Systemic). Monitor therapy
Blonanserin: May diminish the therapeutic effect of EPINEPHrine (Systemic). Avoid combination
Bretylium: May enhance the therapeutic effect of Alpha-/Beta-Agonists (Direct-Acting). Monitor therapy
Bromperidol: May diminish the therapeutic effect of EPINEPHrine (Systemic). Avoid combination
Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy
Chloroprocaine: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Monitor therapy
CloZAPine: May diminish the therapeutic effect of Alpha-/Beta-Agonists. Monitor therapy
Cocaine (Topical): May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Consider therapy modification
COMT Inhibitors: May decrease the metabolism of COMT Substrates. Monitor therapy
Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Monitor therapy
Ergot Derivatives: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Exceptions: Ergoloid Mesylates; Nicergoline. Avoid combination
Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Monitor therapy
Hyaluronidase: May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Management: Avoid the use of hyaluronidase to enhance dispersion or absorption of alpha-/beta-agonists. Use of hyaluronidase for other purposes in patients receiving alpha-/beta-agonists may be considered as clinically indicated. Consider therapy modification
Inhalational Anesthetics: May enhance the arrhythmogenic effect of EPINEPHrine (Systemic). Management: Administer epinephrine with added caution in patients receiving, or who have recently received, inhalational anesthetics. Use lower than normal doses of epinephrine and monitor for the development of cardiac arrhythmias. Consider therapy modification
Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Consider therapy modification
Lurasidone: EPINEPHrine (Systemic) may enhance the hypotensive effect of Lurasidone. Avoid combination
Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of EPINEPHrine (Systemic). Monitor therapy
Promethazine: May diminish the vasoconstricting effect of EPINEPHrine (Systemic). Management: When vasoconstrictive effects are desired in patients receiving promethazine, consider alternatives to epinephrine. Consider use of norepinephrine or phenylephrine, and avoid epinephrine, when treating hypotension associated with promethazine overdose. Consider therapy modification
Serotonin/Norepinephrine Reuptake Inhibitors: May enhance the tachycardic effect of Alpha-/Beta-Agonists. Serotonin/Norepinephrine Reuptake Inhibitors may enhance the vasopressor effect of Alpha-/Beta-Agonists. Consider therapy modification
Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Monitor therapy
Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Monitor therapy
Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy
Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy
Tricyclic Antidepressants: May enhance the vasopressor effect of Alpha-/Beta-Agonists. Management: Avoid, if possible, the use of alpha-/beta-agonists in patients receiving tricyclic antidepressants. If combined, monitor for evidence of increased pressor effects and consider reductions in initial dosages of the alpha-/beta-agonist. Consider therapy modification
Adverse Reactions
Also see individual agents.
<1%, postmarketing, and/or case reports: Methemoglobinemia
Warnings/Precautions
Concerns related to adverse effects:
- Cardiovascular effects: Lidocaine can cause cardiac depression (eg, bradycardia, hypotension); patients with hypovolemia may be at increased risk.
- CNS toxicity: Careful and constant monitoring of the patient's state of consciousness should be done following each local anesthetic injection; at such times, restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression, or drowsiness may be early warning signs of CNS toxicity. Treatment is primarily symptomatic and supportive.
- Hypersensitivity: Anaphylactic reactions may occur following administration.
- Intra-articular infusion related chondrolysis: Continuous intra-articular infusion of local anesthetics after arthroscopic or other surgical procedures is not an approved use; chondrolysis (primarily in the shoulder joint) has occurred following infusion, with some cases requiring arthroplasty or shoulder replacement.
- Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with G6PD deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).
- Respiratory arrest: Local anesthetics have been associated with occurrences of respiratory arrest.
Disease-related concerns:
- Cardiovascular disease: Use with caution in patients with bradycardia, severe shock, heart block, or impaired cardiovascular function; use with caution in areas of the body supplied by end arteries or having otherwise compromised blood supply. Patients with peripheral vascular disease or hypertensive vascular disease may exhibit exaggerated vasoconstrictor response. Ischemic injury (eg, exfoliating, ulcerating lesions) or necrosis may result.
- Diabetes: Use with caution in patients with diabetes.
- Hepatic impairment: Use with caution in patients with hepatic impairment; lidocaine is hepatically metabolized and patients with severe hepatic impairment are at greater risk of lidocaine toxicity.
- Renal impairment: Use with caution in patients with severe renal impairment (lidocaine metabolites may accumulate).
- Thyroid disease: Use with caution in patients with poorly controlled hyperthyroidism.
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Special populations:
- Acutely ill patients: Use with caution in acutely ill; reduce dose consistent with age and physical status.
- Debilitated patients: Use with caution in debilitated patients; reduce dose consistent with age and physical status.
- Elderly: Use with caution in the elderly; reduce dose consistent with age and physical status.
- Pediatric: Use with caution in children; reduce dose consistent with age and physical status.
Dosage form specific issues:
- Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP 1997; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates See manufacturer’s labeling.
- Sodium metabisulfite: May contain sodium metabisulfite; use caution in patients with a sulfite allergy.
Other warnings/precautions:
- Appropriate use: Avoid intravascular injections. Aspirate the syringe prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided. Use with caution when there is inflammation and/or sepsis in the region of the proposed injection. Do not use injections containing preservatives (eg, methylparaben) for epidural or spinal anesthesia, or for any route of administration that would introduce solution into the cerebrospinal fluid.
- Epidural anesthesia: Use lumbar and caudal epidural anesthesia with extreme caution in patients with existing neurological disease, spinal deformities, septicemia, and impaired cardiovascular function (eg, severe hypertension).
- Repeat doses: Repeat doses of lidocaine may cause significant increases in blood levels with each repeated dose due to slow accumulation of the drug or its metabolites. Tolerance to elevated blood levels varies with the status of the patient.
- Trained personnel: Dental practitioners and/or clinicians using local anesthetic agents should be well trained in diagnosis and management of emergencies that may arise from the use of these agents. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.
Monitoring Parameters
Vital signs; ECG during administration of a test dose; state of consciousness after each injection; CNS toxicity.
Pregnancy
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events have not been observed in animal reproduction studies. See individual agents.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Have patient report immediately to prescriber signs of acidosis (confusion, fast breathing, fast heartbeat, abnormal heartbeat, severe abdominal pain, nausea, vomiting, fatigue, shortness of breath, or loss of strength and energy), signs of methemoglobinemia (blue or gray color of the lips, nails, or skin; abnormal heartbeat; seizures; severe dizziness or passing out; severe headache; fatigue; loss of strength and energy; or shortness of breath), lightheadedness, fatigue, confusion, blurred vision, chest pain, sensation of cold, sensation of warmth, dizziness, passing out, agitation, anxiety, vision changes, noise or ringing in the ears, seizures, difficulty breathing, slow breathing, shallow breathing, tremors, twitching, burning or numbness feeling, depression, slow heartbeat, unable to pass urine, leaking of stool, leaking of urine, sexual dysfunction, paralysis, severe headache, back pain, chills, sensitivity to light, or stiff neck (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
