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Lidocaine and Epinephrine

Pronunciation

(LYE doe kane & ep i NEF rin)

Index Terms

  • Epinephrine and Lidocaine
  • Lidocaine HCl/Epinephrine Bit
  • Lidocaine Hydrochloride and Epinephrine Bitartrate
  • Lidocaine/Epinephrine

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)

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)

Brand Names: U.S.

  • Lignospan Forte
  • Lignospan Standard
  • Xylocaine MPF With Epinephrine
  • Xylocaine With Epinephrine

Pharmacologic Category

  • Local Anesthetic

Pharmacology

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.

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).

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

Dosage varies with procedure, degree of anesthesia needed, vascularity of tissue, duration of anesthesia required, and physical condition of patient. Maximum lidocaine dose: 7 mg/kg (up to 500 mg).

Dental anesthesia: 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: Oral infiltration/mandibular block: It is rarely necessary to administer >0.9 to 1 mL (lidocaine 18 mg to 20 mg) per procedure involving a single tooth, maxillary infiltration for 2 to 3 teeth, or mandibular block of an entire quadrant.

Children ≥10 years and Adolescents: Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling. However, accumulation of metabolites may be increased in renal impairment.

Dialysis: Not dialyzable (0% to 5%) by hemo- or peritoneal dialysis; supplemental dose is not necessary (Aronoff 2007).

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution (hepatically metabolized); patients with severe hepatic impairment are at greater risk of lidocaine toxicity.

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: May enhance the vasopressor effect of Alpha-/Beta-Agonists (Direct-Acting). Epinephrine used as a local anesthetic for dental procedures will not likely cause clinically relevant problems. Some beta-adrenoceptor mediated effects of Alpha-/Beta-Agonists (Direct-Acting), including anti-anaphylactic effects of epinephrine, may be diminished by Beta-Blockers. Management: Cardioselective beta-blockers and lower doses of epinephrine may confer a more limited risk. Patients who may require acute subcutaneous epinephrine (e.g., bee sting kits) should probably avoid beta blockers. Consider therapy modification

Blonanserin: May diminish the therapeutic effect of EPINEPHrine (Systemic). Avoid combination

Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy

Cocaine: 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

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

Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Avoid combination

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

MAO 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

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 (Direct-Acting). Management: Avoid, if possible, the use of direct-acting 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

Degree of adverse effects in the central nervous system and cardiovascular system are directly related to the blood levels of lidocaine. The effects below are more likely to occur after systemic administration rather than infiltration.

Cardiovascular: Cardiac conduction delay (decreased electrical excitability, decreased myocardial conduction rate; results in bradycardia and low cardiac output), depression of myocardial contractility

Central nervous system: Acute stress reaction, anxiety, central nervous system depression (results in drowsiness, loss of consciousness, respiratory arrest), confusion, disorientation, dizziness, restlessness, seizure

Gastrointestinal: Nausea, vomiting

Neuromuscular & skeletal: Tremor

<1% (Limited to important or life-threatening): Asthma, hypersensitivity reaction (includes allergic skin reaction, swelling at injection site)

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: Local anesthetics may cause methemoglobinemia.

• 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 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, tachycardia, arrhythmia, severe abdominal pain, nausea, vomiting, fatigue, shortness of breath, or feeling very tired or weak), change in balance, confusion, skin discoloration, severe loss of strength and energy, sensation of cold, sensation of warmth, dizziness, passing out, agitation, anxiety, tinnitus, blurred vision, diplopia, sweating a lot, seizures, difficulty breathing, slow breathing, shallow breathing, tremors, twitching, burning or numbness feeling, depression, vomiting, bradycardia, urinary retention, fecal incontinence, urinary incontinence, sexual dysfunction, paralysis, 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.

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