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Lidocaine and epinephrine: Drug information

Lidocaine and epinephrine: Drug information
(For additional information see "Lidocaine and epinephrine: Patient drug information" and see "Lidocaine and epinephrine: Pediatric drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • D-Care 100X;
  • Lignospan Forte;
  • Lignospan Standard;
  • Xylocaine MPF With Epinephrine;
  • Xylocaine With Epinephrine
Brand Names: Canada
  • Xylocaine With Epinephrine
Pharmacologic Category
  • Local Anesthetic
Dosing: Adult
Anesthesia

Anesthesia:

Dental: Oral infiltration/mandibular block: Lidocaine 2% with epinephrine solution: 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.

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

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

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: Adult

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.

Dosing: Older Adult

Refer to adult dosing; use with caution and at reduced dosages.

Dosing: Pediatric

(For additional information see "Lidocaine and epinephrine: Pediatric drug information")

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

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

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

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.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Pediatric

There are no dosage adjustments provided in the manufacturer's labeling; however, accumulation of metabolites may be increased in renal impairment. Not dialyzable (0% to 5%) by hemo- or peritoneal dialysis; supplemental dose is not necessary (Aronoff 2007).

Dosing: Hepatic Impairment: Pediatric

Use with caution; reduce dose; use with caution (hepatically metabolized); patients with severe hepatic impairment are at greater risk of lidocaine toxicity.

Adverse Reactions

The following adverse drug reaction is derived from product labeling unless otherwise specified. Also see individual agents.

Postmarketing: Hematologic & oncologic: Methemoglobinemia

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).

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.

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.

• Older adult: 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.

Dosage Forms: US

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

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Lidocaine-EPINEPHrine Injection)

0.5%-1:200000 (per mL): $0.09

1%-1:100000 (per mL): $0.23

1.5%-1:200000 (per mL): $1.12 - $1.30

2%-1:100000 (per mL): $0.42 - $0.65

2%-1:200000 (per mL): $0.30

2%-1:50000 (per mL): $0.29

Solution (Xylocaine-MPF/EPINEPHrine Injection)

1%-1:200000 (per mL): $0.41

1.5%-1:200000 (per mL): $0.46

2%-1:200000 (per mL): $0.77

Solution (Xylocaine/EPINEPHrine Injection)

0.5%-1:200000 (per mL): $0.17

1%-1:100000 (per mL): $0.26

2%-1:100000 (per mL): $0.26

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

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.

Administration: Pediatric

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.

Use: Labeled Indications

Anesthesia, local: Production of local anesthesia by nerve block or infiltration for dental procedures.

Medication Safety Issues
High alert medication:

The Institute for Safe Medication Practices (ISMP) includes this medication (epidural administration) among its list of drugs which have a heightened risk of causing significant patient harm when used in error.

Metabolism/Transport Effects

Refer to individual components.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alpha1-Blockers: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy

Amiodarone: May increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

Antidiabetic Agents: Hyperglycemia-Associated Agents may diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy

Atomoxetine: May enhance the hypertensive effect of Sympathomimetics. Atomoxetine may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Azosemide: May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk C: Monitor therapy

Benperidol: May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk C: 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. Risk D: Consider therapy modification

Beta-Blockers (Beta1 Selective): May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk C: Monitor therapy

Beta-Blockers (Nonselective): May enhance the hypertensive effect of EPINEPHrine (Systemic). Risk C: Monitor therapy

Beta-Blockers (with Alpha-Blocking Properties): May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk C: Monitor therapy

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

Bretylium: May enhance the therapeutic effect of Alpha-/Beta-Agonists (Direct-Acting). Risk C: Monitor therapy

Broccoli: May decrease the serum concentration of CYP1A2 Substrates (High risk with Inducers). Risk C: Monitor therapy

Bromocriptine: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Management: Consider alternatives to this combination when possible. If combined, monitor for hypertension and tachycardia, and do not coadminister these agents for more than 10 days. Risk D: Consider therapy modification

Bromperidol: May diminish the therapeutic effect of EPINEPHrine (Systemic). Risk X: Avoid combination

BUPivacaine: Local Anesthetics may enhance the adverse/toxic effect of BUPivacaine. Management: Avoid using any additional local anesthetics within 96 hours after insertion of the bupivacaine implant (Xaracoll) or bupivacaine and meloxicam periarticular solution (Zynrelef) or within 168 hours after subacromial infiltration (Posimir brand). Risk C: Monitor therapy

BUPivacaine (Liposomal): Lidocaine (Systemic) may enhance the adverse/toxic effect of BUPivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with lidocaine. Liposomal bupivacaine may be administered 20 minutes or more after the administration of lidocaine. Lidocaine may be administered 96 hours or more after liposomal bupivacaine administration. Risk D: Consider therapy modification

Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Cannabis: May decrease the serum concentration of CYP1A2 Substrates (High risk with Inducers). Risk C: Monitor therapy

Chloroprocaine (Systemic): May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy

Cimetidine: May increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

CloZAPine: May diminish the therapeutic effect of Alpha-/Beta-Agonists. Risk C: 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. Risk D: Consider therapy modification

COMT Inhibitors: May increase the serum concentration of COMT Substrates. Risk C: Monitor therapy

CYP1A2 Inducers (Moderate): May decrease the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

CYP1A2 Inhibitors (Strong): May increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

CYP3A4 Inhibitors (Moderate): May increase serum concentrations of the active metabolite(s) of Lidocaine (Systemic). Specifically, concentrations of monoethylglycinexylidide (MEGX) may be increased. CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

Dapsone (Topical): May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Risk C: Monitor therapy

Disopyramide: May enhance the arrhythmogenic effect of Lidocaine (Systemic). Disopyramide may increase the serum concentration of Lidocaine (Systemic). Specifically, the unbound/free fraction of lidocaine may be increased. Risk C: Monitor therapy

Doxofylline: Sympathomimetics may enhance the adverse/toxic effect of Doxofylline. Risk C: Monitor therapy

Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Risk X: Avoid combination

Etravirine: May decrease the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy

Haloperidol: May diminish the vasoconstricting effect of EPINEPHrine (Systemic). Management: Consider alternatives to this combination and monitor for reduced epinephrine efficacy, and possible paradoxical effects (ie, hypotension), when combined. Use of alternative vasopressor agents (eg, phenylephrine, metaraminol, norepinephrine) is preferred. Risk D: Consider therapy modification

Hyaluronidase: May enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Management: Do not use hyaluronidase to enhance the 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. Risk D: 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. Risk D: Consider therapy modification

Isoproterenol: May enhance the therapeutic effect of EPINEPHrine (Systemic). Risk X: Avoid combination

Kratom: May enhance the adverse/toxic effect of Sympathomimetics. Risk X: Avoid combination

Lacosamide: Lidocaine (Systemic) may enhance the adverse/toxic effect of Lacosamide. Specifically the risk for bradycardia, ventricular tachyarrhythmias, or a prolonged PR interval may be increased. Risk C: Monitor therapy

Levothyroxine: May enhance the adverse/toxic effect of Sympathomimetics. Specifically, the risk of coronary insufficiency may be increased in patients with coronary artery disease. Levothyroxine may enhance the therapeutic effect of Sympathomimetics. Sympathomimetics may enhance the therapeutic effect of Levothyroxine. Risk C: Monitor therapy

Lidocaine (Topical): May enhance the adverse/toxic effect of Antiarrhythmic Agents (Class IB). Risk C: Monitor therapy

Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Consider initial dose reductions of sympathomimetic agents, and closely monitor for enhanced blood pressure elevations, in patients receiving linezolid. Risk D: Consider therapy modification

Lisuride: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk X: Avoid combination

Local Anesthetics: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy

Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy

Monoamine Oxidase Inhibitors: May enhance the hypertensive effect of EPINEPHrine (Systemic). Risk C: Monitor therapy

Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Risk C: Monitor therapy

Nitric Oxide: May enhance the adverse/toxic effect of Methemoglobinemia Associated Agents. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Risk C: Monitor therapy

Ozanimod: May enhance the hypertensive effect of Sympathomimetics. Risk C: Monitor therapy

Pergolide: May enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy

Prilocaine: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Prilocaine. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Management: Monitor patients for signs of methemoglobinemia (e.g., hypoxia, cyanosis) when prilocaine is used in combination with other agents associated with development of methemoglobinemia. Avoid lidocaine/prilocaine in infants receiving such agents. Risk C: Monitor therapy

Promethazine: May diminish the vasoconstricting effect of EPINEPHrine (Systemic). Management: Avoid epinephrine and consider norepinephrine or phenylephrine when treating hypotension due to promethazine overdose. Consider alternative vasocontrictors in patients treated with promethazine. This combination may be indicated in anaphylaxis treatment. Risk D: Consider therapy modification

Propranolol: May increase the serum concentration of Lidocaine (Systemic). Risk C: Monitor therapy

Saquinavir: May increase the serum concentration of Lidocaine (Systemic). Risk X: Avoid combination

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. Management: If possible, avoid coadministration of direct-acting alpha-/beta-agonists and serotonin/norepinephrine reuptake inhibitors. If coadministered, monitor for increased sympathomimetic effects (eg, increased blood pressure, chest pain, headache). Risk D: Consider therapy modification

Sodium Nitrite: Methemoglobinemia Associated Agents may enhance the adverse/toxic effect of Sodium Nitrite. Combinations of these agents may increase the likelihood of significant methemoglobinemia. Risk C: Monitor therapy

Solriamfetol: Sympathomimetics may enhance the hypertensive effect of Solriamfetol. Sympathomimetics may enhance the tachycardic effect of Solriamfetol. Risk C: Monitor therapy

Spironolactone: May diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy

Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Risk C: Monitor therapy

Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Risk C: Monitor therapy

Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Risk C: Monitor therapy

Tobacco (Smoked): May decrease the serum concentration of Lidocaine (Systemic). Risk C: 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. Risk D: Consider therapy modification

Vasopressin: Alpha-/Beta-Agonists (Direct-Acting) may enhance the hypertensive effect of Vasopressin. The effect of other hemodynamic parameters may also be enhanced. Risk C: Monitor therapy

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies. See individual agents.

Breastfeeding Considerations

It is not known if lidocaine/epinephrine is excreted in breast milk. The manufacturer recommends that caution be exercised when administering lidocaine/epinephrine to nursing women. See individual agents.

Monitoring Parameters

Vital signs; ECG during administration of a test dose; state of consciousness after each injection; CNS toxicity.

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 (Adult Data Unless Noted)

Onset of action: Dental: ≤2 to 4 minutes

Duration: Dental: ~2.5 hours (infiltration); 3 to 3.5 hours (nerve block); dose and anesthetic procedure dependent

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (CO) Colombia: Roxicaina 1% Epinefrina;
  • (PR) Puerto Rico: D care 100x;
  • (QA) Qatar: Lignospan Special | Lignospan Standard | Octocaine 100 | Xilonibsa
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  4. Cote CJ, Lerman J, Anderson B, eds. A Practice of Anesthesia for Infants and Children. 5th ed. Elsevier; 2013.
  5. Gaffen AS and Haas DA, "Retrospective Review of Voluntary Reports of Nonsurgical Paresthesia in Dentistry," J Can Dent Assoc, 2009, 75(8):579. [PubMed 19840499]
  6. Garisto GA, Gaffen AS, Lawrence HP, et al, "Occurrence of Paresthesia After Dental Local Anesthetic Administration in the United States," J Am Dent Assoc, 2010, 141(7):836-44. [PubMed 20592403]
  7. "Inactive" ingredients in pharmaceutical products: update (subject review). American Academy of Pediatrics Committee on Drugs. Pediatrics. 1997;99(2):268-278. [PubMed 9024461]
  8. Kliegman RM, Stanton BMD, St. Geme J, Schor NF, eds. Nelson' s Textbook of Pediatrics. 20th ed. Philadelphia, PA: Saunders Elsevier; 2016.
  9. Lignospan Forte, Lignospan Standard (lidocaine and epinephrine) [prescribing information]. Louisville, CO: Septodont; June 2021.
  10. Miller RD. Miller’s Anesthesia. 8th ed. Philadelphia PA: Saunders; 2015.
  11. Xylocaine (lidocaine and epinephrine) [prescribing information]. Lake Zurich, IL: Fresenius Kabi; August 2020.
  12. Xylocaine (lidocaine and epinephrine) [product monograph]. Mississauga, Ontario, Canada: AstraZeneca Canada Inc; February 2015.
  13. Xylocaine 2% Dental (lidocaine and epinephrine) [prescribing information]. York, PA: Dentsply Pharmaceutical; September 2021.
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