Xylocaine: Rapid and Reliable Local Anesthesia for Medical Procedures
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Synonyms | |||
Xylocaine (lidocaine hydrochloride) is a leading amide-type local anesthetic agent, renowned for its rapid onset and dependable duration of action. It is a cornerstone in both hospital and outpatient settings for infiltration, nerve block, and surface anesthesia. Its well-established pharmacokinetic profile and extensive clinical history make it a preferred choice among healthcare professionals for managing procedural pain. This product card provides a comprehensive, expert-level overview of its appropriate use, mechanisms, and safety considerations.
Features
- Active Ingredient: Lidocaine Hydrochloride
- Drug Class: Amide Local Anesthetic
- Mechanism of Action: Reversible blockade of voltage-gated sodium channels, inhibiting depolarization and subsequent conduction of nerve impulses.
- Onset of Action: Rapid onset, typically within 2-5 minutes for infiltration anesthesia.
- Duration of Action: Intermediate duration, approximately 1-2 hours, which can be prolonged with the addition of a vasoconstrictor like epinephrine.
- Available Formulations: Multiple concentrations and delivery systems, including injectable solutions (with and without epinephrine), topical ointments, gels, sprays, and patches.
- Metabolism: Primarily hepatic via cytochrome P450 enzymes (CYP1A2 and CYP3A4) to active metabolites (monoethylglycinexylidide and glycinexylidide).
- Excretion: Renal excretion of metabolites; less than 10% excreted unchanged.
Benefits
- Predictable and Rapid Analgesia: Provides quick onset of anesthesia, allowing for efficient workflow and patient comfort during a wide array of medical and dental procedures.
- Proven Safety Profile: With decades of clinical use, its pharmacokinetics and side effect profile are well-documented and understood by medical professionals, facilitating safe administration.
- Versatile Application: Its availability in various concentrations and formulations (injectable, topical) makes it suitable for numerous indications, from minor suturing to more complex nerve blocks.
- Dose-Dependent Duration: The duration of anesthetic effect is predictable and can be tailored to the length of the anticipated procedure, enhancing procedural planning.
- Vasoconstrictor Option: The availability of formulations with epinephrine provides hemostasis and prolongs the anesthetic effect by reducing systemic absorption, which is crucial in vascular areas.
Common use
Xylocaine is indicated for the production of local anesthesia by infiltration injection, nerve block, and topical application. Its common uses are extensive and include:
- Infiltration Anesthesia: For minor surgical procedures, suturing of lacerations, and dental procedures.
- Peripheral Nerve Blocks: Such as digital blocks, brachial plexus blocks, intercostal nerve blocks, and Bier blocks (IV regional anesthesia).
- Topical Anesthesia: For mucous membranes of the mouth, pharynx, larynx, and trachea prior to endoscopic procedures or intubation; for the skin prior to venipuncture or minor dermatological procedures.
- Sympathetic Nerve Blocks: For diagnostic or therapeutic purposes.
- Spinal Anesthesia (specific formulations): For lower abdominal and lower extremity surgery.
- Obstetric Analgesia: Via pudendal block or local infiltration.
Dosage and direction
Dosage varies significantly based on the procedure, tissue vascularity, area to be anesthetized, and patient’s physical status. The smallest dose and lowest concentration that provides effective anesthesia should always be used.
- For Infiltration and Minor Nerve Blocks: The maximum recommended dose for plain lidocaine (without epinephrine) is 4.5 mg/kg, not to exceed 300 mg. For lidocaine with epinephrine 1:100,000 or 1:200,000, the maximum dose is 7 mg/kg, not to exceed 500 mg.
- Administration: Always aspirate before injection to avoid intravascular administration. Inject slowly and cautiously. For topical use, apply to the desired area as per the specific product’s instructions (e.g., spray, swab, ointment).
- Dose Calculation Example: For a 70 kg patient, the max dose of plain lidocaine is 70 kg * 4.5 mg/kg = 315 mg (round down to 300 mg max). Using a 1% solution (10 mg/mL), this equals 30 mL.
Precautions
- Cardiovascular Impairment: Use with extreme caution in patients with heart block, severe shock, or other cardiac conduction abnormalities, as lidocaine has cardiac effects.
- Hepatic Impairment: Patients with severe liver disease or reduced hepatic blood flow may have reduced metabolic clearance, leading to an increased risk of toxicity. Dose reduction is necessary.
- Renal Impairment: The active metabolites are renally excreted; accumulation may occur in renal failure, increasing the risk of central nervous system toxicity.
- Elderly and Debilitated Patients: These populations often require reduced doses due to possible increased sensitivity, altered pharmacokinetics, and concomitant conditions.
- Malignant Hyperthermia: While more associated with volatile anesthetics, caution is advised.
- Methemoglobinemia: Risk is higher with certain metabolites and prilocaine, but high doses of lidocaine have been associated with cases. Use caution in patients with congenital or idiopathic methemoglobinemia.
- Local Tissue Toxicity: Repeated injections can cause muscle necrosis. Use the lowest effective concentration.
Contraindications
- Known hypersensitivity to lidocaine, other amide-type local anesthetics, or any component of the formulation.
- Administration of lidocaine with epinephrine is contraindicated in areas supplied by end-arteries (e.g., digits, nose, ears, penis) due to the risk of vasoconstriction-induced ischemia and necrosis.
- The presence of severe shock or heart block.
- Intravenous regional anesthesia (Bier block) is contraindicated in patients with hypertension, vascular disease, or crush injuries.
- Specific formulations (e.g., for spinal use) have their own distinct contraindications.
Possible side effect
Adverse reactions are generally dose-related and result from high plasma levels or unintended intravascular injection.
- Central Nervous System: Nervousness, dizziness, blurred vision, tremors, drowsiness, convulsions, unconsciousness, respiratory depression and arrest. excitability may be a early sign of toxicity.
- Cardiovascular: Hypotension, bradycardia, arrhythmias, cardiovascular collapse, and cardiac arrest.
- Allergic Reactions: Though rare with amides, urticaria, angioedema, bronchospasm, or anaphylaxis can occur, often due to the preservative (methylparaben) rather than the drug itself.
- Local Reactions: Pain at the injection site, persistent sensory deficit.
Drug interaction
- Antiarrhythmics: Concurrent use with other Class IB antiarrhythmics (e.g., mexiletine) may have additive cardiac effects.
- CYP450 Inhibitors: Drugs that inhibit CYP1A2 (e.g., fluvoxamine) or CYP3A4 (e.g., ketoconazole, erythromycin) may decrease lidocaine metabolism, increasing the risk of toxicity.
- Beta-Blockers: Propranolol and metoprolol can decrease lidocaine clearance, potentially leading to increased serum levels.
- Vasopressors: Can cause severe, persistent hypertension when combined with formulations containing epinephrine.
- MAOIs, Tricyclic Antidepressants: May potentiate the pressor effect of epinephrine in vasoconstrictor-containing formulations.
Missed dose
The concept of a “missed dose” is not applicable to Xylocaine, as it is administered as a single procedure-based dose and not on a chronic, scheduled regimen. Anesthesia is provided for the duration of the specific procedure.
Overdose
Overdose is a medical emergency primarily characterized by central nervous system and cardiovascular toxicity.
- Symptoms: Initially may include CNS excitation (restlessness, anxiety, tremors, convulsions) followed by CNS depression (drowsiness, unconsciousness, respiratory arrest). Cardiovascular effects include hypotension, bradycardia, conduction blocks, and cardiac arrest.
- Management:
- Airway Management: Secure and maintain a patent airway. Administer oxygen. Assist or control ventilation as needed.
- Seizure Control: Administer a benzodiazepine (e.g., diazepam, midazolam) IV. Barbiturates or propofol may be used if benzodiazepines are ineffective.
- Cardiovascular Support: Treat hypotension and bradycardia with IV fluids and vasopressors (e.g., epinephrine, norepinephrine) as needed. Avoid beta-blockers.
- Circulatory Support: Initiate CPR if necessary.
- Intravenous Lipid Emulsion (ILE) Therapy: ILE (20% lipid emulsion) is a recognized antidote for severe local anesthetic systemic toxicity (LAST). Bolus 1.5 mL/kg ideal body weight over 1 minute, followed by an infusion of 0.25 mL/kg/min for 30-60 minutes.
Storage
- Store at controlled room temperature, 20°C to 25°C (68°F to 77°F).
- Protect from light.
- Do not freeze.
- Keep all medications out of the reach of children and pets.
Disclaimer
This information is for educational and professional medical purposes only and is not a substitute for the professional judgment of a healthcare provider. It does not constitute medical advice. The prescriber must consult the full official prescribing information for complete details on indications, dosage, warnings, precautions, and interactions before administering Xylocaine. Dosing and administration are the sole responsibility of the treating medical professional based on their clinical evaluation of the patient.
Reviews
- “The gold standard for local anesthesia in the ER. Its rapid onset and predictable duration make it indispensable for everything from simple laceration repair to more complex nerve blocks. A reliable workhorse.” – Emergency Medicine Physician, 15 years experience.
- “As a dentist, I appreciate the versatility of Xylocaine. The different formulations with and without vasoconstrictors allow me to tailor my anesthetic plan perfectly to each procedure and patient, ensuring profound anesthesia and patient comfort.” – General Dentist, 10 years experience.
- “From a pharmacological standpoint, lidocaine’s metabolism and clearance are well-defined, which allows for safer dosing calculations, especially in patients with comorbidities. Its long history means we understand its toxicological profile deeply, which is critical for managing rare adverse events like LAST.” – Clinical Pharmacologist.
- “For topical procedures prior to IV insertion in pediatric patients, the gel formulation is effective and helps reduce anxiety. It’s a crucial part of our pain management protocol.” – Pediatric Nurse Practitioner.