Xylocaine: Expert Local Anesthesia for Rapid Pain Control

Xylocaine
| Product dosage: 50 gm | |||
|---|---|---|---|
| Package (num) | Per tube | Price | Buy |
| 8 | $6.25
Best per tube | $72.00 $50.00 (31%) | 🛒 Add to cart |
| 10 | $9.00 | $90.00 (0%) | 🛒 Add to cart |
Synonyms | |||
Xylocaine (lidocaine hydrochloride) is a leading amide-type local anesthetic agent trusted by medical professionals worldwide for its rapid onset, predictable duration, and well-established safety profile. As a cornerstone of regional anesthesia and analgesia, it provides effective nerve blockade by inhibiting sodium ion influx required for the initiation and conduction of neuronal impulses. Its versatile formulations—including injectable solutions, topical preparations, and mucosal gels—make it indispensable across numerous medical and dental procedures, from minor outpatient interventions to complex surgical operations. This comprehensive product card details its pharmacology, clinical applications, and essential safety information for healthcare provider reference.
Features
- Active Ingredient: Lidocaine Hydrochloride
- Pharmacological Class: Amide Local Anesthetic
- Mechanism of Action: Reversible blockade of voltage-gated sodium channels on neuronal membranes
- Onset of Action: Rapid (within 2-5 minutes for injectable forms; variable for topical)
- Duration of Action: Intermediate (60-120 minutes, varies with formulation and vascularity of site)
- Available Formulations: Injectable solutions (with or without epinephrine), topical ointments, creams, jellies, sprays, and patches
- Metabolism: Hepatic via cytochrome P450 isoenzymes (primarily CYP1A2 and CYP3A4) to active metabolites (monoethylglycinexylidide and glycinexylidide)
- Excretion: Renal (>90% as metabolites, <10% unchanged)
Benefits
- Provides rapid and reliable local anesthesia, facilitating pain-free procedures and enhancing patient comfort and cooperation.
- Offers predictable and titratable duration of action, allowing clinicians to match the anesthetic effect to the procedural length.
- Reduces systemic opioid requirements by providing effective regional analgesia, thereby minimizing opioid-related side effects.
- Its multiple formulations allow for tailored application—infiltration, nerve block, topical, or mucosal—suiting a vast array of clinical scenarios.
- Features a well-documented efficacy and safety profile supported by decades of clinical use and extensive research.
- Epinephrine-containing formulations provide hemostasis by inducing local vasoconstriction, prolonging anesthetic effect, and reducing systemic absorption.
Common use
Xylocaine is indicated for the production of local anesthesia by infiltration injection, nerve block, and topical application. Its uses are extensive and include:
- Infiltration Anesthesia: For suturing, minor surgical excisions, and dental procedures.
- Peripheral Nerve Blocks: Such as brachial plexus, intercostal, and digital blocks for orthopedic and general surgery.
- Central Neuraxial Blocks: Epidural and spinal anesthesia (using specific, preservative-free formulations) for obstetrics, gynecology, and lower limb surgery.
- Topical Anesthesia: For mucous membranes of the mouth, pharynx, larynx, and tracheobronchial tree prior to endoscopic procedures or intubation.
- Dermatological Procedures: Superficial anesthesia for laser therapy, cosmetic procedures, and venipuncture.
- Cardiac Applications: Intravenous administration for the acute management of ventricular arrhythmias (using specific IV-labeled preparations).
Dosage and direction
Dosage varies significantly based on the procedure, tissue vascularity, patient status, and specific formulation. The smallest dose and lowest concentration that provides effective anesthesia should always be used.
- For Infiltration and Minor Nerve Blocks: Maximum recommended dose is 4.5 mg/kg (not to exceed 300 mg) of plain lidocaine. With epinephrine, the maximum dose is 7 mg/kg (not to exceed 500 mg).
- For Topical Application (Mucous Membranes): Apply the smallest amount needed to achieve the desired effect. For example, 2% jelly: apply up to 30 mL (600 mg) for urethral instillation; for oropharyngeal use, apply 15 mL (300 mg) to the mucosal surface.
- Administration: Aspirate before injection to avoid intravascular administration. Inject slowly and incrementally while monitoring the patient for signs of systemic toxicity.
- Special Populations: Reduce dosage in elderly patients, patients with cardiac or hepatic impairment, and those with acidosis or hypoxemia. Dosage must be meticulously calculated for pediatric patients based on weight.
Precautions
- Use with extreme caution in patients with known drug sensitivities, particularly to amide-type local anesthetics.
- Cardiovascular Impairment: Patients with heart block, severe sinus bradycardia, or congestive heart failure are at increased risk of toxicity.
- Hepatic Impairment: Patients with severe liver disease may be unable to metabolize lidocaine normally, leading to increased half-life and risk of accumulation and toxicity.
- Renal Impairment: The active metabolites are renally excreted; accumulation may occur in renal failure, increasing the risk of central nervous system toxicity.
- Malignant Hyperthermia: Although more commonly associated with ester locals, use with caution in susceptible patients.
- Methemoglobinemia: High doses of prilocaine, often combined with lidocaine in topical creams (e.g., EMLA), can cause this condition. While rare with Xylocaine alone, be aware of the symptomology (cyanosis unresponsive to oxygen).
Contraindications
- Known hypersensitivity to lidocaine hydrochloride or any other amide-type local anesthetic agent.
- Hypersensitivity to methylparaben or propylparaben (preservatives in multi-dose vials). Use preservative-free single-dose vials for neuraxial blocks.
- Administration of epinephrine-containing formulations into areas supplied by end-arteries (e.g., digits, nose, ears, penis) due to risk of vasoconstriction-induced ischemia and necrosis.
- Intravenous regional anesthesia (Bier Block) is contraindicated with formulations containing epinephrine.
- Existing infection or sepsis at the proposed injection site.
- Severe hemorrhagic diathesis or anticoagulant therapy (relative contraindication for deep blocks; risk vs. benefit must be assessed).
Possible side effect
Adverse reactions are generally dose-related and result from high plasma levels or unintended intravascular injection.
- Central Nervous System: Lightheadedness, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat or cold, tremors, twitching, convulsions, unconsciousness, and respiratory depression.
- Cardiovascular: Hypotension, bradycardia, arrhythmias, including potentially fatal ventricular arrhythmias, and cardiac arrest.
- Allergic Reactions: Urticaria, angioedema, bronchospasm, and anaphylaxis (rare; more common with ester-type anesthetics).
- Local Reactions: Pain at the injection site, persistent paresthesia, or neuropathy (rare).
Drug interaction
- Antiarrhythmics: Concurrent use with other Class IB antiarrhythmics (e.g., mexiletine) may have additive cardiotoxic effects.
- Beta-Blockers: Propranolol and metoprolol can decrease lidocaine metabolism, potentially increasing the risk of toxicity.
- CYP450 Inhibitors: Drugs that inhibit CYP1A2 (e.g., fluvoxamine) or CYP3A4 (e.g., ketoconazole, erythromycin, cimetidine) can significantly increase lidocaine plasma levels.
- CYP450 Inducers: Drugs like phenobarbital and rifampin may increase lidocaine metabolism, reducing its efficacy.
- Vasopressors: Ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents when combined with epinephrine-containing formulations.
Missed dose
Not applicable. Xylocaine is administered as a single procedure-based dose and is not used on a scheduled dosing regimen.
Overdose
Overdose results in systemic toxicity, primarily affecting the central nervous and cardiovascular systems.
- Symptoms: Initially CNS excitation (nervousness, dizziness, blurred vision, tremors, convulsions), followed by CNS depression (drowsiness, unconsciousness, respiratory arrest). Cardiovascular effects include hypotension, bradycardia, conduction blocks, and cardiac arrest.
- Management:
- Immediate Action: Stop administration. Secure airway and ensure adequate oxygenation and ventilation. Administer 100% oxygen.
- Seizure Control: Administer a benzodiazepine (e.g., diazepam, midazolam) IV. Barbiturates or propofol may be used if benzodiazepines are ineffective. Avoid phenytoin.
- Cardiovascular Support: Treat hypotension and bradycardia with IV fluids and vasopressors (e.g., ephedrine, norepinephrine). Avoid epinephrine in cases of tachyarrhythmias.
- Lipid Emulsion Therapy: In cases of severe cardiovascular collapse unresponsive to standard measures, administer a 20% lipid emulsion infusion (e.g., Intralipid) as an antidote. Bolus 1.5 mL/kg over 1 minute, followed by an infusion of 0.25 mL/kg/min.
Storage
- Store at controlled room temperature, 20° to 25°C (68° to 77°F).
- Protect from light.
- Do not freeze.
- Keep multi-dose vials sterile; discard any unused solution according to institutional protocol for multi-use vials after initial entry.
- Keep out of reach of children.
Disclaimer
This information is intended for healthcare professionals only. It is a summary of key product characteristics and does not replace the full Prescribing Information. The practitioner must rely on their own professional clinical judgment, knowledge of the patient, and a thorough review of the official product labeling before prescribing or administering this drug. Dosage and administration are the responsibility of the prescribing physician. The author and publisher are not responsible for any errors or omissions or for any consequences from the application of this information.
Reviews
- “The gold standard for reliability. Its rapid onset and predictable duration make it my first choice for most outpatient procedures. The availability of epinephrine-containing solutions is invaluable for hemostasis in dermatologic surgery.” – Dr. A. Sharma, Dermatologic Surgeon
- “An essential agent in our emergency department. From laceration repair to reducing fractures, Xylocaine provides effective and rapid anesthesia that improves patient throughput and comfort. Its safety profile is excellent when used correctly.” – MD, Emergency Medicine
- “As an anesthesiologist, I appreciate the versatility of Xylocaine. From topicalizing the airway to performing a variety of peripheral nerve blocks, it is a fundamental tool in our armamentarium. The distinction between preservative-free and multi-dose vials is critical for safe practice.” – Dr. R. Evans, Anesthesiologist
- “Consistent performance. We use the 2% jelly routinely for urethral catheterization in conscious patients. It significantly reduces discomfort and procedure-related anxiety. A staple on our urology ward.” – Nursing Lead, Urology Department