Jasocaine-A DC

 2%+0.00125% Injection
Jayson Pharmaceutical Ltd.

1.8 ml cartridge: ৳ 30.10 (1 x 5: ৳ 150.50)

Indications

Approved Indications:

  • Local and Regional Anesthesia:
    • Infiltration anesthesia for minor surgical and dental procedures.
    • Peripheral nerve block (e.g., brachial plexus block, intercostal block).
    • Field block, spinal, and epidural anesthesia.
  • Hemostasis During Surgery:
    • Epinephrine causes local vasoconstriction to reduce bleeding during procedures.

Clinically Accepted Off-label Uses:

  • Prolonged Postoperative Analgesia
  • Minor Cosmetic and Dermatologic Procedures: Skin lesion excision, suturing, laser treatments.
Dosage & Administration

Adults:

  • Infiltration Anesthesia: Lidocaine 0.5% to 1% with epinephrine (1:100,000 or 1:200,000).
    • Maximum dose: 7 mg/kg of lidocaine with epinephrine (not exceeding 500 mg total).
  • Peripheral Nerve Block: Lidocaine 1% with epinephrine (1:200,000).
  • Epidural Anesthesia: Lidocaine 1.5% with epinephrine (1:200,000).

Pediatrics:

  • Maximum dose: 3–5 mg/kg of lidocaine with epinephrine.
  • Use lower concentration solutions and monitor closely.

Elderly:

  • Use lower doses; increased sensitivity due to reduced hepatic metabolism and comorbidities.

Renal/Hepatic Impairment:

  • Use with caution. Dose reduction may be necessary to avoid systemic toxicity.

Route of Administration:

  • Infiltration, subcutaneous, nerve block, epidural, or spinal injection.
  • Important: Always aspirate before injection to avoid intravascular administration.
Mechanism of Action (MOA)

Lidocaine is an amide-type local anesthetic that inhibits voltage-gated sodium channels on the neuronal cell membrane, preventing the generation and propagation of action potentials, resulting in localized anesthesia. Epinephrine, a sympathomimetic agent, acts on alpha-adrenergic receptors to cause vasoconstriction, reducing systemic absorption of lidocaine, thereby prolonging its action, minimizing toxicity, and reducing bleeding at the site of injection.

Pharmacokinetics
  • Absorption: Rapid absorption from injection site; reduced by epinephrine-induced vasoconstriction.
  • Onset of Action: 1 to 5 minutes depending on the administration site.
  • Duration of Action: 60–180 minutes (prolonged with epinephrine).
  • Distribution: Widely distributed; crosses the blood-brain barrier and placenta.
  • Metabolism: Hepatically metabolized (mainly via CYP1A2 and CYP3A4).
  • Excretion: Renal elimination of metabolites.
  • Half-life: Approximately 90–120 minutes (may be prolonged in hepatic impairment).
Pregnancy Category & Lactation
  • Pregnancy Category:
    • Lidocaine: Category B – Animal studies show no fetal harm. Use only if clearly needed.
    • Epinephrine: Category C – May reduce uterine blood flow. Use only in life-threatening situations.
  • Lactation:
    • Lidocaine is excreted in small amounts in breast milk. Generally considered safe.
    • Epinephrine is also excreted in breast milk in trace amounts; caution is advised.
Therapeutic Class
  • Primary Class: Local Anesthetic
  • Subclass: Amide-type local anesthetic combined with vasoconstrictor (sympathomimetic)
Contraindications
  • Known hypersensitivity to lidocaine, epinephrine, or other amide-type anesthetics
  • Severe heart block or arrhythmia without pacemaker support
  • Use in areas supplied by end-arteries (e.g., fingers, toes, ears, nose, penis) unless diluted and used with extreme caution
  • Local infection at the injection site
  • Concomitant use of monoamine oxidase inhibitors (within 14 days)
Warnings & Precautions
  • Avoid intravascular injection – always aspirate before injection.
  • CNS toxicity risk: early symptoms include tinnitus, confusion, and seizures.
  • Cardiac toxicity: arrhythmias, bradycardia, and hypotension possible with high doses.
  • Use with caution in elderly, hepatic dysfunction, seizure disorders, and cardiac disease.
  • Use caution in hyperthyroid or hypertensive patients due to epinephrine effects.
  • Avoid repeated injections in short intervals.
Side Effects

Common:

  • Local irritation or swelling at injection site
  • Dizziness, tingling, or drowsiness
  • Mild increase in heart rate or blood pressure

Serious or Rare:

  • Seizures (due to systemic lidocaine toxicity)
  • Hypotension or bradycardia
  • Ventricular arrhythmias (from epinephrine)
  • Allergic reactions including rash or anaphylaxis
  • Tissue necrosis if used in end-arterial areas
  • Methemoglobinemia (rare)
Drug Interactions
  • MAO Inhibitors / Tricyclic Antidepressants: Risk of hypertensive crisis with epinephrine.
  • Beta-Blockers: Can enhance epinephrine’s vasoconstrictive effects.
  • Antiarrhythmic Drugs: Additive toxicity with other sodium channel blockers.
  • Inhalational Anesthetics (e.g., halothane): May increase risk of cardiac arrhythmias with epinephrine.
  • CYP3A4 Inhibitors (e.g., ketoconazole): May reduce lidocaine metabolism, increasing toxicity.
Recent Updates or Guidelines
  • New safety guidelines emphasize aspiration before injection to prevent intravascular administration.
  • Emerging literature supports the cautious use of epinephrine-containing solutions in digits and end-arterial areas, if appropriately diluted.
  • Emphasis on limiting cumulative lidocaine doses in prolonged or repeated procedures.
Storage Conditions
  • Storage Temperature: 20°C to 25°C (68°F to 77°F)
  • Light Protection: Protect from direct light; store in original packaging.
  • Humidity: Store in a dry environment.
  • Do Not Freeze.
  • Single-use vials: Discard any unused portion after opening.
  • Solution Stability: Do not use if discolored or containing particulate matter.
Available Brand Names