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Lidocaine HCl 2%

Pharmacokinetics and Metabolism

Lidocaine HCl is rapidly and completely absorbed following parenteral administration. Absorption rates vary based on the administration site and the presence of a vasoconstrictor agent. Blood levels peak highest following intercostal nerve block and lowest after subcutaneous administration. Lidocaine HCl binds to plasma proteins in a concentration-dependent manner, with 60-80% bound at concentrations of 1 to 4 mcg/mL. Binding is also influenced by the plasma concentration of alpha-1-acid glycoprotein.

Lidocaine HCl crosses the blood-brain and placental barriers through passive diffusion. The liver rapidly metabolizes it, and both metabolites and unchanged drug are excreted by the kidneys. Biotransformation includes oxidative N-dealkylation, ring hydroxylation, cleavage of the amide linkage, and conjugation. Major metabolites include monoethylglycinexylidide and glycinexylidide, which are less potent than the parent compound. Approximately 90% of administered lidocaine HCl is excreted as various metabolites, with less than 10% excreted unchanged. The primary urine metabolite is a conjugate of 4-hydroxy-2,6-dimethylaniline.

The elimination half-life following an intravenous bolus injection is 1.5 to 2 hours. Conditions affecting liver function may significantly alter lidocaine HCl kinetics, potentially doubling the half-life in patients with liver dysfunction. Renal dysfunction does not affect lidocaine HCl kinetics but may increase metabolite accumulation. Acidosis and CNS stimulants/depressants can affect the CNS levels needed for systemic effects. Plasma levels above 6 mcg/mL can cause adverse effects, with arterial levels of 18-21 mcg/mL in rhesus monkeys linked to convulsive activity.

Indications and Usage

Lidocaine Hydrochloride Injection is indicated for local or regional anesthesia through infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques (e.g., brachial plexus, intercostal) and central neural techniques (e.g., lumbar, caudal epidural blocks) when standard procedures are observed.


Lidocaine HCl is contraindicated in patients with a known hypersensitivity to amide-type local anesthetics.


Lidocaine Hydrochloride Injection should only be used by clinicians experienced in diagnosing and managing dose-related toxicity and acute emergencies associated with the block employed. Immediate availability of oxygen, resuscitative drugs, cardiopulmonary equipment, and trained personnel is essential. Delay in managing dose-related toxicity, underventilation, or altered sensitivity may lead to acidosis, cardiac arrest, and possibly death.

Pregnancy and Nursing Mothers

  • Pregnancy: Animal studies have shown no harm to the fetus at doses up to 6.6 times the human dose. However, there are no well-controlled studies in pregnant women. Caution is advised, especially during early pregnancy.
  • Nursing Mothers: It is unknown if lidocaine HCl is excreted in human milk. Caution is advised when administering to nursing women.


Acute emergencies related to local anesthetics are often due to high plasma levels or unintended subarachnoid injection. Management includes careful monitoring, maintaining a patent airway, and providing assisted or controlled ventilation with oxygen. If convulsions persist, administer small increments of an ultra-short-acting barbiturate or benzodiazepine intravenously. Supportive treatment of circulatory depression may require intravenous fluids and vasopressors. Standard cardiopulmonary resuscitative measures should be instituted if cardiac arrest occurs. Dialysis is of negligible value.

Notice: All products are intended to be administered by licensed trained technicians. 
Sculpted by Alexis is not responsible for any side effects such as allergic reactions, etc. that may arise after administering the products.
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