Lidocaine Hydrochloride Monohydrate

------------------INDICATIONS AND USAGE------------------- ZINGO is an amide local anesthetic indicated for use on intact skin to provide local analgesia prior to venipuncture or peripheral intravenous cannulation in children 3–18 years of age. (1) ZINGO is indicated for use on intact skin to provide topical local analgesia prior to venipuncture in adults. (1) Important Limitations : For use on intact skin only (1, 2) For external use only (5)

---------------DOSAGE AND ADMINISTRATION--------------- Apply one ZINGO (0.5 mg lidocaine hydrochloride monohydrate) to the site planned for venipuncture or intravenous cannulation, one to three minutes prior to needle insertion. (2.1) Perform the procedure within 10 minutes after ZINGO administration. (2) Use ZINGO only on intact skin. (2)

---------------------ADVERSE REACTIONS--------------------- The most common adverse reactions (>5%) are skin reactions at the site of administration: erythema, petechiae, edema, and pruritus (6.1) To report SUSPECTED ADVERSE REACTIONS, contact 7T Pharma, LLC, at 1-800-941-2848 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. See 17 for PATIENT COUNSELING INFORMATION. Revised: December 2025

12.3 Pharmacokinetics Absorption A single dose of ZINGO in adults did not produce detectable plasma concentrations of lidocaine (limit of quantitation 5 ng/mL) in any subject tested (n = 38). Application of ZINGO to broken or inflamed skin, or multiple ZINGO applications, could result in systemic plasma levels of lidocaine that could produce systemic toxicity. Distribution When lidocaine is administered intravenously to healthy volunteers, the steady-state volume of distribution is approximately 0.8 to 1.3 L/kg. At much higher plasma concentrations (1 to 4 mcg/mL of free base) than those found following application of ZINGO, the plasma protein binding of lidocaine is concentration dependent. Lidocaine crosses the placental and blood brain barriers, presumably by passive diffusion. CNS toxicity may typically be observed around 5000 ng/mL of lidocaine; however a small number of patients reportedly may show signs of toxicity at approximately 1000 ng/mL. Metabolism It is not known if lidocaine is metabolized in the skin. Lidocaine is metabolized rapidly by the liver to a number of metabolites including monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both of which have pharmacologic activity similar to, but less potent than that of lidocaine. The major metabolic pathway of lidocaine, sequential N-deethylation to monoethylglycinexylidide (MEGX) and glycinexylidide (GX), is primarily mediated by CYP1A2 with a minor role of CYP3A4. The metabolite, 2,6-xylidine, has unknown pharmacologic activity. Following intravenous administration of lidocaine, MEGX and GX concentrations in serum range from 11% to 36% and from 5% to 11% of lidocaine concentrations, respectively. Serum concentrations of MEGX are about one-third the serum lidocaine concentrations. Elimination The half-life of lidocaine elimination from the plasma following intravenous administration is approximately 1.8 hours. Lidocaine and its metabolites are excreted by the kidneys. More than 98% of an absorbed dose of lidocaine can be recovered in the urine as metabolites or parent drug. Less than 10% of lidocaine is excreted unchanged in adults, and approximately 20% is excreted unchanged in neonates. The systemic clearance is approximately 8–10 mL/min/kg. During intravenous studies, the elimination half-life of lidocaine was statistically significantly longer in elderly patients (2.5 hours) than in younger patients (1.5 hours).