LIGNOSPAN STANDARD
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LIGNOSPAN STANDARD (LIGNOSPAN STANDARD).
Lidocaine, the active ingredient, inhibits voltage-gated sodium channels, blocking the initiation and conduction of nerve impulses, leading to local anesthesia.
| Metabolism | Primarily metabolized by CYP3A4 to monoethylglycinexylidide and glycinexylidide; also undergoes deethylation and hydrolysis. |
| Excretion | Primarily hepatic metabolism; <10% excreted unchanged in urine. Biliary/fecal excretion is minimal. |
| Half-life | Terminal elimination half-life is approximately 1.5–2 hours in adults. Prolonged in hepatic impairment or heart failure. |
| Protein binding | Approximately 65% bound to plasma proteins, primarily alpha-1-acid glycoprotein (AAG) and albumin. |
| Volume of Distribution | Volume of distribution (Vd) is approximately 0.6–1.0 L/kg. Reflects extensive tissue distribution. |
| Bioavailability | Bioavailability: ~100% for intravenous; approximately 85–90% for intramuscular; negligible after oral administration due to extensive first-pass metabolism. |
| Onset of Action | Onset of anesthesia: 1–3 minutes after intravenous injection; 2–5 minutes after dental infiltration (for lignospan standard, containing epinephrine). |
| Duration of Action | Duration of anesthesia: 30–60 minutes for infiltration (without epinephrine) and 60–120 minutes with epinephrine (as in Lignospan Standard). |
| Molecular Weight | 234.34 |
2% lidocaine with 1:100,000 epinephrine: 1-5 mL (20-100 mg lidocaine) locally infiltrated; max 7 mg/kg lidocaine (up to 500 mg) per procedure. For nerve block: 1-30 mL depending on site. Epinephrine max 0.2 mg (20 mL of 1:100,000 solution) in healthy adults.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for lidocaine; however, caution in severe renal impairment due to potential accumulation of metabolites. GFR <30 mL/min: monitor for toxicity. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated or use with extreme caution; reduce dose by 75% and monitor levels. |
| Pediatric use | Lidocaine 2% with epinephrine: 0.5-2.5 mg/kg per dose (max 4.5 mg/kg lidocaine, epinephrine max 0.01 mL/kg of 1:100,000 solution). For infiltration: 1-2 mL/kg of 0.5-1% solution (without epinephrine in young infants). |
| Geriatric use | Reduce initial doses due to decreased hepatic clearance and increased sensitivity; use lowest effective dose. Maximum single dose: 200 mg lidocaine (without epinephrine) or 300 mg (with epinephrine). Monitor for CNS and cardiac toxicity. |
| 1st trimester | Lidocaine crosses the placenta; fetal effects are minimal at dental doses. Use only if clearly needed. |
| 2nd trimester | Considered safe at dental doses; avoid large doses or repeated administration. |
| 3rd trimester | Safe at dental doses; monitor for fetal bradycardia with high doses. |
Clinical note
Comprehensive clinical and safety monograph for LIGNOSPAN STANDARD (LIGNOSPAN STANDARD).
| Placental transfer | Lidocaine crosses the placenta by passive diffusion; fetal plasma levels are approximately 50-60% of maternal levels after epidural administration. Dental doses result in much lower systemic levels. |
| Breastfeeding | Lidocaine is excreted into breast milk in small amounts. Dental doses are unlikely to cause adverse effects in breastfed infants. |
■ FDA Black Box Warning
Not available.
| Serious Effects |
Hypersensitivity to lidocaine or amide-type anestheticsSevere hepatic impairment (significant metabolism reduction)Myasthenia gravis (may exacerbate weakness)Third-degree AV block (without pacemaker) if used intravenouslyPatients with porphyria (particularly acute intermittent porphyria)
| Precautions | Excessive blood levels may cause CNS and cardiovascular toxicity; use lowest effective dose; caution in patients with hepatic disease, cardiac disease, or epilepsy; monitor for signs of systemic toxicity. |
| Food/Dietary | No significant food interactions. Avoid citrus fruits or acidic foods immediately after injection as they may irritate the injection site. |
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| Lactation Rating |
| L2 (Probably Compatible) |
| Teratogenic Risk | Lignospan standard contains lidocaine and epinephrine. Lidocaine crosses the placenta and is classified as FDA pregnancy category B; no evidence of teratogenicity in animal studies, but human data are limited. Epinephrine may cause uterine vasoconstriction and reduce placental blood flow, especially in high doses or with inadvertent intravascular injection. During the first trimester, risk is minimal with standard doses. In the second and third trimesters, no known increased risk of malformations. During labor and delivery, high doses or repeated administration may lead to fetal bradycardia or neonatal depression due to lidocaine accumulation. |
| Fetal Monitoring | Monitor maternal vital signs, including heart rate and blood pressure, during and after administration. Fetal heart rate monitoring is recommended when used during labor and delivery, especially with epinephrine-containing formulations. Observe for signs of maternal or fetal toxicity (e.g., seizures, arrhythmias, bradycardia). |
| Fertility Effects | No known adverse effects on fertility in human studies. Animal studies have not shown impaired fertility with lidocaine or epinephrine at therapeutic doses. |
| Clinical Pearls | Lignospan Standard is a 2% lidocaine with 1:100,000 epinephrine dental anesthetic. Aspiration before injection is critical to prevent intravascular administration. Avoid use in patients with severe heart block, uncontrolled hypertension, or hyperthyroidism due to epinephrine. Maximum dose: 4.4 mg/kg lidocaine (0.7 mg/kg epinephrine). Use with caution in patients on MAOIs, tricyclic antidepressants, or beta-blockers due to potential hypertensive crisis or reduced heart rate. |
| Patient Advice | Avoid eating or drinking until numbness wears off to prevent accidental biting of tongue or cheek. · Do not operate machinery or drive for at least 30 minutes after injection. · Apply ice to injection site if swelling occurs; report persistent pain or infection. · Inform your dentist of all medications, especially those for depression, high blood pressure, or heart problems. |